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Sample records for sitagliptin phosphate monohydrate

  1. Sitagliptin.

    PubMed

    Lyseng-Williamson, Katherine A

    2007-01-01

    Sitagliptin, an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, improves glycaemic control by inhibiting DPP-4 inactivation of the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. This increases active incretin and insulin levels, and decreases glucagon levels and post-glucose-load glucose excursion. In large, well designed phase III trials in patients with type 2 diabetes mellitus, sitagliptin 100 or 200mg once daily alone or in combination with other antihyperglycaemics was associated with significant improvements relative to placebo in overall glycaemic control and indices for insulin response and beta-cell function. Improvements from baseline in mean glycosylated haemoglobin (HbA(1c)) were significantly greater with sitagliptin monotherapy than with placebo in patients with type 2 diabetes. As add-on therapy in patients with suboptimal glycaemic control despite oral antihyperglycaemic treatment, sitagliptin improved HbA(1c) to a significantly greater extent than placebo when added to metformin or pioglitazone and was noninferior to glipizide when added to metformin. Sitagliptin was well tolerated when administered alone or in combination with other antihyperglycaemics, with an adverse event profile similar to that shown with placebo. The incidence of hypoglycaemia with sitagliptin was similar to that with placebo and, in combination with metformin, lower than that with glipizide. Sitagliptin had a generally neutral effect on bodyweight. PMID:17352516

  2. Improved Chromatographic Separation of Sitagliptin Phosphate and Metformin Hydrochloride

    PubMed Central

    Hendy, Moataz S.

    2015-01-01

    New UPLC method was developed for determination of sitagliptin and metformin using Symmetry C18 column (100 mm × 2.1 mm, 2.2 μm) and isocratic elution (methanol 20%), pH (3.5) as a mobile phase. The ultraviolet detector was operated at 220 nm and the column temperature was 50°C. Linearity parameters were acceptable over the concentration ranges of 2-12 μgml-1 and 5-35 μgml-1 for sitagliptin and metformin, respectively. The variables were premeditated to adjust the chromatographic conditions using design of experiment. The proposed method was proved to be accurate for the quality control of the mentioned drugs in their pharmaceutical dosage form. PMID:26759536

  3. Novel tricalcium silicate/monocalcium phosphate monohydrate composite bone cement.

    PubMed

    Huan, Zhiguang; Chang, Jiang

    2007-08-01

    In this paper, we obtained a novel bone cement composed of tricalcium silicate (Ca(3)SiO(5); C(3)S) and monocalcium phosphate monohydrate (MCPM). The weight ratio of MCPM in the cement is 0, 10, 20, and 30%. The initial setting time was dramatically reduced from 90 min to 30 min as the content of MCPM reached 20%. The workable paste with a liquid/powder (L/P) ratio of 0.8 mL/g could be injected for 2-20 min (nozzle diameter 2.0 mm). The pH variation of the composite cement in simulated body environment was obviously lowered. The compressive strength of the composite cement after setting for 4-28 days was slightly lower than that of the tricalcium silicate paste. The in vitro bioactivity was investigated by soaking in simulated body fluid for 7 days. The result showed that the novel bone cement had good bioactivity and could degrade in tris-(hydroxymethyl)-aminomethane-hydrochloric-acid (Tris-HCl) solution. Our result indicated that the Ca(3)SiO(5)/MCPM paste had good hydraulic properties, bioactivity, and degradability. The novel bone cement could be a potential candidate as bone substitute. PMID:17238165

  4. Review of sitagliptin phosphate: a novel treatment for type 2 diabetes

    PubMed Central

    Gallwitz, Baptist

    2007-01-01

    Sitagliptin (Januvia®, Merck Pharmaceuticals) is a dipeptidyl-peptidase inhibitor (DPP-4 inhibitor) that has recently been approved for the therapy of type 2 diabetes. Like other DPP-4 inhibitors its action is mediated by increasing levels of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). Sitagliptin is effective in lowering HbA1c, and fasting as well as postprandial glucose in monotherapy and in combination with other oral antidiabetic agents. It stimulates insulin secretion when hyperglycemia is present and inhibits glucagon secretion. In clinical studies it is weight neutral. This article gives an overview of the mechanism of action, the pharmacology, and the clinical efficacy and safety of sitagliptin in type 2 diabetes therapy. PMID:17580730

  5. Additive concentration effects on dicalcium phosphate dihydrate cements prepared using monocalcium phosphate monohydrate and hydroxyapatite.

    PubMed

    Santa Cruz Chavez, Grace; Alge, Daniel L; Chu, Tien-Min Gabriel

    2011-11-21

    In our previous study, we investigated the setting time, mechanical properties and microstructure of dicalcium phosphate dihydrate cements prepared using monocalcium phosphate monohydrate (MCPM) and hydroxyapatite (HA). Despite the use of sodium citrate as a setting regulator, setting occurs rapidly in the MCPM/HA system and further studies on other retardants are needed. In the present study, sodium pyrophosphate and sulfuric acid were tested to evaluate their effectiveness in maintaining workability of the cement paste. MCPM/HA cements at a powder to liquid ratio of 1.0 with sodium pyrophosphate and sulfuric acid at 10, 25, 50, 75 and 100 mM were manufactured and studied based on their setting time, mechanical and porosity properties, phase composition, and microstructure. These measurements were compared to our previous data using sodium citrate. The results showed that the additives have a dose-dependent effect on the setting time. Their order of efficiency is sodium pyrophosphate > sodium citrate > sulfuric acid. However, the sulfuric acid group exhibited the highest compressive strength (CS) compared to the other groups. A lack of correlation between the CS and the porosity of the cements suggested that a mechanism other than porosity reduction was responsible for the CS increase. Since x-ray diffraction analysis did not indicate an effect on composition, explanations based on calcium sulfate dihydrate formation and changes in microstructure were proposed based on scanning electron micrograph observations. PMID:22101069

  6. A comparative study of smart spectrophotometric methods for simultaneous determination of sitagliptin phosphate and metformin hydrochloride in their binary mixture.

    PubMed

    Lotfy, Hayam M; Mohamed, Dalia; Mowaka, Shereen

    2015-10-01

    Simple, specific, accurate and precise spectrophotometric methods were developed and validated for the simultaneous determination of the oral antidiabetic drugs; sitagliptin phosphate (STG) and metformin hydrochloride (MET) in combined pharmaceutical formulations. Three methods were manipulating ratio spectra namely; ratio difference (RD), ratio subtraction (RS) and a novel approach of induced amplitude modulation (IAM) methods. The first two methods were used for determination of STG, while MET was directly determined by measuring its absorbance at λmax 232 nm. However, (IAM) was used for the simultaneous determination of both drugs. Moreover, another three methods were developed based on derivative spectroscopy followed by mathematical manipulation steps namely; amplitude factor (P-factor), amplitude subtraction (AS) and modified amplitude subtraction (MAS). In addition, in this work the novel sample enrichment technique named spectrum addition was adopted. The proposed spectrophotometric methods did not require any preliminary separation step. The accuracy, precision and linearity ranges of the proposed methods were determined. The selectivity of the developed methods was investigated by analyzing laboratory prepared mixtures of the drugs and their combined pharmaceutical formulations. Standard deviation values were less than 1.5 in the assay of raw materials and tablets. The obtained results were statistically compared to that of a reported spectrophotometric method. The statistical comparison showed that there was no significant difference between the proposed methods and the reported one regarding both accuracy and precision. PMID:25978011

  7. Monocalcium phosphate monohydrate concentration in soil suspension amended with organic matter

    NASA Astrophysics Data System (ADS)

    Bennani, F.; Badraoui, M.; Mikou, M.

    2005-03-01

    The effect of humic substances, Fe3+, Al3+, and soil clay mineralogy on the availability of monocalcium phosphate monohydrate added at pH5 were investigated. Both solution and suspension experiments showed that humic matter chelates phosphorus and prevents the formation of less soluble forms of phosphorus than monocalcium phosphate. However, Fe3+ and Al3+ ions in the solution lead to the precipitation of Fe-P and Al-P, less soluble compounds. Organic matter, by its chelating power for Ca2+, Fe3+ and Al3+ions, explains the availability of phosphorus in solution at pH5. Clay minerals, especially smectites, induced an increase in solution phosphorus content because of their adsorption properties for Ca2+, Fe3+ and Al3+. Soil organic matter should be maintained at a sufficient level in order to get enough phosphorus in soil solution for plant uptake.

  8. Characterization studies on the additives mixed L-arginine phosphate monohydrate (LAP) crystals

    NASA Astrophysics Data System (ADS)

    Haja Hameed, A. S.; Karthikeyan, C.; Ravi, G.; Rohani, S.

    2011-04-01

    L-arginine phosphate monohydrate (LAP), potassium thiocyanate (KSCN) mixed LAP (LAP:KSCN) and sodium sulfite (Na 2SO 3) mixed LAP (LAP:Na 2SO 3) single crystals were grown by slow cooling technique. The effect of microbial contamination and coloration on the growth solutions was studied. The crystalline powders of the grown crystals were examined by X-ray diffraction and the lattice parameters of the crystals were estimated. From the FTIR spectroscopic analysis, various functional group frequencies associated with the crystals were assigned. Vickers microhardness studies were done on {1 0 0} faces for pure and additives mixed LAP crystals. From the preliminary surface second harmonic generation (SHG) results, it was found that the SHG intensity at (1 0 0) face of LAP:KSCN crystal was much stronger than that of pure LAP.

  9. Novel bioactive composite bone cements based on the beta-tricalcium phosphate-monocalcium phosphate monohydrate composite cement system.

    PubMed

    Huan, Zhiguang; Chang, Jiang

    2009-05-01

    Bioactive composite bone cements were obtained by incorporation of tricalcium silicate (Ca3SiO5, C3S) into a brushite bone cement composed of beta-tricalcium phosphate [beta-Ca3(PO4)2, beta-TCP] and monocalcium phosphate monohydrate [Ca(H2PO4)2.H2O, MCPM], and the properties of the new cements were studied and compared with pure brushite cement. The results indicated that the injectability, setting time and short- and long-term mechanical strength of the material are higher than those of pure brushite cement, and the compressive strength of the TCP/MCPM/C3S composite paste increased with increasing aging time. Moreover, the TCP/MCPM/C3S specimens showed significantly improved in vitro bioactivity in simulated body fluid and similar degradability in phosphate-buffered saline as compared with brushite cement. Additionally, the reacted TCP/MCPM/C3S paste possesses the ability to stimulate osteoblast proliferation and promote osteoblastic differentiation of the bone marrow stromal cells. The results indicated that the TCP/MCPM/C3S cements may be used as a bioactive material for bone regeneration, and might have significant clinical advantage over the traditional beta-TCP/MCPM brushite cement. PMID:18996779

  10. Citrate, not phosphate, can dissolve calcium oxalate monohydrate crystals and detach these crystals from renal tubular cells.

    PubMed

    Chutipongtanate, Somchai; Chaiyarit, Sakdithep; Thongboonkerd, Visith

    2012-08-15

    Dissolution therapy of calcium oxalate monohydrate (COM) kidney stone disease has not yet been implemented due to a lack of well characterized COM dissolution agents. The present study therefore aimed to identify potential COM crystal dissolution compounds. COM crystals were treated with deionized water (negative control), 5 mM EDTA (positive control), 5 mM sodium citrate, or 5mM sodium phosphate. COM crystal dissolution activities of these compounds were evaluated by phase-contrast and video-assisted microscopic examinations, semi-quantitative analysis of crystal size, number and total mass, and spectrophotometric oxalate-dissolution assay. In addition, effects of these compounds on detachment of COM crystals, which adhered tightly onto renal tubular cell surface, were also investigated. The results showed that citrate, not phosphate, had a significant dissolution effect on COM crystals as demonstrated by significant reduction of crystal size (approximately 37% decrease), crystal number (approximately 53% decrease) and total crystal mass (approximately 72% decrease) compared to blank and negative controls. Spectrophotometric oxalate-dissolution assay successfully confirmed the COM crystal dissolution property of citrate. Moreover, citrate could detach up to 85% of the adherent COM crystals from renal tubular cell surface. These data indicate that citrate is better than phosphate for dissolution and detachment of COM crystals. PMID:22713548

  11. ESR and ENDOR studies of x-irradiated single crystals of deoxycytidine 5-phosphate monohydrate (5{prime}dCMP) at 10 K

    SciTech Connect

    Close, D.M.; Hole, E.O.; Sagstuen, E.; Nelson, W.H.; Bernhard, W.A.

    1995-12-31

    Cytosine has received a great deal of attention recently. Results suggest that cytosine may be the primary reduction site in DNA. Also, a dissimilarity in the ESR spectrum from monomers and oligomers of cytosine has focused attention on the protonation state of the cytosine anion. A recent review covers most of the results on radical ions and their reactions in cytosine derivatives. The present work concerns ENDOR studies on single crystals of deoxycytidine 5{prime}phosphate monohydrate (5{prime}dCMP).

  12. In vitro degradation and cytocompatibility of dicalcium phosphate dihydrate cements prepared using the monocalcium phosphate monohydrate/hydroxyapatite system reveals rapid conversion to HA as a key mechanism.

    PubMed

    Alge, Daniel L; Goebel, W Scott; Chu, Tien-Min Gabriel

    2012-04-01

    We previously showed that dicalcium phosphate dihydrate (DCPD) cements can be prepared using monocalcium phosphate monohydrate (MCPM) and hydroxyapatite (HA). In this study, we have characterized the degradation properties and biocompatibility of these novel cements. To study the degradation properties, cements were prepared using MCPM:HA molar ratios of 4:1, 2:1, 2:3, and 2:5. Degradation was evaluated in vitro by static soaking in PBS, and changes in pH, mass, compressive strength, and composition were monitored. Conversion of DCPD to HA was noted in the 4:1 group, which initially consisted of pure DCPD. However, the 2:1 group, which initially consisted of DCPD and an intermediate amount of unreacted HA, underwent rapid conversion to HA associated with significantly greater pH drop and mass loss as well as a complete loss of mechanical integrity. On the basis of these results, we directly compared the cytocompatibility of 2:1 MCPM:HA cements to DCPD cements prepared with an equivalent percent molar excess of β-tricalcium phosphate (β-TCP) using an in vitro cell viability assay. Viability of cells co-cultured with 2:1 MCPM:HA cements was significantly reduced after just 48 h, while viability of cells cultured with the β-TCP-based cements was no different from control cells. In conclusion, this study demonstrates that conversion to HA plays an important role in the degradation of DCPD cements prepared with the MCPM/HA system, affecting both physical properties and cytocompatibility. These results could have important clinical implications for MCPM/HA cements. PMID:22323239

  13. Vibrational spectra and H-bondings in anhydrous and monohydrate {alpha}-Zr phosphates

    SciTech Connect

    Casciola, Mario; Donnadio, Anna; Montanari, Francesca; Piaggio, Paolo Valentini, Valeria

    2007-04-15

    A new FTIR and FT-Raman investigation on {alpha}-zirconium phosphate (Zr(HPO{sub 4}){sub 2}.H{sub 2}O) and its anhydrous form has been performed in order to obtain an affordable assignment of their vibrational spectra as well as to highlight the hydrogen bonding structure formed by the P-OH groups and the intercalated water molecules. To this end the spectral changes induced by both temperature and isotopic exchange were observed on several high-purity grade samples of different morphology especially prepared and well characterized by SEM, RX, DSC and TGA. In particular, it is also presented as a detailed discussion of the results obtained by FTIR-PAS for different sample morphology. The observed spectra have been analyzed and interpreted according to the {alpha}-Zr(HPO{sub 4}){sub 2}.H{sub 2}O crystal structure and H-bond geometry. The obtained results allowed to clarify the mechanism of the {alpha}-Zr(HPO{sub 4}){sub 2}.H{sub 2}O{sup {yields}}{alpha}-Zr(HPO{sub 4}){sub 2} dehydration process as well as the H-bonding changes involved in the high temperature phase transition of anhydrous {alpha}-Zr(HPO{sub 4}){sub 2}. - Graphical abstract: A detailed analysis of the vibrational spectra of {alpha}-zirconium phosphates allowed to obtain an affordable band assignment highlighting the hydrogen bonding structure formed by the P-OH groups and the intercalated water molecules, the dehydration mechanism and the changes in the interlayer region induced by the {alpha} to {beta} phase transition.

  14. Crystal structure of dimanganese(II) zinc bis-[ortho-phosphate(V)] monohydrate.

    PubMed

    Alhakmi, Ghaleb; Assani, Abderrazzak; Saadi, Mohamed; El Ammari, Lahcen

    2015-02-01

    The title compound, Mn2Zn(PO4)2·H2O, was obtained under hydro-thermal conditions. The structure is isotypic with other transition metal phosphates of the type M 3- xM' x (PO4)2·H2O, but shows no statistical disorder of the three metallic sites. The principal building units are distorted [MnO6] and [MnO5(H2O)] octa-hedra, a distorted [ZnO5] square pyramid and two regular PO4 tetra-hedra. The connection of the polyhedra leads to a framework structure. Two types of layers parallel to (-101) can be distinguished in this framework. One layer contains [Zn2O8] dimers linked to PO4 tetra-hedra via common edges. The other layer is more corrugated and contains [Mn2O8(H2O)2] dimers and [MnO6] octa-hedra linked together by common edges. The PO4 tetra-hedra link the two types of layers into a framework structure with channels parallel to [101]. The H atoms of the water mol-ecules point into the channels and form O-H⋯O hydrogen bonds (one of which is bifurcated) with framework O atoms across the channels. PMID:25878806

  15. Crystal structure of dimanganese(II) zinc bis[orthophosphate(V)] monohydrate

    PubMed Central

    Alhakmi, Ghaleb; Assani, Abderrazzak; Saadi, Mohamed; El Ammari, Lahcen

    2015-01-01

    The title compound, Mn2Zn(PO4)2H2O, was obtained under hydrothermal conditions. The structure is isotypic with other transition metal phosphates of the type M 3? xM?x(PO4)2H2O, but shows no statistical disorder of the three metallic sites. The principal building units are distorted [MnO6] and [MnO5(H2O)] octahedra, a distorted [ZnO5] square pyramid and two regular PO4 tetrahedra. The connection of the polyhedra leads to a framework structure. Two types of layers parallel to (-101) can be distinguished in this framework. One layer contains [Zn2O8] dimers linked to PO4 tetrahedra via common edges. The other layer is more corrugated and contains [Mn2O8(H2O)2] dimers and [MnO6] octahedra linked together by common edges. The PO4 tetrahedra link the two types of layers into a framework structure with channels parallel to [101]. The H atoms of the water molecules point into the channels and form OH?O hydrogen bonds (one of which is bifurcated) with framework O atoms across the channels. PMID:25878806

  16. Obtaining Ca(H2PO4)(2)·H2O, monocalcium phosphate monohydrate, via monetite from brushite by using sonication.

    PubMed

    Sánchez-Enríquez, J; Reyes-Gasga, J

    2013-05-01

    Brushite was synthesized by precipitation of calcium chloride (CaCl(2)) and sodium phosphate monobasic (Na(2)HPO(4)) dried in vacuum and monetite was obtained from this brushite by sonication with a frequency of 90kHz at 500W for 90min. Monetite itself was also transformed in Ca(H(2)PO(4))(2)·H(2)O, monocalcium phosphate monohydrate (MCPM), by sonication with a frequency of 90kHz at 500W for 60min followed by lyophilization. The MCPM was sonicated and lyophilized by three times more until reach over 240min, but any other phase transformation was observed. All these phase transformations were analyzed by X-ray diffraction (XRD) and infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) indicated a grain size of about 200nm in all the samples. The morphology observed was a corn-flake-like grain for brushite, a pseudo-needle-like grains for monetite, and lamellar-like grains for MCPM. PMID:23219258

  17. Study on effect of 1,3-dimethyl urea doping on optical properties of L-arginine phosphate monohydrate (LAP) single crystal

    NASA Astrophysics Data System (ADS)

    Wankhade, Pratik M.; Muley, Gajanan G.

    Pure and 1,3-dimethyl urea doped L-arginine phosphate monohydrate (LAP) crystals were grown by a solution growth technique from aqueous solution at a constant temperature. The effect of dopant on the optical properties, crystal structure and second harmonic generation (SHG) efficiency was studied. Dopant modifies the SHG efficiency of the LAP crystal at a greater extent. The SHG efficiency of 0.01 mol% 1,3-dimethyl urea doped LAP crystal corresponds to 1.37 times more as compared to the pure LAP. Absorption and transmission were measured in the spectral range 190-1083 nm. The increase in the optical transparency of the doped crystal is reported. The band gap of the grown crystals has been determined. The presence of the dopant in the doped crystals was confirmed qualitatively by the FT-IR spectroscopy. A slight variation in unit cell parameters has been reported. Thermal and dielectric study of the doped crystal has also been presented.

  18. Effect of sitagliptin treatment on metabolism and cardiac function in genetic diabetic mice.

    PubMed

    Hemmeryckx, Bianca; Swinnen, Melissa; Gallacher, David J; Rong Lu, Hua; Roger Lijnen, H

    2014-01-15

    To investigate the chronic effect of sitagliptin (7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-(3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate, SIT) on metabolism and cardiac function in genetic diabetic Akita mice, 10 weeks old Akita mice were either exposed for 4 months to a high fat and high cholesterol (HF-HC) diet, with or without 10mg/kg/day SIT, or were fed for 3 months with the same diet with or without 50mg/kg/day SIT. SIT treatment of Akita mice at either a low or high dose did not affect body or liver weight. A significant increase in subcutaneous and gonadal fat mass was only observed for the 50mg/kg/day dose of SIT. Furthermore, only the 50mg/kg/day SIT dose resulted in an improvement of glycemic control, as evidenced by a decrease in fasting blood HbA1c levels and an increase in plasma adiponectin levels. Echocardiographic analysis revealed that Akita mice kept on the HF-HC diet with 10mg/kg/day of SIT for 4 months showed an increase in ejection fraction and fractional shortening, whereas the higher dose (50mg/kg/day) had no effect on these parameters, but instead induced left ventricular (LV) hypertrophy as evidenced by an enlarged LV internal diameter, volume and mass. Thus, in the diabetic Akita mouse SIT is cardioprotective at a low dose (10mg/kg/day), whereas improvement of glycemic control requires a higher dose (50mg/kg/day) which, however, induces LV hypertrophy. This mouse model may thus be useful to study the safety of anti-diabetic drugs. PMID:24406339

  19. FT-Raman and high-pressure FT-infrared spectroscopic investigation of monocalcium phosphate monohydrate, Ca(H 2PO 4) 2·H 2O

    NASA Astrophysics Data System (ADS)

    Xu, Jingwei; Gilson, Denis F. R.; Butler, Ian S.

    1998-10-01

    The FT-infrared spectra of monocalcium monohydrate, Ca(H 2PO 4) 2·H 2O, have been measured as a function of pressure up to 50 kbar. A phase transition occurs at 18 kbar. The Lippincott-Schroeder model for the hydrogen bond has been used to explain the pressure dependence of the vibrational frequencies.

  20. From dihydrated iron(III) phosphate to monohydrated ammonium-iron(II) phosphate: Solvothermal reaction mediated by acetone-urea mixtures

    SciTech Connect

    Alfonso, Belen F.; Pique, Carmen; Blanco, Jesus A.

    2012-12-15

    By reaction between synthetic phosphosiderite FePO{sub 4}{center_dot}2H{sub 2}O, urea (NH{sub 2}){sub 2}CO, and acetone (CH{sub 3}){sub 2}CO, we report a novel solvothermal synthesis of polycrystalline NH{sub 4}FePO{sub 4}{center_dot}H{sub 2}O. The preparation of other two individual phases, NH{sub 4}Fe{sub 2}(OH)(PO{sub 4}){sub 2}{center_dot}2H{sub 2}O and NH{sub 4}Fe{sub 2}(PO{sub 4}){sub 2}, is also described. The obtained product is a function of the reaction time and the N/P molar ratio in the reagent mixture, and the existence of structural memory in the dissolution-precipitation processes is discussed. Below 25 K, NH{sub 4}FePO{sub 4}{center_dot}H{sub 2}O behaves magnetically in a complex way, because both ferromagnetic and antiferromagnetic signals are superimposed, suggesting the existence of a canting of iron(II) magnetic moments. - Graphical abstract: Solvothermal synthesis of polycrystalline NH{sub 4}FePO{sub 4}{center_dot}H{sub 2}O is presented. The preparation of other two individual phases, NH{sub 4}Fe{sub 2}(OH)(PO{sub 4}){sub 2}{center_dot}2H{sub 2}O and NH{sub 4}Fe{sub 2}(PO{sub 4}){sub 2} as a function of the N/P molar ratio in the reagent mixture and the reaction time, is also described. Highlights: Black-Right-Pointing-Pointer Solvothermal synthesis of NH{sub 4}FePO{sub 4}{center_dot}H{sub 2}O from an Fe(III) phosphate: reduction process. Black-Right-Pointing-Pointer Formation of two intermediate metastable phases: phase diagram. Black-Right-Pointing-Pointer Thermal decomposition in two steps: mass loss of both water and ammonia. Black-Right-Pointing-Pointer Magnetic behaviour: AF+constant spontaneous magnetization.

  1. Sitagliptin

    MedlinePlus

    ... complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes ( ... diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability ...

  2. Characterization of two cyclic metabolites of sitagliptin.

    PubMed

    Liu, David Q; Arison, Byron H; Stearns, Ralph A; Kim, Dooseop; Vincent, Stella H

    2007-04-01

    Two novel metabolites of the dipeptidyl peptidase inhibitor sitagliptin (MK-0431, (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)-butan-2-amine), were identified after purification from dog urine. The metabolites (referred to as M2 and M5) were characterized by hydrogen/deuterium exchange tandem mass spectrometry and NMR spectroscopy nuclear Overhauser effect experiments as the cis and trans stereoisomers formed by cyclization of the primary amino group with the alpha carbon of the piperazine ring, following oxidative desaturation. PMID:17220240

  3. Rhinorrhea, cough and fatigue in patients taking sitagliptin

    PubMed Central

    2010-01-01

    Sitagliptin is a dipeptidyl peptidase-4 (DPP IV, CD26) inhibitor indicated for treatment of Type II diabetes as a second line therapy after metformin. We report fifteen sitagliptin intolerant patients who developed anterior and posterior rhinorrhea, cough, dyspnea, and fatigue. Symptoms typically developed within 1 to 8 weeks of starting, and resolved within 1 week of stopping the drug. Peak expiratory flow rates increased 34% in 8 patients who stopped sitagliptin. Similar changes were found in 4 out of 5 persons who had confirmatory readministration. Chart review identified 17 patients who tolerated sitagliptin and had no symptomatic changes. The sitagliptin intolerant group had higher rates of clinically diagnosed allergic rhinitis (15/15 vs. 6/18; p = 0.00005), Fisher's Exact test) and angiotensin converting enzyme inhibitor - induced cough (6/13 vs. 1/18; p = 0.012). Nasal and inhaled glucocorticoids may control the underlying allergic inflammation and abrogate this new sitagliptin - induced pharmacological syndrome. Potential mucosal and central nervous system mechanisms include disruption of neuropeptides and/or cytokines that rely on DPP IV for activation or inactivation, and T cell dysfunction. PMID:20462426

  4. Neurobehavioral effects of liraglutide and sitagliptin in experimental models.

    PubMed

    Kamble, Mayur; Gupta, Rachna; Rehan, Harmeet S; Gupta, Lalit K

    2016-03-01

    Glucagon-like peptide (GLP-1) receptor agonists and dipeptidyl peptidase 4 (DPP-4) inhibitors are two currently approved therapies for type 2 diabetes mellitus (T2DM). Present study evaluated the effect of liraglutide (a long-acting GLP-1 agonist) and sitagliptin (a DPP-4 inhibitor) on nociception, anxiety, depression-like behavior and cognition in rats or mice. Nociception was assessed using tail-flick test; anxiety-behavior in open-field test and elevated plus maze (EPM) test while depression-like behavior was evaluated in forced swim test (FST) and tail-suspension test (TST). Cognition was assessed in EPM and Morris water maze (MWM) following memory deficit induced by pentylenetetrazole (PTZ) or scopolamine. In tail-flick test sitagliptin (6mg/kg) produced transient nociceptive effect. Liraglutide (200µg/kg) reduced peripheral square crossings by rats in open field test as well as reduced closed arm entries in the EPM, indicating a decline in exploratory behavior. In FST and TST models for depression, the duration of immobility with sitagliptin (6mg/kg) was reduced significantly in comparison to control group suggesting its antidepressant effect. Liraglutide did not show any antidepressant action. In EPM test for cognition, liraglutide and sitagliptin ameliorated the increase in transfer latency caused by PTZ in a dose-dependent manner. In MWM liraglutide and sitagliptin prevented the scopolamine-induced increase of the escape latency. This study shows that sitagliptin has mild antinociceptive effect and anti-depressant effect in the animal models of depression while liraglutide did not have such an effect. Liraglutide showed anxiogenic effects in the animal models. Both liraglutide and sitagliptin produced cognitive improvement in the animal models. PMID:26849938

  5. Deuterated L-arginine phosphate monohydrate

    SciTech Connect

    Eimerl, D.

    1987-09-29

    An apparatus is described for frequency conversion of light. The apparatus comprises: a laser for generating a laser beam; and at least one crystal according to the formula: (X/sub 2/N)/sub 2/CNX (CH/sub 2/)/sub 3/ CH (NX/sub 3/)/sup +/COO/sup -./ /sup X//sub 3/PO/sub 4/. X/sub 2/O where one or more of the X's represent deuterium replacing hydrogen and with any remaining X locations still being hydrogen. The at least one crystal is placed in the laser beam in an orientation for frequency conversion of the laser beam.

  6. Sitagliptin: new drug. Type 2 diabetes: limited efficacy, too many unknown risks.

    PubMed

    2008-02-01

    (1) Many drugs are available for the treatment of type 2 diabetes, but only metformin and glibenclamide have a proven impact on morbidity and mortality outcomes (only morbidity in the case of glibenclamide). If monotherapy with one of these drugs is inadequately effective, there is a choice of abandoning strict glycaemic control, combining the two drugs, or adding insulin. (2) Sitagliptin, a glucose-lowering inhibitor of DPP-4 (dipeptidyl dipeptidase 4), the enzyme responsible for catabolising physiological incretins, is the latest addition to the list of oral glucose-lowering drugs. (3) Sitagliptin has not been tested for its effect on morbidity or mortality endpoints. (4) Five placebo-controlled trials lasting from 18 to 24 weeks have evaluated sitagliptin monotherapy (3 trials), sitagliptin combined with metformin, or sitagliptin combined with pioglitazone. These trials showed that sitagliptin induced a limited reduction in glycated haemoglobin levels, which usually remained above the cutoff point (7%) generally used to define proper glycaemic controlled. (5) A trial comparing sitagliptin + metformin versus glipizide + metformin, and a direct comparison of sitagliptin versus glipizide, provided a too low level of evidence to convincingly demonstrate the non-inferiority of the sitagliptin combination. (6) In one trial the sitagliptin + metformin combination was significantly more effective on glycated haemoglobin levels than either drug used alone. (7) In the short term, the main adverse effects of sitagliptin are nausea and constipation. In the long term, there is a risk of infections, especially upper respiratory tract infections. Cases of depression have also been reported. Sitagliptin sometimes increases creatinine levels. Pharmacological data suggest there might be an increased risk of cancer and muscular and neurological disorders. (8) In summary, whether used alone or in combination, the antidiabetic effects of sitagliptin, so far studied on surrogate endpoints, are too modest, given the outstanding safety issues, to recommend its use in patients with type 2 diabetes. PMID:18354861

  7. Deacetylnomilin monohydrate

    PubMed Central

    Li, Guo-Qiang; Ye, Yong-Shu; Yang, Yi-Ting; Luo, Hu-Jie; Li, Yao-Lan

    2011-01-01

    In the title compound (systematic name 1-hydroxy-1,2-dihydroobacunoic acid 3,4-lactone monohydrate), C26H32O8H2O, the dihedral angles between the planes of the ester groups and the furan plane are 43.06?(12) and 56.06?(7), while that between the furan plane and the keto group is 58.50?(9). The A/B, B/C and C/D ring junctions are all trans-fused. Intermolecular OH?O hydrogen bonds between the hydroxy and carbonyl groups and the water molecule give rise to a three-dimensional structure. PMID:22065825

  8. Venlafaxine besylate monohydrate.

    PubMed

    Corvalan, Carolina H; Vega, Daniel R

    2013-11-01

    The title compound {systematic name: [2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethyl]dimethylazanium benzene-sulfonate monohydrate}, C17H28NO2 (+)·C6H5O3S(-)·H2O, is a besylate salt hydrate of the anti-depressant drug venlafaxine. In the crystal, besylate anions and water mol-ecules self-assemble, forming hydrogen-bonded dimers linked around inversion centers, with graph set R 4 (4)(6). The crystal packing features a chain of alternate dimers and venlafaxine cations in the b-axis direction with the components linked by O-H⋯O hydrogen bonds and C-H⋯O and C-H⋯π inter-actions. This is the first example of a venlafaxine cation with a closed conformation, as it features an intra-molecular N-H⋯O inter-action involving the protonated N atom. PMID:24454196

  9. Studies on calcium oxalate monohydrate crystallization: influence of inhibitors.

    PubMed

    Grases, F; Kroupa, M; Costa-Bauzá, A

    1994-01-01

    A simple model to study calcium oxalate monohydrate (COM) crystallization on different substrates is presented and the action of different potential inhibitors is evaluated and discussed. COM heterogeneous nucleation was assayed on solid surfaces as calcium phosphate, mixtures of mucin with calcium phosphate, and wax. In the presence of a non-protected non-renewed solid surface in contact with normal urine, COM crystal formation could be detected at short intervals (3 h). The most active heterogeneous nucleation capacity corresponded to calcium phosphate. In the presence of 10% mucin, owing to the renewal of the surface layer no COM crystal were detected on the pellet's surface. The study of citrate and pentosan polysulphate (a semisynthetic polysaccharide) on COM heterogeneous nucleation demonstrated some important inhibitory effects when concentration increased and time decreased. Maximum effects were selectively manifested on calcium phosphate surfaces. Only phytic acid at adequate concentration exhibited a total inhibitory capacity of COM formation, even during longer intervals (15 h). PMID:7521089

  10. Uranyl formate monohydrate spectroscopy

    SciTech Connect

    Porter, J.T. II; Muller, C.H. III; West, W.P.; Malley, M.M.

    1983-10-01

    We report the fluorescence excitation and emission spectra of normal and isotopically labeled uranyl formate monohydrate powder, UO/sub 2/(HCOO)/sub 2/.H/sub 2/O, at 4.2/sup 0/K. Dual fluorescence from the two lowest excited states, I and II, occurs in this compound giving rise to a temperature-dependent lifetime. The lowest vibronic levels are assigned on the basis of the observed oxygen and uranium isotope shifts. The unusual activity and relative frequencies of the symmetric and asymmetric O-U-O stretches in the excited state and can be successfully predicted with the addition of a bond-bond interaction term in addition to the usual valence bond potential. The kinetics of nonresonant energy transfer between isotopic /sup x/OU/sup y/O/sup +2/ antitraps and the U/sup 16/O/sub 2//sup +2/ lattice were measured over the range from 1.7 to 4.2/sup 0/K. The observed rates are in agreement with a quadrupole-quadrupole coupling mechanism accompanied by one and two phonon processes which compensate for the energy defect. The asymmetric lineshapes, broader linewidths and tenfold reduction of absorption intensity for the U/sup 16/O/sub 2//sup +2/ lattice compared to the isolated isotopically doped uranyl ions are attributed to the collective nature of the excited state for the majority species.

  11. Venlafaxine besylate monohydrate

    PubMed Central

    Corvalan, Carolina H.; Vega, Daniel R.

    2013-01-01

    The title compound {systematic name: [2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethyl]dimethylazanium benzene­sulfonate monohydrate}, C17H28NO2 +·C6H5O3S−·H2O, is a besylate salt hydrate of the anti­depressant drug venlafaxine. In the crystal, besylate anions and water mol­ecules self-assemble, forming hydrogen-bonded dimers linked around inversion centers, with graph set R 4 4(6). The crystal packing features a chain of alternate dimers and venlafaxine cations in the b-axis direction with the components linked by O—H⋯O hydrogen bonds and C—H⋯O and C—H⋯π inter­actions. This is the first example of a venlafaxine cation with a closed conformation, as it features an intra­molecular N—H⋯O inter­action involving the protonated N atom. PMID:24454196

  12. 21 CFR 520.1804 - Piperazine phosphate capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Piperazine phosphate capsules. 520.1804 Section... phosphate capsules. (a) Specifications. Each capsule contains 120, 300, or 600 milligrams of piperazine phosphate monohydrate. (b) Sponsor. See No. 051311 in § 510.600(c) of this chapter. (c) Conditions of...

  13. 21 CFR 520.1804 - Piperazine phosphate capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Piperazine phosphate capsules. 520.1804 Section... phosphate capsules. (a) Specifications. Each capsule contains 120, 300, or 600 milligrams of piperazine phosphate monohydrate. (b) Sponsor. See No. 051311 in § 510.600(c) of this chapter. (c) Conditions of...

  14. 21 CFR 520.1804 - Piperazine phosphate capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Piperazine phosphate capsules. 520.1804 Section... phosphate capsules. (a) Specifications. Each capsule contains 120, 300, or 600 milligrams of piperazine phosphate monohydrate. (b) Sponsor. See No. 051311 in § 510.600(c) of this chapter. (c) Conditions of...

  15. 21 CFR 520.1804 - Piperazine phosphate capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Piperazine phosphate capsules. 520.1804 Section... phosphate capsules. (a) Specifications. Each capsule contains 120, 300, or 600 milligrams of piperazine phosphate monohydrate. (b) Sponsor. See No. 051311 in § 510.600(c) of this chapter. (c) Conditions of...

  16. 21 CFR 520.1804 - Piperazine phosphate capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Piperazine phosphate capsules. 520.1804 Section... phosphate capsules. (a) Specifications. Each capsule contains 120, 300, or 600 milligrams of piperazine phosphate monohydrate. (b) Sponsor. See No. 051311 in § 510.600(c) of this chapter. (c) Conditions of...

  17. Efficacy and Safety of Sitagliptin in Japanese Patients With Type 2 Diabetes

    PubMed Central

    Ohmura, Hirotoshi; Mita, Tomoya; Taneda, Yoshinobu; Sugawara, Masahiro; Funayama, Hideaki; Matsuoka, Joe; Watada, Hirotaka; Daida, Hiroyuki

    2015-01-01

    Background The aim of this study was to investigate the clinical efficacy and safety of sitagliptin in Japanese patients with type 2 diabetes. Methods A total of 3,247 subjects treated with sitagliptin were retrospectively recruited. Glucose parameters were collected at baseline, and 1, 3 and 6 months after initiation of sitagliptin. In addition, we explored factors that can be used to predict sitagliptin-induced reduction in HbA1c using linear mixed effect model. Factors associated with hypoglycemic events were examined by logistic analyses. Results We analyzed the available data of 3,201 subjects (1,287 females). Treatment of sitagliptin significantly reduced HbA1c level from 7.441.20% at baseline to 6.730.99% at 6 months (P < 0.0001). Linear mixed effect model analyses demonstrated that reduction of HbA1c was associated with higher baseline HbA1c level, younger age, lower BMI and sitagliptin monotherapy. During this study, 82 cases of hypoglycemia were recorded. Logistic analyses indicated that hypoglycemic events were more frequent in female patients, and patients with low BMI, long history of type 2 diabetes, high HbA1c and on combination therapy experienced. Other adverse events were rare and mild. Conclusions Sitagliptin is effective for diabetic management and generally well tolerated in Japanese patients with type 2 diabetes. This trial was registered with UMIN (no. 000004121). PMID:25699116

  18. Sitagliptin attenuates sympathetic innervation via modulating reactive oxygen species and interstitial adenosine in infarcted rat hearts

    PubMed Central

    Lee, Tsung-Ming; Chen, Wei-Ting; Yang, Chen-Chia; Lin, Shinn-Zong; Chang, Nen-Chung

    2015-01-01

    We investigated whether sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, attenuates arrhythmias through inhibiting nerve growth factor (NGF) expression in post-infarcted normoglycemic rats, focusing on adenosine and reactive oxygen species production. DPP-4 bound adenosine deaminase has been shown to catalyse extracellular adenosine to inosine. DPP-4 inhibitors increased adenosine levels by inhibiting the complex formation. Normoglycemic male Wistar rats were subjected to coronary ligation and then randomized to either saline or sitagliptin in in vivo and ex vivo studies. Post-infarction was associated with increased oxidative stress, as measured by myocardial superoxide, nitrotyrosine and dihydroethidium fluorescent staining. Measurement of myocardial norepinephrine levels revealed a significant elevation in vehicle-treated infarcted rats compared with sham. Compared with vehicle, infarcted rats treated with sitagliptin significantly increased interstitial adenosine levels and attenuated oxidative stress. Sympathetic hyperinnervation was blunted after administering sitagliptin, as assessed by immunofluorescent analysis and western blotting and real-time quantitative RT-PCR of NGF. Arrhythmic scores in the sitagliptin-treated infarcted rats were significantly lower than those in vehicle. Ex vivo studies showed a similar effect of erythro-9-(2-hydroxy-3-nonyl) adenine (an adenosine deaminase inhibitor) to sitagliptin on attenuated levels of superoxide and NGF. Furthermore, the beneficial effects of sitagliptin on superoxide anion production and NGF levels can be reversed by 8-cyclopentyl-1,3-dipropulxanthine (adenosine A1 receptor antagonist) and exogenous hypoxanthine. Sitagliptin protects ventricular arrhythmias by attenuating sympathetic innervation via adenosine A1 receptor and xanthine oxidase-dependent pathways, which converge through the attenuated formation of superoxide in the non-diabetic infarcted rats. PMID:25388908

  19. The risk of pancreatitis with sitagliptin therapy in older adults: a population-based cohort study

    PubMed Central

    McArthur, Eric; Fleet, Jamie L.; Hramiak, Irene; Garg, Amit X.

    2015-01-01

    Background The risk of pancreatitis with sitagliptin use in routine care remains to be established in older patients. We aimed to determine this risk in older adults who were newly prescribed sitagliptin versus an alternative hypoglycemic agent in the outpatient setting. Methods In a population-based retrospective cohort study in Ontario from 2010 until 2012 involving adults aged 66 years and older, we studied those who were newly prescribed sitagliptin or an alternative hypoglycemic agent. Our primary outcome of interest was a hospital encounter (emergency department visit or hospital admission) with acute pancreatitis within 90 days. We used inverse probability of treatment weighting to balance the 2 groups and logistic regression with a robust variance estimate to calculate odds ratios (ORs) and 95% confidence intervals (CIs). Results A total of 57689 patients (mean age 74 yr) were newly prescribed sitagliptin, and 83405 patients (mean age 75 yr) were given an alternative hypoglycemic agent (metformin, glyburide, gliclazide or insulin) during the study period. After weighting, there were no significant differences in measured baseline characteristics between groups. In the weighted sample, sitagliptin was not associated with an increased risk of a hospital encounter with pancreatitis compared with alternative hypoglycemic agents (weighted total 46 of 57689 patients taking sitagliptin [0.08%] v. 48 of 55705 patients taking alternative hypoglycemic agents [0.09%], absolute risk difference 0.01% [95% CI 0.05% to 0.02%], OR 0.92 [95% CI 0.55 to 1.55]). Interpretation Older adults newly prescribed sitagliptin in routine care were not at a substantially higher risk of pancreatitis than those prescribed alternative hypoglycemic agents. These findings are reassuring for those who use or prescribe sitagliptin in the management of type 2 diabetes. PMID:26389095

  20. Acute Pancreatitis in Type 2 Diabetes Treated With Exenatide or Sitagliptin

    PubMed Central

    Garg, Rajesh; Chen, William; Pendergrass, Merri

    2010-01-01

    OBJECTIVE Cases of acute pancreatitis have been reported in association with exenatide, sitagliptin, and type 2 diabetes without use of these medications. It remains unknown whether exenatide or sitagliptin increase the risk of acute pancreatitis. RESEARCH DESIGN AND METHODS A retrospective cohort study of a large medical and pharmacy claims database was performed. Data for 786,656 patients were analyzed. Cox proportional hazard models were built to compare the risk of acute pancreatitis between diabetic and nondiabetic subjects and between exenatide, sitagliptin, and control diabetes medication use. RESULTS Incidence of acute pancreatitis in the nondiabetic control group, diabetic control group, exenatide group, and sitagliptin group was 1.9, 5.6, 5.7, and 5.6 cases per 1,000 patient years, respectively. The risk of acute pancreatitis was significantly higher in the combined diabetic groups than in the nondiabetic control group (adjusted hazard ratio 2.1 [95% CI 1.7–2.5]). Risk of acute pancreatitis was similar in the exenatide versus diabetic control group (0.9 [0.6–1.5]) and sitagliptin versus diabetic control group (1.0 [0.7–1.3]). CONCLUSIONS Our study demonstrated increased incidence of acute pancreatitis in diabetic versus nondiabetic patients but did not find an association between the use of exenatide or sitagliptin and acute pancreatitis. The limitations of this observational claims-based analysis cannot exclude the possibility of an increased risk. PMID:20682680

  1. Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes.

    PubMed

    Gallwitz, Baptist

    2007-01-01

    Novel therapeutic strategies for type 2 diabetes are needed, since the current treatment options neither address all pathophysiological mechanisms nor achieve the glycemic target goals. A general islet-cell dysfunction including insulin- and glucagon-secretion defects contributes to the pathophysiology of type 2 diabetes. Improving islet function by incretin hormone action is a novel therapeutic approach. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are important incretin hormones contributing to 50-70% of the stimulation of insulin secretion after a meal. Dipeptidyl-peptidase IV (DPP-4) inhibitors inhibit the degradation of GLP-1 and GIP as well as that of other regulatory peptides. Sitagliptin, a DPP-4 inhibitor, is orally active and has been shown to be efficacious and safe in clinical studies. Sitagliptin has received approval in Mexico, the United States and other countries. Like other DPP-4 inhibitors, sitagliptin reduces hemoglobin A1c (HbA1c), fasting and postprandial glucose by glucose-dependent stimulation of insulin secretion and inhibition of glucagon secretion. Sitagliptin is weight neutral. Indirect measures show a possible improvement of beta-cell function. Sitagliptin does not cause a higher rate of hypoglycemia in comparison to metformin or placebo. This article gives an overview of the mechanisms of action, pharmacology and clinical trial results of sitagliptin. PMID:17315049

  2. Sitagliptin: profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes (update).

    PubMed

    Gallwitz, Baptist

    2007-11-01

    Novel therapeutic strategies for type 2 diabetes are needed, since the current treatment options neither address all pathophysiological mechanisms nor achieve the glycemic target goals. A general islet-cell dysfunction including insulin- and glucagon-secretion defects contributes to the pathophysiology of type 2 diabetes. Improving islet function by incretin hormone action is a novel therapeutic approach. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are important incretin hormones contributing to 50-70% of the stimulation of insulin secretion after a meal. Dipeptidyl-peptidase IV (DPP-4) inhibitors inhibit the degradation of GLP-1 and GIP as well as that of other regulatory peptides. Sitagliptin, a DPP-4 inhibitor, is orally active and has been shown to be efficacious and safe in clinical studies. Sitagliptin has received approval in Mexico, the United States and other countries. Like other DPP-4 inhibitors, sitagliptin reduces hemoglobin A1c (HbA1c), fasting and postprandial glucose by glucose-dependent stimulation of insulin secretion and inhibition of glucagon secretion. Sitagliptin is weight neutral. Indirect measures show a possible improvement of beta-cell function. Sitagliptin does not cause a higher rate of hypoglycemia in comparison to metformin or placebo. This article gives an overview of the mechanisms of action, pharmacology and clinical trial results of sitagliptin. PMID:18174966

  3. Sitagliptin decreases ventricular arrhythmias by attenuated glucose-dependent insulinotropic polypeptide (GIP)-dependent resistin signalling in infarcted rats

    PubMed Central

    Lee, Tsung-Ming; Chen, Wei-Ting; Chang, Nen-Chung

    2016-01-01

    Myocardial infarction (MI) was associated with insulin resistance, in which resistin acts as a critical mediator. We aimed to determine whether sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, can attenuate arrhythmias by regulating resistin-dependent nerve growth factor (NGF) expression in postinfarcted rats. Normoglycaemic male Wistar rats after ligating coronary artery were randomized to either vehicle or sitagliptin for 4 weeks starting 24 h after operation. Post-infarction was associated with increased myocardial noradrenaline [norepinephrine (NE)] levels and sympathetic hyperinnervation. Compared with vehicle, sympathetic innervation was blunted after administering sitagliptin, as assessed by immunofluorescent analysis of tyrosine hydroxylase, growth-associated factor 43 and neurofilament and western blotting and real-time quantitative RT-PCR of NGF. Arrhythmic scores in the sitagliptin-treated infarcted rats were significantly lower than those in vehicle. Furthermore, sitagliptin was associated with reduced resistin expression and increased Akt activity. Ex vivo studies showed that glucose-dependent insulinotropic polypeptide (GIP) infusion, but not glucagon-like peptide-1 (GLP-1), produced similar reduction in resistin levels to sitagliptin in postinfarcted rats. Furthermore, the attenuated effects of sitagliptin on NGF levels can be reversed by wortmannin (a phosphatidylinositol 3-kinase antagonist) and exogenous resistin infusion. Sitagliptin protects ventricular arrhythmias by attenuating sympathetic innervation in the non-diabetic infarcted rats. Sitagliptin attenuated resistin expression via the GIP-dependent pathway, which inhibited sympathetic innervation through a signalling pathway involving phosphatidylinositol 3-kinase (PI3K) and Akt protein. PMID:26811539

  4. Acute-onset rhabdomyolysis secondary to sitagliptin and atorvastatin interaction

    PubMed Central

    Khan, Muhammad Waqas; Kurian, Saji; Bishnoi, Rohit

    2016-01-01

    Rhabdomyolysis is a serious medical condition in which the skeletal muscle tissue gets damaged and breaks down at rapid rates, potentially leading to death if not managed early on. Rhabdomyolysis in adults has several etiologies such as crush injuries, prolonged immobilization, strenuous exercise, hormonal or metabolic causes, infections, and drug–drug interactions. We present a case report of the interaction of two drugs that are used commonly in the general population. We here discuss a case of a 60-year-old female who presented to the hospital with complaints of generalized weakness, muscle aches, and atypical chest pain for a week after her primary care physician started her on sitagliptin while she was already on atorvastatin. After review of literature, this is the second known case of such an interaction causing acute breakdown of skeletal musculature. PMID:27199569

  5. Sitagliptin with metformin: profile of a combination for the treatment of type 2 diabetes.

    PubMed

    Gallwitz, Baptist

    2007-10-01

    Sitagliptin, a novel orally-active dipeptidyl-peptidase (DPP-4) inhibitor has been introduced into type 2 diabetes therapy. Sitagliptin inhibits the degradation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP), as well as that of other regulatory peptides important for glucose homeostasis. It reduces haemoglobin A1c (HbA1c), fasting and postprandial glucose by glucose- dependent stimulation of insulin secretion and inhibition of glucagon secretion. Sitagliptin is weight neutral. Indirect measures show a possible improvement of beta-cell function. Sitagliptin does not cause hypoglycemia when compared to metformin or placebo. Metformin, which has a different unique mechanism, has been used in type 2 diabetes for approximately 50 years. Metformin improves insulin resistance and is the first-line antidiabetic drug in use today. The combination of a DPP-4 inhibitor with metformin allows a broad and complementary spectrum of antidiabetic actions. This combination does not increase the risk of hypoglycaemia nor does it promote weight gain, an adverse effect of various other oral antidiabetic combinations. This article gives an overview of the data available on the combined antidiabetic effects of metformin and sitagliptin. PMID:17987221

  6. 21 CFR 556.625 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Sodium sulfachloropyrazine monohydrate. 556.625... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate. A tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  7. 21 CFR 556.625 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Sodium sulfachloropyrazine monohydrate. 556.625... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate. A tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  8. 21 CFR 556.625 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Sodium sulfachloropyrazine monohydrate. 556.625... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate. A tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  9. 21 CFR 556.625 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium sulfachloropyrazine monohydrate. 556.625... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate. A tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  10. 21 CFR 556.625 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Sodium sulfachloropyrazine monohydrate. 556.625... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate. A tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  11. Effects of Sitagliptin on Lipid Profiles in Patients With Type 2 Diabetes Mellitus

    PubMed Central

    Fan, Minhua; Li, Yuelan; Zhang, Shihong

    2016-01-01

    Abstract Sitagliptin has been reported to improve lipid profiles, but findings from these studies are conflicting. We conducted this meta-analysis to evaluate the effects of sitagliptin on serum lipids in patients with type 2 diabetes mellitus. We made a comprehensive literature search in PubMed, EMBASE, Cochrane Library, China National Knowledge Infrastructure, Wanfang, and VIP database until June 2015. Eligible studies were randomized clinical trials (RCTs) that investigated the effect of sitagliptin on serum triglycerides (TGs), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), or high-density lipoprotein cholesterol (HDL-C). Eleven RCTs with 2338 patients were identified. Compared with controls, sitagliptin alone or in combination significantly improved serum TG (weighted mean difference [WMD] −0.24 mmol/L; 95% confidence interval [CI] −0.40 to −0.09; P = 0.002) and HDL-C (WMD 0.05 mmol/L; 95% CI 0.02–0.07; P < 0.001).However, no statistical significances were observed in LDL-C (WMD −0.07 mmol/L; 95% CI −0.22 to 0.08; P = 0.337) and TC (WMD −0.14; 95% CI −0.33 to 0.06; P = 0.177). Subgroup analyses revealed that sitagliptin alone achieved greater improvement in serum TG, TC, and HDL-C levels. These findings suggested that sitagliptin alone or in combination significantly improved serum TG and HDL-C levels in patients with type 2 diabetes mellitus. PMID:26765417

  12. Sitagliptin: review of preclinical and clinical data regarding incidence of pancreatitis

    PubMed Central

    Engel, S S; Williams-Herman, D E; Golm, G T; Clay, R J; Machotka, S V; Kaufman, K D; Goldstein, B J

    2010-01-01

    Recent case reports of acute pancreatitis in patients with type 2 diabetes (T2DM) treated with incretin-based therapies have triggered interest regarding the possibility of a mechanism-based association between pancreatitis and glucagon-like peptide-1 mimetics or dipeptidyl peptidase-4 (DPP-4) inhibitors. The objective of this review was to describe the controlled preclinical and clinical trial data regarding the incidence of pancreatitis with sitagliptin, the first DPP-4 inhibitor approved for use in patients with T2DM. Tissue samples from multiple animal species treated with sitagliptin for up to 2 years at plasma exposures substantially in excess of human exposure were evaluated to determine whether any potential gross or histomorphological changes suggestive of pancreatitis occurred. Sections were prepared by routine methods, stained with haematoxylin and eosin and examined microscopically. A pooled analysis of 19 controlled clinical trials, comprising 10,246 patients with T2DM treated for up to 2 years, was performed using patient-level data from each study for the evaluation of clinical and laboratory adverse events. Adverse events were encoded using the Medical Dictionary for Regulatory Activities (MedDRA) version 12.0 system. Incidences of adverse events were adjusted for patient exposure. Tissue samples from preclinical studies in multiple animal species did not reveal any evidence of treatment-related pancreatitis. The pooled analysis of controlled clinical trials revealed similar incidence rates of pancreatitis in patients treated with sitagliptin compared with those not treated with sitagliptin (0.08 events per 100 patient-years vs. 0.10 events per 100 patient-years, respectively). Preclinical and clinical trial data with sitagliptin to date do not indicate an increased risk of pancreatitis in patients with T2DM treated with sitagliptin. PMID:20412332

  13. Sitagliptin protects proliferation of neural progenitor cells in diabetic mice.

    PubMed

    Bachor, Tomás P; Marquioni-Ramella, Melisa D; Suburo, Angela M

    2015-08-01

    Sitagliptin (SIT) is a dipeptidyl peptidase-4 (DPP-4) inhibitor that enhances the effects of incretin hormones, such as Glucose-dependent Insulinotropic Peptide (also known as Gastric Inhibitory Polypeptide, GIP) and Glucagon-Like Peptide 1 (GLP-1). We have now evaluated the effect of SIT on proliferation of neural progenitors in diabetic mice. A condition resembling the non-obese type 2 diabetes mellitus (D2) was achieved by a combination of streptozotocin and nicotinamide (NA-STZ), whereas a type 1-like disease (D1) was provoked by STZ without NA. Non-diabetic mice received vehicle injections. Cell proliferation was estimated by bromodeoxyuridine (BrdU) incorporation in two different regions of the subventricular zone (SVZ), the largest reserve of neural stem cells in the adult brain. SIT treatment did not modify the high fasting blood glucose (BG) levels and intraperitoneal glucose tolerance test (IPGTT) of D1 mice. By contrast, in D2 mice, SIT treatment significantly reduced BG and IPGTT. Both D1 and D2 mice showed a substantial reduction of BrdU labeling in the SVZ. Remarkably, SIT treatment improved BrdU labeling in both conditions. Our findings suggest that SIT would protect proliferation of neural progenitor cells even in the presence of non-controlled diabetic alterations. PMID:25694236

  14. Monohydrated Sulfates in Aurorae Chaos

    NASA Technical Reports Server (NTRS)

    2008-01-01

    This image of sulfate-containing deposits in Aurorae Chaos was taken by the Compact Reconnaissance Imaging Spectrometer for Mars (CRISM) at 0653 UTC (2:53 a.m. EDT) on June 10, 2007, near 7.5 degrees south latitude, 327.25 degrees east longitude. CRISM's image was taken in 544 colors covering 0.36-3.92 micrometers, and shows features as small as 40 meters (132 feet) across. The region covered is roughly 12 kilometers (7.5 miles) wide at its narrowest point.

    Aurorae Chaos lies east of the Valles Marineris canyon system. Its western edge extends toward Capri and Eos Chasmata, while its eastern edge connects with Aureum Chaos. Some 750 kilometers (466 miles) wide, Aurorae Chaos is most likely the result of collapsed surface material that settled when subsurface ice or water was released.

    The top panel in the montage above shows the location of the CRISM image on a mosaic taken by the Mars Odyssey spacecraft's Thermal Emission Imaging System (THEMIS). The CRISM data covers an area featuring several knobs of erosion-resistant material at one end of what appears to be a large teardrop shaped plateau. Similar plateaus occur throughout the interior of Valles Marineris, and they are formed of younger, typically layered rocks that post-date formation of the canyon system. Many of the deposits contain sulfate-rich layers, hinting at ancient saltwater.

    The center left image, an infrared false color image, reveals a swath of light-colored material draped over the knobs. The center right image unveils the mineralogical composition of the area, with yellow representing monohydrated sulfates (sulfates with one water molecule incorporated into each molecule of the mineral).

    The lower two images are renderings of data draped over topography with 5 times vertical exaggeration. These images provide a view of the topography and reveal how the monohydrated sulfate-containing deposits drape over the knobs and also an outcrop in lower-elevation parts of the plateau.

    CRISM is one of six science instruments on NASA's Mars Reconnaissance Orbiter. Led by The Johns Hopkins University Applied Physics Laboratory, Laurel, Md., the CRISM team includes expertise from universities, government agencies and small businesses in the United States and abroad. NASA's Jet Propulsion Laboratory, a division of the California Institute of Technology in Pasadena, manages the Mars Reconnaissance Orbiter and the Mars Science Laboratory for NASA's Science Mission Directorate, Washington. Lockheed Martin Space Systems, Denver, built the orbiter.

  15. Induced Nanocrystallization of Dextrose Monohydrate

    NASA Astrophysics Data System (ADS)

    Johnson, Irudayaraj; Raj, B. Kanickai; Sivagami, V.; Selvi, Naga Pondy

    2013-06-01

    Modern ultrasound induction is very much useful in crystallization process. It uses piezoelectric transducers or quartz crystals to convert mechanical waves to electrical signals and vice versa. Growth of a crystal is environment dependent. The characteristics of grown crystals depend on impurities, temperature, preparation of the solution and mechanical agitation. The properties and size of a crystal can be tailored by controlling any one or all the above factors. The most interesting fact is that the ultrasound influences the properties and size of a crystal. It is found that the characteristics are improved and tailored for a specific need of the industry when a crystal is grown by radiating ultrasonic wave. In some cases, it produces nanocrystals. We used a device which generates the Ultrasonic wave of 15 MHz, which is applied to the crystal right from the time before nucleation till the crystal formation. The Dextrose monohydrate crystals are grown by conventional slow cool batch method. In the same slow cool batch method, Ultrasonic waves of 15 MHz are allowed to pass, influence the nucleation, crystal formation and growing process. The crystal formation process under the exposure of Ultrasound is allowed to continue for a sufficiently long time to yield the desired nanocrystals. The FTIR, UV, microhardness and SEM analysis are taken for the crystals with and without ultrasound.

  16. Chloride- and alkali-containing calcium phosphates as basic materials to prepare calcium phosphate cements.

    PubMed

    Bermúdez, O; Boltong, M G; Driessens, F C; Ginebra, M P; Fernández, E; Planell, J A

    1994-10-01

    Combinations of an alkali-containing calcium phosphate-like rhenanite, sodium whitlockite or calcium potassium phosphate and a chloride-containing calcium phosphate-like spodiosite or chloroapatite with or without additions of other calcium phosphates like monocalcium phosphate monohydrate, dicalcium phosphate or dicalcium phosphate dihydrate were made and mixed with water into pastes. The setting time of these pastes was determined. After soaking for a day in Ringer's solution at 37 degrees C the compressive strength and the diametral tensile strength were determined. Two of the combinations tried in this study resulted in the formation of cements at room temperature. One cement was of the type dicalcium phosphate, whereas the other gave octocalcium phosphate as the solid reaction product. The byproducts formed were an aqueous solution of NaCl and one of K2HPO4, respectively. Applications for bone repair and augmentation are envisaged. PMID:7841290

  17. DPP-4 inhibitor des-F-sitagliptin treatment increased insulin exocytosis from db/db mice {beta} cells

    SciTech Connect

    Nagamatsu, Shinya; Ohara-Imaizumi, Mica; Nakamichi, Yoko; Aoyagi, Kyota; Nishiwaki, Chiyono

    2011-09-09

    Highlights: {yields} Anti-diabetic new drug, DPP-4 inhibitor, can affect the insulin exocytosis. {yields} DPP-4 inhibitor treatment altered syntaxin 1 expression. {yields} Treatment of db/db mice with DPP-4 inhibitor increased insulin release. -- Abstract: Incretin promotes insulin secretion acutely. Recently, orally-administered DPP-4 inhibitors represent a new class of anti-hyperglycemic agents. Indeed, inhibitors of dipeptidyl peptidase-IV (DPP-4), sitagliptin, has just begun to be widely used as therapeutics for type 2 diabetes. However, the effects of sitagliptin-treatment on insulin exocytosis from single {beta}-cells are yet unknown. We therefore investigated how sitagliptin-treatment in db/db mice affects insulin exocytosis by treating db/db mice with des-F-sitagliptin for 2 weeks. Perfusion studies showed that 2 weeks-sitagliptin treatment potentiated insulin secretion. We then analyzed insulin granule motion and SNARE protein, syntaxin 1, by TIRF imaging system. TIRF imaging of insulin exocytosis showed the increased number of docked insulin granules and increased fusion events from them during first-phase release. In accord with insulin exocytosis data, des-F-sitagliptin-treatment increased the number of syntaxin 1 clusters on the plasma membrane. Thus, our data demonstrated that 2-weeks des-F-sitagliptin-treatment increased the fusion events of insulin granules, probably via increased number of docked insulin granules and that of syntaxin 1 clusters.

  18. Effects of 6-Month Sitagliptin Treatment on Metabolic Parameters in Diabetic Patients Taking Oral Glucocorticoids: A Retrospective Cohort Study

    PubMed Central

    Katsuyama, Hisayuki; Sako, Akahito; Adachi, Hiroki; Hamasaki, Hidetaka; Yanai, Hidekatsu

    2015-01-01

    Background There are no guidelines for the treatment of diabetes in patients taking glucocorticoids. We studied to understand the effects of 6-month treatment with sitagliptin on metabolic parameters in diabetic patients taking glucocorticoids. Methods We retrospectively picked up patients who had been prescribed sitagliptin for 6 months during the continuous prescription of oral glucocorticoids between October 2010 and October 2013 by a chart-based analysis, and compared the data before the sitagliptin treatment with the data at 6 months after the sitagliptin treatment started. Results Fifteen patients were eligible for the analyses in our study. The plasma glucose and HbA1c levels were significantly reduced by the sitagliptin treatment. Furthermore, body weight significantly decreased. We found a significant and inverse correlation between the change in HbA1c levels and HbA1c levels at baseline. However, there was no significant correlation between the change in HbA1c levels and the daily glucocorticoid dose at baseline. Conclusions The present study demonstrated that sitagliptin significantly reduced plasma glucose, HbA1c and body weight. Further, sitagliptin was more effective to improve glycemic control in patients taking glucocorticoids with higher HbA1c levels, independently of the daily glucocorticoid dose. PMID:25883713

  19. Inhibition of airway inflammation and remodeling by sitagliptin in murine chronic asthma.

    PubMed

    Nader, Manar A

    2015-12-01

    In this study the role of sitagliptin, dipeptidyl peptidase inhibitor, DPP-4, and dexamethasone in ameliorating inflammation and remodeling of chronic asthma in a mouse model were investigated. Mice sensitized to ovalbumin were chronically challenged with aerosolized antigen for 3days a week continued for 8weeks. During this period animals were treated with sitagliptin or dexamethasone daily. Assessment of inflammatory cell, oxidative markers, total nitrate/nitrite (NOx), interleukin (IL)-13, transforming growth factor-beta1 (TGF-β1) in bronchoalveolar lavage (BAL) and/or lung tissue were done. Also histopathological and immuno-histochemical analysis for lung was carried out. Compared with vehicle alone, treatment with sitagliptin or dexamethasone significantly reduced accumulation of eosinophils and chronic inflammatory cells, subepithelial collagenization, and thickening of the airway epithelium. Also both drug reduced goblet cell hyperplasia, oxidative stress, TGF-β1, IL-13 and epithelial cytoplasmic immunoreactivity for nuclear factor κ-B (NFκ-B). These data indicate that sitagliptin like dexamethasone may play a beneficial role reducing airway inflammation and remodeling in chronic murine model of asthma. PMID:26362207

  20. Regression of Acanthosis Nigricans with the Addition of Sitagliptin and Pioglitazone.

    PubMed

    Adderley-Rolle, E M; Peter, S

    2015-03-01

    Acanthosis nigricans (AN) is a cutaneous disorder associated with various diseases. There are few documented cases of regression of AN. We discuss a case of a 48-year old diabetic woman with resolution of AN after treatment with sitagliptin and pioglitazone. PMID:26360673

  1. Regression of Acanthosis Nigricans with the Addition of Sitagliptin and Pioglitazone

    PubMed Central

    Adderley-Rolle, EM; Peter, S

    2015-01-01

    ABSTRACT Acanthosis nigricans (AN) is a cutaneous disorder associated with various diseases. There are few documented cases of regression of AN. We discuss a case of a 48-year old diabetic woman with resolution of AN after treatment with sitagliptin and pioglitazone. PMID:26360673

  2. Sitagliptin, a DPP-4 Inhibitor, Acutely Inhibits Intestinal Lipoprotein Particle Secretion in Healthy Humans

    PubMed Central

    Xiao, Changting; Dash, Satya; Morgantini, Cecilia; Patterson, Bruce W.

    2014-01-01

    The dipeptidyl peptidase-4 inhibitor sitagliptin, an antidiabetic agent, which lowers blood glucose levels, also reduces postprandial lipid excursion after a mixed meal. The underlying mechanism of this effect, however, is not clear. This study examined the production and clearance of triglyceride-rich lipoprotein particles from the liver and intestine in healthy volunteers in response to a single oral dose of sitagliptin. Using stable isotope tracer techniques and with control of pancreatic hormone levels, the kinetics of lipoprotein particles of intestinal and hepatic origin were measured. Compared with placebo, sitagliptin decreased intestinal lipoprotein concentration by inhibiting particle production, independent of changes in pancreatic hormones, and circulating levels of glucose and free fatty acids. Fractional clearance of particles of both intestinal and hepatic origin, and production of particles of hepatic origin, were not affected. This pleiotropic effect of sitagliptin may explain the reduction in postprandial lipemia seen in clinical trials of this agent and may provide metabolic benefits beyond lowering of glucose levels. PMID:24584549

  3. Safety and tolerability of sitagliptin in patients with type 2 diabetes: a pooled analysis

    PubMed Central

    Williams-Herman, Debora; Round, Elizabeth; Swern, Arlene S; Musser, Bret; Davies, Michael J; Stein, Peter P; Kaufman, Keith D; Amatruda, John M

    2008-01-01

    Background Sitagliptin, a highly selective dipeptidyl peptidase-4 inhibitor, is the first in a new class of oral antihyperglycemic agents (AHAs) for the treatment of patients with type 2 diabetes. Type 2 diabetes is a life-long disease requiring chronic treatment and management. Therefore, robust assessment of the long-term safety and tolerability of newer therapeutic agents is of importance. The purpose of this analysis was to assess the safety and tolerability of sitagliptin by pooling 12 large, double-blind, Phase IIb and III studies up to 2 years in duration. Methods: This analysis included 6139 patients with type 2 diabetes receiving either sitagliptin 100 mg/day (N = 3415) or a comparator agent (placebo or an active comparator) (N = 2724; non-exposed group). The 12 studies from which this pooled population was drawn represent the double-blind, randomized, Phase IIB and III studies that included patients treated with the clinical dose of sitagliptin (100 mg/day) for at least 18 weeks up to 2 years and that were available in a single safety database as of November 2007. These 12 studies assessed sitagliptin as monotherapy, initial combination therapy with metformin, or add-on combination therapy with other oral AHAs (metformin, pioglitazone, sulfonylurea, sulfonylurea + metformin, or metformin + rosiglitazone). Patients in the non-exposed group were taking placebo, pioglitazone, metformin, sulfonylurea, sulfonylurea + metformin, or metformin + rosiglitazone. This safety analysis used patient-level data from each study to evaluate clinical and laboratory adverse experiences. Results For clinical adverse experiences, the incidence rates of adverse experiences overall, serious adverse experiences, and discontinuations due to adverse experiences were similar in the sitagliptin and non-exposed groups. The incidence rates of specific adverse experiences were also generally similar in the two groups, with the exception of an increased incidence rate of hypoglycemia observed in the non-exposed group. The incidence rates of drug-related adverse experiences overall and discontinuations due to drug-related adverse experiences were higher in the non-exposed group, primarily due to the increased incidence rate of hypoglycemia in this group. For cardiac- and ischemia-related adverse experiences (including serious events), there were no meaningful between-group differences. No meaningful differences between groups in laboratory adverse experiences, either summary measures or specific adverse experiences, were observed. Conclusion In patients with type 2 diabetes, sitagliptin 100 mg/day was well tolerated in clinical trials up to 2 years in duration. PMID:18954434

  4. Comparison between sitagliptin and nateglinide on postprandial lipid levels: The STANDARD study

    PubMed Central

    Kojima, Yuichi; Kaga, Hideyoshi; Hayashi, Shinu; Kitazawa, Toru; Iimura, Yuko; Ohno, Makoto; Yoshitsugu, Michiyasu; Fujiwara, Mutsunori; Hiyoshi, Toru

    2013-01-01

    AIM: To assess the effects of sitagliptin and nateglinide on lipid metabolism. METHODS: In a parallel group comparative open trial, patients with type 2 diabetes mellitus under treatment at the Japanese Red Cross Medical Center were randomly assigned to receive either sitagliptin (50 mg once daily) or nateglinide (90 mg three times daily before meals). Eligible patients met the following criteria: age ? 20 years; hemoglobin A1c (HbA1c) > 6.5% despite diet and exercise; HbA1c between 6.5% and 8.0%; fasting glucose < 7.77 mmol/L; diet and exercise therapy for more than 3 mo; and ability to read and understand the information for written informed consent. Exclusion criteria were contraindications to sitagliptin, contraindications to nateglinide, pregnancy or possible pregnancy, and severe liver/renal failure. Patients who were considered to be unsuitable by the attending physician for other reasons were also excluded. Blood samples were collected at one and three hours after intake of a test meal. The primary outcome measure was the area under the curve (AUC) of apolipoprotein (Apo) B48 at three hours postprandially. RESULTS: Twenty patients were randomly assigned to the sitagliptin group and sixteen patients were randomized to the nateglinide group. All 36 patients took the medication as directed by the physician in both groups, and they all were analyzed. Apart from antidiabetic drugs, there was no difference between the two groups with respect to the frequency of combined use of lipid-lowering, antihypertensive, and/or antiplatelet drugs. The doses of these medications were maintained during 12 wk of treatment. Detailed dietary advice, together with adequate exercise therapy, was given to the patients so that other factors apart from the two test drugs were similar in the two groups. There were no significant differences of the baseline characteristics between the two groups, except for body mass index (the sitagliptin group: 25.14 3.05 kg/m2; the nateglinide group: 21.39 2.24 kg/m2). Fasting levels of HbA1c, glycated albumin, 1.5-anhydroglucitol, and blood glucose, as well as the blood glucose levels at one and three hours postprandially, improved in both groups after 12 wk of treatment, and there were no significant differences between the two groups. However, the glucagon level at one hour postprandially (P = 0.040) and the diastolic blood pressure (P < 0.01) only showed a significant decrease in the sitagliptin group. In the nateglinide group, there was no significant change in the AUC of Apo B48, the glucagon level at one hour postprandially, the fasting triglyceride level, or the diastolic blood pressure. Body weight was unchanged in both groups. However, the AUC of Apo B48 at three hours postprandially showed a significant decrease in the sitagliptin group from 2.48 0.11 at baseline to 1.94 0.78 g/L per hour after 12 wk (P = 0.019). The fasting triglyceride level also decreased significantly in the sitagliptin group (P = 0.035). With regard to lipid-related markers other than Apo B48 and fasting triglycerides, no significant changes were observed with respect to Apo A1, Apo B, or Apo C3 in either group. No adverse events occurred in either group. CONCLUSION: Sitagliptin significantly improves some lipid parameters while having a comparable effect on blood glucose to nateglinide. A large-scale prospective study of sitagliptin therapy is warranted. PMID:23493856

  5. Crystal structure of monobasic sodium tartrate monohydrate

    SciTech Connect

    Titaeva, E. K. Somov, N. V.; Portnov, V. N.; Titaev, D. N.

    2015-01-15

    Crystals of a new polymorphic modification of monobasic sodium tartrate monohydrate NaHC{sub 4}H{sub 4}O{sub 6} · H{sub 2}O have been grown in a metasilicate gel. Their atomic structure is solved by X-ray diffraction.

  6. The tableting properties of melibiose monohydrate.

    PubMed

    Lakio, Satu; Sainio, Janne; Heljo, Petteri; Ervasti, Tuomas; Kivikero, Niina; Juppo, Anne

    2013-11-18

    In this research, the tableting properties of α-melibiose monohydrate were studied. Melibiose is a disaccharide which bears structural resemblance to lactose, because they both consist of galactose and glucose monosaccharide subunits. Compactibility and deformation behavior of two melibiose batches from different suppliers were studied and compared with α-lactose monohydrate and some other typical tableting excipients. Differences in the deformation behavior were determined comparing the shape of the Heckel plots, the yield pressure values and the strain rate sensitivity (SRS) indexes. In addition, the effect of moisture on the tabletability was studied. According to the yield pressures and SRS indexes melibiose was concluded to be fragmenting, even at higher degree than lactose monohydrate. However, the overall deformation behavior of melibiose was found to be similar to that of lactose monohydrate. Increase in moisture content resulted in higher tensile strengths of tablets for both melibiose batches, but it seemed to have more effect on compactibility of the other batch. In conclusion, melibiose has potential to be used as an excipient in tablet formulations. PMID:23994759

  7. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 2 2013-04-01 2013-04-01 false Dextrose monohydrate. 168.111 Section 168.111 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners...

  8. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 2 2012-04-01 2012-04-01 false Dextrose monohydrate. 168.111 Section 168.111 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners...

  9. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 2 2014-04-01 2014-04-01 false Dextrose monohydrate. 168.111 Section 168.111 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners...

  10. Effects of metformin and sitagliptin on glycolipid metabolism in type 2 diabetic rats on different diets

    PubMed Central

    Yang, Juhong; Ba, Tu; Chen, Liming; Shan, Chunyan; Zheng, Miaoyan; Wang, Ying; Ren, Huizhu; Chen, Jingli; Xu, Jie; Han, Fei; Zhang, Yi; Yang, Xiaoyun

    2016-01-01

    Introduction The aim of the study was to investigate the effects of metformin and sitagliptin on glycolipid metabolism in type 2 diabetes after different diets. Material and methods Seventy Male Sprague Dawley rats were fed with a high fat diet followed by streptozotocin treatment to induce type 2 diabetes. Then all rats were randomly divided into a control group, a metformin group (200 mg/kg), and a sitagliptin group (10 mg/kg). Each group was further divided into 4 groups receiving one load of high carbohydrate diet (45% glucose, 4.5 ml/kg), high fat diet (20% lipid emulsion, 4.5 ml/kg), high protein diet (20% whey protein, 10 ml/kg) or mixed meal, respectively. The caloric densities were all 33 kJ/kg. Postprandial blood glucose (P2BG), triglyceride (TG), glucagon-like peptide-1 (GLP-1), glucagon and insulin levels were measured. Results In the high carbohydrate group, sitagliptin was more efficient in lowering P2BG compared with metformin (p < 0.05). In the high-fat group, metformin was more powerful in lowering TG (p < 0.05) and P2BG (p < 0.05) levels because of its improvement of insulin sensitivity. In the high protein diet group, metformin did not reduce the P2BG level (p > 0.05), although it did reduce the TG level (p < 0.05). In the mixed diet group, metformin was more efficient in lowering P2BG (p < 0.05) but had a similar effect on TG (p > 0.05) compared with sitagliptin. Conclusions In the type 2 diabetic model, metformin and sitagliptin have different effects on glycolipid metabolism after different diets. If it is proved in type 2 diabetic patients, then different medicines may be recommended according to different diets in order to improve glycolipid metabolism. PMID:27186166

  11. Preliminary Study Characterizing the Use of Sitagliptin for Glycemic Control in Healthy Beagle Dogs with Normal Gluco-Homeostasis

    PubMed Central

    ODA, Hitomi; MORI, Akihiro; LEE, Peter; SAEKI, Kaori; ARAI, Toshiro; SAKO, Toshinori

    2014-01-01

    ABSTRACT Sitagliptin is a dipeptidyl peptidase-4 inhibitor aimed at treating Type 2 diabetes mellitus (T2DM) and T1DM, by increasing blood levels of Glucagon-like peptide 1 (GLP-1) and insulin. The objective of this preliminary study is to characterize Sitagliptin’s ability for glycemic control, in healthy dogs under an oral glucose tolerance test (OGTT) environment. Overall, Sitagliptin did not result in any significant changes to temporal glucose and insulin concentrations. However, a ~55% increase in median total GLP-1 AUC0–120min was observed, as compared to baseline control in healthy dogs (n=5), thus indicating a similar mode of action of Sitagliptin between healthy dogs and humans. Future studies to validate the use of Sitagliptin with dogs suffering from insulin independent diabetes are warranted. PMID:24931645

  12. Sitagliptin can inhibit the development of hepatic steatosis in high-fructose diet-fed ob/ob mice

    PubMed Central

    Sujishi, Tetsuya; Fukunishi, Shinya; Ii, Masaaki; Nakamura, Ken; Yokohama, Keisuke; Ohama, Hideko; Tsuchimoto, Yusuke; Asai, Akira; Tsuda, Yasuhiro; Higuchi, Kazuhide

    2015-01-01

    The beneficial effect of dipeptidyl peptidase-4 inhibition on diet-induced extra-pancreatic effects, especially on liver tissue remains poorly understood. Thus, we made the experimental designs as follows; five-week-old male ob/ob mice, which develop type 2 diabetic mellitus and nonalcoholic fatty liver disease by taking a high-carbohydrate diet (HCD), were divided into a group in which a HCD was given for 8 weeks as control, and another in which a HCD added with 0.0018% sitagliptin was given for 8 weeks. Hepatic steatosis was seen in all mice, but the mean grade of steatosis in the sitagliptin-administrated mice was significantly decreased. The acetyl-CoA concentrations were lower in sitagliptin-administrated mice, although the differences were not significant. However, the malonyl-CoA concentrations were significantly lower in sitagliptin-administrated mice. The expression of acetyl-CoA carboxylase 1 was inhibited in sitagliptin-administrated mice, irrespective of expressions of carbohydrate responsive element-binding protein (ChREBP) or sterol regulatory element-binding protein (SREBP)-1c. In conclusion, sitagliptin may affect the development of nonalcoholic fatty liver disease by inhibiting the production of malonyl-CoA and thus synthesis of fatty acids in the liver. PMID:26566312

  13. Pholcodine monohydrate: Crystal structure and polymorphism

    NASA Astrophysics Data System (ADS)

    Petruševski, Gjorgji; Zbačnik, Marija; Kajdžanoska, Marina; Ugarkovic, Sonja; Trimčeski, Vase; Kaitner, Branko; Jovanovski, Gligor; Makreski, Petre

    2013-07-01

    The first crystal structure elucidation of pholcodine monohydrate, an important antitussive active pharmaceutical ingredient is reported herein. The studied compound crystallizes in the orthorhombic system in the space group P212121. Each H2O molecule is shared by two pholcodine molecules via three strong hydrogen bonds. The detailed crystallization screening from several different organic solvents afforded single crystals with various quality, all exhibiting prism-to-needlelike micro morphology. The investigation of the obtained single crystals by means of several physico-chemical, solid-state instrumental techniques (FT-IR, DSC, TG/DTG and XRPD) proved that pholcodine monohydrate exists in a single crystalline modification, identical to the commercial form of the compound.

  14. Dehydration of cytosine monohydrate at physiological temperatures

    SciTech Connect

    Martel, P.; Powell, B.M.

    1983-01-01

    Neutron diffraction, thermogravimetric, and mass spectrographic measurements have been used to show that cytosine monohydrate loses its water of hydration at physiological temperatures (approx. = 37/sup 0/C) and converts to cytosine. The ''activation energy'' for the dehydration process has been determined from isothermal weight curves and is 27.1 +/- 0.6 kcal . mol/sup -1/. It is suggested that pyrimidine dehydration may be involved in structural changes in DNA.

  15. Iatrogenic angioedema associated with ACEi, sitagliptin, and deficiency of 3 enzymes catabolizing bradykinin.

    PubMed

    Beaudouin, E; Defendi, F; Picaud, J; Drouet, C; Ponard, D; Moneret-Vautrin, D A

    2014-05-01

    New concepts of idiopathic and iatrogenic angioedema underline the role of bradykinin, and the importance of catabolizing enzymes. A case is described of Angiotensin converting enzyme inhibitor (ACEi) and sitagliptin induced angioedema, where AO attacks decreased after the withdrawal of lisinopril but resolved only after the withdrawal of sitagliptin, an inhibitor of dipeptylpeptidase IV. ACE, aminopeptidase P and carboxypeptidase N were decreased down to 17%, 42%, 64% of median references values, and remained low one year after the interruption of these drugs: 56%, 28% and 50%, respectively. The combined deficiency of APP and CPN might enhance the inhibiting effect of the DPP IV inhibitor. The fact that this triple deficiency remained latent before and after the treatment indicates that searching for latent enzyme deficiencies should be carried out when there is intention to treat with a combination of drugs interfering with the bradykinin metabolism. PMID:24853572

  16. Catalytic Enantioselective Allylic Amination of Olefins for the Synthesis of ent-Sitagliptin

    PubMed Central

    Bao, Hongli; Bayeh, Liela; Tambar, Uttam K.

    2014-01-01

    The presence of nitrogen atoms in most chiral pharmaceutical drugs has motivated the development of numerous strategies for the synthesis of enantioenriched amines. Current methods are based on the multi-step transformation of pre-functionalized allylic electrophiles into chiral allylic amines. The enantioselective allylic amination of unactivated olefins represents a more direct and attractive strategy. We report the enantioselective synthesis of ent-sitagliptin via an allylic amination of an unactivated terminal olefin. PMID:25378809

  17. Sitagliptin/Simvastatin: a first combination tablet to treat type 2 diabetes and hypercholesterolemia – a review of its characteristics

    PubMed Central

    Ramadan, Wijdan H; Kabbara, Wissam K

    2015-01-01

    Background The purpose of this study was to review the current literature and information on the combination product Juvisync™ (sitagliptin + simvastatin), which was approved by the US Food and Drug Administration in October 2011. Methods PubMed (2001–2014) was searched for primary and review articles on sitagliptin, simvastatin, or the combination product. Drug manufacturing data and product labeling were also used. Studies of simvastatin, sitagliptin, or the combination were screened and analyzed to include relevant and recent papers. Selected English language trials were limited to those with human subjects and included both safety and efficacy outcomes. Results When compared with glipizide as add-on therapy to metformin, sitagliptin was noninferior but had lower rates of hypoglycemia and weight gain. In addition, when compared with insulin glargine, sitagliptin was less effective in decreasing glycosylated hemoglobin, but was associated with significantly lower rates of hypoglycemia. Further, trials have shown a beneficial effect of using statins in patients with diabetes mellitus with regard to decreasing cardiovascular risk, regardless of baseline lipid levels or the presence of a cardiac disease. Both medications have also demonstrated an acceptable side effect profile. However, caution is needed when coadministering with any drug that may increase simvastatin levels to reduce the risk of myopathy and rhabdomyolysis. Conclusion Juvisync should be used in patients requiring both sitagliptin and simvastatin. Both agents have shown good efficacy and acceptable safety profiles. Sitagliptin is a good option for diabetic patients to improve glycemic control with a lower risk of hypoglycemia and weight gain. PMID:25709467

  18. A Case of Severe Acute Necrotizing Pancreatitis after Administration of Sitagliptin

    PubMed Central

    Sue, Mariko; Yoshihara, Aya; Kuboki, Koji; Hiroi, Naoki; Yoshino, Gen

    2013-01-01

    A 55-year-old Japanese man with a 3-year history of type 2 diabetes mellitus was admitted to our hospital for upper abdominal pain. Control of diabetes mellitus was good with voglibose and metformin, with sitagliptin added to this regimen 8 months prior. His pancreatic enzyme levels were elevated, and abdominal computed tomography (CT) showed diffuse pancreatic swelling with fluid accumulation and ascites of CT grade 3. The patient was diagnosed with severe acute pancreatitis. There were no obvious causes for pancreatitis except the recently administered sitagliptin. Since incretin-related drugs entered the market, the number of incretin-related drugs prescriptions rapidly increased and so did the incidence of pancreatitis. There are several reports suggesting the correlation between incretin-related drugs and pancreatitis, such as a report based on data obtained from the United States Food and Drug Administration (FDA) which revealed a significant correlation between the administration of exenatide or sitagliptin and pancreatitis. However, there also is a report that denied the evidence for such in a large cohort study. The relation between incretin based drugs and pancreatitis is still controversial. PMID:23467428

  19. One year remission of type 1 diabetes mellitus in a patient treated with sitagliptin

    PubMed Central

    Guerra-Alcalá, Ernesto; Contreras, Miguel; Nastasi, José; Noble, Janelle A; Polychronakos, Constantin

    2014-01-01

    Summary Type 1 diabetes mellitus (T1DM) is a chronic disease characterized by the autoimmune destruction of pancreatic β-cells. This paper describes the case of a 19-year-old male patient who presented with glutamic acid decarboxylase (GAD) antibody positive and diabetic ketoacidosis, which mandated intensive insulin treatment. Once the ketoacidosis was controlled, an oral dose of 100 mg of sitagliptin was administered once a day. Ketoacidosis was managed by insulin and insulin daily requirement began to dwindle after one month, until its complete withdrawal at 8 weeks, when partial remission was reached. The patient has now remained on sitagliptin treatment alone for a year, without requiring insulin. The benefit observed with this medication is possibly associated with its immunological effects. Inhibition of dipeptidyl peptidase 4 in animal models deregulates the Th1 immune response, increases secretion of Th2 cytokines, activates CD4+CD25+FoxP3+ regulatory T-cells, and prevents IL17 production. Learning points The use of insulin-dose-adjusted HbA1c constitutes the best way to define partial remission in T1DM patients.The use of sitagliptin in T1DM patients could help to decrease daily requirement of insulin by delaying β-cell loss and improving endogenous insulin production.The determination of antibodies against insulin, islet cells, and GAD permits differentiation of T1DM patients from those with atypical or ketosis-prone diabetes. PMID:25332771

  20. 21 CFR 520.608 - Dicloxacillin sodium monohydrate capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Dicloxacillin sodium monohydrate capsules. 520.608 Section 520.608 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Dicloxacillin sodium monohydrate capsules. (a) Specifications. Each capsule contains dicloxacillin...

  1. 21 CFR 520.2184 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium sulfachloropyrazine monohydrate. 520.2184... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2184 Sodium sulfachloropyrazine monohydrate. (a) Chemical name. 2-Sulfamido-6-chloroxyrazine, sodium. (b) Sponsor. See Nos....

  2. 21 CFR 520.608 - Dicloxacillin sodium monohydrate capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Dicloxacillin sodium monohydrate capsules. 520.608 Section 520.608 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Dicloxacillin sodium monohydrate capsules. (a) Specifications. Each capsule contains dicloxacillin...

  3. 21 CFR 520.2184 - Sodium sulfachloropyrazine monohydrate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Sodium sulfachloropyrazine monohydrate. 520.2184... (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2184 Sodium sulfachloropyrazine monohydrate. (a) Chemical name. 2-Sulfamido-6-chloroxyrazine, sodium. (b) Sponsor. See Nos....

  4. 21 CFR 520.608 - Dicloxacillin sodium monohydrate capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Dicloxacillin sodium monohydrate capsules. 520.608 Section 520.608 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Dicloxacillin sodium monohydrate capsules. (a) Specifications. Each capsule contains dicloxacillin...

  5. 21 CFR 520.608 - Dicloxacillin sodium monohydrate capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Dicloxacillin sodium monohydrate capsules. 520.608 Section 520.608 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Dicloxacillin sodium monohydrate capsules. (a) Specifications. Each capsule contains dicloxacillin...

  6. Does Sitagliptin Affect the Rate of Osteoporotic Fractures in Type 2 Diabetes? Population-Based Cohort Study

    PubMed Central

    Josse, Robert G.; Lin, Mu; Eurich, Dean T.

    2016-01-01

    Context: Type 2 diabetes and osteoporosis are both common, chronic, and increase with age, whereas type 2 diabetes is also a risk factor for major osteoporotic fractures (MOFs). However, different treatments for type 2 diabetes can affect fracture risk differently, with metaanalyses showing some agents increase risk (eg, thiazolidinediones) and some reduce risk (eg, sitagliptin). Objective: To determine the independent association between new use of sitagliptin and MOF in a large population-based cohort study. Design, Setting, and Subjects: A sitagliptin new user study design employing a nationally representative Unites States claims database of 72 738 insured patients with type 2 diabetes. We used 90-day time-varying sitagliptin exposure windows and controlled confounding by using multivariable analyses that adjusted for clinical data, comorbidities, and time-updated propensity scores. Main Outcomes: We compared the incidence of MOF (hip, clinical spine, proximal humerus, distal radius) in new users of sitagliptin vs nonusers over a median 2.2 years follow-up. Results: At baseline, the median age was 52 years, 54% were men, and median A1c was 7.5%. There were 8894 new users of sitagliptin and 63 834 nonusers with a total 181 139 person-years of follow-up. There were 741 MOF (79 hip fractures), with 53 fractures (4.8 per 1000 person-years) among new users of sitagliptin vs 688 fractures (4.0 per 1000 person-years) among nonusers (P = .3 for difference). In multivariable analyses, sitagliptin was not associated with fracture (adjusted hazard ratio 1.1, 95% confidence interval 0.8–1.4; P = .7), although insulin (P < .001), sulfonylureas (P < .008), and thiazolidinedione (P = .019) were each independently associated with increased fracture risk. Conclusions: Even in a young population with type 2 diabetes, osteoporotic fractures were not uncommon. New use of sitagliptin was not associated with fracture, but other commonly used second-line agents for type 2 diabetes were associated with increased risk. These data should be considered when making treatment decisions for those with type 2 diabetes at particularly high risk of fractures. PMID:26930183

  7. [Quantification of sitagliptin in human plasma and urine by LC-MS/MS method and its application].

    PubMed

    Zhao, Qian; Wang, Bo-ya; Jiang, Ji; Hu, Pei

    2015-06-01

    A rapid and sensitive liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method for quantification of sitagliptin in human plasma and urine had been developed. This method was applied to the pharmacokinetics study of sitagliptin tablet after single- and multiple-dosing in Chinese population. Plasma samples were prepared by a liquid-liquid extracted method, and urine samples were diluted. Compounds were analyzed by multiple reaction monitoring (MRM) mode with a electrospray ionization (ESI) interface. Mobile phase consisted of methanol and water (85 : 15, v/v). The linear concentration range of calibration curve was 0.5-1 000 ng.mL-1. and 0.2-100 µg.mL , intra-run/between-run accuracy was 98.98%-103.69% and 97.63%-102.29%, intra-run/between-run precision was <5.51% and 4.26% for plasma and urine sample, respectively. The stability of sitagliptin stock solution was tested for 55 days at -30 °C. Sitagliptin was stable when stored under the following conditions: 24 hours in the autosampler after sample preparation; 24 hours at room temperature, after 3 freeze and thaw cycles (from -30 °C to room temperature), 40 days at -30 °C for plasma and urine samples. The absolute recovery in plasma was 71.1%, and no matrix effect was founded. This method was proved simple, specific, sensitive, rapid and suitable for pharmacokinetics study of sitagliptin in human being. PMID:26521442

  8. Effects of Sitagliptin Treatment on Dysmetabolism, Inflammation, and Oxidative Stress in an Animal Model of Type 2 Diabetes (ZDF Rat)

    PubMed Central

    Ferreira, Liliana; Teixeira-de-Lemos, Edite; Pinto, Filipa; Parada, Belmiro; Mega, Cristina; Vala, Helena; Pinto, Rui; Garrido, Patrícia; Sereno, José; Fernandes, Rosa; Santos, Paulo; Velada, Isabel; Melo, Andreia; Nunes, Sara; Teixeira, Frederico; Reis, Flávio

    2010-01-01

    The purpose of this paper is to evaluate the chronic effect of sitagliptin on metabolic profile, inflammation, and redox status in the Zucker Diabetic Fatty (ZDF) rat, an animal model of obese type 2 diabetes. Diabetic and obese ZDF (fa/fa) rats and their controls (ZDF +/+) were treated during 6 weeks with vehicle (control) and sitagliptin (10 mg/kg/bw). Glucose, HbA1c, insulin, Total-c, TGs, IL-1β, TNF-α, CRPhs, and adiponectin were assessed in serum and MDA and TAS in serum, pancreas, and heart. Pancreatic histology was also evaluated. Sitagliptin in diabetic rats promoted a decrease in glucose, HbA1c, Total-c, and TGs accompanied by a partial prevention of insulinopenia, together, with a decrease in CRPhs and IL-1β. Sitagliptin also showed a positive impact on lipid peroxidation and hypertension prevention. In conclusion, chronic sitagliptin treatment corrected the glycaemic dysmetabolism, hypertriglyceridaemia, inflammation, and hypertension, reduced the severity of the histopathological lesions of pancreatic endocrine and exocrine tissues, together with a favourable redox status, which might be a further advantage in the management of diabetes and its proatherogenic comorbidities. PMID:20652060

  9. Di-peptidyl peptidase-4 inhibitor sitagliptin protects vascular function in metabolic syndrome: possible role of epigenetic regulation.

    PubMed

    Cicek, Figen Amber; Amber, Cicek Figen; Tokcaer-Keskin, Zeynep; Zeynep, Tokcaer-Keskin; Ozcinar, Evren; Evren, Ozcinar; Bozkus, Yosuf; Yusuf, Bozkus; Akcali, Kamil Can; Can, Akcali Kamil; Turan, Belma; Belma, Turan

    2014-08-01

    Metabolic syndrome (MetS) is a complex medical disorder characterized by insulin resistance, hypertension, and high risk of coronary disease and stroke. Microvascular rarefaction and endothelial dysfunction have also been linked with MetS, and recent evidence from clinical studies supports the efficacy of incretin-based antidiabetic therapies for vascular protection in diabetes. Previous studies pointed out the importance of dipeptidyl peptidase-4 (DPP-4) inhibition in endothelial cells due to getting protection against metabolic pathologies. We therefore aimed to investigate the acute effects of a DPP-4 inhibitor, sitagliptin, on vascular function in rats with high-sucrose diet-induced MetS. In order to elucidate the mechanisms implicated in the effects of DPP-4 inhibition, we tested the involvement of NO pathway and epigenetic regulation in the MetS. Acute use of sitagliptin protects the vascular function in the rats with MetS in part due to NO pathway via restoring the depressed aortic relaxation responses mediated by receptors. Application of sitagliptin enhanced the depressed phosphorylation levels of both the endothelial NO synthase and the apoptotic status of protein kinase B, known as Akt, in endothelium-intact thoracic aorta from rats with MetS. One-hour application of sitagliptin on aortic rings from rats with MetS also induced remarkable histon posttranslational modifications such as increased expression of H3K27Me3, but not of H3K27Me2, resulting in an accumulation of the H3K27Me3. Our findings suggest that, in addition to its well-known hypoglycemic action, sitagliptin may also have beneficial effects on hyperglycemia-induced vascular changes in an endotheium-dependent manner. These present results with sitagliptin aside from the glycaemic control, may demonstrate its important role in the treatment of patients with MetS. PMID:24838371

  10. Comparative safety and effectiveness of sitagliptin in patients with type 2 diabetes: retrospective population based cohort study

    PubMed Central

    Simpson, S; Senthilselvan, A; Asche, C V; Sandhu-Minhas, J K; McAlister, F A

    2013-01-01

    Objective To determine if the use of sitagliptin in newly treated patients with type 2 diabetes is associated with any changes in clinical outcomes. Design Retrospective population based cohort study. Setting Large national commercially insured US claims and integrated laboratory database. Participants Inception cohort of new users of oral antidiabetic drugs between 2004 and 2009 followed until death, termination of medical insurance, or December 31 2010. Main outcome measure Composite endpoint of all cause hospital admission and all cause mortality, assessed with time varying Cox proportional hazards regression after adjustment for demographics, clinical and laboratory data, pharmacy claims data, healthcare use, and time varying propensity scores. Results The cohort included 72 738 new users of oral antidiabetic drugs (8032 (11%) used sitagliptin; 7293 (91%) were taking it in combination with other agents) followed for a total of 182 409 patient years. The mean age was 52 (SD 9) years, 54% (39 573) were men, 11% (8111) had ischemic heart disease, and 9% (6378) had diabetes related complications at the time their first antidiabetic drug was prescribed. 14 215 (20%) patients met the combined endpoint. Sitagliptin users showed similar rates of all cause hospital admission or mortality to patients not using sitagliptin (adjusted hazard ratio 0.98, 95% confidence interval 0.91 to 1.06), including patients with a history of ischemic heart disease (adjusted hazard ratio 1.10, 0.94 to 1.28) and those with estimated glomerular filtration rate below 60 mL/min (1.11, 0.88 to 1.41). Conclusions Sitagliptin use was not associated with an excess risk of all cause hospital admission or death compared with other glucose lowering agents among newly treated patients with type 2 diabetes. Most patients prescribed sitagliptin in this cohort were concordant with clinical practice guidelines, in that it was used as add-on treatment. PMID:23618722

  11. Reduction of serum FABP4 level by sitagliptin, a DPP-4 inhibitor, in patients with type 2 diabetes mellitus.

    PubMed

    Furuhashi, Masato; Hiramitsu, Shinya; Mita, Tomohiro; Fuseya, Takahiro; Ishimura, Shutaro; Omori, Akina; Matsumoto, Megumi; Watanabe, Yuki; Hoshina, Kyoko; Tanaka, Marenao; Moniwa, Norihito; Yoshida, Hideaki; Ishii, Junnichi; Miura, Tetsuji

    2015-12-01

    Fatty acid binding protein 4 (FABP4), also known as adipocyte FABP or aP2, is secreted from adipocytes in association with lipolysis as a novel adipokine, and elevated serum FABP4 level is associated with obesity, insulin resistance, and atherosclerosis. However, little is known about the modulation of serum FABP4 level by therapeutic drugs. Sitagliptin (50 mg/day), a dipeptidyl peptidase 4 (DPP-4) inhibitor that increases glucagon-like peptide 1 (GLP-1), was administered to patients with type 2 diabetes (n = 24) for 12 weeks. Treatment with sitagliptin decreased serum FABP4 concentration by 19.7% (17.8 ± 1.8 vs. 14.3 ± 1.5 ng/ml, P < 0.001) and hemoglobin A1c without significant changes in adiposity or lipid variables. In 3T3-L1 adipocytes, sitagliptin or exendin-4, a GLP-1 receptor agonist, had no effect on short-term (2 h) secretion of FABP4. However, gene expression and long-term (24 h) secretion of FABP4 were significantly reduced by sitagliptin, which was not mimicked by exendin-4. Treatment with recombinant DPP-4 increased gene expression and long-term secretion of FABP4, and the effects were cancelled by sitagliptin. Furthermore, knockdown of DPP-4 in 3T3-L1 adipocytes decreased gene expression and long-term secretion of FABP4. In conclusion, sitagliptin decreases serum FABP4 level, at least in part, via reduction in the expression and consecutive secretion of FABP4 in adipocytes by direct inhibition of DPP-4. PMID:26467280

  12. 21 CFR 520.608 - Dicloxacillin sodium monohydrate capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... monohydrate equivalent to 50, 100, 200, or 500 milligrams of dicloxacillin. (b) Sponsor. See No. 000856 in... body weight, three times daily. In severe cases, up to 25 milligrams per pound of body weight...

  13. Safety and tolerability of sitagliptin in clinical studies: a pooled analysis of data from 10,246 patients with type 2 diabetes

    PubMed Central

    2010-01-01

    Background In a previous pooled analysis of 12 double-blind clinical studies that included data on 6,139 patients with type 2 diabetes, treatment with sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, was shown to be generally well tolerated compared with treatment with control agents. As clinical development of sitagliptin continues, additional studies have been completed, and more patients have been exposed to sitagliptin. The purpose of the present analysis is to update the safety and tolerability assessment of sitagliptin by pooling data from 19 double-blind clinical studies. Methods The present analysis included data from 10,246 patients with type 2 diabetes who received either sitagliptin 100 mg/day (N = 5,429; sitagliptin group) or a comparator agent (placebo or an active comparator) (N = 4,817; non-exposed group). The 19 studies from which this pooled population was drawn represent the double-blind, randomized studies that included patients treated with the usual clinical dose of sitagliptin (100 mg/day) for between 12 weeks and 2 years and for which results were available as of July 2009. These 19 studies assessed sitagliptin taken as monotherapy, initial combination therapy with metformin or pioglitazone, or as add-on combination therapy with other antihyperglycemic agents (metformin, pioglitazone, a sulfonylurea ± metformin, insulin ± metformin, or rosiglitazone + metformin). Patients in the non-exposed group were taking placebo, metformin, pioglitazone, a sulfonylurea ± metformin, insulin ± metformin, or rosiglitazone + metformin. The analysis used patient-level data from each study to evaluate between-group differences in the exposure-adjusted incidence rates of adverse events. Results Summary measures of overall adverse events were similar in the sitagliptin and non-exposed groups, except for an increased incidence of drug-related adverse events in the non-exposed group. Incidence rates of specific adverse events were also generally similar between the two groups, except for increased incidence rates of hypoglycemia, related to the greater use of a sulfonylurea, and diarrhea, related to the greater use of metformin, in the non-exposed group and constipation in the sitagliptin group. Treatment with sitagliptin was not associated with an increased risk of major adverse cardiovascular events. Conclusions In this updated pooled safety analysis of data from 10,246 patients with type 2 diabetes, sitagliptin 100 mg/day was generally well tolerated in clinical trials of up to 2 years in duration. PMID:20412573

  14. Stability-indicating RP-HPLC Method for the Simultaneous Determination of Sitagliptin and Simvastatin in Tablets

    PubMed Central

    Ramalingam, P.; Bhaskar, V. Udaya; Reddy, Y. Padmanabha; Kumar, K. Vinod

    2014-01-01

    A new stability-indicating high-performance liquid chromatographic method for simultaneous analysis of sitagliptin and simvastatin in pharmaceutical dosage form was developed and validated. The mobile phase consisted of methanol and water (70:30, v/v) with 0.2 % of n-heptane sulfonic acid adjusted to pH 3.0 with ortho phosphoric acid was used. Retentions of sitagliptin and simvastatin were 4.3 min and 30.4 min, respectively with a flow rate of 1 ml/min on C8 (Qualisil BDS, 250×4.6 mm, 5 μ). Eluents were detected at 253 nm using photodiode diode array detector. The linear regression analysis data for the linearity plot showed correlation coefficient values of 0.9998 and 0.9993 for sitagliptin and simvastatin, with respective concentration ranges of 20-150 μg/ml and 8-60 μg/ml. The relative standard deviation for inter-day precision was lower than 2.0%. The assay of sitagliptin and simvastatin was determined in tablet dosage form was found to be within limits. Both drugs were subjected to a variety of stress conditions such as acidic, basic, oxidation, photolytic, neutral and thermal stress in order to achieve adequate degradation. Results revealed that considerable degradation was found in all stress conditions except oxidative degradations. The method has proven specificity for stability indicating assay method. PMID:25425754

  15. Bifunctional hydrogen bonds in monohydrated cycloether complexes.

    PubMed

    Vallejos, Margarita M; Angelina, Emilio L; Peruchena, Nélida M

    2010-03-01

    In this work, the cooperative effects implicated in bifunctional hydrogen bonds (H-bonds) were studied (in monohydrated six-membered cycloether) within the framework of the atoms in molecules (AIM) theory and of the natural bond orbitals (NBO) analysis. The study was carried out in complexes formed by six-membered cycloether compounds (tetrahydropyrane, 1,4-dioxane, and 1,3-dioxane) and a water molecule. These compounds were used as model systems instead of more complicated molecules of biological importance. All the results were obtained at the second-order Møller-Plesset (MP2) level theory using a 6-311++G(d,p) basis set. Attention was focused on the indicators of the cooperative effects that arise when a water molecule interacts simultaneously with a polar and a nonpolar portion of a six-membered cycloether (via bifunctional hydrogen bonds) and compared with conventional H-bonds where the water molecule only interacts with the polar portion of the cycloether. Different indicators of H-bonds strength, such as structural and spectroscopic data, electron charge density, population analysis, hyperconjugation energy and charge transference, consistently showed significant cooperative effects in bifunctional H-bonds. From the AIM, as well as from the NBO analysis, the obtained results allowed us to state that in the monohydrated six-membered cycloether, where the water molecule plays a dual role, as proton acceptor and proton donor, a mutual reinforcement of the two interactions occurs. Because of this feature, the complexes engaged by bifunctional hydrogen bonds are more stabilized than the complexes linked by conventional hydrogen bonds. PMID:20136161

  16. The effect of sitagliptin on cardiovascular risk profile in Korean patients with type 2 diabetes mellitus: a retrospective cohort study

    PubMed Central

    Shin, Sooyoung; Kim, Hyunah

    2016-01-01

    Background A 2013 postmarketing study suggested a possible link between saxagliptin use and hospital admission for heart failure. Cardiovascular (CV) effects of sitagliptin, the most commonly prescribed antidiabetic in the same class as saxagliptin, have not been evaluated much in Asian patients with type 2 diabetes. This study sought to ascertain the CV safety of sitagliptin in Korean patients. Methods A retrospective cohort study of 4,860 patients who were classified into the sitagliptin and metformin groups was conducted using electronic patient data retrieved from a major tertiary care medical center in Korea. Primary composite end points included CV death, myocardial infarction, and ischemic stroke. Secondary composite end points included the aforementioned individual primary outcomes plus hospitalization due to unstable angina, heart failure, or coronary revascularization. A Cox proportional-hazards model was used to compare CV risk associated with drug exposure. Results Following propensity score (PS) matching in a 1:2 ratio, 1,620 patients in the sitagliptin group and 3,240 patients in the metformin group were identified for cohort entry. The PS-matched hazard ratio (HR) and 95% confidence interval (CI) for sitagliptin relative to metformin were, respectively, 0.831 and 0.536–1.289 (P=0.408) for primary end point and 1.140 and 0.958–1.356 (P=0.139) for secondary end point. Heart failure hospitalization rates did not differ significantly between the two groups, with the PS-matched HR of 0.762 and 95% CI of 0.389–1.495 (P=0.430). When only those patients at high risk of ischemic heart disease were included for analysis, no excess CV risk was observed with sitagliptin compared with metformin. Overall, there were no substantial between-group differences in rates of adverse events, such as hypoglycemia and incident pancreatic disease. Conclusion Sitagliptin was not associated with elevated risk of CV complications including myocardial infarction, ischemic stroke, heart failure, and coronary revascularization, compared to metformin therapy among Korean patients with type 2 diabetes. PMID:27042085

  17. Sitagliptin versus mitiglinide switched from mealtime dosing of a rapid-acting insulin analog in patients with type 2 diabetes: a randomized, parallel-group study

    PubMed Central

    Takeshita, Yumie; Takamura, Toshinari; Kita, Yuki; Takazakura, Akiko; Kato, Ken-ichiro; Isobe, Yuki; Kaneko, Shuichi

    2015-01-01

    Purpose We determined the feasibility of substituting sitagliptin or mitiglinide for bolus insulin injection therapy in patients with type 2 diabetes. Methods 60 patients with type 2 diabetes were enrolled and randomized to switch from mealtime dosing of a rapid-acting insulin analog to either sitagliptin or mitiglinide for 16 weeks. Results Body weight, body mass index, and waist circumference decreased significantly in both groups at the end of the study. Mitiglinide significantly increased fasting plasma glucose (FPG) levels at the end of the study from 146.5±36.3 to 168.0±38.8 mg/dL, whereas sitagliptin did not affect FPG. Glycated hemoglobin (HbA1c) and 1,5-anhydroglucitol increased significantly in both groups. The C peptide immunoreactivity (CPR) responses after arginine were diminished in both groups. γ-GTP and triglycerides increased, and high-density lipoprotein cholesterol and adiponectin decreased, in the sitagliptin group, but not in the mitiglinide group. Mean Diabetes Treatment Satisfaction Questionnaire scores improved significantly in both groups. Patients whose mean total daily doses of rapid-acting insulin analog were 16.6 and 17.8 units were switched to sitagliptin and mitiglinide, respectively, without a change in the HbA1c level. Total insulin doses/body weight predicted changes in HbA1c only in the sitagliptin group, but not in the mitiglinide group. Use of >0.27 IU/kg of a rapid-acting insulin analog predicted an increase in HbA1c after switching to sitagliptin. The CPR index (CPI) was also a predictor for a change in HbA1c in the sitagliptin group, but not in the mitiglinide group; patients with a CPI<1.4 developed a worse HbA1c after switching to sitagliptin. Conclusions Sitagliptin may predominantly act on FPG, whereas mitiglinide may act on postprandial plasma glucose to achieve glycemic control after switching from a bolus insulin regimen. Additional therapy to sitagliptin or mitiglinide is clearly required to obtain equivalent glycemic control in patients using a higher dose of insulin. Trial registration number (UMIN 000007051) PMID:26336611

  18. Sitagliptin downregulates retinol-binding protein 4 and upregulates glucose transporter type 4 expression in a type 2 diabetes mellitus rat model.

    PubMed

    Hu, Honglin; Xu, Min; Qi, Renjuan; Wang, Youmin; Wang, Changjiang; Liu, Jiongjiong; Luo, Li; Xia, Li; Fang, Zhaohui

    2015-01-01

    The present study was designed to investigate the effects of sitagliptin on metabolic parameters as well as the expression levels of retinol-binding protein 4 (RBP4) and glucose transporter type 4 (GLUT4) in a rat model of type 2 diabetes mellitus. A rat model of type 2 diabetes mellitus was established by a combination of a high-fat diet and intraperitoneal injection of low-dose streptozotocin. Rats were divided into three groups: normal control group, diabetes group, and diabetes + sitagliptin group. Body weight, glycemic parameters, lipid profiles, fasting insulin (FINS) and serum RBP4 levels were assessed at baseline and after 6 weeks of therapy. Western blotting was used to detect the tissue RBP4 and GLUT4 expression levels. After treatment for 6 weeks, the diabetes + sitagliptin group displayed significantly improve levels of blood sugar, blood grease, and insulin sensitizing functions (P < 0.05) than the diabetes group. Sitagliptin markedly down regulated RBP4 expression levels and up-regulated GLUT4 expression levels in adipose tissue and skeletal muscle. The results indicate that sitagliptin can modulate the RBP4-GLUT4 system in adipose tissue and skeletal muscle. Modulation of the RBP4-GLUT4 system may be one of the mechanisms by which sitagliptin ameliorates the symptoms of type 2 diabetes mellitus. PMID:26770384

  19. New combination treatments in the management of diabetes: focus on sitagliptin – metformin

    PubMed Central

    Green, Jennifer; Feinglos, Mark

    2008-01-01

    Type 2 diabetes mellitus is an increasingly prevalent condition worldwide. The complications of this disease are known to significantly increase the morbidity and mortality of those affected, resulting in substantial direct and indirect costs. Although good glycemic control has been shown to reduce the incidence and progression of diabetes-related microvascular complications, blood glucose levels are not adequately controlled in most individuals with diabetes. The reasons for this are many, and include issues such as poor adherence to complex medication regimes; costs of prescribed therapies; and the failure of traditionally prescribed medications to preserve beta cell function over time. However, our armamentarium of glucose-lowering drugs has expanded recently with the development of medications that act via the incretin pathway. Sitagliptin, the first commercially available dipeptidyl peptidase-4 inhibitor, inhibits the metabolism and inactivation of the incretin hormones GLP-1 and GIP. The subsequent elevation in levels of these hormones and associated prolongation of their actions has been shown to increase insulin secretion and suppress glucagon secretion in a glucose-appropriate fashion. Sitagliptin therapy in individuals with type 2 diabetes has been found to lower significantly hemoglobin A1c (Hb1c) levels with a minimum of adverse side effects such as weight gain or hypoglycemia. Use of sitagliptin in conjunction with the insulin-sensitizing medication metformin has been shown to decrease HbA1c levels more significantly than does either drug alone. This combination of medications is generally well tolerated, with no adverse effects on weight and a very low likelihood of treatment-related hypoglycemia. Use of both drugs will positively affect many of the underlying metabolic abnormalities associated with type 2 diabetes, including the disordered secretion of insulin and glucagon as well as impaired sensitivity to insulin which are known to accompany this disease. Animal studies also suggest that dipeptidyl peptidase-4 inhibitor treatment may help to preserve beta cell mass; however, it is unclear at present whether or not this will prove to be the case in humans. PMID:19065992

  20. Effect of sitagliptin on epicardial fat thickness in subjects with type 2 diabetes and obesity: a pilot study.

    PubMed

    Lima-Martínez, Marcos M; Paoli, Mariela; Rodney, Marianela; Balladares, Nathalie; Contreras, Miguel; D'Marco, Luis; Iacobellis, Gianluca

    2016-03-01

    The aim of the study was to assess the effect of sitagliptin addition on the epicardial adipose tissue (EAT) thickness in subjects with type 2 diabetes mellitus inadequately controlled on metformin monotherapy. This was a 24-week interventional pilot study in 26 consecutive type 2 diabetic patients, 14 females and 12 males average age of 43.8 ± 9.0 years, with Hemoglobin A1c (HbA1c) ≥7 % on metformin monotherapy. Subjects who met the inclusion criteria were added on sitagliptin and started on sitagliptin/metformin combination at the dosage of 50 mg/1000 mg twice daily. EAT and visceral and total body fat were measured, respectively, with echocardiography and bioelectrical impedance analysis at baseline and after 24 weeks of sitagliptin/metformin treatment in each subject. HbA1c and plasma lipids were also measured. EAT decreased significantly from 9.98 ± 2.63 to 8.10 ± 2.11 mm, p = 0.001, accounting for a percentage of reduction (∆ %) of -15 % after 24 weeks of sitagliptin addition, whereas total body fat percentage, visceral fat, and body mass index (BMI), decreased by 8, 12, and 7 %, respectively (p = 0.001 for all). After 6 month, EAT ∆ % was significantly correlated with ∆ % of visceral fat (r = 0.456; p = 0.01), whereas no correlation with either BMI ∆ % (r = 0.292; p = 0.147) or HbA1c ∆ % was found. The addition of Sitagliptin produced a significant and rapid reduction of EAT, marker of organ-specific visceral fat, in overweight/obese individuals with type 2 diabetes inadequately controlled on metformin monotherapy. EAT as measured with ultrasound can serve as no invasive and accurate marker of visceral fat changes during pharmaceutical interventions targeting the fat. PMID:26233684

  1. A novel data-mining approach leveraging social media to monitor consumer opinion of sitagliptin.

    PubMed

    Akay, Altug; Dragomir, Andrei; Erlandsson, Björn-Erik

    2015-01-01

    A novel data mining method was developed to gauge the experience of the drug Sitagliptin (trade name Januvia) by patients with diabetes mellitus type 2. To this goal, we devised a two-step analysis framework. Initial exploratory analysis using self-organizing maps was performed to determine structures based on user opinions among the forum posts. The results were a compilation of user's clusters and their correlated (positive or negative) opinion of the drug. Subsequent modeling using network analysis methods was used to determine influential users among the forum members. These findings can open new avenues of research into rapid data collection, feedback, and analysis that can enable improved outcomes and solutions for public health and important feedback for the manufacturer. PMID:25561458

  2. Exploration of Excited State Deactivation Pathways of Adenine Monohydrates.

    PubMed

    Chaiwongwattana, Sermsiri; Sapunar, Marin; Ponzi, Aurora; Decleva, Piero; Došlić, Nađa

    2015-10-29

    Binding of a single water molecule has a dramatic effect on the excited state lifetime of adenine. Here we report a joint nonadiabatic dynamics and reaction paths study aimed at understanding the sub-100 fs lifetime of adenine in the monohydrates. Our nonadiabatic dynamics simulations, performed using the ADC(2) electronic structure method, show a shortening of the excited state lifetime in the monohydrates with respect to bare adenine. However, the computed lifetimes were found to be significantly longer that the observed one. By comparing the reaction pathways of several excited state deactivation processes in adenine and adenine monohydrates, we show that electron-driven proton transfer from water to nitrogen atom N3 of the adenine ring may be the process responsible for the observed ultrafast decay. The inaccessibility of the electron-driven proton transfer pathway to trajectory-based nonadiabatic dynamics simulation is discussed. PMID:26439365

  3. Influence of impurities on the crystallization of dextrose monohydrate

    NASA Astrophysics Data System (ADS)

    Markande, Abhay; Nezzal, Amale; Fitzpatrick, John; Aerts, Luc; Redl, Andreas

    2012-08-01

    The effects of impurities on dextrose monohydrate crystallization were investigated. Crystal nucleation and growth kinetics in the presence of impurities were studied using an in-line focused beam reflectance monitoring (FBRM) technique and an in-line process refractometer. Experimental data were obtained from runs carried out at different impurity levels between 4 and 11 wt% in the high dextrose equivalent (DE) syrup. It was found that impurities have no significant influence on the solubility of dextrose in water. However, impurities have a clear influence on the nucleation and growth kinetics of dextrose monohydrate crystallization. Nucleation and growth rate were favored by low levels of impurities in the syrup.

  4. Effect of Metformin and Sitagliptin on Doxorubicin-Induced Cardiotoxicity in Rats: Impact of Oxidative Stress, Inflammation, and Apoptosis.

    PubMed

    Kelleni, Mina Thabet; Amin, Entesar Farghaly; Abdelrahman, Aly Mohamed

    2015-01-01

    Doxorubicin (DOX) is a widely used antineoplastic drug whose efficacy is limited by its cardiotoxicity. The aim of this study was to investigate the possible protective role of the antidiabetic drugs metformin (250?mg/kg dissolved in DW p.o. for seven days) and sitagliptin (10?mg/kg dissolved in DW p.o. for seven days) in a model of DOX-induced (single dose 15?mg/kg i.p. at the fifth day) cardiotoxicity in rats. Results of our study revealed that pretreatment with metformin or sitagliptin produced significant (P < 0.05) cardiac protection manifested by a significant decrease in serum levels of LDH and CK-MB enzymes and cardiac MDA and total nitrites and nitrates levels, a significant increase in cardiac SOD activity, and remarkable improvement in the histopathological features as well as a significant reduction in the immunohistochemical expression of COX-2, iNOS, and caspase-3 enzymes as compared to DOX group. These results may suggest using metformin and/or sitagliptin as preferable drugs for diabetic patients suffering from cancer and receiving DOX in their chemotherapy regimen. PMID:26880912

  5. Comparison of extended release GLP-1 receptor agonist therapy versus sitagliptin in the management of type 2 diabetes

    PubMed Central

    Stolar, Mark W; Grimm, Michael; Chen, Steve

    2013-01-01

    Exenatide once weekly (EQW), the first glucose-lowering agent for type 2 diabetes that is dosed one time per week, contains exenatide encapsulated in microspheres of a dissolvable matrix, which release active agent slowly and continuously into the circulation following subcutaneous injection. In two direct head-to-head comparisons, EQW resulted in better long-term glucose control, greater reductions in fasting plasma glucose, and more significant weight loss than sitagliptin. In other trials, glucose-lowering effects of EQW compared favorably with those of metformin, pioglitazone, and basal insulin. Patients on EQW exhibited a higher incidence of nausea than those on sitagliptin, although gastrointestinal adverse events occurred primarily during the first 6–8 weeks of therapy and declined thereafter. EQW was also associated with a lower incidence of nausea than two other glucagon-like peptide-1 receptor agonists, exenatide twice daily and liraglutide. Mild hypoglycemic episodes were uncommon with EQW, although risk of hypoglycemia increased in combination with sulfonylureas. When choosing between EQW and a dipeptidyl peptidase-4 (DPP-4) inhibitor, such as sitagliptin, clinicians and patients should consider the differences between the two medications in terms of glucose control (EQW superior to DPP-4 inhibitors), weight control (EQW superior to DPP-4 inhibitors), gastrointestinal tolerability during treatment initiation (EQW inferior to DPP-4 inhibitors), and mode of administration (once-weekly subcutaneous administration versus once-daily oral administration). PMID:24285927

  6. Effect of Metformin and Sitagliptin on Doxorubicin-Induced Cardiotoxicity in Rats: Impact of Oxidative Stress, Inflammation, and Apoptosis

    PubMed Central

    Kelleni, Mina Thabet; Amin, Entesar Farghaly; Abdelrahman, Aly Mohamed

    2015-01-01

    Doxorubicin (DOX) is a widely used antineoplastic drug whose efficacy is limited by its cardiotoxicity. The aim of this study was to investigate the possible protective role of the antidiabetic drugs metformin (250 mg/kg dissolved in DW p.o. for seven days) and sitagliptin (10 mg/kg dissolved in DW p.o. for seven days) in a model of DOX-induced (single dose 15 mg/kg i.p. at the fifth day) cardiotoxicity in rats. Results of our study revealed that pretreatment with metformin or sitagliptin produced significant (P < 0.05) cardiac protection manifested by a significant decrease in serum levels of LDH and CK-MB enzymes and cardiac MDA and total nitrites and nitrates levels, a significant increase in cardiac SOD activity, and remarkable improvement in the histopathological features as well as a significant reduction in the immunohistochemical expression of COX-2, iNOS, and caspase-3 enzymes as compared to DOX group. These results may suggest using metformin and/or sitagliptin as preferable drugs for diabetic patients suffering from cancer and receiving DOX in their chemotherapy regimen. PMID:26880912

  7. A concise review of the bioanalytical methods for the quantitation of sitagliptin, an important dipeptidyl peptidase-4 (DPP4) inhibitor, utilized for the characterization of the drug.

    PubMed

    Suresh, P S; Srinivas, Nuggehally R; Mullangi, Ramesh

    2016-05-01

    Inhibition of dipeptidyl peptidase-4 (DPP4) is an emerging therapeutic approach for treating type 2 diabetes and has revolutionized the concept of diabetes management. Sitagliptin is the first approved orally active, potent, selective and nonpeptidomimetic DPP4 inhibitor. Incidence of hypoglycemia and weight gain is negligible with sitagliptin treatment. It is used as monotherapy or in combination with other anti-diabetic drugs to treat type 2 diabetes. There are numerous bioanalytical methods published for the analysis of sitagliptin in preclinical and clinical samples. This review focuses on the various HPLC and LC-MS/MS methods that have been used to analyze sitagliptin in various biological matrices. A small section is devoted to the bioanalysis of other DPP4 inhibitors such as vildagliptin, saxagliptin and linagliptin. This review provides key information in a concise manner regarding sample processing options, chromatographic/detection conditions and validation parameters of the chosen methods for sitagliptin and other DPP4 inhibitors. Copyright © 2016 John Wiley & Sons, Ltd. PMID:26873580

  8. Phosphate salts

    MedlinePlus

    ... as a laxative to clean the bowels before surgery or intestinal tests. Healthcare providers sometimes give potassium phosphate intravenously (by IV) for treating low phosphate and high calcium levels in the blood, and for preventing low phosphate in patients who are being tube-fed.

  9. Combining sitagliptin/metformin with a functional fiber delays diabetes progression in Zucker rats.

    PubMed

    Reimer, Raylene A; Grover, Gary J; Koetzner, Lee; Gahler, Roland J; Lyon, Michael R; Wood, Simon

    2014-03-01

    Our primary objective was to determine whether administering the viscous and fermentable polysaccharide PolyGlycopleX (PGX) with metformin (MET) or sitagliptin/metformin (S/MET) reduces hyperglycemia in Zucker diabetic fatty (ZDF) rats more so than monotherapy of each. Glucose tolerance, adiposity, satiety hormones and mechanisms related to dipeptidyl peptidase 4 activity, gut microbiota and, hepatic and pancreatic histology were examined. Male ZDF rats (9-10 weeks of age) were randomized to: i) cellulose/vehicle (control, C); ii) PGX (5% wt/wt)/vehicle (PGX); iii) cellulose/metformin (200  mg/kg) (MET); iv) cellulose/S/MET (10  mg/kg+200  mg/kg) (S/MET); v) PGX (5%)+MET (200  mg/kg) (PGX+MET); vi) cellulose/sitagliptin/MET (5%)+(10  mg/kg+200  mg/kg) (PGX+S/MET) for 6 weeks. PGX+MET and PGX+S/MET reduced glycemia compared with C and singular treatments (P=0.001). Weekly fasted and fed blood glucose levels were lower in PGX+MET and PGX+S/MET compared with all other groups at weeks 4, 5, and 6 (P=0.001). HbA1c was lower in PGX+S/MET than C, MET, S/MET, and PGX at week 6 (P=0.001). Fat mass was lower and GLP1 was higher in PGX+S/MET compared with all other groups (P=0.001). β-cell mass was highest and islet degeneration lowest in PGX+S/MET. Hepatic lipidosis was significantly lower in PGX+S/MET compared with PGX or S/MET alone. When combined with PGX, both MET and S/MET markedly reduce glycemia; however, PGX+S/MET appears advantageous over PGX+MET in terms of increased β-cell mass and reduced adiposity. Both combination treatments attenuated diabetes in the obese Zucker rat. PMID:24389593

  10. Pleiotropic effects of sitagliptin versus voglibose in patients with type 2 diabetes inadequately controlled via diet and/or a single oral antihyperglycemic agent: a multicenter, randomized trial

    PubMed Central

    Matsushima, Yukiko; Takeshita, Yumie; Kita, Yuki; Otoda, Toshiki; Kato, Ken-ichiro; Toyama-Wakakuri, Hitomi; Akahori, Hiroshi; Shimizu, Akiko; Hamaguchi, Erika; Nishimura, Yasuyuki; Kanamori, Takehiro; Kaneko, Shuichi; Takamura, Toshinari

    2016-01-01

    Purpose A step-up strategy for diet therapy and/or single oral antihyperglycemic agent (OHA) regimens has not yet been established. The aim of this study was to evaluate hemoglobin A1c (HbA1c) as a primary end point, and the pleiotropic effects on metabolic and cardiovascular parameters as secondary end points, of sitagliptin versus voglibose in patients with type 2 diabetes with inadequate glycemic control while on diet therapy and/or treatment with a single OHA. Methods In this multicenter, randomized, open-label, parallel-group trial, a total of 260 patients with inadequately controlled type 2 diabetes (HbA1c levels >6.9%) were randomly assigned to receive either sitagliptin (50 mg, once daily) or voglibose (0.6 mg, thrice daily) for 12 weeks. The primary end point was HbA1c levels. Results Patients receiving sitagliptin showed a significantly greater decrease in HbA1c levels (−0.78±0.69%) compared with those receiving voglibose (−0.30±0.78%). Sitagliptin treatment also lowered serum alkaline phosphatase levels and increased serum creatinine, uric acid, cystatin-C and homeostasis model assessment-β values. Voglibose increased low-density lipoprotein-cholesterol levels and altered serum levels of several fatty acids, and increased Δ-5 desaturase activity. Both drugs increased serum adiponectin. The incidence of adverse events (AEs) was significantly lower in the sitagliptin group, due to the decreased incidence of gastrointestinal AEs. Conclusions Sitagliptin shows superior antihyperglycemic effects compared with voglibose as a first-line or second-line therapy. However, both agents possess unique pleiotropic effects that lead to reduced cardiovascular risk in Japanese people with type 2 diabetes. Trial registration number UMIN 000003503. PMID:27110370

  11. Divergent Effects of Liraglutide, Exendin-4, and Sitagliptin on Beta-Cell Mass and Indicators of Pancreatitis in a Mouse Model of Hyperglycaemia

    PubMed Central

    Mondragon, Angeles; Davidsson, Daniel; Kyriakoudi, Styliana; Bertling, Annika; Gomes-Faria, Rosa; Cohen, Patrizia; Rothery, Stephen; Chabosseau, Pauline; Rutter, Guy A.; da Silva Xavier, Gabriela

    2014-01-01

    Aims Glucagon-like peptide-1 (GLP-1) receptor agonists and dipeptidyl peptidase-4 (DPP4) inhibitors improve glucose tolerance by still incompletely understood mechanisms. Each class of antihyperglycemic drugs has also been proposed to increase pancreatitis risk. Here, we compare systematically the effects of two widely-used GLP-1 analogues, liraglutide and exendin-4, and the DPP4 inhibitor, sitagliptin, in the mouse. Methods C57BL6 mice were maintained for 131 days on a normal diet (ND) or a diet comprising 60% fat (HFD) before measurements of fasting blood glucose and insulin, and intraperitoneal glucose tolerance. Beta- and alpha- cell volume, and Reg3b immunoreactivity, were measured by immunohistochemical analysis of pancreatic slices. Results Whereas liraglutide (200 µg/kg) and exendin-4 (10 µg/kg) treatment reduced body weight and/or improved glucose tolerance, sitagliptin (10 mg/kg) was without effect on either parameter. Liraglutide caused a sharp reduction in beta-cell mass in both ND and HFD mice, whereas exendin-4 exerted no effect. By contrast, sitagliptin unmasked an action of high fat diet to increase beta-cell mass. Reg3B positive area was augmented by all three agents in normal chow-fed mice, whilst sitagliptin and exendin-4, but not liraglutide, affected this parameter in HFD animals. Correspondingly sitagliptin, but not the GLP-1 analogues, increased circulating amylase levels in ND and HFD mice. Conclusions Liraglutide improves glucose tolerance in the mouse whilst exerting relatively modest effects on pancreatitis risk. Conversely, exendin-4 and sitagliptin, at doses which exert, respectively, minor or no effects on metabolic parameters, lead to signs of pancreatitis. PMID:25119717

  12. Mechanistic insight into the evaporative crystallization of two polymorphs of nitrofurantoin monohydrate

    NASA Astrophysics Data System (ADS)

    Tian, F.; Qu, H.; Louhi-Kultanen, M.; Rantanen, J.

    2009-04-01

    This study was conducted to gain a deeper understanding of the crystallization behavior of both known nitrofurantoin (NF) monohydrates (monohydrates I and II). NF monohydrate crystals were obtained by evaporative crystallization from a series of acetone-water mixtures. The water activity of each solution together with the solubility of NF was used for calculation of the NF supersaturation profiles during evaporative crystallization. The crystallization process for each solution was monitored in situ by optical and Raman microscopy. It was found that the fraction of the metastable monohydrate I in the final product increased with decreasing water fraction, suggesting that the nucleation rate of monohydrate I increases with decreasing water activity. In addition, the morphology of both monohydrate forms was affected by the water fraction in the solvent. The in situ images and Raman spectra taken during the evaporative crystallization from water-acetone mixture (0.67 mole fraction of water) demonstrated that the crystallization of the stable monohydrate II was encountered first, and the nucleation of the metastable monohydrate I happened afterwards at a reduced supersaturation level. This indicates that the crystal packing of the NF monohydrate from acetone-water solutions was affected by both supersaturation and water activity.

  13. Effect of Exenatide, Sitagliptin, or Glimepiride on β-Cell Secretory Capacity in Early Type 2 Diabetes

    PubMed Central

    Gudipaty, Lalitha; Rosenfeld, Nora K.; Fuller, Carissa S.; Gallop, Robert; Schutta, Mark H.

    2014-01-01

    OBJECTIVE Agents that augment GLP-1 effects enhance glucose-dependent β-cell insulin production and secretion and thus are hoped to prevent progressive impairment in insulin secretion characteristic of type 2 diabetes (T2D). The purpose of this study was to evaluate GLP-1 effects on β-cell secretory capacity, an in vivo measure of functional β-cell mass, early in the course of T2D. RESEARCH DESIGN AND METHODS We conducted a randomized controlled trial in 40 subjects with early T2D who received the GLP-1 analog exenatide (n = 14), the dipeptidyl peptidase IV inhibitor sitagliptin (n = 12), or the sulfonylurea glimepiride (n = 14) as an active comparator insulin secretagogue for 6 months. Acute insulin responses to arginine (AIRarg) were measured at baseline and after 6 months of treatment with 5 days of drug washout under fasting, 230 mg/dL (glucose potentiation of arginine-induced insulin release [AIRpot]), and 340 mg/dL (maximum arginine-induced insulin release [AIRmax]) hyperglycemic clamp conditions, in which AIRmax provides the β-cell secretory capacity. RESULTS The change in AIRpot was significantly greater with glimepiride versus exenatide treatment (P < 0.05), and a similar trend was notable for the change in AIRmax (P = 0.1). Within each group, the primary outcome measure, AIRmax, was unchanged after 6 months of treatment with exenatide or sitagliptin compared with baseline but was increased with glimepiride (P < 0.05). α-Cell glucagon secretion (AGRmin) was also increased with glimepiride treatment (P < 0.05), and the change in AGRmin trended higher with glimepiride than with exenatide (P = 0.06). CONCLUSIONS After 6 months of treatment, exenatide or sitagliptin had no significant effect on functional β-cell mass as measured by β-cell secretory capacity, whereas glimepiride appeared to enhance β- and α-cell secretion. PMID:24969577

  14. Fabrication of interconnected pore forming α-tricalcium phosphate foam granules cement.

    PubMed

    Shariff, Khairul Anuar; Tsuru, Kanji; Ishikawa, Kunio

    2016-01-01

    Interconnected pore forming calcium phosphate cement is useful for the reconstruction of bone defects as well as scaffold fabrication in tissue engineering. In this study, interconnected pore forming calcium phosphate cement was fabricated using α-tricalcium phosphate (α-TCP) foam granules. When α-TCP foam granules were mixed with acidic calcium phosphate solution prepared from monocalcium phosphate monohydrate (MCPM) and phosphoric acid solution, brushite crystals were precipitated. These crystals bridged the α-TCP foam granules immediately upon mixing. As a result of the brushite bridge between the α-TCP foam granules, fully interconnected macroporous α-TCP was obtained. The amount of brushite precipitate and the mechanical strength of the set cement increased with acidic calcium phosphate concentration. PMID:26329353

  15. Potential impact of sitagliptin on collagen-derived dipeptides in diabetic osteoporosis.

    PubMed

    Baerts, L; Glorie, L; Maho, W; Eelen, A; Verhulst, A; D'Haese, P; Covaci, A; De Meester, I

    2015-10-01

    It is known that diabetes coincides with an increased risk of osteoporosis. While a disturbed collagen metabolism is proposed as a possible cause, much remains unknown about the enzymes involved and changes in the collagen-derived dipeptides and amino acids. Therefore, we sought to study this intricate pathway and the effect of dipeptidyl peptidase 4 (DPP4) inhibitors. Control and streptozotocin-nicotinamide-induced diabetic rats were treated for 12 weeks with vehicle or sitagliptin, a DPP4 inhibitor (Con/VH, Con/SG, DM/VH and DM/SG). The activities of four key enzymes involved in collagen breakdown were determined in serum (DPP4, matrix metalloproteinase 2 and 9 and prolidase). Dipeptide (Ala-Pro, Gly-Pro, Pro-Pro and Pro-Hyp) and amino acid (Pro and Hyp) concentrations were measured by liquid chromatography coupled to mass spectrometry. We found three-fold higher MMP9 activities in DM/VH than in controls, while in DM/SG this rise was attenuated. MMP2 and prolidase did not differ in the investigated groups. Furthermore, we are the first to report on two-fold higher Ala-Pro and Pro-Pro levels in diabetes compared to controls. In contrast, Pro-Hyp concentrations were lower in diabetes (DM/VH and DM/SG). DPP4 inhibition does not seem to have a direct influence on the collagen metabolism in streptozotocin-nicotinamide-induced diabetic rats. Instead, it probably acts through its effect on osteoprotective substrates. In diabetes, increased MMP9 activities seem to favour the production of Ala-Pro and Pro-Pro containing collagen fragments. The high Pro-Hyp levels in untreated controls might have a bone-stimulating effect. Nevertheless, the biological significance of these dipeptides is not yet clear and should be further investigated. PMID:26342756

  16. Rationale, design, and organization of a randomized, controlled Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS) in patients with type 2 diabetes and established cardiovascular disease.

    PubMed

    Green, Jennifer B; Bethel, M Angelyn; Paul, Sanjoy K; Ring, Arne; Kaufman, Keith D; Shapiro, Deborah R; Califf, Robert M; Holman, Rury R

    2013-12-01

    Sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, lowers blood glucose when administered as monotherapy or in combination with other antihyperglycemic agents. TECOS will evaluate the effects of adding sitagliptin to usual diabetes care on cardiovascular outcomes and clinical safety. TECOS is a pragmatic, academically run, multinational, randomized, double-blind, placebo-controlled, event-driven trial recruiting approximately 14,000 patients in 38 countries who have type 2 diabetes (T2DM), are at least 50 years old, have cardiovascular disease, and have an hemoglobin A1c value between 6.5% and 8.0%. Eligible participants will be receiving stable mono- or dual therapy with metformin, sulfonylurea, or pioglitazone, or insulin alone or in combination with metformin. Randomization is 1:1 to double-blind sitagliptin or matching placebo, in addition to existing therapy in a usual care setting. Follow-up occurs at 4-month intervals in year 1 and then twice yearly until 1300 confirmed primary end points have occurred. Glycemic equipoise between randomized groups is a desired aim. The primary composite cardiovascular endpoint is time to the first occurrence of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or hospitalization for unstable angina, with cardiovascular events adjudicated by an independent committee blinded to study therapy. TECOS is a pragmatic-design cardiovascular outcome trial assessing the cardiovascular effects of sitagliptin when added to usual T2DM management. PMID:24268212

  17. Effects of dipeptidyl peptidase IV inhibitor sitagliptin on immunological parameters of lymphocytes in intact animals and animals with experimental autoimmune process.

    PubMed

    Robinson, M V; Mel'nikova, E V; Trufakin, V A

    2014-11-01

    The effects of dipeptidyl peptidase IV inhibitor sitagliptin on immunological parameters were studied in animals with experimental autoimmune process. The effects of the drug administered in preventive (before manifestation of autoimmune processes) and therapeutic (after manifestation of autoimmune process) modes were studied. PMID:25408522

  18. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  19. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  20. 21 CFR 520.1263 - Lincomycin hydrochloride monohydrate oral dosage forms.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride monohydrate oral dosage forms. 520.1263 Section 520.1263 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263 Lincomycin hydrochloride monohydrate oral dosage forms....

  1. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole... furoate monohydrate equivalent to 1 mg mometasone furoate, and 1 mg posaconazole. (b) Sponsor. See...

  2. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole... furoate monohydrate equivalent to 1 mg mometasone furoate, and 1 mg posaconazole. (b) Sponsor. See...

  3. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole... furoate monohydrate equivalent to 1 mg mometasone furoate, and 1 mg posaconazole. (b) Sponsor. See...

  4. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole... furoate monohydrate equivalent to 1 mg mometasone furoate, and 1 mg posaconazole. (b) Sponsor. See...

  5. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole... furoate monohydrate equivalent to 1 mg mometasone furoate, and 1 mg posaconazole. (b) Sponsor. See...

  6. Modulation of Adipocytokines Production and Serum NEFA Level by Metformin, Glimepiride, and Sitagliptin in HFD/STZ Diabetic Rats

    PubMed Central

    Saad, Mohamed I.; Kamel, Maher A.; Hanafi, Mervat Y.

    2015-01-01

    Type 2 diabetes mellitus (T2DM) is a group of metabolic disorders characterized by hyperglycemia owing to insulin resistance and/or insulin deficiency. Current theories of T2DM pathophysiology include a decline in β-cells function, a defect in insulin signaling pathways, and a dysregulation of secretory function of adipocytes. This study aimed to investigate the effect of different antidiabetic drugs on serum levels of certain adipocytokines and nonesterified fatty acids (NEFA) in high-fat diet (HFD)/streptozotocin- (STZ-) induced diabetic rats. All treatments significantly decreased serum NEFA level. Metformin and sitagliptin increased serum adiponectin level, whereas they decreased serum leptin level. Glimepiride showed significant decline in serum levels of both adiponectin and leptin. All treatments remarkably ameliorated insulin resistance, suggested by an improvement of glycemic control, a significant reduction in homeostasis model assessment of insulin resistance (HOMA-IR), and a correction in lipid profile. Modulation of adipocytokines production (i.e., increased serum adiponectin and decreased serum leptin) may also underlie the improvement of insulin resistance and could be a possible mechanism for the beneficial cardiovascular effects of metformin and sitagliptin. PMID:25838947

  7. Factor Analysis of Changes in Hemoglobin A1c After 12 Months of Sitagliptin Therapy in Patients With Type 2 Diabetes

    PubMed Central

    Yuasa, Shouhei; Sato, Kazuyoshi; Takai, Masahiko; Ishikawa, Masashi; Umezawa, Shinichi; Kubota, Akira; Maeda, Hajime; Kanamori, Akira; Miyakawa, Masaaki; Tanaka, Yasushi; Terauchi, Yasuo; Matsuba, Ikuro

    2016-01-01

    Background Sitagliptin, a dipeptidyl peptidase-4 inhibitor, is an effective oral antidiabetic agent as both monotherapy and when combined with insulin. Data from three observational studies performed in patients with type 2 diabetes receiving sitagliptin therapy in the routine clinical setting were integrated to conduct factor analysis of the changes in hemoglobin A1c (HbA1c), body weight, and estimated glomerular filtration rate (eGFR) over 12 months. Methods Among patients with type 2 diabetes attending medical institutions affiliated with Kanagawa Physicians Association, those using sitagliptin were followed for 1 year. In the ASSET-K and ASSIST-K studies, patients were managed by diabetologists, while they were managed by non-diabetologists in the ATTEST-K study. Patients were not administered insulin in ASSET-K, whereas insulin was administered in ASSIST-K. HbA1c (National Glycohemoglobin Standardization Program), blood glucose (fasting/postprandial), body weight, and renal function (serum creatinine and eGFR) were the efficacy endpoints. Factor analysis was performed by analysis of variance using the magnitude of the change in HbA1c, body weight, and eGFR after 12 months of sitagliptin therapy as response variables, and the study, sex, and age as explanatory variables. Results Of 1,327 patients registered in ASSET-K (diabetologists/without insulin), 1,167 patients in ASSIST-K (diabetologists/with insulin), and 530 patients in ATTEST-K (non-diabetologists), statistical analysis was carried out on 1,074, 854, and 411 patients, respectively. There were significant inter-study differences in patient characteristics (complications, duration of diabetes, and baseline HbA1c), the sitagliptin dose, and the use of other antidiabetic agents. HbA1c decreased significantly in all three studies. According to factor analysis, the magnitude of the change in HbA1c over 12 months showed significant inter-study differences and was also significantly influenced by the age, duration of diabetes, and baseline HbA1c. Conclusions Comparison of three observational studies identified differences in patient characteristics, treatment of diabetes (use/non-use of insulin), and the level of specialist care (diabetologist/non-diabetologist). Despite such differences, consistent reduction of HbA1c by sitagliptin was demonstrated in all three studies. The patients showing most improvement in HbA1c with sitagliptin therapy were older patients with a short duration of diabetes and high baseline HbA1c level. PMID:27222674

  8. Efficacy and Safety of Dulaglutide Versus Sitagliptin After 52 Weeks in Type 2 Diabetes in a Randomized Controlled Trial (AWARD-5)

    PubMed Central

    Nauck, Michael; Weinstock, Ruth S.; Umpierrez, Guillermo E.; Guerci, Bruno; Skrivanek, Zachary

    2014-01-01

    OBJECTIVE To compare the efficacy and safety of two doses of once-weekly dulaglutide, a glucagon-like peptide 1 receptor agonist, to sitagliptin in uncontrolled, metformin-treated patients with type 2 diabetes. The primary objective was to compare (for noninferiority and then superiority) dulaglutide 1.5 mg versus sitagliptin in change from baseline in glycosylated hemoglobin A1c (HbA1c) at 52 weeks. RESEARCH DESIGN AND METHODS This multicenter, adaptive, double-blind, parallel-arm study randomized patients (N = 1,098; mean baseline age 54 years; HbA1c 8.1% [65 mmol/mol]; weight 86.4 kg; diabetes duration 7 years) to dulaglutide 1.5 mg, dulaglutide 0.75 mg, sitagliptin 100 mg, or placebo (placebo-controlled period up to 26 weeks). The treatment period lasted 104 weeks, with 52-week primary end point data presented. RESULTS The mean HbA1c changes to 52 weeks were (least squares mean ± SE): −1.10 ± 0.06% (−12.0 ± 0.7 mmol/mol), −0.87 ± 0.06% (9.5 ± 0.7 mmol/mol), and −0.39 ± 0.06% (4.3 ± 0.7 mmol/mol) for dulaglutide 1.5 mg, dulaglutide 0.75 mg, and sitagliptin, respectively. Both dulaglutide doses were superior to sitagliptin (P < 0.001, both comparisons). No events of severe hypoglycemia were reported. Mean weight changes to 52 weeks were greater with dulaglutide 1.5 mg (−3.03 ± 0.22 kg) and dulaglutide 0.75 mg (−2.60 ± 0.23 kg) compared with sitagliptin (−1.53 ± 0.22 kg) (P < 0.001, both comparisons). The most common gastrointestinal treatment-emergent adverse events in dulaglutide 1.5- and 0.75-mg arms were nausea, diarrhea, and vomiting. CONCLUSIONS Both dulaglutide doses demonstrated superior glycemic control versus sitagliptin at 52 weeks with an acceptable tolerability and safety profile. PMID:24742660

  9. Factors Predicting Therapeutic Efficacy of Combination Treatment With Sitagliptin and Insulin in Type 2 Diabetic Patients: The ASSIST-K Study

    PubMed Central

    Ishikawa, Masashi; Takai, Masahiko; Maeda, Hajime; Kanamori, Akira; Kubota, Akira; Amemiya, Hikaru; Iizuka, Takashi; Iemitsu, Kotaro; Iwasaki, Tomoyuki; Uehara, Goro; Umezawa, Shinichi; Obana, Mitsuo; Kaneshige, Hideaki; Kaneshiro, Mizuki; Kawata, Takehiro; Sasai, Nobuo; Saito, Tatsuya; Takuma, Tetsuo; Takeda, Hiroshi; Tanaka, Keiji; Tsurui, Nobuaki; Nakajima, Shigeru; Hoshino, Kazuhiko; Honda, Shin; Machimura, Hideo; Matoba, Kiyokazu; Minagawa, Fuyuki; Minami, Nobuaki; Miyairi, Yukiko; Mokubo, Atsuko; Motomiya, Tetsuya; Waseda, Manabu; Miyakawa, Masaaki; Naka, Yoshikazu; Terauchi, Yasuo; Tanaka, Yasushi; Matsuba, Ikuro

    2015-01-01

    Background It is unclear whether dipeptidyl peptidase-4 inhibitors decrease hemoglobin A1c (HbA1c) in a glucose-dependent manner in patients on insulin therapy who have impaired insulin secretion. This study investigated factors influencing the efficacy of sitagliptin when used concomitantly with insulin to treat type 2 diabetes mellitus (T2DM) in the real-world setting. Methods A retrospective study was conducted of 1,004 T2DM patients at 36 Japanese clinics associated with the Diabetes Task Force of the Kanagawa Physicians Association. Eligible patients had been on insulin for at least 6 months, with a baseline HbA1c of 7.0% (53 mmol/mol) or higher. Baseline characteristics and laboratory data from 495 patients were subjected to multiple regression analysis to identify factors influencing the change of HbA1c. Results Most patients (n = 809) received sitagliptin at a dose of 50 mg. In the 1,004 patients, HbA1c decreased by 0.74% (6 mmol/mol) and body weight increased by 0.1 kg after 6 months of combination therapy. Multiple regression analysis showed that a higher baseline HbA1c, older age, and lower body mass index influenced the change of HbA1c after 6 months. Hypoglycemic symptoms occurred in 7.4%, but none were severe. Conclusions These results emphasize the importance of a higher HbA1c at the commencement of sitagliptin therapy in patients on insulin. Glucose-dependent suppression of glucagon secretion by sitagliptin may be useful in patients with impaired insulin secretion. Sitagliptin can be used concomitantly with insulin irrespective of the insulin regimen, duration of insulin treatment, and concomitant medications. PMID:26124906

  10. Characterization of calcium phosphate cements modified by addition of amorphous calcium phosphate.

    PubMed

    Van den Vreken, Natasja M F; Pieters, Ilse Y; Declercq, Heidi A; Cornelissen, Maria J; Verbeeck, Ronald M H

    2010-02-01

    In this study the influence of amorphous calcium phosphate (ACP) on the setting of, and the formed apatite crystallite size in, a calcium phosphate cement (CPC) based on alpha-tricalcium phosphate (alpha-TCP) or tetracalcium phosphate (TTCP)/monocalcium phosphate monohydrate (MCPM) was investigated. Setting times at 22 degrees C were measured in air atmosphere; those at 37 degrees C were measured at 100% relative humidity. The phase composition of the set cements was investigated after 1 week using X-ray diffractometry and infrared spectroscopy and the morphology was investigated using scanning electron microscopy. The compressive strength (CS) of the set CPCs was measured after 1 day. Viability of MC3T3-E1 cells on the CPCs was analyzed after 7, 14 and 21 days of incubation using the CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay. The alpha-TCP-based cement exhibited long setting times, a high CS and was converted to a calcium-deficient hydroxyapatite (CDHAp). The TTCP/MCPM-based CPC was only partly converted to CDHAp, produced acceptable setting times and had a low CS. Addition of ACP to these two CPCs resulted in cements that exhibited good setting times, CS suitable for non-load-bearing applications and a full conversion to nanocrystalline CDHAp. Moreover, the ACP containing CPCs demonstrated good cell viability, making them suitable candidates for bone substitute materials. PMID:19654057

  11. Effect of Concomitant Administration of L-Glutamine and Cycloart-23-ene-3β, 25-diol (B2) with Sitagliptin in GLP-1 (7–36) Amide Secretion, Biochemical and Oxidative Stress in Streptozotocin - Nicotinamide Induced Diabetic Sprague Dawley Rats

    PubMed Central

    Raut, Chandrashekhar G.; Zanwar, Anand A.

    2013-01-01

    Previously we have reported that, cycloart-23-ene-3β, 25-diol (called as B2) and L-glutamine stimulated glucagon like peptide-1 (GLP-1) (7–36) amide secretion diabetic rats. The objective of present investigation was to investigate the concomitant administration of cycloart-23-ene-3β, 25-diol+sitagliptin and L-glutamine+sitagliptin in streptozotocin - nicotinamide induced diabetic Sprague Dawley. Type 2 diabetes was induced in overnight fasted male Sprague Dawley rats pre-treated with nicotinamide (100 mg/kg, i.p.) followed by administration of streptozotocin (55 mg/kg, i.p.) 20 min after. The rats were divided into; I- non-diabetic, II- diabetic control, III- Sitagliptin (5 mg/kg, p.o.)+cycloart-23-ene-3β, 25-diol (1 mg/kg, p.o.), IV- Sitagliptin (5 mg/kg, p.o.)+L-glutamine (1000 mg/kg, p.o.). The concomitant treatment of cycloart-23-ene-3β, 25-diol and L-glutamine with sitagliptin was 8 weeks. Plasma glucose, body weight, food and water intake were determined every week. Glycosylated haemoglobin, lipid profile, plasma and colonic active (GLP-1) (7–36) amide, plasma and pancreatic insulin, histology of pancreata and biomarkers of oxidative stress were measured after 8th week treatment. Concomitant administration of cycloart-23-ene-3β, 25-diol and L-glutamine with sitagliptin significantly (p<0.001) reduced plasma glucose, glyoxylated haemoglobin, lipid profile and oxidative stress parameters compared to diabetic control groups. Both concomitant treatment increased plasma and pancreatic insulin as well as plasma and colonic active (GLP-1) (7–36) amide secretion. Histological analysis by Gomori staining observed less destruction of pancreatic β cells. The result obtained from this study; it is concluded that concomitant administration of cycloart-23-ene-3β, 25-diol+sitagliptin and L-glutamine+sitagliptin showed additive antihyperglycaemic effect in diabetic rats. PMID:24023648

  12. Antiresorption implant coatings based on calcium alendronate and octacalcium phosphate deposited by matrix assisted pulsed laser evaporation.

    PubMed

    Boanini, Elisa; Torricelli, Paola; Forte, Lucia; Pagani, Stefania; Mihailescu, Natalia; Ristoscu, Carmen; Mihailescu, Ion N; Bigi, Adriana

    2015-12-01

    The integration of an implant material with bone tissue depends on the chemistry and physics of the implant surface. In this study we applied matrix assisted pulsed laser evaporation (MAPLE) in order to synthesize calcium alendronate monohydrate (a bisphosphonate obtained by calcium sequestration from octacalcium phosphate by alendronate) and calcium alendronate monohydrate/octacalcium phosphate composite thin films on titanium substrates. Octacalcium phosphate coatings were prepared as reference material. The powders, which were synthesized in aqueous medium, were suspended in deionised water, frozen at liquid nitrogen temperature and used as targets for MAPLE experiments. The transfer was conducted with a KrF* excimer laser source (λ = 248 nm, τFWHM ≤ 25 ns) in mild conditions of temperature and pressure. XRD, FTIR and SEM analyses confirmed that the coatings contain the same crystalline phases as the as-prepared powder samples. Osteoblast derived from stem cells and osteoclast derived from monocytes of osteoporotic subjects were co-cultured on the coatings up to 14 days. Osteoclast displayed significantly reduced proliferation and differentiation in the presence of calcium alendronate monohydrate, pointing to a clear role of the coatings containing this bisphosphonate on inhibiting excessive bone resorption. At variance, osteoblast production of alkaline phosphatase and type I pro-collagen were promoted by the presence of bisphosphonate, which also decreased the production of interleukin 6. The positive influence towards osteoblast differentiation was even more enhanced in the composite coatings, thanks to the presence of octacalcium phosphate. PMID:26445021

  13. Effect of single oral dose of proanthocyanidin on postprandial hyperglycemia in healthy rats: A comparative study with sitagliptin

    PubMed Central

    Sulaiman, Amal Ajaweed

    2014-01-01

    Background: Many of flavonoid rich natural products found to have a significant influence on postprandial hyperglycemia, a major risk factor for diabetic complications. Enhancement of insulinotropic gut hormones by inhibition of dipeptidyl peptidase-IV (DPP-IV) are among the newest strategies for treatments of Type 2 diabetes which thought to be the underlying action through which flavonoid can reduce postprandial hyperglycemia. Aim: This study aim was designed to investigate the potential role of standardized grape seed proanthocyanidin in controlling postprandial hyperglycemia by enhancing the regulatory incretin effect of gut hormones in response to oral and intraperitoneal (I.P) glucose load in healthy rats. Materials and Methods: Five groups of animals each of six rats were used in this study, which was conducted in March 2013. Groups (II and V) treated with single oral dose of proanthocyanidin (50 mg/kg), Group III received single oral dose of sitagliptin (40 mg/kg) and Groups (I and IV) treated with vehicle serve as control groups. All treatments were given 30 min before oral or I.P glucose load. Blood glucose was estimated over 2 h duration at (0, 30, 60, 90, and 120) min from glucose load. Result: Both proanthocyanidin and sitagliptin significantly improve hyperglycemia induced by oral glucose load relative to control. While non-significant changes were achieved by proanthocyanidin after I.P glucose challenge compared to untreated control group. Conclusion: The result of this study indicated that proanthocyanidin may possess an enhancement of incretin effect of gut peptides, which could be responsible for some of its action on glucose homeostasis. This finding may provide an opportunity for further pharmacological studies using more specific models to clarify the possible action of proanthocyanidin as a natural DPP-IV inhibitor. PMID:26401351

  14. The low temperature formation of octacalcium phosphate

    NASA Astrophysics Data System (ADS)

    Graham, Stephan; Brown, Paul W.

    1993-09-01

    The low temperature formation of octacalcium phosphate (Ca 8(HPO 4) 2(PO 4) 4·5H 2O) was investigated. Octacalcium phosphate (OCP) was formed by the hydrolysis of α-tricalcium phosphate (α-TCP), and by reaction between monocalcium phosphate monohydrate (MCPM) and tetracalcium phosphate (TetCP). Relationships between phase formation, microstructural evolution, and variations in solution chemistry were examined. Hydrolysis of α-TCP to form OCP occurs more rapidly at elevated temperatures. At the highest temperature studied, 70°C, initial precipitation of OCP occurs in about one hour, but its inevitable hydrolysis to the more stable HAp phase takes place over several days. At room temperature, nearly three days are required to initiate OCP formation, yet remains a final product phase for well over a period of months. When the initial solution pH is less than 7, pure phase OCP is the final product, while HAp forms when initial pH values are higher than this. Furthermore, OCP precipitates faster at the highest initial pH values where its formation is observed. OCP formation by reaction between MCPM and TetCP is also dependent on temperature and time of reaction. For temperatures between 40 and 55°C and at reasonable times (less than four days) the product is phase pure OCP. After that time, inevitable hydrolysis of the OCP product to HAp occurs. Between 30 and 40°C, DCPD (CaHPO 4·2H 2O) is simultaneously present with OCP, and below 30°C, HAp and DCPD coexist within this aforementioned time span. Conversely, between 55 and 60°C, DCP (CaHPO 4) and OCP are the product phases (in the allowed time of reaction, before the eventual degradation of OCP), and above 60°C HAp and DCP are the final products.

  15. Conformational preferences of monohydrated clusters of imidazole derivatives revisited.

    PubMed

    Bhattacherjee, Aditi; Wategaonkar, Sanjay

    2015-08-21

    We present the IR spectroscopic investigations of benzimidazole (BIM), N-methylbenzimidazole (MBIM), and their monohydrates (W1) carried out in a supersonic jet in the region of N-H, C-H, and O-H stretching fundamentals. The C-H stretching modes in the monomers were studied with the aim of identifying the C(2)H mode (the C atom between the two N atoms in the imidazole moiety) which is known to play an important role as a H-bond donor in enzymes and ionic liquids. The assignment was aided by quantum chemical calculations as well as the literature data for FTIR measurements in the matrix. The monohydrated clusters were investigated for a global comparison with previously reported conformations of hydrated imidazole and related derivatives in the gas phase, matrices, and He nanodroplets. The BIM-W1 complex showed the presence of three conformers; an N-H∙∙∙O bound conformer (A') and two O-H∙∙∙N bound conformers, tilted towards the phenyl side (A) and the imidazole side (B), respectively. Although both A' and B type conformers have been reported in the literature, our experiments identify a new conformer (conformer A) in the gas phase for the first time which has also been reported in crystal structures of histidine containing proteins. The binding energies of the three conformers were found to be of comparable magnitude, with the N-HO bound structure lying in between (∼0.02-0.04 kcal mol(-1)) the O-H∙∙∙N bound ones at the counterpoise corrected (cp) MP2/aug-cc-pVDZ level of theory. The formation of two distinct but closely related O-H∙∙∙N bound conformers (A and B) was additionally confirmed by studying the MBIM-W1 complex. Binding energies of the MBIM-W1 conformers were found to be higher than those of the analogous BIM-W1 conformers by 0.2 kcal mol(-1) at the cp-MP2/aug-cc-pVDZ level. The C(2)-H∙∙∙O or π bound water structures were not observed in the beam for monohydrated clusters of either monomer. While QTAIM calculations predicted secondary stabilization in the A type conformer by a C(4)-HO hydrogen bond, such an effect due to a possible C(2)-HO interaction was not found for conformer B. Experimentally, however, no spectral evidence was found for either the C(4)-H∙∙∙O or the C(2)-H∙∙∙O interaction. PMID:26138267

  16. Vildagliptin vs liraglutide as a second-line therapy switched from sitagliptin-based regimens in patients with type 2 diabetes: A randomized, parallel-group study

    PubMed Central

    Takeshita, Yumie; Takamura, Toshinari; Kita, Yuki; Otoda, Toshiki; Kato, Ken-ichiro; Wakakuri, Hitomi; Yamada, Masayuki; Misu, Hirofumi; Matsushima, Yukiko; Kaneko, Shuichi

    2015-01-01

    Introduction A step-up strategy for dipeptidyl peptidase (DPP)-4 inhibitor-based regimens has not yet been established. In addition, similarities and differences between DPP-4 inhibitors and glucagon-like peptide (GLP)-1 receptor agonists remain to be elucidated in humans. We investigated the pleiotropic effects of vildagliptin vs liraglutide in patients with type 2 diabetes on sitagliptin-based regimens in an open-label, randomized, clinical trial. Materials and Methods A total of 122 patients with type 2 diabetes that was inadequately controlled by sitagliptin-based regimens were randomly assigned to either vildagliptin (50 mg, twice daily) or liraglutide treatment (0.9 mg, once daily) for 12 weeks. The primary outcomes were glycated hemoglobin and body mass index. Results Both vildagliptin and liraglutide significantly lowered glycated hemoglobin within 12 weeks after switching from sitagliptin, but liraglutide produced a greater reduction (−0.67 ± 0.12% vs −0.36 ± 0.53%). Liraglutide lowered body mass index, whereas vildagliptin did not affect body mass index. Vildagliptin lowered fasting C-peptide immunoreactivity, but liraglutide did not. Vildagliptin increased serum levels of adiponectin, arachidonic acid, eicosapentaenoic acid and docosahexaenoic acid, whereas liraglutide had no effect on these levels. Quality of life, assessed using the diabetes treatment satisfaction questionnaire, was not impaired in either group. The most common adverse events were gastrointestinal symptoms, which occurred with similar frequencies in both groups. Conclusions Vildagliptin-mediated improvements in glycemic control did not correlate with indices for insulin secretion and insulin sensitivity. Switching from sitagliptin to liraglutide is useful in managing hyperglycemia and weight. Each agent exerts unique pleiotropic effects. This trial was registered with the University Hospital Medical Information Network Clinical Trials Registry (no. 000004953). PMID:25802727

  17. Reaction of zirconium fluoride monohydrate and ammonium bifluoride; Its effect on fluoride glass preparation and quality

    SciTech Connect

    Ewing, K.J.; Sanghera, J.S.; Miklos, R.E.; Sachon, M.G.; Pietersen, L.; Hart, P.; Aggarwal, I. . Optical Sciences Div.)

    1989-08-01

    The products obtained from the room-temperature reaction of ammonium bifluoride and zirconium fluoride monohydrate are ammonium heptafluorozirconate ((NH/sub 4/)/sub 3/ZrF/sub 7/), liquid water, and hydrogen fluoride. This paper discusses ammonium bifluoride and zirconium fluoride monohydrate reacted prior to glass batching, producing dry ammonium heptafluorozirconate which was used to prepare a high-quality ZBLAN fluoride glass.

  18. Comparative activity of proline-containing dipeptide noopept and inhibitor of dipeptidyl peptidase-4 sitagliptin in a rat model of developing diabetes.

    PubMed

    Ostrovskaya, R U; Ozerova, I V; Gudascheva, T A; Kapitsa, I G; Ivanova, E A; Voronina, T A; Seredenin, S B

    2014-01-01

    Developing diabetes was modeled on adult male Wistar rats by repeated intraperitoneal injections of streptozotocin in a subdiabetogenic dose of 30 mg/kg for 3 days. Proline-containing dipeptide drug Noopept or a standard diabetic drug dipeptidyl peptidase-4 inhibitor sitagliptin was administered per os in a dose of 5 mg/kg before each injection of the toxin and then for 16 days after streptozotocin course. In active control group, spontaneously increase glucose level and reduced tolerance to glucose load (1000 mg/kg intraperitoneally) were observed on the next day after the third administration of toxin. Basal glucose level decreased by day 16, but glucose tolerance remained impaired. Noopept normalized the basal blood glucose level and tolerance to glucose load on the next day after administration of streptozotocin. The effect of Noopept persisted to the end of the experiment. At early terms of the experiment, sitagliptin was somewhat superior to Noopept by the effect on baseline glucose level, but was inferior by the influence on glucose tolerance.. By the end of the experiment, Noopept significantly (by 2 times) surpassed sitagliptin by its effect on glucose tolerance. PMID:24771372

  19. Effects of sitagliptin on coronary atherosclerosis evaluated using integrated backscatter intravascular ultrasound in patients with type 2 diabetes: rationale and design of the TRUST study.

    PubMed

    Nozue, Tsuyoshi; Fukui, Kazuki; Koyama, Yutaka; Fujii, Hiroyuki; Kunishima, Tomoyuki; Hikita, Hiroyuki; Hibi, Kiyoshi; Miyazawa, Akiyoshi; Michishita, Ichiro

    2016-05-01

    Patients with diabetes mellitus are at high risk for developing coronary artery disease (CAD), even if they are treated with statins. Several studies have shown the beneficial effects of dipeptidyl peptidase-4 (DPP-4) inhibitors on the cardiovascular system in an animal model. However, recent clinical trials using DPP-4 inhibitors have shown that these inhibitors fail to reduce the occurrence of cardiovascular events. Therefore, this study will be performed to evaluate the effects of sitagliptin, a DPP-4 inhibitor, on coronary atherosclerosis in patients with type 2 diabetes. This study will be a prospective, open-label, randomized multicenter trial performed in 6 centers in Japan. Stable CAD patients with type 2 diabetes who have undergone successful percutaneous coronary intervention under integrated backscatter (IB)-intravascular ultrasound (IVUS) guidance will be studied. They will be randomly assigned to either the sitagliptin group or a control group. After 48 weeks' treatment, the IVUS examination will be repeated in the same coronary artery as at baseline. The primary end point will be the percentage change in plaque volume measured using grayscale IVUS from baseline to the 48-week follow-up. This study will be the first multicenter trial to evaluate the effects of a DPP-4 inhibitor on coronary atherosclerosis evaluated using IB-IVUS, and the findings will clarify the anti-atherogenic effects of sitagliptin. PMID:25794984

  20. Microelectrophoretic study of calcium oxalate monohydrate in macromolecular solutions

    NASA Technical Reports Server (NTRS)

    Curreri, P. A.; Onoda, G. Y., Jr.; Finlayson, B.

    1987-01-01

    Electrophoretic mobilities were measured for calcium oxalate monohydrate (COM) in solutions containing macromolecules. Two mucopolysaccharides (sodium heparin and chondroitin sulfate) and two proteins (positively charged lysozyme and negatively charged bovine serum albumin) were studied as adsorbates. The effects of pH, calcium oxalate surface charge (varied by calcium or oxalate ion activity), and citrate concentration were investigated. All four macromolecules showed evidence for adsorption. The macromolecule concentrations needed for reversing the surface charge indicated that the mucopolysaccharides have greater affinity for the COM surface than the proteins. Citrate ions at high concentrations appear to compete effectively with the negative protein for surface sites but show no evidence for competing with the positively charged protein.

  1. Transformation of zinc hydroxide chloride monohydrate to crystalline zinc oxide.

    PubMed

    Moezzi, Amir; Cortie, Michael; McDonagh, Andrew

    2016-04-25

    Thermal decomposition of layered zinc hydroxide double salts provides an interesting alternative synthesis for particles of zinc oxide. Here, we examine the sequence of changes occurring as zinc hydroxide chloride monohydrate (Zn5(OH)8Cl2·H2O) is converted to crystalline ZnO by thermal decomposition. The specific surface area of the resultant ZnO measured by BET was 1.3 m(2) g(-1). A complicating and important factor in this process is that the thermal decomposition of zinc hydroxide chloride is also accompanied by the formation of volatile zinc-containing species under certain conditions. We show that this volatile compound is anhydrous ZnCl2 and its formation is moisture dependent. Therefore, control of atmospheric moisture is an important consideration that affects the overall efficiency of ZnO production by this process. PMID:27030646

  2. Structure, hydrogen bonding and thermal expansion of ammonium carbonate monohydrate

    PubMed Central

    Fortes, A. Dominic; Wood, Ian G.; Alfè, Dario; Hernández, Eduardo R.; Gutmann, Matthias J.; Sparkes, Hazel A.

    2014-01-01

    We have determined the crystal structure of ammonium carbonate monohydrate, (NH4)2CO3·H2O, using Laue single-crystal diffraction methods with pulsed neutron radiation. The crystal is orthorhombic, space group Pnma (Z = 4), with unit-cell dimensions a = 12.047 (3), b = 4.453 (1), c = 11.023 (3) Å and V = 591.3 (3) Å3 [ρcalc = 1281.8 (7) kg m−3] at 10 K. The single-crystal data collected at 10 and 100 K are complemented by X-ray powder diffraction data measured from 245 to 273 K, Raman spectra measured from 80 to 263 K and an athermal zero-pressure calculation of the electronic structure and phonon spectrum carried out using density functional theory (DFT). We find no evidence of a phase transition between 10 and 273 K; above 273 K, however, the title compound transforms first to ammonium sesquicarbonate monohydrate and subsequently to ammonium bicarbonate. The crystallographic and spectroscopic data and the calculations reveal a quite strongly hydrogen-bonded structure (E HB ≃ 30–40 kJ mol−1), on the basis of H⋯O bond lengths and the topology of the electron density at the bond critical points, in which there is no free rotation of the ammonium cation at any temperature. The barrier to free rotation of the ammonium ions is estimated from the observed librational frequency to be ∼ 36 kJ mol−1. The c-axis exhibits negative thermal expansion, but the thermal expansion behaviour of the a and b axes is ormal. PMID:25449618

  3. Structure, hydrogen bonding and thermal expansion of ammonium carbonate monohydrate.

    PubMed

    Fortes, A Dominic; Wood, Ian G; Alfè, Dario; Hernández, Eduardo R; Gutmann, Matthias J; Sparkes, Hazel A

    2014-12-01

    We have determined the crystal structure of ammonium carbonate monohydrate, (NH4)2CO3·H2O, using Laue single-crystal diffraction methods with pulsed neutron radiation. The crystal is orthorhombic, space group Pnma (Z = 4), with unit-cell dimensions a = 12.047 (3), b = 4.453 (1), c = 11.023 (3) Å and V = 591.3 (3) Å(3) [ρcalc = 1281.8 (7) kg m(-3)] at 10 K. The single-crystal data collected at 10 and 100 K are complemented by X-ray powder diffraction data measured from 245 to 273 K, Raman spectra measured from 80 to 263 K and an athermal zero-pressure calculation of the electronic structure and phonon spectrum carried out using density functional theory (DFT). We find no evidence of a phase transition between 10 and 273 K; above 273 K, however, the title compound transforms first to ammonium sesquicarbonate monohydrate and subsequently to ammonium bicarbonate. The crystallographic and spectroscopic data and the calculations reveal a quite strongly hydrogen-bonded structure (EHB ≃ 30-40 kJ mol(-1)), on the basis of H...O bond lengths and the topology of the electron density at the bond critical points, in which there is no free rotation of the ammonium cation at any temperature. The barrier to free rotation of the ammonium ions is estimated from the observed librational frequency to be ∼ 36 kJ mol(-1). The c-axis exhibits negative thermal expansion, but the thermal expansion behaviour of the a and b axes is ormal. PMID:25449618

  4. Sulfuric Acid Monohydrate: Formation and Heterogeneous Chemistry in the Stratosphere

    NASA Technical Reports Server (NTRS)

    Zhang, Renyi; Leu, Ming-Taun; Keyser, Leon F.

    1995-01-01

    We have investigated some thermodynamic properties (i.e., freezing/melting points) and heterogeneous chemistry of sulfuric acid monohydrate (SAM, H2SO4.H2O), using a fast flow reactor coupled to a quadrupole mass spectrometer. The freezing point observations of thin liquid sulfuric acid films show that for acid contents between 75 and 85 wt % the monohydrate crystallizes readily at temperatures between 220 and 240 K on a glass substrate. Once formed, SAM can be thermodynamically stable in the H2O partial pressure range of (1-4) x 10(exp -4) torr and in the temperature range of 220-240 K. For a constant H2O partial pressure, lowering the temperature causes SAM to melt when the temperature and water partial pressure conditions are out of its stability regime. The reaction probability measurements indicate that the hydrolysis of N2O5 is significantly suppressed owing to the formation of crystalline SAM: The reaction probability on water-rich SAM (with higher relative humidity, or RH) is of the order of 10(exp -3) at 210 K and decreases by more than an order of magnitude for the acid-rich form (with lower RH). The hydrolysis rate of ClONO2 on water-rich SAM is even smaller, of the order of 10(exp -4) at 195 K. These reported values on crystalline SAM are much smaller than those on liquid solutions. No enhancement of these reactions is observed in the presence of HCl vapor at the stratospheric concentrations. In addition, Brunauer, Emmett, and Teller analysis of gas adsorption isotherms and photomicrography have been performed to characterize the surface roughness and porosities of the SAM substrate. The results suggest the possible formation of SAM in some regions of the middle- or low-latitude stratosphere and, consequently, much slower heterogeneous reactions on the frozen aerosols.

  5. Fabrication of optical element from unidirectional grown imidazole-imidazolium picrate monohydrate (IIP) organic crystals for nonlinear optical applications

    NASA Astrophysics Data System (ADS)

    Vivek, P.; Murugakoothan, P.

    2014-12-01

    Nonlinear optical bulk single crystal of Imidazole-imidazolium picrate monohydrate (IIP) has been grown by Sankaranarayanan-Ramasamy (SR) method using acetonitrile as solvent. First time we report the bulk growth of IIP crystal by SR method. The transparent IIP single crystal of maximum diameter 21 mm and length 46 mm was obtained by employing SR method. The grown crystal was subjected to high resolution X-ray diffraction, UV-vis-NIR transmittance, refractive index, hardness, dielectric and laser damage threshold studies. The crystalline perfection of the grown crystal was analyzed using HRXRD. Cut off wavelength and optical transmission window of the crystal was assessed by UV-vis-NIR and the refractive index of the crystal was found. The mechanical property of the crystal was estimated by Vicker's hardness test. The dielectric property of the crystal was measured as a function of frequency. The laser damage threshold value was determined. The particle size dependent second harmonic generation efficiency for IIP was evaluated with standard reference material potassium dihydrogen phosphate (KDP) by Kurtz-Perry powder method using Nd:YAG laser, which established the existence of phase matching. The second harmonic generation (SHG) of IIP crystal was investigated by the SHG Maker fringes technique. The mechanism of growth is revealed by carrying out chemical etching using acetonitrile as etchant.

  6. Aggregation of Calcium Phosphate and Oxalate Phases in the Formation of Renal Stones

    PubMed Central

    2015-01-01

    The majority of human kidney stones are comprised of multiple calcium oxalate monohydrate (COM) crystals encasing a calcium phosphate nucleus. The physiochemical mechanism of nephrolithiasis has not been well determined on the molecular level; this is crucial to the control and prevention of renal stone formation. This work investigates the role of phosphate ions on the formation of calcium oxalate stones; recent work has identified amorphous calcium phosphate (ACP) as a rapidly forming initial precursor to the formation of calcium phosphate minerals in vivo. The effect of phosphate on the nucleation of COM has been investigated using the constant composition (CC) method in combination with scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Our findings indicate COM nucleation is strongly promoted by the presence of phosphate; this occurs at relatively low phosphate concentrations, undersaturated with respect to brushite (dicalcium phosphate dehydrate, DCPD) formation. The results show that ACP plays a crucial role in the nucleation of calcium oxalate stones by promoting the aggregation of amorphous calcium oxalate (ACO) precursors at early induction times. The coaggregations of ACP and ACO precursors induce the multiple-point nucleation of COM. These novel findings expand our knowledge of urinary stone development, providing potential targets for treating the condition at the molecular level. PMID:25598742

  7. Why sildenafil and sildenafil citrate monohydrate crystals are not stable?

    PubMed Central

    Sawatdee, Somchai; Pakawatchai, Chaveng; Nitichai, Kwanjai; Srichana, Teerapol; Phetmung, Hirihattaya

    2015-01-01

    Sildenafil citrate was crystallized by various techniques aiming to determine the behavior and factors affecting the crystal growth. There are only 2 types of sildenafil obtaining from crystallization: sildenafil (1) and sildenafil citrate monohydrate (2). The used techniques were (i) crystallization from saturated solutions, (ii) addition of an antisolvent, (iii) reflux and (iv) slow solvent evaporation method. By pursuing these various methods, our work pointed that the best formation of crystal (1) was obtained from technique no. (i). Surprisingly, the obtained crystals (1) were perfected if the process was an acidic pH at a cold temperature then perfect crystals occurred within a day. Crystals of compound (2) grew easily using technique no. (ii) which are various polar solvents over a wide range of pH and temperature preparation processes. The infrared spectroscopy and nuclear magnetic resonance spectra fit well with these two X-ray crystal structures. The crystal structures of sildenafil free base and salt forms were different from their different growing conditions leading to stability difference. PMID:26594116

  8. Ab initio structural and vibrational investigation of sulfuric acid monohydrate.

    PubMed

    Partanen, Lauri; Hänninen, Vesa; Halonen, Lauri

    2012-03-22

    We employ ab initio methods to find stable geometries and to calculate potential energy surfaces and vibrational wavenumbers for sulfuric acid monohydrate. Geometry optimizations are carried out with the explicitly correlated coupled-cluster approach that includes single, double, and perturbative triple excitations (CCSD(T)-F12a) with a valence double-ζ basis set (VDZ-F12). Four different stable geometries are found, and the two lowest are within 0.41 kJ mol(-1) (or 34 cm(-1)) of each other. Vibrational harmonic wavenumbers are calculated at both the density-fitted local spin component scaled second-order Møller-Plesset perturbation theory (DF-SCS-LMP2) with the aug-cc-pV(T+d)Z basis set and the CCSD-F12/VDZ-F12 level. Water O-H stretching vibrations and two highly anharmonic large-amplitude motions connecting the three lowest potential energy minima are considered by limiting the dimensionality of the corresponding potential energy surfaces to small two- or three-dimensional subspaces that contain only strongly coupled vibrational degrees of freedom. In these anharmonic domains, the vibrational problem is solved variationally using potential energy surfaces calculated at the CCSD(T)-F12a/VDZ-F12 level. PMID:22260481

  9. L-Tryptophan L-tryptophanium bromide: Anhydrous and monohydrate

    NASA Astrophysics Data System (ADS)

    Ghazaryan, V. V.; Giester, G.; Fleck, M.; Petrosyan, A. M.

    2015-12-01

    L-Tryptophan L-tryptophanium bromide (I) and L-tryptophan L-tryptophanium bromide monohydrate (II) are new salts with (A⋯A+) type dimeric cation. The salt (I) crystallizes in the monoclinic system (space group P21, Z = 2) and is isostructural with respective chloride (V.V. Ghazaryan et al., Spectrochim. Acta A 136(2015) 743-750), while the salt (II) was obtained previously (T. Takigawa et al., Bull. Chem. Soc. Jap. 39(1966) 2369-2378) and described as hemyhydrate without structure determination. The salt (II) crystallizes in orthorhombic system (space group P212121, Z = 4). The dimeric cations in (I) and (II) are formed by O-H⋯O hydrogen bonds with the O⋯O distances equal to 2.538(3) Å and 2.481(3) Å respectively. The infrared and Raman spectra of the crystals are studied and compared with the spectra of L-tryptophan L-tryptophanium chloride and L-tryptophanium bromide.

  10. The electrokinetic behavior of calcium oxalate monohydrate in macromolecular solutions

    NASA Technical Reports Server (NTRS)

    Curreri, P. A.; Onoda, G. Y., Jr.; Finlayson, B.

    1988-01-01

    Electrophoretic mobilities were measured for calcium oxalate monohydrate (COM) in solutions containing macromolecules. Two mucopolysaccharides (sodium heparin and chrondroitin sulfate) and two proteins (positively charged lysozyme and negatively charged bovine serum albumin) were studied as adsorbates. The effects of pH, calcium oxalate surface charge (varied by calcium or oxalate ion activity), and citrate concentration were investigated. All four macromolecules showed evidence for chemical adsorption. The macromolecule concentrations needed for reversing the surface charge indicated that the mucopopolysacchrides have greater affinity for the COM surface than the proteins. The amount of proteins that can chemically adsorb appears to be limited to approximately one monomolecular layer. When the surface charge is high, an insufficient number of proteins can chemically adsorb to neutralize or reverse the surface charge. The remaining surface charge is balanced by proteins held near the surface by longer range electrostatic forces only. Citrate ions at high concentrations appear to compete effectively with the negative protein for surface sites but show no evidence for competing with the positively charged protein.

  11. Hypoglycemic effects of vanadium on alloxan monohydrate induced diabetic dogs

    PubMed Central

    Kim, Joo-Min; Chung, Jin-Young; Lee, Sook-Yeon; Choi, Eun-Wha; Kim, Min-Kyu; Hwang, Cheol-Yong

    2006-01-01

    The hypoglycemic effects after oral administration of vanadium have been studied previously in many species such as rats, mice and even humans. However, there has been no prior report on the glucose lowering effect of vanadium on diabetic dogs. Therefore, the purpose of this study was to evaluate the hypoglycemic effects of oral vanadium on diabetic dogs. Diabetes mellitus in the dogs studied was induced by alloxan monohydrate intravenous injection. The dogs were divided into two groups, one was the diabetic control (DC) group (n = 4) and the other was the vanadium treated (DV) group (n = 6). Fresh water was supplied to the dogs in the DC group, but sodium metavanadate solution (0.1~0.2 mg/ml) was given to the dogs in DV group from one week after the alloxan injection. The fasting glucose levels, fructosamine and serum chemistry profiles were compared between the two groups weekly for three weeks. The fasting blood glucose levels in DV group were significantly lower than those in the DC group (p < 0.01). Fructosamine levels in the DV group were also lower than those in the DC group (p < 0.05). The serum chemistry profiles were not significantly different in comparisons between the two groups. However, the cholesterol levels were significantly lower in the DV group compared to the DC group (p < 0.05). Our findings showed that oral vanadium administration had a hypoglycemic effect on chemically induced diabetic dogs. PMID:17106233

  12. Why sildenafil and sildenafil citrate monohydrate crystals are not stable?

    PubMed

    Sawatdee, Somchai; Pakawatchai, Chaveng; Nitichai, Kwanjai; Srichana, Teerapol; Phetmung, Hirihattaya

    2015-10-01

    Sildenafil citrate was crystallized by various techniques aiming to determine the behavior and factors affecting the crystal growth. There are only 2 types of sildenafil obtaining from crystallization: sildenafil (1) and sildenafil citrate monohydrate (2). The used techniques were (i) crystallization from saturated solutions, (ii) addition of an antisolvent, (iii) reflux and (iv) slow solvent evaporation method. By pursuing these various methods, our work pointed that the best formation of crystal (1) was obtained from technique no. (i). Surprisingly, the obtained crystals (1) were perfected if the process was an acidic pH at a cold temperature then perfect crystals occurred within a day. Crystals of compound (2) grew easily using technique no. (ii) which are various polar solvents over a wide range of pH and temperature preparation processes. The infrared spectroscopy and nuclear magnetic resonance spectra fit well with these two X-ray crystal structures. The crystal structures of sildenafil free base and salt forms were different from their different growing conditions leading to stability difference. PMID:26594116

  13. Characterization of a new anhydrous form of Rotundine and its monohydrate

    NASA Astrophysics Data System (ADS)

    Yang, Shiying; Du, Guanhua; Lu, Yang

    2015-09-01

    Rotundine is a chemical drug developed from Chinese traditional medicines that exhibits pseudopolymorphism. The anhydrous form and monohydrate are isolated and prepared via systemic crystallization screening, and the anhydrous form is reported for the first time. In this article single crystal X-ray diffractometry, powder X-ray diffractometry and FT-IR spectroscopy are used to characterize the Rotundine modifications. The analysis results show that the factors of crystal symmetry, intermolecular arrangements, conformational flexibility, hydrogen bonding interactions, and the incorporation of water finally lead to produce the polymorphic phenomenon. Via the in-vivo bioavailability of two forms, it is found that the new anhydrous form presents absorbable superiority relative to monohydrate, specifically Cmax and AUC of anhydrous form were approximately 1.5 times those of monohydrate. Study on the transformation of two forms show that they can convert to each other in certain conditions at solid state.

  14. Glycemic Effects and Safety of L-Glutamine Supplementation with or without Sitagliptin in Type 2 Diabetes Patients—A Randomized Study

    PubMed Central

    Samocha-Bonet, Dorit; Chisholm, Donald J.; Gribble, Fiona M.; Coster, Adelle C. F.; Carpenter, Kevin H.; Jones, Graham R. D.; Holst, Jens J.; Greenfield, Jerry R.

    2014-01-01

    Background and Aims L-glutamine is an efficacious glucagon-like peptide (GLP)-1 secretagogue in vitro. When administered with a meal, glutamine increases GLP-1 and insulin excursions and reduces postprandial glycaemia in type 2 diabetes patients. The aim of the study was to assess the efficacy and safety of daily glutamine supplementation with or without the dipeptidyl peptidase (DPP)-4 inhibitor sitagliptin in well-controlled type 2 diabetes patients. Methods Type 2 diabetes patients treated with metformin (n = 13, 9 men) with baseline glycated hemoglobin (HbA1c) 7.1±0.3% (54±4 mmol/mol) received glutamine (15 g bd)+ sitagliptin (100 mg/d) or glutamine (15 g bd) + placebo for 4 weeks in a randomized crossover study. Results HbA1c (P = 0.007) and fructosamine (P = 0.02) decreased modestly, without significant time-treatment interactions (both P = 0.4). Blood urea increased (P<0.001) without a significant time-treatment interaction (P = 0.8), but creatinine and estimated glomerular filtration rate (eGFR) were unchanged (P≥0.5). Red blood cells, hemoglobin, hematocrit, and albumin modestly decreased (P≤0.02), without significant time-treatment interactions (P≥0.4). Body weight and plasma electrolytes remained unchanged (P≥0.2). Conclusions Daily oral supplementation of glutamine with or without sitagliptin for 4 weeks decreased glycaemia in well-controlled type 2 diabetes patients, but was also associated with mild plasma volume expansion. Trial Registration ClincalTrials.gov NCT00673894 PMID:25412338

  15. Sildenafil citrate monohydrate-cyclodextrin nanosuspension complexes for use in metered-dose inhalers.

    PubMed

    Sawatdee, Somchai; Phetmung, Hirihattaya; Srichana, Teerapol

    2013-10-15

    Sildenafil is a selective phosphodiesterase-5 inhibitor used for the treatment of erectile dysfunction and pulmonary hypertension. Sildenafil citrate monohydrate was complexed with α-, hydroxypropyl-β- and γ-cyclodextrin (α-CD, HP-β-CD and γ-CD, respectively) to enhance its water solubility. The complexes of sildenafil citrate monohydrate with all types of CDs were characterized by phase solubility diagrams, (1)H and (13)C NMR, and dielectric constants. Sildenafil citrate monohydrate complexed with CDs was developed as nanosuspensions for use in a pressurized metered-dose inhaler (pMDI). Sildenafil citrate monohydrate pMDI formulations were prepared by a bottom-up process using dried ethanol as a solvent and HFA-134a as an antisolvent and propellant in order to form nanosuspensions. A 3×3 factorial design was applied for the contents of the dried ethanol and HFA-134a propellant. The phase solubility profiles of the sildenafil and cyclodextrins were described as AL type with a mole ratio 1:1. The piperazine moiety of sildenafil formed an inclusion in the cavity of the CDs. The particle diameters of the sildenafil citrate monohydrate suspensions in pMDIs were all within a nanosuspension size range. An assay of the sildenafil content showed that the formation of complexes with CDs was close to 100%. In the case of the formulations with CDs, the emitted doses varied within 97.4±10.8%, the fine particle fractions (FPFs) were in a range of 45-81%, the fine particle dose (FPD) was 12.6±2.0 μg and the mass median aerodynamic diameters (MMADs) were 1.86±0.41 μm. In contrast, the formulations without CDs produced a low emitted dose of sildenafil (<60%). Therefore, only sildenafil citrate monohydrate pMDI formulations containing CDs were suitable for use as aerosols. PMID:23876498

  16. Premixed acidic calcium phosphate cement: characterization of strength and microstructure.

    PubMed

    Aberg, J; Brisby, H; Henriksson, H B; Lindahl, A; Thomsen, P; Engqvist, H

    2010-05-01

    By using a premixed calcium phosphate cement (CPC), the handling properties of the cement are drastically improved, which is a challenge for traditional injectable CPCs. Previously premixed cements have been based on apatitic cements. In this article, acidic cement has been developed and evaluated. Monocalcium phosphate monohydrate and beta-tricalcium phosphate were mixed with glycerol to form a paste. As the paste does not contain water, no setting reaction starts and thus the working time is indefinite. Powder/liquid ratios (P/L) of 2.25, 3.5 and 4.75 were evaluated. Setting time (ST) and compressive strength (CS) were measured after 1 day, 1 week and 4 weeks in phosphate buffered saline (PBS) solution, and the corresponding microstructure was evaluated using electron microscopy and X-ray diffraction. The ST started when the cements were placed in PBS and ranged from 28 to 75 min, higher P/L gave a lower ST. Higher P/L also gave a higher CS, which ranged from 2 to 16 MPa. The microstructure mainly consisted of monetite, 1-5 microm in grain size. After 4 weeks in PBS, the strength increased. As acidic cements are resorbed faster in vivo, this cement should allow faster bone regeneration than apatitic cements. Premixed cements show a great handling benefit when compared with normal CPCs and can be formulated with similar ST and mechanical properties. PMID:20127991

  17. Guanidine-phosphate non-covalent interaction in LAP crystal growth solution evidenced from spectroscopy studies

    NASA Astrophysics Data System (ADS)

    Wang, L.; Zhang, G. H.; Wang, X. Q.; Zhu, L. Y.; Xu, D.

    2015-09-01

    The similar L-arginine molecule aggregation has been found in L-arginine (LA) and L-arginine phosphate monohydrate (LAP) aqueous solutions. The special fluorescence emission at 380 nm of LA aggregates in LAP solution has been found, compared with the emission of LA solution at 415 nm, which has an obvious blue shift. By comparing the fluorescence spectra of several solutions for L-arginine and L-lysine salts, the interaction between phosphate and guanidine in LAP solution was considered to be the cause of its special fluorescence emission. Meanwhile, when LAP molecule formed in solution, the fluorescence emission wavelength and the UV absorption intensity at 296 nm of L-arginine solutions have mutated. Therefore, the group interaction involved by guanidine has changed the fluorescence properties of L-arginine aggregates in LAP solution, indicating that the specific interaction between phosphate and guanidine exists in LAP molecule.

  18. Prediction of calcium oxalate monohydrate stone composition during ureteroscopy

    NASA Astrophysics Data System (ADS)

    Hamidizedah, Reza; Melnyk, Megan; Teichman, Joel M. H.

    2012-02-01

    Introduction: Prior research shows that Ho:YAG lithotripsy produces tiny dust fragments at low pulse energy (0.2J). However, calcium oxalate monohydrate (COM) stones may not fragment at this low pulse energy setting. Stone composition is rarely known until after surgery and historically, attempts to predict stone composition on the basis of endoscopic stone appearance were unsuccessful. Current endoscopic technology permits visual details that previously were not evident. As COM appears black under ambient light, we attempt to predict COM stone composition at the time of ureteroscopy based on its endoscopic appearance. Methods: Consecutive subjects undergoing ureteroscopy for stone disease were studied. Any portion of the stone that appeared black under endoscopic vision was considered clinical evidence of COM. Predicted stone composition was correlated with post-operative calculus analysis. Results: 46 consecutive ureteroscopic stone cases were analyzed prospectively. 25 of 28 subjects (89%) with black stones had stones later proven to be COM by composition analysis, versus one of 18 patients (6%) with non-black stones that were COM (p<0.0001). A black endoscopic stone appearance had a positive predictive value for COM of 89% and a non-black endoscopic stone appearance had a negative predictive value for COM of 94% (sensitivity 96%, specificity 83%). Conclusions: COM may reasonably be predicted intra-operatively by its black endoscopic appearance. The clinical utility would be to use higher laser pulse energy settings than for non-COM compositions. This data raises the possibility that more sophisticated optical characterization of endoscopic stone appearance may prove to be a useful tool to predict stone composition.

  19. Effects of dextromethorphan as add-on to sitagliptin on blood glucose and serum insulin concentrations in individuals with type 2 diabetes mellitus: a randomized, placebo-controlled, double-blinded, multiple crossover, single-dose clinical trial.

    PubMed

    Marquard, J; Stirban, A; Schliess, F; Sievers, F; Welters, A; Otter, S; Fischer, A; Wnendt, S; Meissner, T; Heise, T; Lammert, E

    2016-01-01

    In this clinical trial, we investigated the blood glucose (BG)-lowering effects of 30, 60 and 90 mg dextromethorphan (DXM) as well as 100 mg sitagliptin alone versus combinations of DXM and sitagliptin during an oral glucose tolerance test (OGTT) in 20 men with T2DM. The combination of 60 mg DXM plus 100 mg sitagliptin was observed to have the strongest effect in the OGTT. It lowered maximum BG concentrations and increased the baseline-adjusted area under the curve for serum insulin concentrations in the first 30 min of the OGTT (mean ± standard deviation 240 ± 47 mg/dl and 8.1 ± 6.1 mU/l/h, respectively) to a significantly larger extent than did 100 mg sitagliptin alone (254 ± 50 mg/dl and 5.8 ± 2.5 mU/l/h, respectively; p < 0.05) and placebo (272 ± 49 mg/dl and 3.9 ± 3.0 mU/l/h, respectively; p < 0.001). All study drugs were well tolerated, alone and in combination, without serious adverse events or hypoglycaemia. Long-term clinical trials are now warranted to investigate the potential of the combination of 30 or 60 mg DXM and dipeptidyl peptidase-4 inhibitors in the treatment of individuals with T2DM, in particular as preclinical studies have identified the β-cell protective properties of DXM. PMID:26362564

  20. Comparison of the Effects of Continuous Subcutaneous Insulin Infusion and Add-On Therapy with Sitagliptin in Patients with Newly Diagnosed Type 2 Diabetes Mellitus.

    PubMed

    Wan, Heng; Zhao, Defu; Shen, Jie; Lu, Lu; Zhang, Tong; Chen, Zhi

    2016-01-01

    To identify a new regimen to optimize treatment for patients with newly diagnosed type 2 diabetes (T2DM) by short-term continuous subcutaneous insulin infusion (CSII) alone. Methods. 60 patients with newly diagnosed T2DM were randomized into two groups (n = 30 each) and treated for 2 weeks with CSII alone (CSII group) or with CSII plus sitagliptin (CSII + Sig group). The glycemic variability of the patients was measured using a continuous glucose monitoring system (CGMS) for the last 72 hours. A standard meal test was performed before and after the interventions, and the levels of glycated albumin, fasting glucose, fasting C-peptide, postprandial 2 h blood glucose, and postprandial 2 h C-peptide were examined. Results. Compared with the CSII group, the indicators of glycemic variability, such as the mean amplitude of glycemic excursion (MAGE) and the standard deviation of blood glucose (SDBG), were decreased significantly in the CSII + Sig group. The changes before and after treatment in the C-peptide reactivity index (ΔCPI) and the secretory unit of islet in transplantation index (ΔSUIT) indicated a significant improvement in the CSII + Sig group. Conclusions. Add-on therapy with sitagliptin may be an optimized treatment for patients with newly diagnosed T2DM compared with short-term CSII alone. PMID:26798658

  1. Comparison of the Effects of Continuous Subcutaneous Insulin Infusion and Add-On Therapy with Sitagliptin in Patients with Newly Diagnosed Type 2 Diabetes Mellitus

    PubMed Central

    Wan, Heng; Zhao, Defu; Shen, Jie; Lu, Lu; Zhang, Tong; Chen, Zhi

    2016-01-01

    To identify a new regimen to optimize treatment for patients with newly diagnosed type 2 diabetes (T2DM) by short-term continuous subcutaneous insulin infusion (CSII) alone. Methods. 60 patients with newly diagnosed T2DM were randomized into two groups (n = 30 each) and treated for 2 weeks with CSII alone (CSII group) or with CSII plus sitagliptin (CSII + Sig group). The glycemic variability of the patients was measured using a continuous glucose monitoring system (CGMS) for the last 72 hours. A standard meal test was performed before and after the interventions, and the levels of glycated albumin, fasting glucose, fasting C-peptide, postprandial 2 h blood glucose, and postprandial 2 h C-peptide were examined. Results. Compared with the CSII group, the indicators of glycemic variability, such as the mean amplitude of glycemic excursion (MAGE) and the standard deviation of blood glucose (SDBG), were decreased significantly in the CSII + Sig group. The changes before and after treatment in the C-peptide reactivity index (ΔCPI) and the secretory unit of islet in transplantation index (ΔSUIT) indicated a significant improvement in the CSII + Sig group. Conclusions. Add-on therapy with sitagliptin may be an optimized treatment for patients with newly diagnosed T2DM compared with short-term CSII alone. PMID:26798658

  2. Sitagliptin inhibits endothelin-1 expression in the aortic endothelium of rats with streptozotocin-induced diabetes by suppressing the nuclear factor-κB/IκBα system through the activation of AMP-activated protein kinase

    PubMed Central

    TANG, SONG-TAO; SU, HUAN; ZHANG, QIU; TANG, HAI-QIN; WANG, CHANG-JIANG; ZHOU, QING; WEI, WEI; ZHU, HUA-QING; WANG, YUAN

    2016-01-01

    Emerging evidence suggests that dipeptidyl peptidase-4 (DPP-4) inhibitors, including sitagliptin, exert favourable effects on the vascular endothelium. DPP-4 inhibitors suppress the degradation of glucagon-like peptide-1 (GLP-1), which has been reported to enhance nitric oxide (NO) production. However, the effects of DPP-4 inhibitors on endothelin-1 (ET-1) expression in the aorta, as well as the underlying mechanisms responsible for these effects, have yet to be investigated in animal models of diabetes mellitus (DM). In the present study, the rats were randomly divided into the following four groups: i) control; ii) DM; iii) DM + low-dose sitagliptin (10 mg/kg); and iv) DM + high-dose sitagliptin (30 mg/kg). Apart from the control group, all the rats received a high-fat diet for 8 weeks prior to the induction of diabetes with an intraperitoneal injection of streptozotocin. The treatments were then administered for 12 weeks. The serum levels of ET-1, NO, GLP-1 and insulin were measured as well as endothelial function. The expression of ET-1, AMP-activated protein kinase (AMPK) and nuclear factor (NF)-κB/IκBα were determined. After 12 weeks of treatment, the diabetic rats receiving sitagliptin showed significantly elevated serum levels of GLP-1 and NO, and reduced levels of ET-1. Moreover, sitagliptin significantly attenuated endothelial dysfunction as well as the remodeling of the aortic wall. Notably, sitagliptin inhibited ET-1 expression at the transcriptional and translational level in the aorta, which may have been mediated by the suppression of the NF-κB/IκBα system induced by AMPK activation. The majority of the above-mentioned effects were dose dependent. Taken together, the findings of the present study indicate that sitagliptin inhibits ET-1 expression in the aortic endothelium by suppressing the NF-κB/IκBα system through the activation of the AMPK pathway in diabetic rats. These findings further demonstrate some of the vasoprotective properties of DPP-4 inhibitors in vivo. PMID:27122056

  3. Sitagliptin inhibits endothelin-1 expression in the aortic endothelium of rats with streptozotocin-induced diabetes by suppressing the nuclear factor-κB/IκBα system through the activation of AMP-activated protein kinase.

    PubMed

    Tang, Song-Tao; Su, Huan; Zhang, Qiu; Tang, Hai-Qin; Wang, Chang-Jiang; Zhou, Qing; Wei, Wei; Zhu, Hua-Qing; Wang, Yuan

    2016-06-01

    Emerging evidence suggests that dipeptidyl peptidase-4 (DPP-4) inhibitors, including sitagliptin, exert favourable effects on the vascular endothelium. DPP-4 inhibitors suppress the degradation of glucagon-like peptide-1 (GLP‑1), which has been reported to enhance nitric oxide (NO) production. However, the effects of DPP-4 inhibitors on endothelin-1 (ET-1) expression in the aorta, as well as the underlying mechanisms responsible for these effects, have yet to be investigated in animal models of diabetes mellitus (DM). In the present study, the rats were randomly divided into the following four groups: i) control; ii) DM; iii) DM + low‑dose sitagliptin (10 mg/kg); and iv) DM + high‑dose sitagliptin (30 mg/kg). Apart from the control group, all the rats received a high-fat diet for 8 weeks prior to the induction of diabetes with an intraperitoneal injection of streptozotocin. The treatments were then administered for 12 weeks. The serum levels of ET-1, NO, GLP-1 and insulin were measured as well as endothelial function. The expression of ET-1, AMP-activated protein kinase (AMPK) and nuclear factor (NF)-κB/IκBα were determined. After 12 weeks of treatment, the diabetic rats receiving sitagliptin showed significantly elevated serum levels of GLP-1 and NO, and reduced levels of ET-1. Moreover, sitagliptin significantly attenuated endothelial dysfunction as well as the remodeling of the aortic wall. Notably, sitagliptin inhibited ET-1 expression at the transcriptional and translational level in the aorta, which may have been mediated by the suppression of the NF-κB/IκBα system induced by AMPK activation. The majority of the above-mentioned effects were dose dependent. Taken together, the findings of the present study indicate that sitagliptin inhibits ET-1 expression in the aortic endothelium by suppressing the NF-κB/IκBα system through the activation of the AMPK pathway in diabetic rats. These findings further demonstrate some of the vasoprotective properties of DPP-4 inhibitors in vivo. PMID:27122056

  4. Regulation of serum phosphate

    PubMed Central

    Lederer, Eleanor

    2014-01-01

    The regulation of serum phosphate, an acknowledged risk factor for chronic kidney disease and cardiovascular mortality, is poorly understood. The discovery of fibroblast growth factor 23 (FGF23) as a key regulator of renal phosphate handling and activation of vitamin D has revolutionized our comprehension of phosphate homeostasis. Through as yet undetermined mechanisms, circulating and dietary phosphate appear to have a direct effect on FGF23 release by bone cells that, in turn, causes renal phosphate excretion and decreases intestinal phosphate absorption through a decrease in vitamin D production. Thus, the two major phosphaturic hormones, PTH and FGF23, have opposing effects on vitamin D production, placing vitamin D at the nexus of phosphate homeostasis. While our understanding of phosphate homeostasis has advanced, the factors determining regulation of serum phosphate level remain enigmatic. Diet, time of day, season, gender, age and genetics have all been identified as significant contributors to serum phosphate level. The effects of these factors on serum phosphate have major implications for what is understood as ‘normal’ and for studies of phosphate homeostasis and metabolism. Moreover, other hormonal mediators such as dopamine, insulin-like growth factor, and angiotensin II also affect renal handling of phosphate. How the major hormone effects on phosphate handling are regulated and how the effect of these other factors are integrated to yield the measurable serum phosphate are only now beginning to be studied. PMID:24973411

  5. Monohydrate catalysis of excited-state double-proton transfer in 7-azaindole

    SciTech Connect

    Pi-Tai Chou; Martinez, M.L.; Cooper, W.C.

    1992-06-25

    In this paper, the green fluorescence of 7-azaindole polyhydrate in liquid water solution is likely not due to tautomerization but due to solvent rearrangement inhibition. 7-azaindole monohydrate also undergoes excited-state double-proton transfer. 17 refs., 3 figs.

  6. Influence of solvents on the habit modification of alpha lactose monohydrate single crystals

    NASA Astrophysics Data System (ADS)

    Parimaladevi, P.; Srinivasan, K.

    2013-02-01

    Restricted evaporation of solvent method was adopted for the growth of alpha lactose monohydrate single crystals from different solvents. The crystal habits of grown crystals were analysed. The form of crystallization was confirmed by powder x-ray diffraction analysis. Thermal behaviour of the grown crystals was studied by using differential scanning calorimetry.

  7. Growth and adhesion properties of monosodium urate monohydrate (MSU) crystals

    NASA Astrophysics Data System (ADS)

    Perrin, Clare M.

    The presence of monosodium urate monohydrate (MSU) crystals in the synovial fluid has long been associated with the joint disease gout. To elucidate the molecular level growth mechanism and adhesive properties of MSU crystals, atomic force microscopy (AFM), scanning electron microscopy, and dynamic light scattering (DLS) techniques were employed in the characterization of the (010) and (1-10) faces of MSU, as well as physiologically relevant solutions supersaturated with urate. Topographical AFM imaging of both MSU (010) and (1-10) revealed the presence of crystalline layers of urate arranged into v-shaped features of varying height. Growth rates were measured for both monolayers (elementary steps) and multiple layers (macrosteps) on both crystal faces under a wide range of urate supersaturation in physiologically relevant solutions. Step velocities for monolayers and multiple layers displayed a second order polynomial dependence on urate supersaturation on MSU (010) and (1-10), with step velocities on (1-10) generally half of those measured on MSU (010) in corresponding growth conditions. Perpendicular step velocities on MSU (010) were obtained and also showed a second order polynomial dependence of step velocity with respect to urate supersaturation, which implies a 2D-island nucleation growth mechanism for MSU (010). Extensive topographical imaging of MSU (010) showed island adsorption from urate growth solutions under all urate solution concentrations investigated, lending further support for the determined growth mechanism. Island sizes derived from DLS experiments on growth solutions were in agreement with those measured on MSU (010) topographical images. Chemical force microscopy (CFM) was utilized to characterize the adhesive properties of MSU (010) and (1-10). AFM probes functionalized with amino acid derivatives and bio-macromolecules found in the synovial fluid were brought into contact with both crystal faces and adhesion forces were tabulated into histograms for comparison. AFM probes functionalized with -COO-, -CH3, and -OH functionalities displayed similar adhesion force with both crystal surfaces of MSU, while adhesion force on (1-10) was three times greater than (010) for -NH2+ probes. For AFM probes functionalized with bovine serum albumin, adhesion force was three times greater on MSU (1-10) than (010), most likely due to the more ionic nature of (1-10).

  8. Microbial solubilization of phosphate

    DOEpatents

    Rogers, R.D.; Wolfram, J.H.

    1993-10-26

    A process is provided for solubilizing phosphate from phosphate containing ore by treatment with microorganisms which comprises forming an aqueous mixture of phosphate ore, microorganisms operable for solubilizing phosphate from the phosphate ore and maintaining the aqueous mixture for a period of time and under conditions operable to effect the microbial solubilization process. An aqueous solution containing soluble phosphorus can be separated from the reacted mixture by precipitation, solvent extraction, selective membrane, exchange resin or gravity methods to recover phosphate from the aqueous solution. 6 figures.

  9. Microbial solubilization of phosphate

    DOEpatents

    Rogers, Robert D.; Wolfram, James H.

    1993-01-01

    A process is provided for solubilizing phosphate from phosphate containing ore by treatment with microorganisms which comprises forming an aqueous mixture of phosphate ore, microorganisms operable for solubilizing phosphate from the phosphate ore and maintaining the aqueous mixture for a period of time and under conditions operable to effect the microbial solubilization process. An aqueous solution containing soluble phosphorous can be separated from the reacted mixture by precipitation, solvent extraction, selective membrane, exchange resin or gravity methods to recover phosphate from the aqueous solution.

  10. beta-TCP/MCPM-based premixed calcium phosphate cements.

    PubMed

    Han, Bing; Ma, Peng-Wei; Zhang, Li-Li; Yin, Yu-Ji; Yao, Kang-De; Zhang, Fu-Jiang; Zhang, Yong-Dong; Li, Xiu-Lan; Nie, Wei

    2009-10-01

    Novel premixed calcium phosphate cements (CPCs) were prepared by combining cement liquids comprised of glycerol or polyethylene glycol with CPC powders that consisted of beta-tricalcium phosphate (beta-TCP) and monocalcium phosphate monohydrate (MCPM). Changing the powder to liquid mass ratio enabled the setting time to be regulated, and improved the compressive strength of the CPCs. Although some ratios of the new premixed CPCs had long setting times, these ranged from 12.4 to 27.8 min which is much shorter than the hour or more reported previously for a premixed CPC. The premixed CPCs had tolerable washout resistance before final setting, and the cements had strengths matching that of cancellous bone (5-10 MPa); their maximum compressive strength was up to 12 MPa. The inflammatory response around the premixed CPCs implanted in the subcutaneous tissue in rabbits was more prominent than that of apatite cement. These differences might be due to the much faster resorption rate of the premixed CPCs. PMID:19427931

  11. Retrospective Analysis on the Efficacy, Safety and Treatment Failure Group of Sitagliptin for Mean 10-Month Duration

    PubMed Central

    Kim, Won Jun; Jeong, Eun Haeng; Seo, Jeong Youn; Seol, Ji Soo; Park, Se Eun; Rhee, Eun Jung; Lee, Won Young; Oh, Ki Won; Park, Sung Woo; Kim, Sun Woo

    2011-01-01

    Background To investigate the clinical results of sitagliptin (SITA) and the characteristics of the treatment failure group or of low responders to SITA. Methods A retrospective study of type 2 diabetic patients reviewed 99 cases, including 12 treatment failure cases, who stopped SITA because of worsening patients' condition, and 87 cases, who continued treatment over five visits (total 9.9±10.1 months) after receiving the prescription of SITA from December 2008 to June 2009. Subjects were classified as five groups administered SITA as an initial combination with metformin (MET), add-on to metformin or sulfonylurea, and switching from sulfonylurea or thiazolidinedione. The changes in HbA1c level from the first to last visit (ΔHbA1c) in treatment maintenance group were subanalyzed. Results The HbA1c level was significantly reduced in four groups, including initial coadministration of SITA with metformin (ΔHbA1c=-1.1%, P<0.001), add-on to MET (ΔHbA1c=-0.6%, P=0.017), add-on to sulfonylurea (ΔHbA1c=-0.5%, P<0.001), and switching from thiazolidinedione (ΔHbA1c=-0.3%, P=0.013). SITA was noninferior to sulfonlyurea (ΔHbA1c=-0.2%, P=0.63). There was no significant adverse effect. The treatment failure group had a longer diabeties duration (P=0.008), higher HbA1c (P=0.001) and fasting plasma glucose (P=0.003) compared to the maintenance group. Subanalysis on the tertiles of ΔHbA1c showed that low-response to SITA (tertile 1) was associated with a longer diabetes duration (P=0.009) and lower HbA1c (P<0.001). Conclusion SITA was effective and safe for use in Korean type 2 diabetic patients. However, its clinical responses and long-term benefit-harm profile is yet to be established. PMID:21785750

  12. Sorption behavior of Zn(II) ions on synthetic apatitic calcium phosphates

    NASA Astrophysics Data System (ADS)

    Sebei, Haroun; Pham Minh, Doan; Nzihou, Ange; Sharrock, Patrick

    2015-12-01

    The synthesis, characterization and the reactivity of apatitic calcium phosphates (Ca-HA, chemical formula Ca10(PO4)6(OH)2) is reported. Calcium carbonate (CaCO3) and potassium dihydrogen orthophosphate (KH2PO4) were selected as economical starting materials for the synthesis of Ca-HA under atmospheric conditions. Monocalcium phosphate monohydrate (MCPM), dicalcium phosphate dihydrate (DCPD), and octacalcium phosphate pentahydrate (OCP) were identified as the main intermediates of the synthesis reaction. The product obtained after 48 h of reaction contains mainly low-crystalline Ca-HA and small amounts of other calcium phosphates such as octacalcium phosphate (OCP), B-type carbonate apatite (CAP), as well as unreacted calcium carbonate. This Ca-HA was found to be active for the removal of Zn2+ from an aqueous solution. Its sorption capacity reached up to 120 mg of Zn2+ per g of Ca-HA powder after 24 h of reaction. The monitoring of soluble Zn, Ca and P during the sorption experiment allowed characterizing the mechanism of Zn uptake. Dissolution-precipitation, ionic exchange and surface complexation are the three main mechanisms involved in the sorption processes. The contribution of these mechanisms is discussed in detail.

  13. Chloroquine Phosphate Oral

    MedlinePlus

    Chloroquine phosphate is in a class of drugs called antimalarials and amebicides. It is used to prevent and treat ... Chloroquine phosphate comes as a tablet to take by mouth. For prevention of malaria in adults, one dose is ...

  14. Uranium from phosphate ores

    SciTech Connect

    Hurst, F.J.

    1983-01-01

    The following topics are described briefly: the way phosphate fertilizers are made; how uranium is recovered in the phosphate industry; and how to detect covert uranium recovery operations in a phsophate plant.

  15. Effects of phosphates on microstructure and bioactivity of micro-arc oxidized calcium phosphate coatings on Mg-Zn-Zr magnesium alloy.

    PubMed

    Pan, Y K; Chen, C Z; Wang, D G; Zhao, T G

    2013-09-01

    Calcium phosphate (CaP) coatings were prepared on Mg-Zn-Zr magnesium alloy by micro-arc oxidation (MAO) in electrolyte containing calcium acetate monohydrate (CH3COO)2Ca·H2O) and different phosphates (i.e. disodium hydrogen phosphate dodecahydrate (Na2HPO4·12H2O), sodium phosphate (Na3PO4·H2O) and sodium hexametaphosphate((NaPO3)6)). Scanning electron microscope (SEM), energy-dispersive X-ray spectrometry (EDS) and X-ray diffractometer (XRD) were employed to characterize the microstructure, elemental distribution and phase composition of the CaP coatings. Simulated body fluid (SBF) immersion test was used to evaluate the coating bioactivity and degradability. Systemic toxicity test was used to evaluate the coating biocompatibility. Fluoride ion selective electrode (ISE) was used to measure F(-) ions concentration during 30 days SBF immersion. The CaP coatings effectively reduced the corrosion rate and the surfaces of CaP coatings were covered by a new layer formed of numerous needle-like and scale-like apatites. The formation of these calcium phosphate apatites indicates that the coatings have excellent bioactivity. The coatings formed in (NaPO3)6-containging electrolyte exhibit thicker thickness, higher adhesive strength, slower degradation rate, better apatite-inducing ability and biocompatibility. PMID:23603036

  16. Understanding the molecular dynamics of type-2 diabetes drug target DPP-4 and its interaction with Sitagliptin and inhibitor Diprotin-A.

    PubMed

    Chakraborty, Chiranjib; Hsu, Minna J; Agoramoorthy, Govindasamy

    2014-11-01

    The occurrence of type 2 diabetes (T2D) accounts for 90-95 % of all diabetes. Intestine hormone glucagon-like peptide-1 (GLP-1) has an antidiabetic role that enhances insulin secretion and pancreatic β-cell proliferation. GLP-1 is degraded by the enzyme dipeptidyl peptidase-4 (DPP-4) rapidly. Hence, the DPP-4 inhibition has been preferred not only for the treatment but also as a major drug target. Sitagliptin and Diprotin-A are antihyperglycemic agents for the treatment of T2D. However, little is known on the molecular dynamics of DPP-4 and the interaction properties with its ligands, namely Sitagliptin and Diprotin-A. This study has used the latest bioinformatic tools to understand the molecular dynamics and its interaction properties of DPP-4. This study has explored the number of α helices, β strands, β hairpins, Ψ loop, β bulges, β turns, and ϒ turns and they were 19, 46, 25, 1, 14, 70, and 4, respectively. The highest number of H-bonds was recorded in α helix of domain-1, and the lowest number H-bonds were noted in α helix of domain-2. During interaction between residues, in A- and B-chain, 47 and 48 residues are involved for interaction, and interaction interface area was more in A-Chain (2176 Å(2)). From DPP-4 and Sitagliptin interaction, three residues in active sites such as Try226, Glu205, and Glu206 were involved in three H-bond formation, while 10 other amino acids (Try547, Try667, Asn710, Val711, His740, Ser630, Ser209, Arg358, Phe357, and Val207) were involved in hydrophobic interactions. In this review, we have shown the importance of bioinformatics as an excellent tool for a rapid method to assess the molecular dynamics and its interaction properties of DPP-4. Our predictions highlighted in this review will help researchers to understand the interaction properties and recognition of interactive sites to design more DPP-4 inhibitors for the treatment of T2D and drug discovery. PMID:24809328

  17. Porosity prediction of calcium phosphate cements based on chemical composition.

    PubMed

    Öhman, Caroline; Unosson, Johanna; Carlsson, Elin; Ginebra, Maria Pau; Persson, Cecilia; Engqvist, Håkan

    2015-07-01

    The porosity of calcium phosphate cements has an impact on several important parameters, such as strength, resorbability and bioactivity. A model to predict the porosity for biomedical cements would hence be a useful tool. At the moment such a model only exists for Portland cements. The aim of this study was to develop and validate a first porosity prediction model for calcium phosphate cements. On the basis of chemical reaction, molar weight and density of components, a volume-based model was developed and validated using calcium phosphate cement as model material. 60 mol% β-tricalcium phosphate and 40 mol% monocalcium phosphate monohydrate were mixed with deionized water, at different liquid-to-powder ratios. Samples were set for 24 h at 37°C and 100% relative humidity. Thereafter, samples were dried either under vacuum at room temperature for 24 h or in air at 37 °C for 7 days. Porosity and phase composition were determined. It was found that the two drying protocols led to the formation of brushite and monetite, respectively. The model was found to predict well the experimental values and also data reported in the literature for apatite cements, as deduced from the small absolute average residual errors (<2.0%). In conclusion, a theoretical model for porosity prediction was developed and validated for brushite, monetite and apatite cements. The model gives a good estimate of the final porosity and has the potential to be used as a porosity prediction tool in the biomedical cement field. PMID:26169187

  18. Reactive calcium-phosphate-containing poly(ester-co-ether) methacrylate bone adhesives: setting, degradation and drug release considerations.

    PubMed

    Zhao, Xin; Olsen, Irwin; Pratten, Jonathan; Knowles, Jonathan C; Young, Anne M

    2011-09-01

    This study has investigated novel bone adhesives consisting of fluid photo-polymerizable poly(lactide-co-propylene glycol-co-lactide)dimethacrylate (PGLA-DMA) mixed with systematically varying fillers of β-tricalcium phosphate (β-TCP) and monocalcium phosphate monohydrate (MCPM), for the delivery of an antibacterial drug chlorhexidine (CHX). All formulations were found to polymerize fully within 200 s after exposure to blue light. In addition, water sorption by the polymerized materials catalyzed varying filler conversion to dicalcium phosphate (DCP) (i.e. brushite and monetite). With greater DCP levels, faster degradation was observed. Moreover, increase in total filler content enhanced CHX release, associated with higher antibacterial activity. These findings thus suggest that such rapid-setting and degradable adhesives with controllable drug delivery property could have potential clinical value as bone adhesives with antibacterial activity. PMID:21706218

  19. Crystal growth mechanisms of the (0 1 0) face of α-lactose monohydrate crystals

    NASA Astrophysics Data System (ADS)

    Dincer, T. D.; Ogden, M. I.; Parkinson, G. M.

    2009-04-01

    The growth rates of the (0 1 0) face of α-lactose monohydrate crystals were measured at 30, 40 and 50 °C in the relative supersaturation range 0.55-2.33 in aqueous solutions. The mechanisms of growth were investigated. Spiral growth was found to be the mechanism of growth up to a critical relative supersaturation ( s-1) crit=1.9 at 30 °C. Above the critical relative supersaturation, the crystal growth mechanisms were predicted to change. All growth models fit equally well to the growth rates. No two-dimensional nucleation was observed above critical supersaturation by AFM. On the other hand increased step height and roughness on the edges of steps were observed. It was concluded that the growth mechanism of the (0 1 0) face of α-lactose monohydrate crystal is spiral growth. A parabolic relationship was obtained below critical supersaturation followed by a linear relationship with relative supersaturation.

  20. Stability of the crystalline form of cefaclor monohydrate and its pharmaceutical preparations.

    PubMed

    Medenecka, Beata; Jelińska, Anna; Zajac, Marianna; Bałdyka, Magdalena; Juszkiewicz, Krzysztof; Oszczapowicz, Irena

    2009-01-01

    The influence of temperature and relative air humidity on the stability of cefaclor monohydrate in crystalline form and in its pharmaceutical preparations (oral suspension and slow release tablets) was investigated. The process of degradation was studied by using high-performance liquid chromatography with ultraviolet (UV) detection, as described in the monograph of cefaclor in European Pharmacopoeia. The degradation of cefaclor monohydrate in substance, in oral suspension and tablets at relative air humidity RH > 50% is a first-order autocatalytic reaction relative to substrate concentration, while at 0% RH the degradation of cefaclor in substance is a first-order reaction relative to substrate concentration. The kinetic and thermodynamic parameters of degradation were calculated. PMID:19894653

  1. Exercise performance and muscle contractile properties after creatine monohydrate supplementation in aerobic-anaerobic training rats.

    PubMed

    Boyadjiev, Nickolay; Popov, Dobrin; Delchev, Slavi

    2007-01-01

    The purpose of this study was to investigate the effects of creatine monohydrate supplementation on exercise performance and contractile variables in aerobic-anaerobic training rats. Twenty 90-day-old male Sprague Dawley rats were divided into two groups - creatine (Cr) and controls (K). The creatine group received creatine monohydrate as a nutritional supplement, whereas the control group was given placebo. Both groups were trained 5 days a week on a treadmill for 20 days in a mixed (aerobic-anaerobic) metabolic working regimen (27 m·min(-1), 15% elevation for 40 min). The exercise performance (sprint-test), contractile properties (m. tibialis anterior), oxidative enzyme activity (SDH, LDH, NADH2) in m. soleus and blood hematological and chemical variables were assessed in the groups at the end of the experiment. It was found out that creatine supplementation improved the exercise performance after 20 days of administration in a dose of 60 mg per day on the background of a mixed (aerobic-anaerobic) exercise training. At the end of the trial the Cr-group demonstrated better values for the variables which characterize the contractile properties of m. tibialis anterior containing predominantly types IIA and IIB muscle fibers. On the other hand, a higher oxidative capacity was found out in m. soleus (type I muscle fibers) as a result of 20-day creatine supplementation. No side effects of creatine monohydrate supplementation were assessed by the hematological and blood biochemical indices measured in this study. Key pointsThe creatine monohydrate supplementation of the rats diet improves their exercise performance after 20 days administration in a dose of 60 mg per day on the background of a mixed (aerobic-anaerobic) exercise training.The creatine supplemented rats demonstrate better contractile properties of m. tibialis anterior which muscle contains predominantly types IIA and IIB muscle fibers.The soleus muscle (type I muscle fibers) demonstrates a higher oxidative capacity as a result of 20-days creatine supplementation. PMID:24149473

  2. Kinetic studies on the loss of water from α-D-glucose monohydrate.

    PubMed

    Ponschke, Michelle A; House, James E

    2011-10-18

    Although the dehydration of α-D-glucose monohydrate is an important aspect of several industrial processes, there is uncertainty with regard to the applicable rate law and other factors that affect dehydration. Therefore, the dehydration of three glucose monohydrate samples has been studied using isothermal gravimetric analysis. Dehydration follows a one-dimensional contraction (R1) rate law for the majority of kinetic runs, and an activation energy of 65.0±3.9 kJ mol(-1) results when the rate constants are fitted to the Arrhenius equation. Fitting the rate constants to the Eyring equation results in values of 62.1±3.7 kJ mol(-1) and -77.8±4.7 J mol(-1)K(-1) for ΔH(‡) and ΔS(‡), respectively. The impedance effect on the loss of water vapor has also been investigated to determine the values for activation energy, enthalpy, and entropy for diffusion of water. The results obtained for the activation parameters are interpreted in terms of the absolute entropies of anhydrous glucose and the monohydrate. PMID:21831365

  3. Preparation of bis-(1(2)H-tetrazol-5-yl)-amine monohydrate

    DOEpatents

    Naud, Darren L.; Hiskey, Michael A.

    2003-05-27

    A process of preparing bis-(1(2)H-tetrazol-5-yl)-amine monohydrate is provided including combining a dicyanamide salt, an azide salt and water to form a first reaction mixture, adding a solution of a first strong acid characterized as having a pKa of less than about 1 to said first reaction mixture over a period of time characterized as providing a controlled reaction rate so as to gradually form hydrazoic acid without loss of significant quantities of hydrazoic acid from the solution while heating the first reaction mixture at temperatures greater than about 65.degree. C., heating the resultant reaction mixture at temperatures greater than about 65.degree. C. for a period of time sufficient to substantially completely form a reaction product, treating the reaction product with a solution of a second strong acid to form a product of bis-(1(2)H-tetrazol-5-yl)-amine monohydrate, and, recovering the bis-(1(2)H-tetrazol-5-yl)-amine monohydrate product.

  4. Phosphate, inositol and polyphosphates.

    PubMed

    Livermore, Thomas M; Azevedo, Cristina; Kolozsvari, Bernadett; Wilson, Miranda S C; Saiardi, Adolfo

    2016-02-15

    Eukaryotic cells have ubiquitously utilized the myo-inositol backbone to generate a diverse array of signalling molecules. This is achieved by arranging phosphate groups around the six-carbon inositol ring. There is virtually no biological process that does not take advantage of the uniquely variable architecture of phosphorylated inositol. In inositol biology, phosphates are able to form three distinct covalent bonds: phosphoester, phosphodiester and phosphoanhydride bonds, with each providing different properties. The phosphoester bond links phosphate groups to the inositol ring, the variable arrangement of which forms the basis of the signalling capacity of the inositol phosphates. Phosphate groups can also form the structural bridge between myo-inositol and diacylglycerol through the phosphodiester bond. The resulting lipid-bound inositol phosphates, or phosphoinositides, further expand the signalling potential of this family of molecules. Finally, inositol is also notable for its ability to host more phosphates than it has carbons. These unusual organic molecules are commonly referred to as the inositol pyrophosphates (PP-IPs), due to the presence of high-energy phosphoanhydride bonds (pyro- or diphospho-). PP-IPs themselves constitute a varied family of molecules with one or more pyrophosphate moiety/ies located around the inositol. Considering the relationship between phosphate and inositol, it is no surprise that members of the inositol phosphate family also regulate cellular phosphate homoeostasis. Notably, the PP-IPs play a fundamental role in controlling the metabolism of the ancient polymeric form of phosphate, inorganic polyphosphate (polyP). Here we explore the intimate links between phosphate, inositol phosphates and polyP, speculating on the evolution of these relationships. PMID:26862212

  5. Brushite-based calcium phosphate cement with multichannel hydroxyapatite granule loading for improved bone regeneration.

    PubMed

    Sarkar, Swapan Kumar; Lee, Byung Yeol; Padalhin, Andrew Reyas; Sarker, Avik; Carpena, Nathaniel; Kim, Boram; Paul, Kallyanshish; Choi, Hwan Jun; Bae, Sang-Ho; Lee, Byong Taek

    2016-01-01

    In this work, we report brushite-based calcium phosphate cement (CPC) system to enhance the in vivo biodegradation and tissue in-growth by incorporation of micro-channeled hydroxyapatite (HAp) granule and silicon and sodium addition in calcium phosphate precursor powder. Sodium- and silicon-rich calcium phosphate powder with predominantly tri calcium phosphate (TCP) phase was synthesized by an inexpensive wet chemical route to react with mono calcium phosphate monohydrate (MCPM) for making the CPC. TCP nanopowder also served as a packing filler and moderator of the reaction kinetics of the setting mechanism. Strong sintered cylindrical HAp granules were prepared by fibrous monolithic (FM) process, which is 800 µm in diameter and have seven micro-channels. Acid sodium pyrophosphate and sodium citrate solution was used as the liquid component which acted as a homogenizer and setting time retarder. The granules accelerated the degradation of the brushite cement matrix as well as improved the bone tissue in-growth by permitting an easy access to the interior of the CPC through the micro-channels. The addition of micro-channeled granule in the CPC introduced porosity without sacrificing much of its compressive strength. In vivo investigation by creating a critical size defect in the femur head of a rabbit model for 1 and 2 months showed excellent bone in-growth through the micro-channels. The granules enhanced the implant degradation behavior and bone regeneration in the implanted area was significantly improved after two months of implantation. PMID:26333790

  6. Effects of the glucagon-like peptide-1 (GLP-1) analogues exenatide, exenatide extended-release, and of the dipeptidylpeptidase-4 (DPP-4) inhibitor sitagliptin on glucose metabolism in healthy cats.

    PubMed

    Padrutt, I; Lutz, T A; Reusch, C E; Zini, E

    2015-04-01

    Incretin analogues and inhibitors of the breakdown of endogenous incretins are antidiabetic drugs that increase β-cell proliferation and glucose-stimulated insulin secretion in rodents and humans. Objectives were to test whether exenatide, exenatide extended-release, and sitagliptin can be safely used in cats, to identify the most effective drug, and to test the effects of prolonged exenatide extended-release administration. Three cats each were given exenatide (0.2-2 µg/kg, q12h, subcutaneously, 5 days), exenatide extended-release (40-400 µg/kg, subcutaneously, once), and sitagliptin (1-10 mg/kg, q24h, orally, 5 days). Before and after treatment, glucose, insulin and glucagon areas under the curve (AUC) were assessed by meal response tests (MRT). Exenatide increased insulin AUC by 224%, 258%, 331% and 93%, exenatide extended-release by 127%, 169%, 178% and 95%, and sitagliptin by 32%, 69%, 62%, and 43%, respectively. The tested drugs are safe to use in cats and enhance insulin secretion. Incretin-based therapy may be beneficial in cats with diabetes mellitus. PMID:25648286

  7. Ab initio studies on the photophysics of uric acid and its monohydrates: role of the water molecule.

    PubMed

    Yamazaki, Shohei; Urashima, Shu-hei; Saigusa, Hiroyuki; Taketsugu, Tetsuya

    2014-02-13

    The photophysical behavior of three lowest-energy tautomers of uric acid and seven most stable isomers of uric acid monohydrate is comprehensively studied by ab initio calculations. Ground-state energies are calculated with the CCSD(T) method, while excitation and ionization energies as well as excited-state potential energy profiles of photoinduced processes are calculated with the CC2 method. For the (1)??* state, it is found that the excitation energy of the monohydrate cluster is significantly lower than that of isolated uric acid when the water molecule is hydrogen-bonded at a specific carbonyl group. The calculated excited-state potential energy profiles suggest that some monohydrate isomers can undergo a migration of the water molecule from one site to another site in the (1)??* state with a small energy barrier. It is also found for both uric acid and its monohydrate that nonradiative decay via the NH bond dissociation in the (1)??* state is likely to occur at higher excitation energies. On the basis of the computational results, possible mechanisms for the absence of specific isomers of uric acid monohydrate from the resonant two-photon ionization spectrum are discussed. PMID:24446809

  8. Zinc phosphate conversion coatings

    DOEpatents

    Sugama, Toshifumi

    1997-01-01

    Zinc phosphate conversion coatings for producing metals which exhibit enhanced corrosion prevention characteristics are prepared by the addition of a transition-metal-compound promoter comprising a manganese, iron, cobalt, nickel, or copper compound and an electrolyte such as polyacrylic acid, polymethacrylic acid, polyitaconic acid and poly-L-glutamic acid to a phosphating solution. These coatings are further improved by the incorporation of Fe ions. Thermal treatment of zinc phosphate coatings to generate .alpha.-phase anhydrous zinc phosphate improves the corrosion prevention qualities of the resulting coated metal.

  9. Zinc phosphate conversion coatings

    DOEpatents

    Sugama, T.

    1997-02-18

    Zinc phosphate conversion coatings for producing metals which exhibit enhanced corrosion prevention characteristics are prepared by the addition of a transition-metal-compound promoter comprising a manganese, iron, cobalt, nickel, or copper compound and an electrolyte such as polyacrylic acid, polymethacrylic acid, polyitaconic acid and poly-L-glutamic acid to a phosphating solution. These coatings are further improved by the incorporation of Fe ions. Thermal treatment of zinc phosphate coatings to generate {alpha}-phase anhydrous zinc phosphate improves the corrosion prevention qualities of the resulting coated metal. 33 figs.

  10. Modulation of calcium oxalate monohydrate crystallization kinetics in vitro.

    PubMed

    Kok, D J; Papapoulos, S E; Blomen, L J; Bijvoet, O L

    1988-09-01

    The effects of several low and high molecular weight (mol wt) compounds on the kinetics of calcium oxalate crystallization were examined using a seeded crystal growth method in which the solubility, the growth and the agglomeration of calcium oxalate crystals were measured as three separate and system-independent parameters. Citrate, magnesium, phosphate, pyrophosphate, chondroitinsulphate, pentosanpolysulphate and heparin were tested in a wide range of concentrations. The solubility of calcium oxalate crystals was increased only by citrate and magnesium. The crystal growth was inhibited by all compounds tested, but those with the high mol wt had the greatest effect at low concentrations. In contrast, inhibition of crystal agglomeration was achieved only by the low mol wt compounds; citrate was found to be the most potent inhibitor at concentrations likely to be present in normal urine. The high mol wt substances, despite their potent crystal growth inhibitory activity, had no effect on agglomeration. The results show that growth and agglomeration of calcium oxalate crystals are separate processes which are differently modulated by various compounds. They further provide a possible explanation for the pathogenetic role of citrate in hypocitraturic renal stone disease. PMID:2459439

  11. CADMIUM PHOSPHATE GLASS

    DOEpatents

    Carpenter, H.W.; Johnson, P.D.

    1963-04-01

    A method of preparing a cadmium phosphate glass that comprises providing a mixture of solid inorganic compounds of cadmuim and phosphate having vaporizable components and heating the resulting composition to a temperature of at least 850 un. Concent 85% C is presented. (AEC)

  12. Effect of mechanical grinding of MCPM and CaO mixtures on their composition and on the mechanical properties of the resulting self-setting hydraulic calcium phosphate cements.

    PubMed

    Serraj, S; Boudeville, P; Terol, A

    2001-01-01

    Calcium bis-dihydrogenophosphate monohydrate (or monocalcium phosphate monohydrate, MCPM) is often used as the acid calcium phosphate in hydraulic calcium phosphate cement formulations. But commercial MCPM is not pure; it contains a small amount of orthophosphoric acid and moisture. Consequently, MCPM is difficult to mill and the powder is sticky and presents aggregates. Because granularity influences the mechanical properties of the hardened cements, a possible way to get around this difficulty that has been proposed is to premix it with other materials before grinding. We therefore ground commercial MCPM with CaO. A rapid decrease in the amount of MCPM was observed during mechanical grinding by a solid-solid reaction with calcium oxide. The final products were anhydrous or dihydrate dicalcium phosphate and/or hydroxyapatite or calcium-deficient hydroxyapatite depending on the initial calcium-to-phosphate (Ca/P) ratio. The mechanical properties (compressive strength and setting time) of cements made from MCPM and CaO were affected whatever the Ca/P ratio as a consequence of the change in composition of the starting materials. Storage at different temperatures of MCPM and CaO mixtures manually ground in a mortar for only 2 min and without mechanical grinding did not affect their composition, but a decrease was observed in the compressive strength of cements made from these mixtures. PMID:15348376

  13. NTP Toxicology and Carcinogenesis Studies of Manganese (II) Sulfate Monohydrate (CAS No. 10034-96-5) in F344/N Rats and B6C3F1 Mice (Feed Studies).

    PubMed

    1993-12-01

    Manganese is the 12th most abundant element in the earth's crust. The base metal does not occur naturally, but is a component of more than 100 minerals, including sulfides, oxides, carbonates, silicates, phosphates, and borates. In addition to occurring in foods and drinking water, manganese occurs in the atmosphere from dust, volcanic activity, forest fires, and industrial emissions. Manganese (II) sulfate monohydrate was chosen for study because of its stability, solubility, and availability. Toxicology and carcinogenesis studies were conducted by administering manganese (II) sulfate monohydrate (97% pure) in feed to groups of male and female F344/N rats and B6C3F1 mice for 14 days, 13 weeks, and 2 years. Genetic toxicology studies were conducted in Salmonella typhimurium, germ cells of Drosophila melanogaster, and cultured Chinese hamster ovary cells. 14-DAY STUDY IN RATS: Groups of five male and five female rats received diets containing 0, 3,130, 6,250, 12,500, 25,000, or 50,000 ppm manganese (II) sulfate monohydrate. All rats survived to the end of the study. Male rats exposed to 50,000 ppm had a mean body weight gain 57% lower and a final mean body weight 13% lower than those of the controls. The mean body weight gain of 50,000 ppm females was 20% lower and the final mean body weight was 7% lower than those of the controls. During the second week, 50,000 ppm males and females exhibited diarrhea. 14-DAY STUDY IN MICE: Groups of five male and five female mice received diets containing 0, 3,130, 6,250, 12,500, 25,000, or 50,000 ppm manganese (II) sulfate monohydrate. One female mouse in the 25,000 ppm group died on day 1 of unknown causes; all other mice survived to the end of the study. Differences in body weights between exposed and control mice could not be attributed to chemical administration. 13-WEEK STUDY IN RATS: Groups of 10 male and 10 female rats received diets containing 0, 1,600, 3,130, 6,250, 12,500, or 25,000 ppm manganese (II) sulfate monohydrate. Mean daily ingestion of manganese (II) sulfate monohydrate ranged from 110 to 1,700 mg/kg body weight in males and 115 to 2,000 mg/kg in females. All rats survived to the end of the study. Mean body weight gains were marginally lower than that of controls in males exposed to 3,130 ppm or more; mean body weight gains were significantly lower than that of the controls in females exposed to 6,250,12,500, or 25,000 ppm. At the end of the study, absolute and relative liver weights of all exposed male rats and of 25,000 ppm female rats were significantly lower than those of controls. The total leukocyte count in males was similar between exposed and control rats; however, neutrophil counts of all exposed groups were greater than those of the controls, whereas lymphocyte counts of the 6,250, 12,500, and 25,000 ppm groups were significantly lower than those of the controls. Total leukocyte counts in 6,250,12,500, and 25,000 ppm females were significantly decreased because of a decrease in lymphocytes. Male rats also demonstrated marginal but significant increases in percent hematocrit and erythrocyte count in the 6,250,12,500, and 25,000 ppm groups. No clinical or histopathologic findings in rats were chemical related. 13-WEEK STUDY IN MICE: Groups of 10 male and 10 female mice received diets containing 0, 3,130, 6,250, 12,500, 25,000, or 50,000 ppm manganese (II) sulfate monohydrate. Mean daily ingestion of manganese (II) sulfate monohydrate ranged from 330 to 7,400 mg/kg body weight in males and 390 to 6,900 mg/kg body weight in females. No deaths were chemical related. The mean body weight gains of exposed male mice and of 50,000 ppm female mice were significantly lower than those of controls. The absolute and relative liver weights of 50,000 ppm males were significantly lower than those of controls. The percent hematocrit and hemoglobin concentration of males and females exposed to 50,000 ppm were lower than those of the controls, and the mean erythrocyte volumes were significantly lower than those of the controls. The total leukocyte counts of males in the 25,eukocyte counts of males in the 25,000 and 50,000 ppm groups were significantly lower than that of the controls. No clinical findings were attributed to manganese (II) sulfate monohydrate ingestion. Epithelial hyperplasia and hyperkeratosis of the forestomach occurred in three 50,000 ppm males. 2-YEAR STUDY IN RATS: Groups of 70 male and 70 female rats were fed diets containing 0, 1,500, 5,000, or 15,000 ppm manganese (II) sulfate monohydrate. Based on average daily feed consumption, these doses resulted in the daily ingestion of 60, 200, or 615 mg/kg body weight (males) or 70, 230, or 715 mg/kg (females). Eight to 10 rats from each group were evaluated at 9 and 15 months. Survival, Body Weights, Feed Consumption, and Clinical Findings: Survival of 15,000 ppm male rats in the 2-year study was significantly lower than that of the control group. The deaths of males in the control and exposure groups were attributed to a variety of spontaneous neoplastic and nonneoplastic lesions; however, the greater number of deaths in the 15,000 ppm group resulted from increased incidences of advanced renal disease related to ingestion of manganese (II) sulfate monohydrate. The decreased survival of the 15,000 ppm males did not occur until approximately week 93 of the study; before week 93, survival was similar in all groups. Survival of exposed females was similar to that of the controls. The mean body weight of 15,000 ppm male rats was within 5% of the control group until week 89, by week 104, the mean body weight of 15,000 ppm males was 10% lower than that of the control group. The mean body weights of 1,500 and 5,000 ppm male rats and all exposed female groups were similar to those of the controls throughout the study. Feed consumption by all exposure groups was similar to that by the control groups. No clinical findings were attributed to manganese (II) sulfate monohydrate ingestion. Hematology, Clinical Chemistry, and Tissue Metal Concentration Analyses No differences in hematology and clinical chemistry parameters attributable to the ingestion of manganese (II) sulfate monohydrate occurred between exposed and control groups. At both the 9- and 15-month interim evaluations, tissue concentrations of manganese were significantly elevated in the livers of 5,000 and 15,000 ppm male and female rats, with an accompanying depression of hepatic iron. Pathology Findings: The ingestion of diets containing 15,000 ppm manganese (II) sulfate monohydrate was associated with a marginal increase in the average severity of nephropathy in male rats (0 ppm, 2.9; 1,500 ppm, 3.0; 5,000 ppm, 3.0; 15,000 ppm, 3.2). The increased severity of nephropathy in the 15,000 ppm male rats was accompanied by significantly increased incidences of mineralization of the blood vessels (4/52, 10/51, 6/51,17/52) and glandular stomach (8/52,13/51, 9/51, 23/52), parathyroid gland hyperplasia (14/51, 14/46, 12/49, 23/50), and fibrous osteodystrophy of the femur (12/52,14/51,12/51, 24/52). These lesions are manifestations of renal failure, uremia, and secondary hyperparathyroidism. The increased incidence of advanced renal disease caused reduced survival of the high-dose male rats. No increase in the incidence of neoplasms in male or female rats was attributed to the ingestion of diets containing manganese (II) sulfate monohydrate. 2-YEAR STUDY IN MICE: Groups of 70 male and 70 female mice received diets containing 0, 1,500, 5,000, or 15,000 ppm manganese (II) sulfate monohydrate. These levels resulted in an average daily ingestion of 160, 540, or 1,800 mg/kg body weight (males) or 200, 700, or 2,250 mg/kg (females). Nine or 10 mice from each group were evaluated at the 9-month and 15-month interim evaluations. Survival, Body Weights, Feed Consumption, and Clinical Findings: Survival rates of exposed male and female mice in the 2-year study were similar to those of the control groups. The mean body weights of exposed male mice were similar to that of the control group. Compared to controls, female mice had exposure related lower mean body weights after week 37, and the final mean body weights for the 1,500, 5,000, and 15,000 ppm groups were 6%, 9%, and 13% lower than that of the control group. Feed consumption by all exposure groups was similar to that by the control groups. No clinical findings were attributed to the administration of manganese (II) sulfate monohydrate. Hematology, Clinical Chemistry, and Tissue Metal Concentration Analyses No chemical-related differences between exposed and control groups occurred in hematology or clinical chemistry parameters. At the 9- and 15-month interim evaluations, tissue concentrations of manganese were significantly elevated in the livers of the 5,000 and 15,000 ppm groups. Hepatic iron levels were significantly lower in exposed females at the 9-month interim evaluation and in 5,000 and 15,000 males and all exposed females at the 15-month interim evaluation. Pathology Findings: Incidences of thyroid follicular dilatation and hyperplasia were significantly greater in 15,000 ppm male and female mice than in controls. Follicular cell adenomas occurred in one 15,000 ppm male at the 15-month interim evaluation and in three 15,000 ppm males at the end of the study but not in the lower exposure groups or the control group. Follicular cell adenomas also occurred in two control, one 1,500, and five 15,000 ppm female mice at the end of the study. It is uncertain if the slightly increased incidence of follicular cell adenoma is related to the ingestion of manganese (II) sulfate monohydrate. The incidences of focal hyperplasia of the forestomach epithelium were significantly greater in the 15,000 ppm male and exposed female groups. The hyperplasia was associated with ulcers and inflammation in some mice, particularly males. GENETIC TOXICOLOGY: Manganese (II) sulfate monohydrate was not mutagenic in Salmonella typhimurium strains TA97, TA98, TA100, TA1535, or TA1537, with or without exogenous metabolic activation (S9), and did not induce sex-linked recessive lethal mutations in germ cells of male Drosophila melanogaster. Tests for induction of sister chromatid exchanges and chromosomal aberrations in cultured Chinese hamster ovary cells treated without S9 were positive; with S9, only the sister chromatid exchange test with manganese (11) sulfate monohydrate was positive. CONCLUSIONS: Under the conditions of these 2-year feed studies, there was no evidence of carcinogenic activity of manganese (II) sulfate monohydrate in male or female F344/N rats receiving 1,500, 5,000, or 15,000 ppm. There was equivocal evidence of carcinogenic activity of manganese (II) sulfate monohydrate in male and female B6C3F1 mice, based on the marginally increased incidences of thyroid gland follicular cell adenoma and the significantly increased incidences of follicular cell hyperplasia. The ingestion of diets containing manganese (II) sulfate monohydrate was associated with an increased severity of nephropathy in male rats, focal squamous hyperplasia of the forestomach in male and female mice, and ulcers and inflammation of the forestomach in male mice. These studies were not designed to assess any neurotoxicity that might have been expected with chronic exposure to sufficiently high doses of manganese. Synonyms: Manganese sulfate; manganous sulfate; sulfuric acid. manganese2+ salt (1:1), monohydrate PMID:12616303

  14. PHOSPHATE MANAGEMENT: FY2010 RESULTS OF PHOSPHATE PRECIPITATION TESTS

    SciTech Connect

    Hay, M.; King, W.

    2011-04-04

    The Phosphate Management program seeks to develop treatment options for caustic phosphate solutions resulting from the caustic leaching of the bismuth phosphate sludge. The SRNL subtask investigated the precipitation of phosphate salts from caustic solutions through addition of fluoride and by crystallization. The scoping tests examined the: precipitation of phosphate by the addition of sodium fluoride to form the sodium fluorophosphate double salt, Na{sub 7}F(PO{sub 4}){sub 2} {center_dot} 19H{sub 2}O, crystallization of phosphate by reducing the temperature of saturated phosphate solutions, and combinations of precipitation and crystallization. A simplified leachate simulant was used in the study produced by dissolving sodium phosphate in 1 M to 3.5 M sodium hydroxide solutions. The results show that all three processes; precipitation with sodium fluoride, crystallization, and combined precipitation/crystallization can be effective for removing large amounts of phosphate from solution. The combined process of precipitation/crystallization showed >90% removal of phosphate at all hydroxide concentrations when cooling a non-saturated phosphate solution from 65 C to 25 C. Based on the measured solubility of sodium phosphate, pH adjustment/caustic addition will also remove large amounts of phosphate from solution (>80%). For all three processes, the phosphate concentration in the caustic solution must be managed to keep the phosphate from becoming too concentrated and thereby potentially forming a solid mass of sodium phosphate after an effective phosphate removal process.

  15. Crystal studies, vibrational spectra and non-linear optical properties of L-histidine chloride monohydrate.

    PubMed

    Ben Ahmed, A; Feki, H; Abid, Y; Boughzala, H; Minot, C

    2010-01-01

    This paper presents the results of our calculations on the geometric parameters, vibrational spectra and hyperpolarizability of a non-linear optical material L-histidine chloride monohydrate. Due to the lack of sufficiently precise information on geometric parameters available in literature, theoretical calculations were preceded by re-determination of the crystal X-ray structure. Single crystal of L-histidine chloride monohydrate has been growing by slow evaporation of an aqueous solution at room temperature. The compound crystallizes in the non-Centro-symmetric space group P2(1)2(1)2(1) of orthorhombic system. IR spectrum has been recorded in the range [400-4000 cm(-1)]. All the experimental vibrational bands have been discussed and assigned to normal mode or to combinations on the basis of our calculations. The optimized geometric bond lengths and bond angles obtained by using DFT//B3LYP/6-31G (d) method show a good agreement with the experimental data. The calculated vibrational spectra are in well agreement with the experimental one. To investigate microscopic second-order non-linear optical NLO behavior of the examined complex, the electric dipole mu, the polarizability alpha and the hyperpolarizability beta were computed using DFT//B3LYP/6-31G (d) method. The time-dependent density functional theory (TD-DFT) was employed to descript the molecular electron structure of the title compound using the B3LYP/6-31G (d) method. According to our calculations, L-histidine chloride monohydrate exhibits non-zero beta value revealing microscopic second-order NLO behavior. PMID:19926520

  16. Creatine monohydrate supplementation on lower-limb muscle power in Brazilian elite soccer players

    PubMed Central

    2014-01-01

    Background Studies involving chronic creatine supplementation in elite soccer players are scarce. Therefore, the aim of this study was to examine the effects of creatine monohydrate supplementation on lower-limb muscle power in Brazilian elite soccer players (n = 14 males) during pre-season training. Findings This was a randomized, double-blind, placebo-controlled parallel-group study. Brazilian professional elite soccer players participated in this study. During the pre-season (7 weeks), all the subjects underwent a standardized physical and specific soccer training. Prior to and after either creatine monohydrate or placebo supplementation, the lower-limb muscle power was measured by countermovement jump performance. The Jumping performance was compared between groups at baseline (p = 0.99). After the intervention, jumping performance was lower in the placebo group (percent change = - 0.7%; ES = - 0.3) than in the creatine group (percent change = + 2.4%; ES = + 0.1), but it did not reach statistical significance (p = 0.23 for time x group interaction). Fisher’s exact test revealed that the proportion of subjects that experienced a reduction in jumping performance was significantly greater in the placebo group than in the creatine group (5 and 1, respectively; p = 0.05) after the training. The magnitude-based inferences demonstrated that placebo resulted in a possible negative effect (50%) in jumping performance, whereas creatine supplementation led to a very likely trivial effect (96%) in jumping performance in the creatine group. Conclusions Creatine monohydrate supplementation prevented the decrement in lower-limb muscle power in elite soccer players during a pre-season progressive training. PMID:24991195

  17. Radiolysis of Sulfuric Acid, Sulfuric Acid Monohydrate, and Sulfuric Acid Tetrahydrate and Its Relevance to Europa

    NASA Technical Reports Server (NTRS)

    Loeffler, M. J.; Hudson, R. L.; Moore, M. H.; Carlson, R. W.

    2011-01-01

    We report laboratory studies on the 0.8 MeV proton irradiation of ices composed of sulfuric acid (H2SO4), sulfuric acid monohydrate (H2SO4 H2O), and sulfuric acid tetrahydrate (H2SO4 4H2O) between 10 and 180 K. Using infrared spectroscopy, we identify the main radiation products as H2O, SO2, (S2O3)x, H3O+, HSO4(exp -), and SO4(exp 2-). At high radiation doses, we find that H2SO4 molecules are destroyed completely and that H2SO4 H2O is formed on subsequent warming. This hydrate is significantly more stable to radiolytic destruction than pure H2SO4, falling to an equilibrium relative abundance of 50% of its original value on prolonged irradiation. Unlike either pure H2SO4 or H2SO4 H2O, the loss of H2SO4 4H2O exhibits a strong temperature dependence, as the tetrahydrate is essentially unchanged at the highest irradiation temperatures and completely destroyed at the lowest ones, which we speculate is due to a combination of radiolytic destruction and amorphization. Furthermore, at the lower temperatures it is clear that irradiation causes the tetrahydrate spectrum to transition to one that closely resembles the monohydrate spectrum. Extrapolating our results to Europa s surface, we speculate that the variations in SO2 concentrations observed in the chaotic terrains are a result of radiation processing of lower hydration states of sulfuric acid and that the monohydrate will remain stable on the surface over geological times, while the tetrahydrate will remain stable in the warmer regions but be destroyed in the colder regions, unless it can be reformed by other processes, such as thermal reactions induced by diurnal cycling.

  18. An Understanding of Renal Stone Development in a Mixed Oxalate–Phosphate System

    PubMed Central

    Guan, Xiangying; Wang, Lijun; Dosen, Anja; Tang, Ruikang; Giese, Rossman F.; Giocondi, Jennifer L.; Orme, Christine A.; Hoyer, John R.; Nancollas, George H.

    2009-01-01

    The in vivo formation of calcium oxalate concretions having calcium phosphate nidi is simulated in an in vitro (37 °C, pH 6.0) dual constant composition (DCC) system undersaturated (σDCPD = −0.330) with respect to brushite (DCPD, CaHPO4 · 2H2O) and slightly supersaturated (σCOM = 0.328) with respect to calcium oxalate monohydrate (COM, CaC2O4 · H2O). The brushite dissolution provides calcium ions that raise the COM supersaturation, which is heterogeneously nucleated either on or near the surface of the dissolving calcium phosphate crystals. The COM crystallites may then aggregate, simulating kidney stone formation. Interestingly, two intermediate phases, anhydrous dicalcium phosphate (monetite, CaHPO4) and calcium oxalate trihydrate (COT), are also detected by X-ray diffraction during this brushite–COM transformation. In support of clinical observations, the results of these studies demonstrate the participation of calcium phosphate phases in COM crystallization providing a possible physical chemical mechanism for kidney stone formation. PMID:18557638

  19. Loading and release of doxycycline hyclate from strontium-substituted calcium phosphate cement.

    PubMed

    Alkhraisat, M Hamdan; Rueda, C; Cabrejos-Azama, J; Lucas-Aparicio, J; Mariño, F Tamimi; Torres García-Denche, J; Jerez, L Blanco; Gbureck, U; Cabarcos, E Lopez

    2010-04-01

    Novel Sr-substituted calcium phosphate cement (CPC) loaded with doxycycline hyclate (DOXY-h) was employed to elucidate the effect of strontium substitution on antibiotic delivery. The cement was prepared using as reactants Sr-substituted beta-tricalcium phosphate (Sr-beta-TCP) and acidic monocalcium phosphate monohydrate. Two different methods were used to load DOXY-h: (i) the adsorption on CPC by incubating the set cement in drug-containing solutions; and (ii) the use of antibiotic solution as the cement liquid phase. The results revealed that the Sr-substituted cement efficiently adsorbs the antibiotic, which is attributed to an enhanced accessibility to the drug-binding sites within this CPC. DOXY-h desorption is influenced by the initial adsorbed amount and the cement matrix type. Furthermore, the fraction of drug released from CPCs set with DOXY-h solution was higher, and the release rate was faster for the CPC prepared with 26.7% Sr-beta-TCP. The analysis of releasing profiles points to Fickian diffusion as the mechanism responsible for antibiotic delivery. We can conclude that Sr substitution in secondary calcium phosphate cements improves their efficiency for DOXY-h adsorption and release. The antibiotic loading method provides a way to switch from rapid and complete to slower and prolonged drug release. PMID:19879982

  20. In vitro Evaluation of Terminalia arjuna on Calcium Phosphate and Calcium Oxalate Crystallization.

    PubMed

    Chaudhary, A; Singla, S K; Tandon, C

    2010-05-01

    Urinary stones are one of the oldest and the most common afflictions in humans. This disease has tormented humans since the earliest records of civilization. Ten percent of men and 3 % of women have a stone during their adult lives. Calcium containing stones are the most common comprising about 75 % of all urinary calculi, which may be in the form of pure calcium oxalate (50 %) or calcium phosphate (5 %) or a mixture of both (45 %). A number of plants have been mentioned in the Indian ayurvedic system, which plays a vital role in the inhibition of kidney stones. In the present study, the inhibitory potency of crude extracts or fractions of successive solvent extractions of Terminalia arjuna bark was evaluated on various stages of formation of calcium phosphate and on the growth of calcium oxalate monohydrate crystals in vitro. Results obtained indicated that Terminalia arjuna bark has the potential to inhibit the formation of both calcium phosphate and calcium oxalate crystals in vitro. Butanol fraction of Terminalia arjuna extract was the most effective in inhibiting formation of calcium phosphate and calcium oxalate crystals in vitro. PMID:21188043

  1. In vitro Evaluation of Terminalia arjuna on Calcium Phosphate and Calcium Oxalate Crystallization

    PubMed Central

    Chaudhary, A.; Singla, S. K.; Tandon, C.

    2010-01-01

    Urinary stones are one of the oldest and the most common afflictions in humans. This disease has tormented humans since the earliest records of civilization. Ten percent of men and 3 % of women have a stone during their adult lives. Calcium containing stones are the most common comprising about 75 % of all urinary calculi, which may be in the form of pure calcium oxalate (50 %) or calcium phosphate (5 %) or a mixture of both (45 %). A number of plants have been mentioned in the Indian ayurvedic system, which plays a vital role in the inhibition of kidney stones. In the present study, the inhibitory potency of crude extracts or fractions of successive solvent extractions of Terminalia arjuna bark was evaluated on various stages of formation of calcium phosphate and on the growth of calcium oxalate monohydrate crystals in vitro. Results obtained indicated that Terminalia arjuna bark has the potential to inhibit the formation of both calcium phosphate and calcium oxalate crystals in vitro. Butanol fraction of Terminalia arjuna extract was the most effective in inhibiting formation of calcium phosphate and calcium oxalate crystals in vitro. PMID:21188043

  2. Effect of Creatine Monohydrate on Clinical Progression in Patients With Parkinson Disease

    PubMed Central

    2015-01-01

    IMPORTANCE There are no treatments available to slow or prevent the progression of Parkinson disease, despite its global prevalence and significant health care burden. The National Institute of Neurological Disorders and Stroke Exploratory Trials in Parkinson Disease program was established to promote discovery of potential therapies. OBJECTIVE To determine whether creatine monohydrate was more effective than placebo in slowing long-term clinical decline in participants with Parkinson disease. DESIGN, SETTING, AND PATIENTS The Long-term Study 1, a multicenter, double-blind, parallel-group, placebo-controlled, 1:1 randomized efficacy trial. Participants were recruited from 45 investigative sites in the United States and Canada and included 1741 men and women with early (within 5 years of diagnosis) and treated (receiving dopaminergic therapy) Parkinson disease. Participants were enrolled from March 2007 to May 2010 and followed up until September 2013. INTERVENTIONS Participants were randomized to placebo or creatine (10 g/d) monohydrate for a minimum of 5 years (maximum follow-up, 8 years). MAIN OUTCOMES AND MEASURES The primary outcome measure was a difference in clinical decline from baseline to 5-year follow-up, compared between the 2 treatment groups using a global statistical test. Clinical status was defined by 5 outcome measures: Modified Rankin Scale, Symbol Digit Modalities Test, PDQ-39 Summary Index, Schwab and England Activities of Daily Living scale, and ambulatory capacity. All outcomes were coded such that higher scores indicated worse outcomes and were analyzed by a global statistical test. Higher summed ranks (range, 5–4775) indicate worse outcomes. RESULTS The trial was terminated early for futility based on results of a planned interim analysis of participants enrolled at least 5 years prior to the date of the analysis (n = 955). The median follow-up time was 4 years. Of the 955 participants, the mean of the summed ranks for placebo was 2360 (95% CI, 2249–2470) and for creatine was 2414 (95% CI, 2304–2524). The global statistical test yielded t1865.8 = −0.75 (2-sided P = .45). There were no detectable differences (P < .01 to partially adjust for multiple comparisons) in adverse and serious adverse events by body system. CONCLUSIONS AND RELEVANCE Among patients with early and treated Parkinson disease, treatment with creatine monohydrate for at least 5 years, compared with placebo did not improve clinical outcomes. These findings do not support the use of creatine monohydrate in patients with Parkinson disease. TRIAL REGISTRATION clinicaltrials.gov Identifier: NCT00449865 PMID:25668262

  3. The nucleation and growth of calcium oxalate monohydrate on self- assembled monolayers (SAMs)

    SciTech Connect

    Campbell, A.A.; Tarasevich, B.J.; Graff, G.L.; Fryxell, G.E.; Rieke, P.C.

    1992-05-01

    A physical chemical approach was used to study calcium oxalate monohydrate (COM) nucleation and growth on various organic interfaces. Self-assembling monolayers (SAMs), containing derivatized organic functional groups, were designed to mimic various amino acid residues present in both urine and stone matrix macromolecules. Derivatized surfaces include SAMs with terminal methyl, bromo, imidazole, and thiazolidine-carboxylic acid functional groups. Pronounced differences in COM deposition were observed for the various interfaces with the imidazole and thiazolidine surfaces having the greatest effect and the methyl and bromo groups having little or no nucleating potential.

  4. In vivo comet assay of acrylonitrile, 9-aminoacridine hydrochloride monohydrate and ethanol in rats.

    PubMed

    Nakagawa, Yuzuki; Toyoizumi, Tomoyasu; Sui, Hajime; Ohta, Ryo; Kumagai, Fumiaki; Usumi, Kenji; Saito, Yoshiaki; Yamakage, Kohji

    2015-07-01

    As part of the Japanese Center for the Validation of Alternative Methods (JaCVAM)-initiative international validation study of the in vivo rat alkaline comet assay, we examined the ability of acrylonitrile, 9-aminoacridine hydrochloride monohydrate (9-AA), and ethanol to induce DNA damage in the liver and glandular stomach of male rats. Acrylonitrile is a genotoxic carcinogen, 9-AA is a genotoxic non-carcinogen, and ethanol is a non-genotoxic carcinogen. Positive results were obtained in the liver cells of male rats treated with known genotoxic compounds, acrylonitrile and 9-AA. PMID:26212299

  5. Biosynthesis of Dolichyl Phosphate

    PubMed Central

    Hopp, H. Esteban; Daleo, Gustavo R.; Romero, Pedro A.; Lezica, Rafael Pont

    1978-01-01

    This is the first report not only on the presence of polyprenyl phosphates and their site of synthesis in algae, but also on the formation of their sugar derivatives in this system. A glucose acceptor lipid was isolated from the nonphotosynthetic alga Prototheca zopfii. The lipid was acidic and resistant to mild acid and alkaline treatments. The glucosylated lipid was labile to mild acid hydrolysis and resistant to phenol treatment and catalytic hydrogenation, as dolichyl phosphate glucose is. These results are consistent with the properties of an α-saturated polyprenyl phosphate. The polyprenylic nature of the lipid was confirmed by biosynthesis from radioactive mevalonate. The [14C]lipid had the same chromatographic properties as dolichyl phosphate in DEAE-cellulose and Sephadex LH-20. Strong alkaline treatment and enzymic hydrolysis liberated free alcohols with chain lengths ranging from C90 to C105, C95 and C100 being the most abundant molecular forms. The glucose acceptor activity of the biosynthesized polyprenyl phosphate was confirmed. The ability of different subcellular fractions to synthesize dolichyl phosphate was studied. Mitochondria and the Golgi apparatus were the sites of dolichyl phosphate synthesis from mevalonate. PMID:16660269

  6. Extremely high damage threshold of a new nonlinear crystal L-arginine phosphate and its deuterium compound

    SciTech Connect

    Yokotani, A.; Sasaki, T.; Yoshida, K.; Nakai, S. )

    1989-12-25

    L-arginine phosphate monohydrate (LAP) and deuterated LAP (DLAP) are new organic nonlinear optical materials useful for higher harmonics of radiation from high-power lasers. We measured the bulk laser damage threshold of these crystals using light from a 1.05 {mu}m laser with 1 and 25 ns pulse widths and 0.53 {mu}m laser light with 0.6 and 20 ns pulse widths. In every case, these crystals show much higher thresholds than potassium dihydrogen phosphate (KDP) and fused silica. These crystals are very interesting not only as a frequency converter but also as other optical components of high-power lasers, because of their extremely high damage threshold.

  7. Metal-phosphate binders

    DOEpatents

    Howe, Beth Ann [Lewistown, IL; Chaps-Cabrera, Jesus Guadalupe [Coahuila, MX

    2009-05-12

    A metal-phosphate binder is provided. The binder may include an aqueous phosphoric acid solution, a metal-cation donor including a metal other than aluminum, an aluminum-cation donor, and a non-carbohydrate electron donor.

  8. Phosphate control in dialysis

    PubMed Central

    Cupisti, Adamasco; Gallieni, Maurizio; Rizzo, Maria Antonietta; Caria, Stefania; Meola, Mario; Bolasco, Piergiorgio

    2013-01-01

    Prevention and correction of hyperphosphatemia is a major goal of chronic kidney disease–mineral and bone disorder (CKD–MBD) management, achievable through avoidance of a positive phosphate balance. To this aim, optimal dialysis removal, careful use of phosphate binders, and dietary phosphate control are needed to optimize the control of phosphate balance in well-nourished patients on a standard three-times-a-week hemodialysis schedule. Using a mixed diffusive–convective hemodialysis tecniques, and increasing the number and/or the duration of dialysis tecniques are all measures able to enhance phosphorus (P) mass removal through dialysis. However, dialytic removal does not equal the high P intake linked to the high dietary protein requirement of dialysis patients; hence, the use of intestinal P binders is mandatory to reduce P net intestinal absorption. Unfortunately, even a large dose of P binders is able to bind approximately 200–300 mg of P on a daily basis, so it is evident that their efficacy is limited in the case of an uncontrolled dietary P load. Hence, limitation of dietary P intake is needed to reach the goal of neutral phosphate balance in dialysis, coupled to an adequate protein intake. To this aim, patients should be informed and educated to avoid foods that are naturally rich in phosphate and also processed food with P-containing preservatives. In addition, patients should preferentially choose food with a low P-to-protein ratio. For example, patients could choose egg white or protein from a vegetable source. Finally, boiling should be the preferred cooking procedure, because it induces food demineralization, including phosphate loss. The integrated approach outlined in this article should be actively adapted as a therapeutic alliance by clinicians, dieticians, and patients for an effective control of phosphate balance in dialysis patients. PMID:24133374

  9. Competing Insertion and External Binding Motifs in Hydrated Neurotransmitters: Infrared Spectra of Protonated Phenylethylamine Monohydrate.

    PubMed

    Bouchet, Aude; Schütz, Markus; Dopfer, Otto

    2016-01-01

    Hydration has a drastic impact on the structure and function of flexible biomolecules, such as aromatic ethylamino neurotransmitters. The structure of monohydrated protonated phenylethylamine (H(+) PEA-H2 O) is investigated by infrared photodissociation (IRPD) spectroscopy of cold cluster ions by using rare-gas (Rg=Ne and Ar) tagging and dispersion-corrected density functional theory calculations at the B3LYP-D3/aug-cc-pVTZ level. Monohydration of this prototypical neurotransmitter gives an insight into the first step of the formation of its solvation shell, especially regarding the competition between intra- and intermolecular interactions. The spectra of Rg-tagged H(+) PEA-H2 O reveal the presence of a stable insertion structure in which the water molecule is located between the positively charged ammonium group and the phenyl ring of H(+) PEA, acting both as a hydrogen bond acceptor (NH(+) ⋅⋅⋅O) and donor (OH⋅⋅⋅π). Two other nearly equivalent isomers, in which water is externally H bonded to one of the free NH groups, are also identified. The balance between insertion and external hydration strongly depends on temperature. PMID:26584245

  10. A complementary experimental and computational study of loxapine succinate and its monohydrate.

    PubMed

    Bhardwaj, Rajni M; Johnston, Blair F; Oswald, Iain D H; Florence, Alastair J

    2013-11-01

    The crystal structures of loxapine succinate [systematic name: 4-(2-chlorodibenzo[b,f][1,4]oxazepin-11-yl)-1-methylpiperazin-1-ium 3-carboxypropanoate], C18H19ClN3O(+)·C4H5O4(-), and loxapine succinate monohydrate {systematic name: bis[4-(2-chlorodibenzo[b,f][1,4]oxazepin-11-yl)-1-methylpiperazin-1-ium] succinate succinic acid dihydrate}, 2C18H19ClN3O(+)·C4H4O4(2-)·C4H6O4·2H2O, have been determined using X-ray powder diffraction and single-crystal X-ray diffraction, respectively. Fixed cell geometry optimization calculations using density functional theory confirmed that the global optimum powder diffraction derived structure also matches an energy minimum structure. The energy calculations proved to be an effective tool in locating the positions of the H atoms reliably and verifying the salt configuration of the structure determined from powder data. Crystal packing analysis of these structures revealed that the loxapine succinate structure is based on chains of protonated loxapine molecules while the monohydrate contains dispersion stabilized centrosymmetric dimers. Incorporation of water molecules within the crystal lattice significantly alters the molecular packing and protonation state of the succinic acid. PMID:24192171

  11. Uranium from phosphate ores

    SciTech Connect

    Hurst, F.J.

    1983-01-01

    Phosphate rock, the major raw material for phosphate fertilizers, contains uranium that can be recovered when the rock is processed. This makes it possible to produce uranium in a country that has no uranium ore deposits. The author briefly describes the way that phosphate fertilizers are made, how uranium is recovered in the phosphate industry, and how to detect uranium recovery operations in a phosphate plant. Uranium recovery from the wet-process phosphoric acid involves three unit operations: (1) pretreatment to prepare the acid; (2) solvent extraction to concentrate the uranium; (3) post treatment to insure that the acid returning to the acid plant will not be harmful downstream. There are 3 extractants that are capable of extracting uranium from phosphoric acid. The pyro or OPPA process uses a pyrophosphoric acid that is prepared on site by reacting an organic alcohol (usually capryl alcohol) with phosphorous pentoxide. The DEPA-TOPO process uses a mixture of di(2-ethylhexyl)phosphoric acid (DEPA) and trioctyl phosphine oxide (TOPO). The components can be bought separately or as a mixture. The OPAP process uses octylphenyl acid phosphate, a commercially available mixture of mono- and dioctylphenyl phosphoric acids. All three extractants are dissolved in kerosene-type diluents for process use.

  12. Synthesis of 4,2-iodonio-3-phenyl-1,2-benzisoxazole tetrafluoroboride and the crystal structure of its monohydrate

    SciTech Connect

    Batsanov, A.S.; Petrov, V.N.; Struchkov, Yu.T.; Egorova, L.D.; Lisichkina, I.N.; Tolstaya, T.P.

    1986-04-20

    4,2'-Iodonio-3-phenyl-1,2-benzisoxazole tetrafluoroboride monohydrate (IV) was synthesized and an x-ray diffraction structural study showed that the cation (IV) is a tetracyclic system and the crystal structure is insular with I...F and I...OH/sub 2/ ionic and ion-dipole interactions.

  13. Density Functional Study of the Infrared Spectrum of Glucose and Glucose Monohydrates in the OH Stretch Region

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Density functional theory (DFT) has been used to calculate the structures and infrared spectra of glucose and glucose monohydrates. Both the alpha and beta anomers were studied, with all possible combinations of hydroxymethyl rotamer (gg, gt, or tg) and hydroxyl orientation (clockwise or counter-cl...

  14. Reactive calcium-phosphate-containing poly(ester-co-ether) methacrylate bone adhesives: chemical, mechanical and biological considerations.

    PubMed

    Zhao, Xin; Olsen, Irwin; Li, Haoying; Gellynck, Kris; Buxton, Paul G; Knowles, Jonathan C; Salih, Vehid; Young, Anne M

    2010-03-01

    A poly(propylene glycol-co-lactide) dimethacrylate adhesive with monocalcium phosphate monohydrate (MCPM)/beta-tricalcium phosphate (beta-TCP) fillers in various levels has been investigated. Water sorption by the photo-polymerized materials catalyzed varying filler conversion to dicalcium phosphate (DCP). Polymer modulus was found to be enhanced upon raising total calcium phosphate content. With greater DCP levels, faster release of phosphate and calcium ions and improved buffering of polymer degradation products were observed. This could reduce the likelihood of pH-catalyzed bulk degradation and localized acid production and thereby may prevent adverse biological responses. Bone-like MG-63 cells were found to attach, spread and have normal morphology on both the polymer and composite surfaces. Moreover, composites implanted into chick embryo femurs became closely apposed to the host tissue and did not appear to induce adverse immunological reaction. The above results suggest that the new composite materials hold promise as clinical effective bone adhesives. PMID:19800424

  15. Phosphate metabolism and vitamin D.

    PubMed

    Fukumoto, Seiji

    2014-01-01

    Phosphate plays many essential roles in our body. To accomplish these functions, serum phosphate needs to be maintained in a certain range. Serum phosphate level is regulated by intestinal phosphate absorption, renal phosphate handling and equilibrium of extracellular phosphate with that in bone or intracellular fluid. Several hormones such as parathyroid hormone, 1,25-dihydroxyvitamin D (1,25(OH)2D) and fibroblast growth factor 23 (FGF23) regulate serum phosphate by modulating intestinal phosphate absorption, renal phosphate reabsorption and/or bone metabolism. In addition, dietary phosphate rapidly enhances renal phosphate excretion, although detailed mechanisms of this adaptation remain to be clarified. Physiologically, extracellular concentrations of phosphate and these hormones are maintained by several negative feedback loops. For example, 1,25(OH)2D enhances FGF23 production and FGF23 reduces 1,25(OH)2D level. In addition, phosphate affects 1,25(OH)2D and FGF23 levels. Dysfunction of these negative feedback loops results in several diseases with abnormal phosphate and 1,25(OH)2D levels. Especially, excess actions of FGF23 cause several hypophosphatemic rickets/osteomalacia with relatively low level of 1,25(OH)2D that had been classified as vitamin D-resistant rickets/osteomalacia. In contrast, deficient actions of FGF23 cause hyperphosphatemic familial tumoral calcinosis. However, there still remain several unanswered questions regarding phosphate and vitamin D metabolism. PMID:24605214

  16. Phosphate metabolism and vitamin D

    PubMed Central

    Fukumoto, Seiji

    2014-01-01

    Phosphate plays many essential roles in our body. To accomplish these functions, serum phosphate needs to be maintained in a certain range. Serum phosphate level is regulated by intestinal phosphate absorption, renal phosphate handling and equilibrium of extracellular phosphate with that in bone or intracellular fluid. Several hormones such as parathyroid hormone, 1,25-dihydroxyvitamin D (1,25(OH)2D) and fibroblast growth factor 23 (FGF23) regulate serum phosphate by modulating intestinal phosphate absorption, renal phosphate reabsorption and/or bone metabolism. In addition, dietary phosphate rapidly enhances renal phosphate excretion, although detailed mechanisms of this adaptation remain to be clarified. Physiologically, extracellular concentrations of phosphate and these hormones are maintained by several negative feedback loops. For example, 1,25(OH)2D enhances FGF23 production and FGF23 reduces 1,25(OH)2D level. In addition, phosphate affects 1,25(OH)2D and FGF23 levels. Dysfunction of these negative feedback loops results in several diseases with abnormal phosphate and 1,25(OH)2D levels. Especially, excess actions of FGF23 cause several hypophosphatemic rickets/osteomalacia with relatively low level of 1,25(OH)2D that had been classified as vitamin D-resistant rickets/osteomalacia. In contrast, deficient actions of FGF23 cause hyperphosphatemic familial tumoral calcinosis. However, there still remain several unanswered questions regarding phosphate and vitamin D metabolism. PMID:24605214

  17. INHIBITION OF GAP-JUNCTIONAL INTERCELLULAR COMMUNICATION BETWEEN CHINESE HAMSTER LUNG FIBROBLASTS BY DI(2-ETHYLHEXYL) PHTHALATE(DEHP) AND TRISODIUM NITRILOTRIACETATE MONOHYDRATE (NTA)

    EPA Science Inventory

    Di(2-ethylhexyl)phthalate and trisodium nitrilotriacetate monohydrate, two apparently nongenotoxic carcinogens, were tested for effects on gap-junctional communication between Chinese hamster V79 lung fibroblasts. oth compounds inhibited gap-junctional communication in vitro corr...

  18. Entropy and crystal structure of hydrates of disodium hydrogen phosphate

    SciTech Connect

    Templeton, D.H.; Ruben, H.W.; Zalkin, A. )

    1990-10-04

    Structures determined by X-ray diffraction are reported for crystals of Na{sub 2}HPO{sub 4}{center dot}xH{sub 2}O (x = 1, 2, 7, and 12). The new monohydrate phase is triclinic, space group P{bar 1}, a = 5.575 (1) {angstrom}, b = 7.949 (1) {angstrom}, c = 5.735 (1) {angstrom}, {alpha} = 103.83 (1){degree}, {beta} = 102.15 (1){degree}, {gamma} = 107.47 (1){degree}, Z = 2, R = 0.020 for 3329 independent reflections. The other structures are in agreement with independent determinations already published. For x = 1, 2, or 7 no disorder is observed, and there are unique configurations of protons in hydrogen bonds. The dodecahydrate (x = 12) has two kinds of disorder, randomness of phosphate ion orientations and of proton positions in hydrogen bonds. A model for this disorder gives 2.65 cal K{sup {minus}1} mol{sup {minus}1} as the residual entropy at low temperature, compared with 3.1 {plus minus} 0.5 and 3.5 {plus minus} 0.4 cal K{sup {minus}1} mol{sup {minus}1} derived from two thermodynamic cycles.

  19. Effects of monohydric alcohols and polyols on the thermal stability of a protein.

    PubMed

    Murakami, Shota; Kinoshita, Masahiro

    2016-03-28

    The thermal stability of a protein is lowered by the addition of a monohydric alcohol, and this effect becomes larger as the size of hydrophobic group in an alcohol molecule increases. By contrast, it is enhanced by the addition of a polyol possessing two or more hydroxyl groups per molecule, and this effect becomes larger as the number of hydroxyl groups increases. Here, we show that all of these experimental observations can be reproduced even in a quantitative sense by rigid-body models focused on the entropic effect originating from the translational displacement of solvent molecules. The solvent is either pure water or water-cosolvent solution. Three monohydric alcohols and five polyols are considered as cosolvents. In the rigid-body models, a protein is a fused hard spheres accounting for the polyatomic structure in the atomic detail, and the solvent is formed by hard spheres or a binary mixture of hard spheres with different diameters. The effective diameter of cosolvent molecules and the packing fractions of water and cosolvent, which are crucially important parameters, are carefully estimated using the experimental data of properties such as the density of solid crystal of cosolvent, parameters in the pertinent cosolvent-cosolvent interaction potential, and density of water-cosolvent solution. We employ the morphometric approach combined with the integral equation theory, which is best suited to the physical interpretation of the calculation result. It is argued that the degree of solvent crowding in the bulk is the key factor. When it is made more serious by the cosolvent addition, the solvent-entropy gain upon protein folding is magnified, leading to the enhanced thermal stability. When it is made less serious, the opposite is true. The mechanism of the effects of monohydric alcohols and polyols is physically the same as that of sugars. However, when the rigid-body models are employed for the effect of urea, its addition is predicted to enhance the thermal stability, which conflicts with the experimental fact. We then propose, as two essential factors, not only the solvent-entropy gain but also the loss of protein-solvent interaction energy upon protein folding. The competition of changes in these two factors induced by the cosolvent addition determines the thermal-stability change. PMID:27036482

  20. Effects of monohydric alcohols and polyols on the thermal stability of a protein

    NASA Astrophysics Data System (ADS)

    Murakami, Shota; Kinoshita, Masahiro

    2016-03-01

    The thermal stability of a protein is lowered by the addition of a monohydric alcohol, and this effect becomes larger as the size of hydrophobic group in an alcohol molecule increases. By contrast, it is enhanced by the addition of a polyol possessing two or more hydroxyl groups per molecule, and this effect becomes larger as the number of hydroxyl groups increases. Here, we show that all of these experimental observations can be reproduced even in a quantitative sense by rigid-body models focused on the entropic effect originating from the translational displacement of solvent molecules. The solvent is either pure water or water-cosolvent solution. Three monohydric alcohols and five polyols are considered as cosolvents. In the rigid-body models, a protein is a fused hard spheres accounting for the polyatomic structure in the atomic detail, and the solvent is formed by hard spheres or a binary mixture of hard spheres with different diameters. The effective diameter of cosolvent molecules and the packing fractions of water and cosolvent, which are crucially important parameters, are carefully estimated using the experimental data of properties such as the density of solid crystal of cosolvent, parameters in the pertinent cosolvent-cosolvent interaction potential, and density of water-cosolvent solution. We employ the morphometric approach combined with the integral equation theory, which is best suited to the physical interpretation of the calculation result. It is argued that the degree of solvent crowding in the bulk is the key factor. When it is made more serious by the cosolvent addition, the solvent-entropy gain upon protein folding is magnified, leading to the enhanced thermal stability. When it is made less serious, the opposite is true. The mechanism of the effects of monohydric alcohols and polyols is physically the same as that of sugars. However, when the rigid-body models are employed for the effect of urea, its addition is predicted to enhance the thermal stability, which conflicts with the experimental fact. We then propose, as two essential factors, not only the solvent-entropy gain but also the loss of protein-solvent interaction energy upon protein folding. The competition of changes in these two factors induced by the cosolvent addition determines the thermal-stability change.

  1. Phosphate Mines, Jordan

    NASA Technical Reports Server (NTRS)

    2008-01-01

    Jordan's leading industry and export commodities are phosphate and potash, ranked in the top three in the world. These are used to make fertilizer. The Jordan Phosphate Mines Company is the sole producer, having started operations in 1935. In addition to mining activities, the company produces phosphoric acid (for fertilizers, detergents, pharmaceuticals), diammonium phosphate (for fertilizer), sulphuric acid (many uses), and aluminum fluoride (a catalyst to make aluminum and magnesium).

    The image covers an area of 27.5 x 49.4 km, was acquired on September 17, 2005, and is located near 30.8 degrees north latitude, 36.1 degrees east longitude.

    The U.S. science team is located at NASA's Jet Propulsion Laboratory, Pasadena, Calif. The Terra mission is part of NASA's Science Mission Directorate.

  2. Characterization of dicalcium phosphate dihydrate cements prepared using a novel hydroxyapatite-based formulation.

    PubMed

    Alge, Daniel L; Santa Cruz, Grace; Goebel, W Scott; Chu, Tien-Min Gabriel

    2009-04-01

    Dicalcium phosphate dihydrate (DCPD) cements are typically prepared using beta-tricalcium phosphate (beta-TCP) as the base component. However, hydroxyapatite (HA) is an interesting alternative because of its potential for reducing cement acidity, as well as modulating cement properties via ionic substitutions. In the present study, we have characterized DCPD cements prepared with a novel formulation based on monocalcium phosphate monohydrate (MCPM) and HA. Cements were prepared using a 4:1 MCPM:HA molar ratio. The reactivity of HA in this system was verified by showing DCPD formation using poorly crystalline HA, as well as highly crystalline HA. Evaluation of cements prepared with poorly crystalline HA revealed that setting occurs rapidly in the MCPM/HA system, and that the use of a setting regulator is necessary to maintain workability of the cement paste. Compressive testing showed that MCPM/HA cements have strengths comparable to what has previously been published for DCPD cements. However, preliminary in vitro analysis of cement degradation revealed that conversion of DCPD to HA may occur much more rapidly in the MCPM/HA system compared to cements prepared with beta-TCP. Future studies should investigate this property further, as it could have important implications for the use of HA-based DCPD cement formulations. PMID:19349655

  3. Effect of Acarbose, Sitagliptin and combination therapy on blood glucose, insulin, and incretin hormone concentrations in experimentally induced postprandial hyperglycemia of healthy cats.

    PubMed

    Mori, Akihiro; Ueda, Kaori; Lee, Peter; Oda, Hitomi; Ishioka, Katsumi; Arai, Toshiro; Sako, Toshinori

    2016-06-01

    Acarbose (AC) and Sitagliptin (STGP) are oral hypoglycemic agents currently used either alone or in conjunction with human diabetic (Type 2) patients. AC has been used with diabetic cats, but not STGP thus far. Therefore, the objective of this study was to determine the potential use of AC or STGP alone and in combination for diabetic cats, by observing their effect on short-term post-prandial serum glucose, insulin, and incretin hormone (active glucagon-like peptide-1 (GLP-1) and total glucose dependent insulinotropic polypeptide (GIP)) concentrations in five healthy cats, following ingestion of a meal with maltose. All treatments tended (p<0.10; 5-7.5% reduction) to reduce postprandial glucose area under the curve (AUC), with an accompanying significant reduction (p<0.05, 35-45%) in postprandial insulin AUC as compared to no treatment. Meanwhile, a significant increase (p<0.05) in postprandial active GLP-1 AUC was observed with STGP (100% higher) and combined treatment (130% greater), as compared to either AC or no treatment. Lastly, a significant reduction (p<0.05) in postprandial total GIP AUC was observed with STGP (21% reduction) and combined treatment (7% reduction) as compared to control. Overall, AC, STGP, or combined treatment can significantly induce positive post-prandial changes to insulin and incretin hormone levels of healthy cats. Increasing active GLP-1 and reducing postprandial hyperglycemia appear to be the principal mechanisms of combined treatment. Considering the different, but complementary mechanisms of action by which AC and STGP induce lower glucose and insulin levels, combination therapy with both these agents offers great potential for treating diabetic cats in the future. PMID:27234550

  4. Molecular structures and thermodynamic properties of monohydrated gaseous iodine compounds: Modelling for severe accident simulation

    NASA Astrophysics Data System (ADS)

    Sudolská, Mária; Cantrel, Laurent; Budzák, Šimon; Černušák, Ivan

    2014-03-01

    Monohydrated complexes of iodine species (I, I2, HI, and HOI) have been studied by correlated ab initio calculations. The standard enthalpies of formation, Gibbs free energy and the temperature dependence of the heat capacities at constant pressure were calculated. The values obtained have been implemented in ASTEC nuclear accident simulation software to check the thermodynamic stability of hydrated iodine compounds in the reactor coolant system and in the nuclear containment building of a pressurised water reactor during a severe accident. It can be concluded that iodine complexes are thermodynamically unstable by means of positive Gibbs free energies and would be represented by trace level concentrations in severe accident conditions; thus it is well justified to only consider pure iodine species and not hydrated forms.

  5. Aripiprazole long-acting injectable formulations for schizophrenia: aripiprazole monohydrate and aripiprazole lauroxil.

    PubMed

    Citrome, Leslie

    2016-02-01

    Aripiprazole monohydrate (AM) and aripiprazole lauroxil (AL) are two different long-acting injectable formulations of aripiprazole. AM 400 mg administered once monthly demonstrated efficacy in an acute, double-blind, placebo-controlled, randomized clinical trial, as well as in a double-blind, placebo-controlled, randomized-withdrawal maintenance study, and in two non-inferiority maintenance studies. AL is a prodrug of aripiprazole and available in 441 mg, 662 mg or 882 mg strengths. AL 441 mg and 882 mg administered once monthly demonstrated efficacy in an acute, double-blind, placebo-controlled, randomized clinical trial. The pharmacokinetic profile of AL also led to approval of dosing intervals of every 6 weeks for the 882 mg dose. The overall tolerability profiles of both products are consistent with what is known about oral aripiprazole. PMID:26573020

  6. The crystal structure of ytterbium diiodide monohydrate by X-ray powder diffraction

    SciTech Connect

    Lasocha, W.

    1995-02-01

    The crystal structure of the ytterbium diiodide monohydrate was determined by the X-ray powder diffraction method. Ytterbium atoms are octahedrally coordinated by five iodine atoms and one oxygen atom; space group: Pnma (62); lattice parameters: a = 10.4792(7), b = 4.5138(3), c = 13.0602(9) {angstrom}. Rietveld refinement of a mixture of ytterbium diiodide hydrate and a silicon standard results in the discrepancy factors R{sub B} = 8.04, R{sub wp} = 9.17%. The powder pattern previously reported for YbI{sub 2}{center_dot}2H{sub 2}O is shown to be identical to that of YbI{sub 2}{center_dot}H{sub 2}O.

  7. Nucleation of Alpha lactose monohydrate induced using flow through a venturi orifice

    NASA Astrophysics Data System (ADS)

    McLeod, J. S.; Paterson, A. H. J.; Bronlund, J. E.; Jones, J. R.

    2010-03-01

    Nucleation is a determinant of the final crystal size distribution produced during a crystallization process. Other studies in the literature have shown that mixing influences alpha lactose monohydrate nucleation. To investigate this in more detail, three different sized Venturi orifices were used to provide a point of passive mixing for supersaturated lactose solutions. This system allowed the study of different factors associated with characterising the mixing process, including cavitation, power input, Reynolds number and vortex formation. A strong relationship was found between the number of vortices created in the system and the nucleation rate. It is speculated that the vortices decrease the distance required for diffusion of molecules in the system, increasing the rate at which they can come together to form a stable nuclei.

  8. Inhibition of calcium oxalate monohydrate crystallization by the combination of citrate and osteopontin

    NASA Astrophysics Data System (ADS)

    Wang, Lijun; Zhang, Wei; Qiu, S. Roger; Zachowicz, William J.; Guan, Xiangying; Tang, Ruikang; Hoyer, John R.; De Yoreo, James J.; Nancollas, George H.

    2006-05-01

    The design of effective crystallization inhibitors of calcium oxalate monohydrate (COM), the primary constituent of kidney stones, is a significant goal. Inhibitory molecules identified in urine include a small organic anion, citrate, and osteopontin (OPN), an aspartic acid-rich protein. The results of molecular-scale analyses combining force microscopy with molecular modeling raised the possibility that inhibition of COM crystallization might be increased by the additive effects of citrate and OPN because they act on different crystal faces. Constant composition (CC) kinetics studies of COM crystal growth now confirm that additive effects are, indeed, achieved in vitro when both citrate and OPN are present. These results suggest that a strategy employing combinations of inhibitors may provide a useful therapeutic approach to urinary stone disease.

  9. Reverse engineering the kidney: modelling calcium oxalate monohydrate crystallization in the nephron.

    PubMed

    Borissova, A; Goltz, G E; Kavanagh, J P; Wilkins, T A

    2010-07-01

    Crystallization of calcium oxalate monohydrate in a section of a single kidney nephron (distal convoluted tubule) is simulated using a model adapted from industrial crystallization. The nephron fluid dynamics is represented as a crystallizer/separator series with changing volume to allow for water removal along the tubule. The model integrates crystallization kinetics and crystal size distribution and allows the prediction of the calcium oxalate concentration profile and the nucleation and growth rates. The critical supersaturation ratio for the nucleation of calcium oxalate crystals has been estimated as 2 and the mean crystal size as 1 mum. The crystal growth order, determined as 2.2, indicates a surface integration mechanism of crystal growth and crystal growth dispersion. The model allows the exploration of the effect of varying the input calcium oxalate concentration and the rate of water extraction, simulating real life stressors for stone formation such as dietary loading and dehydration. PMID:20424925

  10. Polarized Raman and hyperpolarizability studies of Hydroxyethylammonium (L) tartrate monohydrate for quadratic nonlinear optics

    NASA Astrophysics Data System (ADS)

    Nagalakshmi, R.; Krishnakumar, V.; Hagemann, Hans; Muthunatesan, S.

    2011-03-01

    Single crystals of Hydroxyethylammonium L-tartrate monohydrate [HEALT] have been grown by slow evaporation technique using water as a solvent. The structural and vibrational properties of the crystals were studied. Besides these characterizations ab initio quantum chemical calculations have been performed at HF/6-31G (d) level to derive first order hyperpolarizability. It is shown that the first order hyperpolarizability is found to be 14.2 times more than that of urea. The characteristic vibrational frequencies obtained from polarized Raman spectra in different scattering configurations have been assigned based on the complete factor group analysis. Vibrational analysis of IR and Raman reveals that the charge transfer interaction must be responsible for nonlinear optical (NLO) properties of the present system. The UV absorption measurements have also been carried out to confirm the utility of the material for optical applications.

  11. Sodium (1R)-d-glucit-1-yl-sulfonate monohydrate.

    PubMed

    Haines, Alan H; Hughes, David L

    2012-04-01

    The title salt, Na(+)·C(6)H(13)O(9)S(-)·H(2)O, crystallizes with three independent cations, molecular anions and solvent water molecules in the asymmetric unit. This crystalline monohydrate addition product, formed by reaction of d-glucose and sodium hydrogen sulfite in water, forms a three-dimensional network through complex cation coordination and extensive inter-molecular hydrogen bonding. Each of the independent mol-ecules has an open-chain structure with the carbon chains adopting a sickle-like conformation, similar to that found in the potassium salt [Cole et al. (2001 ▶). Carbohydr. Res.335, 1-10], but there are significant differences in the patterns of complexation. PMID:22589769

  12. Role of magnesium in the growth of calcium oxalate monohydrate and calcium oxalate dihydrate crystals.

    PubMed

    Oka, T; Yoshioka, T; Koide, T; Takaha, M; Sonoda, T

    1987-01-01

    Since about 85% of synthesized calcium oxalate dihydrate (COD) crystals proved not to have changed into calcium oxalate monohydrate (COM) crystals at 30 min of incubation time at 37 degrees C when our evaluation method of the COD-to-COM ratio was being used, we made a comparative study of the inhibitory effects of magnesium, one of the well-known inhibitors of calcium oxalate stone formation, on the growth of seeded COM and COD crystals. The results demonstrated that magnesium in identical concentrations might have stronger inhibitory effects on the growth of COM crystals than on that of COD crystals and suggested that these different effects of magnesium on the growth of COM and COD crystals might arise not only from the difference between the specific surface areas of COM and COD crystals, but also from that between the direct inhibitory effects of magnesium on these two types of calcium oxalate crystal growth. PMID:3617248

  13. Premixed rapid-setting calcium phosphate composites for bone repair.

    PubMed

    Carey, Lisa E; Xu, Hockin H K; Simon, Carl G; Takagi, Shozo; Chow, Laurence C

    2005-08-01

    Although calcium phosphate cement (CPC) is promising for bone repair, its clinical use requires on site powder-liquid mixing. To shorten surgical time and improve graft properties, it is desirable to develop premixed CPC in which the paste remains stable during storage and hardens only after placement into the defect. The objective of this study was to develop premixed CPC with rapid setting when immersed in a physiological solution. Premixed CPCs were formulated using the following approach: Premixed CPC = CPC powder + nonaqueous liquid + gelling agent + hardening accelerator. Three premixed CPCs were developed: CPC-monocalcium phosphate monohydrate (MCPM), CPC-chitosan, and CPC-tartaric. Setting time for these new premixed CPCs ranged from 5.3 to 7.9 min, significantly faster than 61.7 min for a premixed control CPC reported previously (p < 0.05). SEM revealed the formation of nano-sized needle-like hydroxyapatite crystals after 1 d immersion and crystal growth after 7 d. Diametral tensile strength for premixed CPCs at 7 d ranged from 2.8 to 6.4 MPa, comparable to reported strengths for cancellous bone and sintered porous hydroxyapatite implants. Osteoblast cells attained a normal polygonal morphology on CPC-MCPM and CPC-chitosan with cytoplasmic extensions adhering to the nano-hydroxyapatite crystals. In summary, fast-setting premixed CPCs were developed to avoid the powder-liquid mixing in surgery. The pastes hardened rapidly once immersed in physiological solution and formed hydroxyapatite. The cements had strengths matching those of cancellous bone and sintered porous hydroxyapatite and non-cytotoxicity similar to conventional non-premixed CPC. PMID:15769536

  14. Premixed rapid-setting calcium phosphate composites for bone repair✩

    PubMed Central

    Carey, Lisa E.; Xu, Hockin H.K.; Simon, Carl G.; Takagi, Shozo; Chow, Laurence C.

    2009-01-01

    Although calcium phosphate cement (CPC) is promising for bone repair, its clinical use requires on site powder–liquid mixing. To shorten surgical time and improve graft properties, it is desirable to develop premixed CPC in which the paste remains stable during storage and hardens only after placement into the defect. The objective of this study was to develop premixed CPC with rapid setting when immersed in a physiological solution. Premixed CPCs were formulated using the following approach: Premixed CPC = CPC powder+nonaqueous liquid+gelling agent+hardening accelerator. Three premixed CPCs were developed: CPC–monocalcium phosphate monohydrate (MCPM), CPC–chitosan, and CPC–tartaric. Setting time for these new premixed CPCs ranged from 5.3 to 7.9 min, significantly faster than 61.7 min for a premixed control CPC reported previously (p<05). SEM revealed the formation of nano-sized needle-like hydroxyapatite crystals after 1 d immersion and crystal growth after 7 d. Diametral tensile strength for premixed CPCs at 7 d ranged from 2.8 to 6.4 MPa, comparable to reported strengths for cancellous bone and sintered porous hydroxyapatite implants. Osteoblast cells attained a normal polygonal morphology on CPC–MCPM and CPC–chitosan with cytoplasmic extensions adhering to the nano-hydroxyapatite crystals. In summary, fast-setting premixed CPCs were developed to avoid the powder–liquid mixing in surgery. The pastes hardened rapidly once immersed in physiological solution and formed hydroxyapatite. The cements had strengths matching those of cancellous bone and sintered porous hydroxyapatite and non-cytotoxicity similar to conventional non-premixed CPC. PMID:15769536

  15. Rotational spectroscopy of the atmospheric photo-oxidation product o-toluic acid and its monohydrate.

    PubMed

    Schnitzler, Elijah G; Zenchyzen, Brandi L M; Jäger, Wolfgang

    2016-01-01

    o-Toluic acid, a photo-oxidation product in the atmosphere, and its monohydrate were characterized in the gas phase by pure rotational spectroscopy. High-resolution spectra were measured in the range of 5-14 Hz using a cavity-based molecular beam Fourier-transform microwave spectrometer. Possible conformers were identified computationally, at the MP2/6-311++G(2df,2pd) level of theory. For both species, one conformer was identified experimentally, and no methyl internal rotation splittings were observed, indicative of relatively high barriers to rotation. In the monomer, rocking of the carboxylic acid group is a large amplitude motion, characterized by a symmetrical double-well potential. This and other low-lying out-of-plane vibrations contribute to a significant (methyl top-corrected) inertial defect (-1.09 amu Å(2)). In the monohydrate, wagging of the free hydrogen atom of water is a second large amplitude motion, so the average structure is planar. As a result, no c-type transitions were observed. Water tunneling splittings were not observed, because the water rotation coordinate is characterized by an asymmetrical double-well potential. Since the minima are not degenerate, tunneling is precluded. Furthermore, a concerted tunneling path involving simultaneous rotation of the water moiety and rocking of the carboxylic acid group is precluded, because the hilltop along this coordinate is a virtual, rather than a real, saddle-point. Inter- and intramolecular non-covalent bonding is discussed in terms of the quantum theory of atoms in molecules. The percentage of o-toluic acid hydrated in the atmosphere is estimated to be about 0.1% using statistical thermodynamics. PMID:26616640

  16. Sodium Phosphate Rectal

    MedlinePlus

    ... liquid using a measuring spoon. Then replace the bottle cap.To use the sodium phosphate enema, follow these steps: Remove the protective shield from the tip of the enema. Lie down on ... insert the enema bottle into your rectum with the tip pointing toward ...

  17. Reflectance spectra of hydrated sulfates, phosphates and perchlorates

    NASA Astrophysics Data System (ADS)

    Bishop, J. L.; Lane, M. D.; Dyar, M. D.

    2012-12-01

    Reflectance spectra of hydrated sulfates, phosphates, and perchlorates have multiple strong absorptions in the VNIR region. These bands are important for identification of hydrated salt minerals on Mars using CRISM and OMEGA data. Detecting specific minerals or mineral classes in this group provides constraints on the geochemical environments during their formation. Orbital detections of hydrated salt minerals by CRISM on Mars can support characterization of minerals on the surface by the MER and MSL rovers and the Phoenix lander. VNIR SPECTRAL CHARACTER OF HYDRATED SALTS Many spectral features are diagnostic of specific minerals, but others are common to all of these hydrated salts. Monohydrated sulfate spectra have strong bands near 2.1 and 2.4 μm, while polyhydrated sulfate spectra generally exhibit a band near 1.92-1.98 μm and a drop in reflectance near 2.4 μm. Phosphates appear to exhibit spectral properties similar to sulfates with features near 1.4-1.5 and 1.92-1.98 μm for hydrated samples. Several OH-bearing minerals exhibit features near 2.2 μm that could be confused with the band near 2.2 μm that is commonly attributed to Al/Si-OH bearing clays/silica on Mars. Perchlorate spectra have three dominant bands near 1.43-1.47, 1.93-2.0, and 2.41-2.44 μm depending on the type of cation present. Spectra are shown from 0.4-2.65 μm for selected sulfates (Figure 1) and phosphates/perchlorates (Figure 2) as this region is predominantly used by CRISM for identification of minerals. Figure 1. Spectra of selected hydrated sulfates: coquimbite, (Fe3+)2(SO4)3●9H2O, butlerite, Fe3+SO4(OH)●2H2O, rozenite, Fe2+SO4●4H2O, and szomolnokite, Fe2+SO4●H2O. Figure 2. Spectra of selected perchlorates and phosphates: wavellite, Al3(PO4)2(OH,F)3●5H2O, and baricite, (Mg,Fe2+)3(PO4)2●H2O.

  18. Nanouric acid or nanocalcium phosphate as central nidus to induce calcium oxalate stone formation: a high-resolution transmission electron microscopy study on urinary nanocrystallites

    PubMed Central

    Gao, Jie; Xue, Jun-Fa; Xu, Meng; Gui, Bao-Song; Wang, Feng-Xin; Ouyang, Jian-Ming

    2014-01-01

    Purpose This study aimed to accurately analyze the relationship between calcium oxalate (CaOx) stone formation and the components of urinary nanocrystallites. Method High-resolution transmission electron microscopy (HRTEM), selected area electron diffraction, fast Fourier transformation of HRTEM, and energy dispersive X-ray spectroscopy were performed to analyze the components of these nanocrystallites. Results The main components of CaOx stones are calcium oxalate monohydrate and a small amount of dehydrate, while those of urinary nanocrystallites are calcium oxalate monohydrate, uric acid, and calcium phosphate. The mechanism of formation of CaOx stones was discussed based on the components of urinary nanocrystallites. Conclusion The formation of CaOx stones is closely related both to the properties of urinary nanocrystallites and to the urinary components. The combination of HRTEM, fast Fourier transformation, selected area electron diffraction, and energy dispersive X-ray spectroscopy could be accurately performed to analyze the components of single urinary nanocrystallites. This result provides evidence for nanouric acid and/or nanocalcium phosphate crystallites as the central nidus to induce CaOx stone formation. PMID:25258530

  19. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Magnesium phosphate. 184.1434 Section 184.1434... Listing of Specific Substances Affirmed as GRAS § 184.1434 Magnesium phosphate. (a) Magnesium phosphate includes both magnesium phosphate, dibasic, and magnesium phosphate, tribasic. Magnesium phosphate,...

  20. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Magnesium phosphate. 184.1434 Section 184.1434... GRAS § 184.1434 Magnesium phosphate. (a) Magnesium phosphate includes both magnesium phosphate, dibasic, and magnesium phosphate, tribasic. Magnesium phosphate, dibasic (MgHPO4·3H2O, CAS Reg. No....

  1. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Magnesium phosphate. 184.1434 Section 184.1434 Food... Specific Substances Affirmed as GRAS § 184.1434 Magnesium phosphate. (a) Magnesium phosphate includes both magnesium phosphate, dibasic, and magnesium phosphate, tribasic. Magnesium phosphate, dibasic...

  2. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Magnesium phosphate. 184.1434 Section 184.1434... Listing of Specific Substances Affirmed as GRAS § 184.1434 Magnesium phosphate. (a) Magnesium phosphate includes both magnesium phosphate, dibasic, and magnesium phosphate, tribasic. Magnesium phosphate,...

  3. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Magnesium phosphate. 184.1434 Section 184.1434... Listing of Specific Substances Affirmed as GRAS § 184.1434 Magnesium phosphate. (a) Magnesium phosphate includes both magnesium phosphate, dibasic, and magnesium phosphate, tribasic. Magnesium phosphate,...

  4. Observation of the asymmetric O--U--O stretch in the vibronic absorption spectrum of uranyl formate monohydrate

    SciTech Connect

    West, W.P.; Muller, C.H. III; Porter, J.T. II; Malley, M.M.

    1983-03-15

    Fluorescence excitation spectra of uranyl formate monohydrate UO/sub 2/ (HCOO)/sub 2/xH/sub 2/O at 4.2 K show the UO/sup +2//sub 2/ asymmetric mode to be active in the vibronic absorption. This assignment is based on the measure uranium isotope shift. It is also observed that the asymmetric mode occurs with a lower frequency than the symmetric in this compound, contrary to the order reported in other uranyl compounds.

  5. Biomediated continuous release phosphate fertilizer

    SciTech Connect

    Goldstein, Alan H.; Rogers, Robert D.

    1999-01-01

    A composition is disclosed for providing phosphate fertilizer to the root zone of plants. The composition comprises a microorganism capable of producing and secreting a solubilization agent, a carbon source for providing raw material for the microorganism to convert into the solubilization agent, and rock phosphate ore for providing a source of insoluble phosphate that is solubilized by the solubilization agent and released as soluble phosphate. The composition is provided in a physical form, such as a granule, that retains the microorganism, carbon source, and rock phosphate ore, but permits water and soluble phosphate to diffuse into the soil. A method of using the composition for providing phosphate fertilizer to plants is also disclosed.

  6. Biomediated continuous release phosphate fertilizer

    DOEpatents

    Goldstein, A.H.; Rogers, R.D.

    1999-06-15

    A composition is disclosed for providing phosphate fertilizer to the root zone of plants. The composition comprises a microorganism capable of producing and secreting a solubilization agent, a carbon source for providing raw material for the microorganism to convert into the solubilization agent, and rock phosphate ore for providing a source of insoluble phosphate that is solubilized by the solubilization agent and released as soluble phosphate. The composition is provided in a physical form, such as a granule, that retains the microorganism, carbon source, and rock phosphate ore, but permits water and soluble phosphate to diffuse into the soil. A method of using the composition for providing phosphate fertilizer to plants is also disclosed. 13 figs.

  7. Differentiation of Calcium Oxalate Monohydrate and Calcium Oxalate Dihydrate Stones Using Quantitative Morphological Information from Micro-Computerized and Clinical Computerized Tomography

    PubMed Central

    Duan, Xinhui; Qu, Mingliang; Wang, Jia; Trevathan, James; Vrtiska, Terri; Williams, James C.; Krambeck, Amy; Lieske, John; McCollough, Cynthia

    2014-01-01

    Purpose We differentiated calcium oxalate monohydrate and calcium oxalate dihydrate kidney stones using micro and clinical computerized tomography images. Materials and Methods A total of 22 calcium oxalate monohydrate and 15 calcium oxalate dihydrate human kidney stones were scanned using a commercial micro-computerized tomography scanner with a pixel size of 7 to 23 μm. Under an institutional review board approved protocol, image data on 10 calcium oxalate monohydrate and 9 calcium oxalate dihydrate stones greater than 5 mm were retrieved from a total of 80 patients who underwent clinical dual energy computerized tomography for clinical indications and had stones available for infrared spectroscopic compositional analysis. Micro and clinical computerized tomography images were processed using in-house software, which quantified stone surface morphology with curvature based calculations. A shape index was generated as a quantitative shape metric to differentiate calcium oxalate monohydrate from calcium oxalate dihydrate stones. Statistical tests were used to test the performance of the shape index. Results On micro-computerized tomography images the shape index of calcium oxalate monohydrate and calcium oxalate dihydrate stones significantly differed (ROC curve AUC 0.92, p <0.0001). At the optimal cutoff sensitivity was 0.93 and specificity was 0.91. On clinical computerized tomography images a significant morphological difference was also detected (p = 0.007). AUC, sensitivity and specificity were 0.90, 1 and 0.73, respectively. Conclusions On micro and clinical computerized tomography images a morphological difference was detectable in calcium oxalate monohydrate and calcium oxalate dihydrate stones larger than 5 mm. The shape index is a highly promising method that can distinguish calcium oxalate monohydrate and calcium oxalate dihydrate stones with reasonable accuracy. PMID:23142201

  8. Dysregulation of phosphate metabolism and conditions associated with phosphate toxicity.

    PubMed

    Brown, Ronald B; Razzaque, Mohammed S

    2015-01-01

    Phosphate homeostasis is coordinated and regulated by complex cross-organ talk through delicate hormonal networks. Parathyroid hormone (PTH), secreted in response to low serum calcium, has an important role in maintaining phosphate homeostasis by influencing renal synthesis of 1,25-dihydroxyvitamin D, thereby increasing intestinal phosphate absorption. Moreover, PTH can increase phosphate efflux from bone and contribute to renal phosphate homeostasis through phosphaturic effects. In addition, PTH can induce skeletal synthesis of another potent phosphaturic hormone, fibroblast growth factor 23 (FGF23), which is able to inhibit renal tubular phosphate reabsorption, thereby increasing urinary phosphate excretion. FGF23 can also fine-tune vitamin D homeostasis by suppressing renal expression of 1-alpha hydroxylase (1α(OH)ase). This review briefly discusses how FGF23, by forming a bone-kidney axis, regulates phosphate homeostasis, and how its dysregulation can lead to phosphate toxicity that induces widespread tissue injury. We also provide evidence to explain how phosphate toxicity related to dietary phosphorus overload may facilitate incidence of noncommunicable diseases including kidney disease, cardiovascular disease, cancers and skeletal disorders. PMID:26131357

  9. Renal phosphate handling: Physiology

    PubMed Central

    Prasad, Narayan; Bhadauria, Dharmendra

    2013-01-01

    Phosphorus is a common anion. It plays an important role in energy generation. Renal phosphate handling is regulated by three organs parathyroid, kidney and bone through feedback loops. These counter regulatory loops also regulate intestinal absorption and thus maintain serum phosphorus concentration in physiologic range. The parathyroid hormone, vitamin D, Fibrogenic growth factor 23 (FGF23) and klotho coreceptor are the key regulators of phosphorus balance in body. PMID:23961477

  10. Efficacy and Safety of Exenatide Once Weekly Versus Metformin, Pioglitazone, and Sitagliptin Used as Monotherapy in Drug-Naive Patients With Type 2 Diabetes (DURATION-4)

    PubMed Central

    Russell-Jones, David; Cuddihy, Robert M.; Hanefeld, Markolf; Kumar, Ajay; González, Jose G.; Chan, Melanie; Wolka, Anne M.; Boardman, Marilyn K.

    2012-01-01

    OBJECTIVE To test the safety and efficacy of exenatide once weekly (EQW) compared with metformin (MET), pioglitazone (PIO), and sitagliptin (SITA) over 26 weeks, in suboptimally treated (diet and exercise) drug-naive patients with type 2 diabetes. RESEARCH DESIGN AND METHODS Patients were randomized to subcutaneous (SC) EQW 2.0 mg + oral placebo (n = 248), MET 2,000 mg/day + SC placebo (n = 246), PIO 45 mg/day + SC placebo (n = 163), or SITA 100 mg/day + SC placebo (n = 163) for 26 weeks. MET and PIO therapies were increased to maximum-tolerated dosages. Injections with EQW or placebo were administered weekly, while oral medication or placebo was administered daily. RESULTS Baseline characteristics were as follows: 59% men, 67% Caucasian, mean age 54 years, HbA1c 8.5%, fasting serum glucose 9.9 mmol/L, body weight 87.0 kg, and diabetes duration 2.7 years. HbA1c reductions (%) at 26 weeks (least-squares means) with EQW versus MET, PIO, and SITA were −1.53 vs. −1.48 (P = 0.620), −1.63 (P = 0.328), and −1.15 (P < 0.001), respectively. Weight changes (kg) were −2.0 vs. −2.0 (P = 0.892), +1.5 (P < 0.001), and −0.8 (P < 0.001), respectively. Common adverse events were as follows: EQW, nausea (11.3%) and diarrhea (10.9%); MET, diarrhea (12.6%) and headache (12.2%); PIO, nasopharyngitis (8.6%) and headache (8.0%); and SIT, nasopharyngitis (9.8%) and headache (9.2%). Minor (confirmed) hypoglycemia was rarely reported. No major hypoglycemia occurred. CONCLUSIONS EQW was noninferior to MET but not PIO and superior to SITA with regard to HbA1c reduction at 26 weeks. Of the agents studied, EQW and MET provided similar improvements in glycemic control along with the benefit of weight reduction and no increased risk of hypoglycemia. PMID:22210563

  11. Skeletal repair in rabbits with calcium phosphate cements incorporated phosphorylated chitin.

    PubMed

    Wang, Xiaohong; Ma, Jianbiao; Feng, Qingling; Cui, Fuzhai

    2002-12-01

    The effects of phosphorylated chitin (P-chitin) on the tissue responses to two kinds of calcium phosphate cements (CPCs) were investigated using experimental rabbits. One of them consisting of monocalcium phosphate monohydrate, calcium oxide, 1 M phosphate buffer (pH: 7.4) and different amounts of P-chitin (CPC-I or P-CPC-I) with relatively neutral initial pH was filled as paste into tibial defects of the rabbits for 1, 4, 12 and 22 weeks. The other kind of cement made from dicacium phosphate dihydrate/calcium hydroxide/1 M Na2HPO4/different amounts of P-chitin (CPC-II or P-CPC-II) with relatively higher initial pH was implanted as prehardened cylinders into the radial defects of the rabbits for the same periods. Pure CPC-I and CPC-II were used as controls. Histological and histomorphological studies were performed on thin un-decalcified and decalcified sections. Three different bone formation types in the resorption lacuna of the P-CPCs were found during this study. The biodegradation rate of the P-CPCs had a negative relationship with the P-chitin content. Most of the low P-chitin-containing samples were bioabsorbed in 16 weeks, while the high P-chitin-containing samples disappeared in 22 weeks. The newly formed bone was identified with back scattered scanning electron microscopy and X-ray energy-dispersive spectrometry. The results show that with P-chitin component in a certain range, the P-CPCs are biocompatible, bioabsorbable and osteoinductive and could be used as promising candidates of bone repair materials. PMID:12322980

  12. Preparation, Characterization, and Structure of α-Zirconium Hydrogen Phosphate Hemihydrate

    NASA Astrophysics Data System (ADS)

    Alberti, G.; Costantino, U.; Millini, R.; Perego, G.; Vivani, R.

    1994-12-01

    A hemihydrate form of layered zirconium phosphate was obtained by reacting ZrO2 with concentrated H3PO4 (17 M) at 230°C for 2 days, Zr(HPO4)2 · 0.5H2O crystallizes in the monoclinic symmetry with cell constants a = 9.1478(5) Å, b = 5.3242(3) Å, c = 15.288(1) Å, β = 103.848(6)°, space group C2/c. It undergoes a reversible phase transition at about 70°C, without losing the lattice water; the interlayer distance is reduced to 7.30 Å and the symmetry changes to the trigonal one (a = 5.3743(5) Å, c = 21.982(2) Å, space group R3¯). The crystal structure of the hemihydrate phase at room temperature was determined by using 36 unambiguously indexed reflections, obtained by the decomposition of the X-ray diffraction pattern, in a conventional single-crystal analysis. A geometric model was assumed for the high-temperature phase. Refinement of the crystal structures was performed by the Rietveld method. In the low-temperature phase, the crystallization water forms interlayer hydrogen bonds with the P-OH of the α-layers, which accounts for the very long times or the elevated temperature required for complete dehydration to occur. Accordingly, the hemihydrate does not transform into the monohydrate phase even when dipped into boiling water and it does not seem obtainable from partial dehydration of the monohydrate form.

  13. Alpha Klotho and phosphate homeostasis

    PubMed Central

    Bian, Ao; Xing, Changying; Hu, Ming Chang

    2015-01-01

    The Klotho family consists of three single-pass transmembrane proteins—αKlotho, βKlotho and γKlotho. Each of them combines with fibroblast growth factor (FGF) receptors (FGFRs) to form receptor complexes for various FGF’s. αKlotho is a co-receptor for physiological FGF23 signaling and appears essential for FGF23-mediated regulation of mineral metabolism. αKlotho protein also plays a FGF23-independent role in phosphate homeostasis. Animal experimental studies and clinical observations have demonstrated that αKlotho deficiency leads to severe hyperphosphatemia; moderate elevation of αKlotho reduces serum phosphate and extremely high αKlotho induces hypophosphatemia and high-FGF23. αKlotho maintains circulating phosphate in a narrow range by modulating intestinal phosphate absorption, urinary phosphate excretion by the kidney, and phosphate distribution into bone rather than soft tissue in concerted interaction with other calciophosphotropic hormones such as PTH, FGF23, and 1,25-(OH)2 vitamin D. The role of αKlotho in maintenance of phosphate homeostasis is mediated by direct suppression of Na-dependent phosphate cotransporters in target organs. Therefore, αKlotho manipulation may be a novel strategy for genetic and acquired phosphate disorders and for medical conditions with αKlotho deficiency such as chronic kidney disease in future. PMID:25194425

  14. Specific Adsorption of Osteopontin and Synthetic Polypeptides to Calcium Oxalate Monohydrate Crystals

    PubMed Central

    Taller, Adam; Grohe, Bernd; Rogers, Kem A.; Goldberg, Harvey A.; Hunter, Graeme K.

    2007-01-01

    Protein-crystal interactions are known to be important in biomineralization. To study the physicochemical basis of such interactions, we have developed a technique that combines confocal microscopy of crystals with fluorescence imaging of proteins. In this study, osteopontin (OPN), a protein abundant in urine, was labeled with the fluorescent dye AlexaFluor-488 and added to crystals of calcium oxalate monohydrate (COM), the major constituent of kidney stones. In five to seven optical sections along the z axis, scanning confocal microscopy was used to visualize COM crystals and fluorescence imaging to map OPN adsorbed to the crystals. To quantify the relative adsorption to different crystal faces, fluorescence intensity was measured around the perimeter of the crystal in several sections. Using this method, it was shown that OPN adsorbs with high specificity to the edges between {100} and {121} faces of COM and much less so to {100}, {121}, or {010} faces. By contrast, poly-L-aspartic acid adsorbs preferentially to {121} faces, whereas poly-L-glutamic acid adsorbs to all faces approximately equally. Growth of COM in the presence of rat bone OPN results in dumbbell-shaped crystals. We hypothesize that the edge-specific adsorption of OPN may be responsible for the dumbbell morphology of COM crystals found in human urine. PMID:17496021

  15. Periodic Hartree-Fock study of nitric acid monohydrate crystal. Bulk and clean surface

    SciTech Connect

    Poshusta, R.D.; Tseng, D.C. ); Hess, A.C.; McCarthy, M.I. )

    1993-07-15

    This study reports the first quantum mechanical investigation of crystalline nitric acid monohydrate (NAM), HNO[sub 3]-H[sub 2]O. The goal of this work is to characterize the physical properties of NAM in order to better understand its role as a catalyst in the destruction of polar stratospheric ozone in the Antarctic. The computations probed energetic, electronic, and elastic properties of the crystalline material using the Periodic Hartree-Fock (PHF) method (as implemented in the program CRYSTAL92). All calculations were performed by using standard Pople basis sets. A description of the bulk material was obtained from calculations of the estimated cohesive binding energy, optimized lattice constants, band structure, total and projected density of states, Mulliken population analysis, electrostatic potentials, and elastic constants. The computed intracrystal interactions are consistent with the proposed hydronium/nitrate ionic crystal structure inferred from X-ray diffraction data. The calculated elastic constants, interlayer electrostatic potential maps, and characterization of the bonding in the crystal indicate that NAM is composed of weakly bound puckered layers aligned parallel to the (100) plane in the crystal. 55 refs., 6 figs., 3 tabs.

  16. The molecular structure and vibrational, (1)H and (13)C NMR spectra of lidocaine hydrochloride monohydrate.

    PubMed

    Badawi, Hassan M; Förner, Wolfgang; Ali, Shaikh A

    2016-01-01

    The structure, vibrational and NMR spectra of the local anesthetic drug lidocaine hydrochloride monohydrate salt were investigated by B3LYP/6-311G(∗∗) calculations. The lidocaine·HCl·H2O salt is predicted to have the gauche structure as the predominant form at ambient temperature with NCCN and CNCC torsional angles of 110° and -123° as compared to 10° and -64°, respectively in the base lidocaine. The repulsive interaction between the two N-H bonds destabilized the gauche structure of lidocaine·HCl·H2O salt. The analysis of the observed vibrational spectra is consistent with the presence of the lidocaine salt in only one gauche conformation at room temperature. The (1)H and (13)C NMR spectra of lidocaine·HCl·H2O were interpreted by experimental and DFT calculated chemical shifts of the lidocaine salt. The RMSD between experimental and theoretical (1)H and (13)C chemical shifts for lidocaine·HCl·H2O is 2.32 and 8.21ppm, respectively. PMID:26196935

  17. In situ investigation of growth rates and growth rate dispersion of α-lactose monohydrate crystals

    NASA Astrophysics Data System (ADS)

    Dincer, T. D.; Ogden, M. I.; Parkinson, G. M.

    2009-02-01

    The growth rates and growth rate dispersion (GRD) of four different faces of α-lactose monohydrate crystal were measured at 30, 40 and 50 °C in the relative supersaturation range 0.55-2.33 in aqueous solutions. The overall growth rate of the crystal is around 50-60% of the (0 1 0) face of the crystal. The power law was applied to the growth rates of the four faces and the activation energies were calculated to be between 9.5 and 13.7 kcal/mol. This indicates a diffusion-controlled growth, but the exponents calculated are between 2.5 and 3.1 which are higher than unity. Introduction of critical supersaturation decreased the exponents to between 1.8 and 2.4. The variance of GRD for the (0 1 0) face is twice the variance of the GRD of the (1 1 0) and (1 0 0) faces and 10 times higher than the (1 1¯ 1¯) face at the same supersaturations and temperatures. The GRD of the four faces were similar when expressed as a function of growth rate. However, the (0 1 1) face displayed lower GRD than the other faces at the same temperatures and supersaturations.

  18. Monosodium glutamate in its anhydrous and monohydrate form: Differentiation by Raman spectroscopies and density functional calculations

    NASA Astrophysics Data System (ADS)

    Peica, N.; Lehene, C.; Leopold, N.; Schlücker, S.; Kiefer, W.

    2007-03-01

    Monosodium glutamate (MSG), a common flavor enhancer, is detected in aqueous solutions by Raman and surface-enhanced Raman (SERS) spectroscopies at the micromolar level. The presence of different species, such as protonated and unprotonated MSG, is demonstrated by concentration and pH dependent Raman and SERS experiments. In particular, the symmetric bending modes of the amino group and the stretching modes of the carboxy moiety are employed as marker bands. The protonation of the NH 2 group at acidic pH values, for example, is detected in the Raman spectra. From the measured SERS spectra, a strong chemical interaction of MSG with the colloidal particles is deduced and a geometry of MSG adsorbed on the silver surface is proposed. In order to assign the observed Raman bands, calculations employing density functional theory (DFT) were performed. The calculated geometries, harmonic vibrational wavenumbers and Raman scattering activities for both MSG forms are in good agreement with experimental data. The set of theoretical data enables a complete vibrational assignment of the experimentally detected Raman spectra and the differentiation between the anhydrous and monohydrate forms of MSG.

  19. Effect of alkalinization on calcium oxalate monohydrate calculi during extracorporeal shock wave lithotripsy: in vivo experiments.

    PubMed

    Vandeursen, H; De Ridder, D; Demeulenaere, R; Pittomvils, G; Boving, R; Baert, L

    1992-01-01

    Previous in vitro experiments demonstrated the reduced microhardness of calcium oxalate monohydrate (COM) calculi, relative to dry values, when saturated with an alkaline solution (pH = 9.5). Nineteen patients with a COM calculus in the distal ureter which had been resistant to prior extracorporeal shock wave lithotripsy in situ, were treated when the stone was surrounded by alkaline urine. The urine of 14 patients was alkalinized orally by administration of acetazolamine and citrate solution; in 5 other patients direct percutaneous irrigation of sodium bicarbonate via a nephrostomy tube was carried out. The urinary pH just before lithotripsy was greater than or equal to 9 in 17/19 patients. 4,000 shock waves, averaging 18.1 kV generated by the Siemens Lithostar, were delivered onto the calculus. No significant increase of comminution rate was apparent at radiographic control immediately after the treatment and only in half of the cases was evacuation obtained within 3 months. PMID:1316663

  20. Growth and characterization of new semiorganic nonlinear optical and piezoelectric lithium sulfate monohydrate oxalate single crystals

    SciTech Connect

    Yadav, Harsh; Sinha, Nidhi; Kumar, Binay

    2015-04-15

    Highlights: • A new semiorganic single crystal of LSO grown by slow evaporation technique. • Morphological studies of the LSO crystal deduced by BFDH law. • In the UV–vis spectrum wide transparent region and large band gap were found. • SHG is equal to KDP crystal and d{sub 33} was found to be equal to 6pC/N. • Grown crystal belongs to softer category. - Abstract: New semiorganic crystal of lithium sulfate monohydrate oxalate (LSO) for nonlinear application was synthesized by controlled slow evaporation method. The growth rate of various planes of the grown crystal was estimated by morphological study. Single crystal XRD analysis confirmed that the crystal belongs to triclinic lattice with space group P1. High transparency (∼95%) with large band gap (4.57 eV) was analyzed by UV–vis studies. FTIR and Raman spectroscopy were used to identify various functional groups present in the LSO crystal. SHG efficiency was found to be equal to the KDP crystal. Thermal stability (up to 117.54 °C) and melting point (242 °C) of the crystal were studied by TG-DTA. In dielectric measurements, the value of dielectric constant decreases with increase in frequency. Hardness studies confirmed soft nature of crystals. The piezoelectric coefficient was found to be 6pC/N along [0 0 1].

  1. A practical approach to N-glycan production by hydrazinolysis using hydrazine monohydrate.

    PubMed

    Nakakita, Shin-ichi; Sumiyoshi, Wataru; Miyanishi, Nobumitsu; Hirabayashi, Jun

    2007-10-26

    Hydrazinolysis is a versatile method to liberate N-linked glycans from glycoproteins. However, the method is usually performed with anhydrous hydrazine, a highly toxic and explosive chemical used in rocket fuel. Thus despite the need to produce functionally important glyco-materials, hydrazinolysis is limited to small scale (e.g., 0.2-1 mL) reactions. In the present study, we report an alternative procedure for hydrazinolysis using hydrazine monohydrate in place of anhydrous hydrazine. The developed procedure was applied to both purified glycoproteins (Taka-amylase and transferrin) and hen egg yolk protein fraction with comparable yields to the traditional method using anhydrous hydrazine. The sialyl linkage of alpha2-6disialobiantennary oligosaccharides proved to be fully stable. The developed procedure facilitated the large-scale preparation of N-linked glycans. The new method should make a substantial contribution to both small- and large-scale production of functional glycans, including therapeutically relevant human-type glycans. PMID:17727814

  2. The molecular structure and vibrational, 1H and 13C NMR spectra of lidocaine hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Badawi, Hassan M.; Förner, Wolfgang; Ali, Shaikh A.

    2016-01-01

    The structure, vibrational and NMR spectra of the local anesthetic drug lidocaine hydrochloride monohydrate salt were investigated by B3LYP/6-311G∗∗ calculations. The lidocaine·HCl·H2O salt is predicted to have the gauche structure as the predominant form at ambient temperature with NCCN and CNCC torsional angles of 110° and -123° as compared to 10° and -64°, respectively in the base lidocaine. The repulsive interaction between the two N-H bonds destabilized the gauche structure of lidocaine·HCl·H2O salt. The analysis of the observed vibrational spectra is consistent with the presence of the lidocaine salt in only one gauche conformation at room temperature. The 1H and 13C NMR spectra of lidocaine·HCl·H2O were interpreted by experimental and DFT calculated chemical shifts of the lidocaine salt. The RMSD between experimental and theoretical 1H and 13C chemical shifts for lidocaine·HCl·H2O is 2.32 and 8.21 ppm, respectively.

  3. Crystal structure of potassium (1S)-d-lyxit-1-yl-sulfonate monohydrate.

    PubMed

    Haines, Alan H; Hughes, David L

    2015-08-01

    The title compound, K(+)·C5H11O8S(-)·H2O [systematic name: potassium (1S,2S,3S,4R)-1,2,3,4,5-penta-hydroxy-pentane-1-sulfonate monohydrate], formed by reaction of d-lyxose with potassium hydrogen sulfite in water, crystallizes as colourless square prisms. The anion has an open-chain structure in which the S atom, the C atoms of the sugar chain and the oxygen atom of the hy-droxy-methyl group form an essentially all-trans chain with the corresponding torsion angles lying between 178.61 (12) and 157.75 (10)°. A three-dimensional bonding network exists in the crystal structure involving coordination of two crystallographically independent potassium ions by O atoms (one cation being hexa- and the other octa-coordinate, with each lying on a twofold rotation axis), and extensive inter-molecular O-H⋯O hydrogen bonding. PMID:26396774

  4. Growth and characterization of a third order nonlinear optical single crystal: Ethylenediamine-4-nitrophenolate monohydrate

    SciTech Connect

    Dhanalakshmi, B.; Ponnusamy, S.; Muthamizhchelvan, C.; Subhashini, V.

    2015-10-15

    Highlights: • EDA4NPH crystal possesses negative nonlinear refractive index. • The crystal exhibits high third-order NLO susceptibility. • Wide transparency of the crystal makes it suitable for NLO applications. • Dielectric studies substantiate the suitability for electro-optic applications. • The crystal possesses suitable mechanical strength for device fabrication. - Abstract: Bulk crystals of the charge-transfer complex, ethylenediamine-4-nitrophenolate monohydrate, were grown by slow solvent evaporation method from aqueous solution at room temperature. The X-ray diffraction measurements showed that the crystal belongs to centrosymmetric space group C2/c of monoclinic system. The functional groups in the complex were identified using FTIR, FTRaman and FTNMR analyses. The Z-scan measurements revealed the negative nonlinear refractive index of the crystal. The nonlinear absorption coefficient and third order nonlinear optical susceptibility calculated from the measurements were −3.5823 × 10{sup −3} cm/W and 2.3762 × 10{sup −6} esu respectively. The crystal was shown to be highly transparent above 366 nm by UV–vis spectroscopy and a yellow fluorescence was observed from PL spectrum. The TG–DTA and DSC analyses showed that the crystal is thermally stable up to 117.4 °C. The crystals were characterized by dielectric, etching and microhardness studies.

  5. IR spectroscopy of monohydrated tryptamine cation: Rearrangement of the intermolecular hydrogen bond induced by photoionization

    NASA Astrophysics Data System (ADS)

    Sakota, Kenji; Kouno, Yuuki; Harada, Satoshi; Miyazaki, Mitsuhiko; Fujii, Masaaki; Sekiya, Hiroshi

    2012-12-01

    Rearrangement of intermolecular hydrogen bond in a monohydrated tryptamine cation, [TRA(H2O)1]+, has been investigated in the gas phase by IR spectroscopy and quantum chemical calculations. In the S0 state of TRA(H2O)1, a water molecule is hydrogen-bonded to the N atom of the amino group of a flexible ethylamine side chain [T. S. Zwier, J. Phys. Chem. A 105, 8827 (2001), 10.1021/jp011659+]. A remarkable change in the hydrogen-bonding motif of [TRA(H2O)]+ occurs upon photoionization. In the D0 state of [TRA(H2O)1]+, the water molecule is hydrogen-bonded to the NH group of the indole ring of TRA+, indicating that the water molecule transfers from the amino group to NH group. Quantum chemical calculations are performed to investigate the pathway of the water transfer. Two potential energy barriers emerge in [TRA(H2O)1]+ along the intrinsic reaction coordinate of the water transfer. The water transfer event observed in [TRA(H2O)1]+ is not an elementary but a complex process.

  6. Crystal structure of potassium (1S)-d-lyxit-1-yl­sulfonate monohydrate

    PubMed Central

    Haines, Alan H.; Hughes, David L.

    2015-01-01

    The title compound, K+·C5H11O8S−·H2O [systematic name: potassium (1S,2S,3S,4R)-1,2,3,4,5-penta­hydroxy­pentane-1-sulfonate monohydrate], formed by reaction of d-lyxose with potassium hydrogen sulfite in water, crystallizes as colourless square prisms. The anion has an open-chain structure in which the S atom, the C atoms of the sugar chain and the oxygen atom of the hy­droxy­methyl group form an essentially all-trans chain with the corresponding torsion angles lying between 178.61 (12) and 157.75 (10)°. A three-dimensional bonding network exists in the crystal structure involving coordination of two crystallographically independent potassium ions by O atoms (one cation being hexa- and the other octa-coordinate, with each lying on a twofold rotation axis), and extensive inter­molecular O—H⋯O hydrogen bonding. PMID:26396774

  7. Crystallization of calcium oxalate monohydrate at dipalmitoylphosphatidylcholine monolayers in the presence of chondroitin sulfate A

    NASA Astrophysics Data System (ADS)

    Ouyang, Jian-Ming; Deng, Sui-Ping; Zhong, Jiu-Ping; Tieke, Bernd; Yu, Shu-Hong

    2004-10-01

    The growth and aggregation of calcium oxalate monohydrate (COM) crystals beneath dipalmitoylphosphatidylcholine (DPPC) monolayers in the presence of chondroitin sulfate A (C4S) was systematically examined under different surface pressure. The results indicated that the addition of C4S can inhibit the crystal growth and prevent the aggregation of COM crystals. Under a DPPC monolayer, well-defined three-dimensional hexagonal prisms and three-dimensional rhombus prisms with sharply angled tips were obtained. The DPPC monolayer at a surface pressure of 10 mN/m can match the Ca2+ distance of the (1 bar 0 1) face of COM better than at 20 mN/m. The addition of C4S could cooperatively modulate the interaction strength between the monolayer (or itself) with the specific morphology determining faces such as (1 bar 0 1) and (0 2 0), and thus results in remarkable stabilization of the (1 bar 0 1) faces. The dramatic changes in morphological details were due to the strong electrostatic interactions between the Ca2+-rich (1 bar 0 1) crystal faces of COM and the polyanionic polysaccharide C4S together with the negatively charged sites of the zwitterionic DPPC monolayers. The increase of the concentration of C4S can further enhance the stabilization of the (1 bar 0 1) face.

  8. 2-(4-Hy-droxy-phen-yl)-1H-benzimidazol-3-ium chloride monohydrate.

    PubMed

    González-Padilla, Jazmin E; Rosales-Hernández, Martha Cecila; Padilla-Martínez, Itzia I; García-Báez, Efren V; Rojas-Lima, Susana

    2013-01-01

    The title mol-ecular salt, C13H11N2O(+)·Cl(-)·H2O, crystallizes as a monohydrate. In the cation, the phenol and benzimidazole rings are almost coplanar, making a dihedral angle of 3.18 (4)°. The chloride anion and benzimidazole cation are linked by two N(+)-H⋯Cl(-) hydrogen bonds, forming chains propagating along [010]. These chains are linked through O-H⋯Cl hydrogen bonds involving the water mol-ecule and the chloride anion, which form a diamond core, giving rise to the formation of two-dimensional networks lying parallel to (10-2). Two π-π inter-actions involving the imidazolium ring with the benzene and phenol rings [centroid-centroid distances = 3.859 (3) and 3.602 (3) Å, respectively], contribute to this second dimension. A strong O-H⋯O hydrogen bond involving the water mol-ecule and the phenol substituent on the benzimidazole unit links the networks, forming a three-dimensional structure. PMID:24427105

  9. Solid-State Characterization and Interconversion of Recrystallized Amodiaquine Dihydrochloride in Aliphatic Monohydric Alcohols.

    PubMed

    Sirikun, Wiriyaporn; Chatchawalsaisin, Jittima; Sutanthavibul, Narueporn

    2016-04-01

    Amodiaquine dihydrochloride monohydrate (AQ-DM) was obtained by recrystallizing amodiaquine dihydrochloride dihydrate (AQ-DD) in methanol, ethanol, and n-propanol. Solid-state characterization of AQ-DD and AQ-DM was performed using X-ray powder diffractometry, Fourier transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. All recrystallized samples were identified as AQ-DM. Crystal habits of AQ-DD and AQ-DM were shown to be needle-like and rhombohedral crystals, respectively. When AQ-DD and AQ-DM were exposed to various relative humidity in dynamic vapor sorption apparatus, no solid-state interconversion was observed. However, AQ-DM showed higher solubility than AQ-DD when exposed to bulk water during solubility study, while excess AQ-DM was directly transformed back to a more stable AQ-DD structure. Heating AQ-DM sample to temperatures ≥190°C induced initial change to metastable amorphous form (AQ-DA) which was rapidly recrystallized to AQ-DD upon ≥80%RH moisture exposure. AQ-DD was able to be recrystallized in alcohols (C1-C3) as AQ-DM solid-state structure. In summary, AQ-DM was shown to have different solubility, moisture and temperature stability, and interconversion pathways when compared to AQ-DD. Thus, when AQ-DM was selected for any pharmaceutical applications, these critical transformation and property differences should be observed and closely monitored. PMID:26206402

  10. 21 CFR 137.175 - Phosphated flour.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Related Products § 137.175 Phosphated flour. Phosphated flour, phosphated white flour, and phosphated wheat flour, conform to the definition and standard of identity, and are subject to the requirements for... 21 Food and Drugs 2 2010-04-01 2010-04-01 false Phosphated flour. 137.175 Section 137.175 Food...

  11. A multicenter, inpatient, phase 2, double-blind, placebo-controlled dose-ranging study of LY2140023 monohydrate in patients with DSM-IV schizophrenia.

    PubMed

    Kinon, Bruce J; Zhang, Lu; Millen, Brian A; Osuntokun, Olawale O; Williams, Judy E; Kollack-Walker, Sara; Jackson, Kimberley; Kryzhanovskaya, Ludmila; Jarkova, Natalia

    2011-06-01

    The primary objective of this study was to test the hypothesis that 1 or more dose levels of LY2140023 monohydrate, an oral prodrug of the potent metabotropic glutamate (mGlu) 2/3 receptor agonist LY404039, given to patients with schizophrenia for 4 weeks would demonstrate significantly greater efficacy than placebo. The HBBI study was a multicenter, randomized, double-blind, parallel, placebo- and active-controlled trial. Male and female patients aged 18 to 65 years who met the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition (DSM-IV) criteria for schizophrenia were randomized in a 2:2:2:2:2:1 ratio to receive 5-, 20-, 40-, or 80-mg LY2140023 monohydrate twice daily, placebo twice daily, or placebo (am) and 15 mg of olanzapine (pm) daily. Efficacy was defined as the change from baseline on the Positive and Negative Syndrome Scale (PANSS) total score assessed at 4 weeks. The primary analysis did not show that any of the 4 LY2140023 monohydrate doses were more efficacious than placebo as measured by the PANSS total score. Similarly, olanzapine did not significantly separate from placebo. A higher-than-anticipated treatment effect (14.6-point improvement) in the placebo group was observed on PANSS total score. LY2140023 monohydrate was generally well tolerated, although 4 patients reported the serious adverse event of convulsion. LY2140023 monohydrate-treated patients showed little change in dopamine-related adverse events and weight. The results of the HBBI study are considered to be inconclusive because LY2140023 monohydrate and the active control olanzapine did not separate from placebo in the treatment of patients with acutely exacerbated schizophrenia. Additional efficacy, safety, and tolerability testing are needed. PMID:21508856

  12. Acid sulfate alteration of fluorapatite, basaltic glass and olivine by hydrothermal vapors and fluids: Implications for fumarolic activity and secondary phosphate phases in sulfate-rich Paso Robles soil at Gusev Crater, Mars

    NASA Astrophysics Data System (ADS)

    Hausrath, E. M.; Golden, D. C.; Morris, R. V.; Agresti, D. G.; Ming, D. W.

    2013-01-01

    Phosphate-rich rocks and a nearby phosphate-rich soil, Paso Robles, were analyzed in Gusev Crater, Mars, by the Mars Exploration Rover Spirit and interpreted to be highly altered, possibly by hydrothermal or fumarolic alteration of primary, phosphate-rich material. To test mineral phases resulting from such alteration, we performed hydrothermal acid-vapor and acid-fluid experiments on olivine (Ol), fluorapatite (Ap), and basaltic glass (Gl) as single phases and a mixture of phases. Minerals formed include Ca-, Al-, Fe- and Mg-sulfates with different hydration states (anhydrite, bassanite, gypsum; alunogen; hexahydrite, and pentahydrite). Phosphate-bearing minerals formed included monocalcium phosphate monohydrate (MCP) (acid-vapor and acid-fluid alteration of fluorapatite only) and ferrian giniite (acid-fluid alteration of the Ol + Gl + Ap mixture). MCP is likely present in Paso Robles if primary Ca-phosphate minerals reacted with sulfuric acid with little transport of phosphate. Under fluid:rock ratios allowing transport of phosphate, a ferric phosphate phase such as ferrian giniite might form instead. Mössbauer measurements of ferrian giniite-bearing alteration products and synthetic ferrian giniite are consistent with Spirit's Mössbauer measurements of the ferric-bearing phase in Paso Robes soil, but are also consistent with ferric sulfate phases in the low-P soil Arad_Samra. Therefore, Mössbauer data alone do not constrain the fluid:rock ratio. However, the excess iron (hematite) in Paso Robles soil, which implies aqueous transport, combined with our laboratory experiments, suggest acid-sulfate alteration in a hydrothermal (fumarolic) environment at fluid:rock ratios sufficient to allow dissolution, transport, and precipitation of secondary chemical components including a ferric phosphate such as ferrian giniite.

  13. Matrix isolation infrared spectrum of the sulfuric acid-monohydrate complex: new assignments and resolution of the "missing H-Bonded v(OH) band" issue.

    PubMed

    Rozenberg, M; Loewenschuss, A

    2009-04-30

    The matrix isolation infrared spectra of "dry" and "wet" vapors of sulfuric acid have been investigated as trapped in solid argon matrices. The availability of a spectrum of trapped anhydrous acid vapor and its comparison with the spectra of trapped water containing vapors of the acid allowed the identification of the hydrogen-bonding shifted hydroxyl bands for both the acid and the water moieties of the monohydrated H(2)SO(4).H(2)O complex. The experimental results are compared to the various theoretically calculated wavenumber values of the acid and its monohydrated complex. The complex stabilization energies, as obtained from calculations and empirical correlations, are compared. PMID:19385678

  14. Inositol phosphates in the environment.

    PubMed Central

    Turner, Benjamin L; Papházy, Michael J; Haygarth, Philip M; McKelvie, Ian D

    2002-01-01

    The inositol phosphates are a group of organic phosphorus compounds found widely in the natural environment, but that represent the greatest gap in our understanding of the global phosphorus cycle. They exist as inositols in various states of phosphorylation (bound to between one and six phosphate groups) and isomeric forms (e.g. myo, D-chiro, scyllo, neo), although myo-inositol hexakisphosphate is by far the most prevalent form in nature. In terrestrial environments, inositol phosphates are principally derived from plants and accumulate in soils to become the dominant class of organic phosphorus compounds. Inositol phosphates are also present in large amounts in aquatic environments, where they may contribute to eutrophication. Despite the prevalence of inositol phosphates in the environment, their cycling, mobility and bioavailability are poorly understood. This is largely related to analytical difficulties associated with the extraction, separation and detection of inositol phosphates in environmental samples. This review summarizes the current knowledge of inositol phosphates in the environment and the analytical techniques currently available for their detection in environmental samples. Recent advances in technology, such as the development of suitable chromatographic and capillary electrophoresis separation techniques, should help to elucidate some of the more pertinent questions regarding inositol phosphates in the natural environment. PMID:12028785

  15. Phosphonomethyl analogues of hexose phosphates.

    PubMed

    Webster, D; Jondorf, W R; Dixon, H B

    1976-05-01

    The analogue of fructose 1,6-bisphosphate in which the phosphate group, -O-PO3H2, on C-6 is replaced by the phosphonomethyl group, -CH2-PO3H2, was made enzymically from the corresponding analogue of 3-phosphoglycerate. It was a substrate for aldolase, which was used to form it, but not for fructose 1,6-bisphosphatase. It was hydrolysed chemically to yield the corresponding analogue of fructose 6-phosphate [i.e. 6-deoxy-6-(phosphonomethyl)-D-fructose, or, more strictly, 6,7-dideoxy-7-phosphono-D-arabino-2-heptulose]. This proved to be a substrate for the sequential actions of glucose 6-phosphate isomerase, glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase. Thus seven out of the nine enzymes of the glycolytic and pentose phosphate pathways so far tested catalyse the reactions of the phosphonomethyl isosteres of their substrates. PMID:7247

  16. Sphingosine 1-phosphate signalling

    PubMed Central

    Mendelson, Karen; Evans, Todd; Hla, Timothy

    2014-01-01

    Sphingosine 1-phosphate (S1P) is a lipid mediator formed by the metabolism of sphingomyelin. In vertebrates, S1P is secreted into the extracellular environment and signals via G protein-coupled S1P receptors to regulate cell-cell and cell-matrix adhesion, and thereby influence cell migration, differentiation and survival. The expression and localization of S1P receptors is dynamically regulated and controls vascular development, vessel stability and immune cell trafficking. In addition, crucial events during embryogenesis, such as angiogenesis, cardiogenesis, limb development and neurogenesis, are regulated by S1P signalling. Here, and in the accompanying poster, we provide an overview of S1P signalling in development and in disease. PMID:24346695

  17. Light weight phosphate cements

    DOEpatents

    Wagh, Arun S.; Natarajan, Ramkumar,; Kahn, David

    2010-03-09

    A sealant having a specific gravity in the range of from about 0.7 to about 1.6 for heavy oil and/or coal bed methane fields is disclosed. The sealant has a binder including an oxide or hydroxide of Al or of Fe and a phosphoric acid solution. The binder may have MgO or an oxide of Fe and/or an acid phosphate. The binder is present from about 20 to about 50% by weight of the sealant with a lightweight additive present in the range of from about 1 to about 10% by weight of said sealant, a filler, and water sufficient to provide chemically bound water present in the range of from about 9 to about 36% by weight of the sealant when set. A porous ceramic is also disclosed.

  18. Templated, layered manganese phosphate

    SciTech Connect

    Thoma, Steven G.; Bonhomme, Francois R.

    2004-08-17

    A new crystalline maganese phosphate composition having an empirical formula: O). The compound was determined to crystallize in the trigonal space group P-3c1 with a=8.8706(4) .ANG., c=26.1580(2) .ANG., and V (volume)=1783 .ANG..sup.3. The structure consists of sheets of corner sharing Mn(II)O.sub.4 and PO.sub.4 tetrahedra with layers of (H.sub.3 NCH.sub.2 CH.sub.2).sub.3 N and water molecules in-between. The pronated (H.sub.3 NCH.sub.2 CH.sub.2).sub.3 N molecules provide charge balancing for the inorganic sheets. A network of hydrogen bonds between water molecules and the inorganic sheets holds the structure together.

  19. Crystallization of calcium phosphate in polyacrylamide hydrogels containing phosphate ions

    NASA Astrophysics Data System (ADS)

    Yokoi, Taishi; Kawashita, Masakazu; Kikuta, Koichi; Ohtsuki, Chikara

    2010-08-01

    Calcium phosphate crystals were formed in polyacrylamide (PAAm) hydrogels containing phosphate ions by diffusion of calcium ions from calcium nitrate (Ca(NO 3) 2) solutions covering the gels. Changes in crystalline phases and crystal morphology of calcium phosphate, and in ion concentrations of the Ca(NO 3) 2 solutions were investigated as a function of reaction time. Single or two coexisting crystalline phases of calcium phosphate, hydroxyapatite (HAp), HAp/dicalcium phosphate dihydrate (DCPD) or octacalcium phosphate (OCP)/DCPD were formed in the gels. HAp crystals are formed near the surface of the gels. The dense HAp layer and HAp/DCPD layer prevented diffusion of calcium ions from the Ca(NO 3) 2 solution, thus formation of calcium phosphate in the gel phase was inhibited. Formation of DCPD was observed to follow the formation of OCP or HAp. The size of the OCP crystals gradually increased with reaction time, while changes in size of HAp crystals were not observed. The reaction time required for DCPD formation depended on the degree of supersaturation with respect to DCPD in the systems. DCPD formed within 1 day under high supersaturation conditions, whereas it formed at 10 days in low supersaturation conditions.

  20. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    .... (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance produced by the growth of Streptomyces erythreus or the same antibiotic substance produced by any other...

  1. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    .... (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance produced by the growth of Streptomyces erythreus or the same antibiotic substance produced by any other...

  2. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    .... (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance produced by the growth of Streptomyces erythreus or the same antibiotic substance produced by any other...

  3. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    .... (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance produced by the growth of Streptomyces erythreus or the same antibiotic substance produced by any other...

  4. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    .... (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance produced by the growth of Streptomyces erythreus or the same antibiotic substance produced by any other...

  5. Modulation of calcium oxalate monohydrate crystallization by citrate through selective binding to atomic steps

    SciTech Connect

    Qiu, S R; Wierzbicki, A; Salter, E A; Zepeda, S; Orme, C A; Hoyer, J R; Nancollas, G H; Cody, A M; De Yoreo, J J

    2004-10-19

    The majority of human kidney stones are composed primarily of calcium oxalate monohydrate (COM) crystals. Thus, determining the molecular mechanisms by which urinary constituents modulate calcium oxalate crystallization is crucial for understanding and controlling urolithiassis in humans. A comprehensive molecular-scale view of COM shape modification by citrate, a common urinary constituent, obtained through a combination of in situ atomic force microscopy (AFM) and molecular modeling is now presented. We show that citrate strongly influences the growth morphology and kinetics on the (-101) face but has much lower effect on the (010) face. Moreover, binding energy calculations show that the strength of the citrate-COM interaction is much greater at steps than on terraces and is highly step-specific. The maximum binding energy, -166.5 kJ {center_dot} mol{sup -1}, occurs for the [101] step on the (-101) face. In contrast, the value is only -56.9 kJ {center_dot} mol-1 for the [012] step on the (010) face. The binding energies on the (-101) and (010) terraces are also much smaller, -65.4 and -48.9 kJ {center_dot} mol{sup -1} respectively. All other binding energies lie between these extremes. This high selectivity leads to preferential binding of citrate to the acute [101] atomic steps on the (-101) face. The strong citrate-step interactions on this face leads to pinning of all steps, but the anisotropy in interaction strength results in anisotropic reductions in step kinetics. These anisotropic changes in step kinetics are, in turn, responsible for changes in the shape of macroscopic COM crystals. Thus, the molecular scale growth morphology and the bulk crystal habit in the presence of citrate are similar, and the predictions of molecular simulations are fully consistent with the experimental observations.

  6. Ionic strength and ion ratio effects on the single crystal growth of calcium oxalate monohydrate

    SciTech Connect

    DeLong, J.D.; Briedis, D.M.

    1987-01-01

    Single crystal growth rates of calcium oxalate monohydrate, CaC/sub 2/O/sub 4/ . H/sub 2/O, were measured as a function of ionic strength and of calcium to oxalate free ion ratio. The photomicroscopic technique was used which allowed measurement of the growth rates of individual faces of single crystals. The amounts of reagents required to maintain a constant relative supersaturation of 3.7 for all experiments were determined using an iterative computer algorithm which allowed the use of various background electrolytes, ionic strength, and free ion ratios. For a range of ionic strengths of I = .0024 to 0.5 for each of the background electrolytes KCl, LiCl, and KClO/sub 4/, and a free ion ratio (Ca/sup 2+/)/(C/sub 2/O/sub 4//sup 2-/) = 1, facial growth rate showed a steady increase with ionic strength towards an asymptotic maximum. The curves of growth rate, R, versus ionic strength followed approximately the form R = k I/sup n/ with 0 < n < 1, suggesting a mechanism of growth enhancement with increasing ionic strength by compression of the electrical double layer at the crystal/solution interface. For a range of free ion ratios (Ca/sup 2+/)/(C/sub 2/O/sub 4//sup 2-/) = 0.01 to 100 and an ionic strength of I = 0.15 M, the observed growth rate showed a maximum at equimolar free ion conditions, with decreasing growth rates observed at lower and higher ion ratios. This growth rate maximum was not apparent under conditions with no added background electrolyte. These results indicate that relative supersaturation as usually used for crystal growth may not be the complete or appropriate driving force for describing electrolyte crystal growth.

  7. Charge density in pyroelectric lithium sulfate monohydrate at 80 and 298 K

    SciTech Connect

    Karppinen, M.; Liminga, R.; Lundgren, J.; Kvick, A.; Abrahams, S.C.

    1986-11-01

    Lithium sulfate monohydrate has been studied at 80 and 298 K by x-ray diffraction. The monoclinic crystal with space group P2/sub 1/ has lattice dimensions at 298 K of a -- 5.4553(1), b -- 4.8690(1), c -- 8.1761(2) A, and ..beta.. -- 107.337(2)/sup 0/; lattice dimensions at 80 K were reported in our neutron study (J. Chem. Phys. 80, 423 (1984)). Least-squares refinement based on 3486 (80 K) and 3390 (298 K) independent reflections, assuming a spherical atom model, results in final R( F /sup 2/) values of 0.024 (80 K) and 0.026 (298 K). Static deformation and charge density model refinement, based on Hirshfeld-type multipole functions, greatly reduces the residual electron density and gives R( F /sup 2/) values of 0.017 (80 K) and 0.016 (298 K). Refinement of the resulting multipole parameters within the Gaussian radial dependence model allows a qualitative estimation of the differences in electron densities between 80 and 298 K. A change of about 0.2 e A/sup -3/ in the deformation density of the O-H bonds in the water molecule over this temperature range is related to the contraction in hydrogen bonding at 80 K. Changes in the sulfate oxygen atom lone-pair deformation densities, caused by contractions in the SO/sup 2-//sub 4/-Li/sup +/ contacts between 298 and 80 K, are also found between the two temperatures. X-ray-neutron diffraction deformation density calculations indicate a substantial electron deficiency in the sulfur valence shell. Kappa refinement leads to a point charge model with positive atomic charge close to 1.8 on sulfur, about -1.0 on each sulfate oxygen atom, and -0.8 on the water oxygen atom.

  8. Crystal structure of magnesium copper(II) bis-[orthophosphate(V)] monohydrate.

    PubMed

    Khmiyas, Jamal; Assani, Abderrazzak; Saadi, Mohamed; El Ammari, Lahcen

    2015-01-01

    Single crystals of magnesium copper(II) bis-[orthophosphate(V)] monohydrate, Mg1.65Cu1.35(PO4)2H2O, were grown under hydro-thermal conditions. The crystal structure is formed by three types of cationic sites and by two unique (PO4)(3-) anions. One site is occupied by Cu(2+), the second site by Mg(2+)and the third site by a mixture of the two cations with an Mg(2+):Cu(2+) occupancy ratio of 0.657?(3):0.343?(3). The structure is built up from more or less distorted [MgO6] and [(Mg/Cu)O5(H2O)] octa-hedra, [CuO5] square-pyramids and regular PO4 tetra-hedra, leading to a framework structure. Within this framework, two types of layers parallel to (-101) can be distinguished. The first layer is formed by [Cu2O8] dimers linked to PO4 tetra-hedra via common edges. The second, more corrugated layer results from the linkage between [(Cu/Mg)2O8(H2O)2] dimers and [MgO6] octa-hedra by common edges. The PO4 units link the two types of layers, leaving space for channels parallel [101], into which the H atoms of the water mol-ecules protrude. The latter are involved in O-H?O hydrogen-bonding inter-actions (one bifurcated) with framework O atoms across the channels. PMID:25705450

  9. Crystal structure of magnesium copper(II) bis[orthophosphate(V)] monohydrate

    PubMed Central

    Khmiyas, Jamal; Assani, Abderrazzak; Saadi, Mohamed; El Ammari, Lahcen

    2015-01-01

    Single crystals of magnesium copper(II) bis[orthophosphate(V)] monohydrate, Mg1.65Cu1.35(PO4)2H2O, were grown under hydrothermal conditions. The crystal structure is formed by three types of cationic sites and by two unique (PO4)3? anions. One site is occupied by Cu2+, the second site by Mg2+and the third site by a mixture of the two cations with an Mg2+:Cu2+ occupancy ratio of 0.657?(3):0.343?(3). The structure is built up from more or less distorted [MgO6] and [(Mg/Cu)O5(H2O)] octahedra, [CuO5] square-pyramids and regular PO4 tetrahedra, leading to a framework structure. Within this framework, two types of layers parallel to (-101) can be distinguished. The first layer is formed by [Cu2O8] dimers linked to PO4 tetrahedra via common edges. The second, more corrugated layer results from the linkage between [(Cu/Mg)2O8(H2O)2] dimers and [MgO6] octahedra by common edges. The PO4 units link the two types of layers, leaving space for channels parallel [101], into which the H atoms of the water molecules protrude. The latter are involved in OH?O hydrogen-bonding interactions (one bifurcated) with framework O atoms across the channels. PMID:25705450

  10. Calcium oxalate monohydrate crystals internalized into renal tubular cells are degraded and dissolved by endolysosomes.

    PubMed

    Chaiyarit, Sakdithep; Singhto, Nilubon; Thongboonkerd, Visith

    2016-02-25

    Interaction between calcium oxalate crystals and renal tubular cells has been recognized as one of the key mechanisms for kidney stone formation. While crystal adhesion and internalization have been extensively investigated, subsequent phenomena (i.e. crystal degradation and dissolution) remained poorly understood. To explore these mechanisms, we used fluorescein isothiocyanate (FITC)-labelled calcium oxalate monohydrate (COM) crystals (1000 μg/ml of crystals/culture medium) to confirm crystal internalization into MDCK (Type II) renal tubular cells after exposure to the crystals for 1 h and to trace the internalized crystals. Crystal size, intracellular and extracellular fluorescence levels were measured using a spectrofluorometer for up to 48 h after crystal internalization. Moreover, markers for early endosome (Rab5), late endosome (Rab7) and lysosome (LAMP-2) were examined by laser-scanning confocal microscopy. Fluorescence imaging and flow cytometry confirmed that FITC-labelled COM crystals were internalized into MDCK cells (14.83 ± 0.85%). The data also revealed a reduction of crystal size in a time-dependent manner. In concordance, intracellular and extracellular fluorescence levels were decreased and increased, respectively, indicating crystal degradation/dissolution inside the cells and the degraded products were eliminated extracellularly. Moreover, Rab5 and Rab7 were both up-regulated and were also associated with the up-regulated LAMP-2 to form large endolysosomes in the COM-treated cells at 16-h after crystal internalization. We demonstrate herein, for the first time, that COM crystals could be degraded/dissolved by endolysosomes inside renal tubular cells. These findings will be helpful to better understand the crystal fate and protective mechanism against kidney stone formation. PMID:26748311

  11. Citric acid monohydrate as a release-modifying agent in melt extruded matrix tablets.

    PubMed

    Schilling, Sandra U; Bruce, Caroline D; Shah, Navnit H; Malick, A Waseem; McGinity, James W

    2008-09-01

    Incomplete drug release and particle size-dependent dissolution performance can compromise the quality of controlled release matrix systems. The objective of the current study was to investigate the ability of citric acid monohydrate (CA MH) to enhance the release of diltiazem hydrochloride from melt extruded Eudragit RS PO tablets and to eliminate drug particle size effects. Preformulation studies demonstrated the thermal stability of all components, drug insolubility in the polymer but miscibility with the CA MH. Tablets with either constant polymer levels or constant drug-to-polymer ratios and containing different drug particle size fractions and increasing amounts of CA MH were manufactured by melt extrusion and characterized by dissolution testing, powder X-ray diffraction and scanning electron microscopy. The addition of CA MH to the formulation promoted the thermal processibility and matrix integrity by plasticization of the polymer. The drug release from systems with constant drug-to-polymer ratio was significantly increased when CA MH was added as a result of enhanced pore formation. Particle size effects were eliminated when large amounts of CA MH were used due to the loss of drug crystallinity. Matrix tablets with CA MH furthermore showed a faster and more complete drug release compared to systems with drug only or alternative pore formers (sucrose, NaCl, or PEG 3350). The enhanced drug release was attributed to the amorphous character of the soluble components, improved drug dispersion in the plasticized polymer along with increased polymer permeability. In summary, CA MH promoted the miscibility between the drug and Eudragit RS PO during hot-melt extrusion, resulting in the extrusion of an amorphous system with improved dissolution characteristics. PMID:18582547

  12. Development of a 3D polymer reinforced calcium phosphate cement scaffold for cranial bone tissue engineering

    NASA Astrophysics Data System (ADS)

    Alge, Daniel L.

    The repair of critical-sized cranial bone defects represents an important clinical challenge. The limitations of autografts and alloplastic materials make a bone tissue engineering strategy desirable, but success depends on the development of an appropriate scaffold. Key scaffold properties include biocompatibility, osteoconductivity, sufficient strength to maintain its structure, and resorbability. Furthermore, amenability to rapid prototyping fabrication methods is desirable, as these approaches offer precise control over scaffold architecture and have the potential for customization. While calcium phosphate cements meet many of these criteria due to their composition and their injectability, which can be leveraged for scaffold fabrication via indirect casting, their mechanical properties are a major limitation. Thus, the overall goal of this work was to develop a 3D polymer reinforced calcium phosphate cement scaffold for use in cranial bone tissue engineering. Dicalcium phosphate dihydrate (DCPD) setting cements are of particular interest because of their excellent resorbability. We demonstrated for the first time that DCPD cement can be prepared from monocalcium phosphate monohydrate (MCPM)/hydroxyapatite (HA) mixtures. However, subsequent characterization revealed that MCPM/HA cements rapidly convert to HA during degradation, which is undesirable and led us to choose a more conventional formulation for scaffold fabrication. In addition, we developed a novel method for calcium phosphate cement reinforcement that is based on infiltrating a pre-set cement structure with a polymer, and then crosslinking the polymer in situ. Unlike prior methods of cement reinforcement, this method can be applied to the reinforcement of 3D scaffolds fabricated by indirect casting. Using our novel method, composites of poly(propylene fumarate) (PPF) reinforced DCPD were prepared and demonstrated as excellent candidate scaffold materials, as they had increased strength and ductility and were biocompatible in vitro. Furthermore, 3D PPF reinforced DCPD scaffolds had strengths comparable to trabecular bone. Based on these results, 3D PPF reinforced DCPD scaffolds were evaluated in vivo using a rabbit calvarial defect model. Although bone formation was not enhanced by the addition of mesenchymal stem cells, significant bone ingrowth from the surrounding tissue was observed. The results of this work provide a foundation for future research on 3D polymer reinforced calcium phosphate cement scaffolds.

  13. Synthesis, crystal growth and spectroscopic investigation of novel metal organic crystal: β-Alanine cadmium bromide monohydrate (β-ACBM)

    NASA Astrophysics Data System (ADS)

    Renugadevi, R.; Kesavasamy, R.

    2014-07-01

    β-Alanine cadmium bromide monohydrate (β-ACBM), a new metal organic crystal has been grown from aqueous solution by slow evaporation technique. The grown crystals have been subjected to single crystal X-ray diffraction analysis to determine the crystal structure. The β-ACBM crystallized in monoclinic system with space group P21/c. The presence of protons and carbons in the β-alanine cadmium bromide monohydrate was confirmed by 1H and 13C nuclear magnetic resonance spectral analysis. The mode of vibration of different molecular groups present in β-ACBM was identified by FT-IR spectral analysis. Transparency of crystals in UV-Vis-NIR region has also been studied. The thermal characteristics of as-grown crystals were analyzed using thermo gravimetric and differential thermal analyses. The magnetic property of the grown crystal was investigated using Vibrating Sample Magnetometer (VSM) at ambient temperature. The mechanical stability of β-ACBM was evaluated by Vickers microhardness measurement.

  14. Ab initio simulation of ammonia monohydrate (NH3ṡH2O) and ammonium hydroxide (NH4OH)

    NASA Astrophysics Data System (ADS)

    Fortes, A. D.; Brodholt, J. P.; Wood, I. G.; Vočadlo, L.; Jenkins, H. D. B.

    2001-10-01

    We report the results of the first pseudopotential plane-wave simulations of the static properties of ammonia monohydrate phase I (AMH I) and ammonium hydroxide. Our calculated fourth-order logarithmic equation of state, at zero pressure and temperature, has molar volume, V0=36.38(3) cm3 mol-1, bulk modulus, K0=9.59(9) GPa, and the first derivative of the bulk modulus with respect to pressure, K0'=5.73(21). Both this and the lattice parameters are in very good agreement with experimental values. The monohydrate transforms, via a solid-state proton transfer reaction, to ammonium hydroxide (NH4OH) at 5.0(4) GPa. The equation of state of ammonium hydroxide is, V0=31.82(5) cm3 mol-1, K0=14.78(62) GPa, K0'=2.69(48). We calculate the reaction enthalpy, ΔH(NH4OH,s→NH3ṡH2O,s)=-14.8(5) kJ mol-1 at absolute zero, and thus estimate the enthalpy of formation, ΔfH⊖(NH4OH,s)=-356 kJ mol-1 at 298 K. This result places an upper limit of 84 kJ mol-1 on the barrier to rotation of the ammonium cation, and yields an average hydrogen bond enthalpy of ˜23 kJ mol-1.

  15. The influence of dietary protein on market barrows and gilts supplemented creatine monohydrate in conjunction with a high glycemic carbohydrate.

    PubMed

    Berg, E P; Stahl, C A; Shannon, M S; McNamara-Perry, D L; Schmidt, T B; Wiegand, B R

    2011-07-01

    The objective of the study was to determine if additional dietary protein improves the lean tissue deposition and carcass merit of pigs supplemented creatine monohydrate in combination with a high glycemic carbohydrate (dextrose). Forty-eight crossbred barrows and gilts (91±0.18 kg) were blocked by sex assigned to 1 of 12 pens (4 pigs/pen, 16 pigs/treatment). Treatments included: control (CON; basal diet consisting of a ground corn-soybean base), combination diet (COMBO; basal diet supplemented with 0.92% creatine monohydrate and 2.75% dextrose), and a combination high protein diet (COMBOHP; COMBO formulated to contain a minimum of 16% crude protein). Barrows on the COMBOHP gained the least 10th rib fat and expressed the highest percentage fat-free carcass lean (P<0.01) after 28 days on test. No significant treatment differences were noted in the fat and lean tissue accretion of gilts. Treatments had no affect the meat quality parameters of barrow and gilt carcasses. PMID:21333458

  16. Synthesis and non linear optical properties of new inorganic-organic hybrid material: 4-Benzylpiperidinium sulfate monohydrate

    NASA Astrophysics Data System (ADS)

    Kessentini, Yassmin; Ahmed, Ali Ben; Al-Juaid, Salih S.; Mhiri, Tahar; Elaoud, Zakaria

    2016-03-01

    Single crystals of 4-benzyl-piperidine sulfate monohydrate were grown by slow evaporation method at room temperature. The synthesized compound was characterized by means of single-crystal X-ray diffraction, FT-IR and Raman spectroscopy, UV-visible and photoluminescence studies. The title compound crystallises at room temperature in the non centrosymmetric space group P212121.The recorded UV-visible spectrum show good transparency in the visible region and indicates a non-zero value of the first Hyperpolarizability. Photoluminescence spectrum shows a broad and intense band at 440 nm and indicates that the crystal emits blue fluorescence. We also report DFT calculations of the electric dipole moments (μ), Polarizability (α), the static first Hyperpolarizability (β) and HOMO-LUMO analysis of the title compound was theoretically investigated by GAUSSIAN 03 package. The calculated static first Hyperpolarizability is equal to 6.4022 × 10-31 esu. The results show that 4-benzyl-piperidine sulfate monohydrate crystal might have important non linear optical behavior and can be a potential non linear optical material of interest.

  17. Synthesis, crystal growth and spectroscopic investigation of novel metal organic crystal: β-alanine cadmium bromide monohydrate (β-ACBM).

    PubMed

    Renugadevi, R; Kesavasamy, R

    2014-07-15

    β-Alanine cadmium bromide monohydrate (β-ACBM), a new metal organic crystal has been grown from aqueous solution by slow evaporation technique. The grown crystals have been subjected to single crystal X-ray diffraction analysis to determine the crystal structure. The β-ACBM crystallized in monoclinic system with space group P2(1)/c. The presence of protons and carbons in the β-alanine cadmium bromide monohydrate was confirmed by (1)H and (13)C nuclear magnetic resonance spectral analysis. The mode of vibration of different molecular groups present in β-ACBM was identified by FT-IR spectral analysis. Transparency of crystals in UV-Vis-NIR region has also been studied. The thermal characteristics of as-grown crystals were analyzed using thermo gravimetric and differential thermal analyses. The magnetic property of the grown crystal was investigated using Vibrating Sample Magnetometer (VSM) at ambient temperature. The mechanical stability of β-ACBM was evaluated by Vickers microhardness measurement. PMID:24691377

  18. A water setting tetracalcium phosphate-dicalcium phosphate dihydrate cement.

    PubMed

    Burguera, E F; Guitián, F; Chow, L C

    2004-11-01

    The development of a calcium phosphate cement, comprising tetracalcium phosphate (TTCP) and dicalcium phosphate dihydrate (DCPD), that hardens in 14 min with water as the liquid or 6 min with a 0.25 mol/L sodium phosphate solution as the liquid, without using hydroxyapatite (HA) seeds as setting accelerator, is reported. It was postulated that reduction in porosity would increase cement strength. Thus, the effects of applied pressure during the initial stages of the cement setting reaction on cement strength and porosity were studied. The cement powder comprised an equimolar mixture of TTCP and DCPD (median particle sizes 17 and 1.7 microm, respectively). Compressive strengths (CS) of samples prepared with distilled water were 47.6 +/- 2.4 MPa, 50.7 +/- 4.2 MPa, and 52.9 +/- 4.7 MPa at applied pressures of 5 MPa, 15 MPa, and 25 MPa, respectively. When phosphate solution was used, the CS values obtained were 41.5 +/- 2.3 MPa, 37.9 +/- 1.7 MPa, and 38.1 +/- 2.3 MPa at the same pressure levels. Statistical analysis of the results showed that pressure produced an improvement in CS when water was used as liquid but not when the phosphate solution was used. Compared to previously reported TTCP-DCPD cements, the greater CS values and shorter setting times together with a simplified formulation should make the present TTCP-DCPD cement a useful material as a bone substitute for clinical applications. PMID:15386489

  19. ANALYSIS OF OH STRETCHING FREQUENCIES IN GLUCOSE AND GLUCOSE MONOHYDRATES CALCULATED BY DFT: ROTOMER AND WATER PLACEMENT EFFECTS ON THE CALCULATED SPECTRUM

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Infrared spectra were calculated for glucose molecules and glucose monohydrate complexes, based on geometry optimization at the B3LYP/6-311++G** level of theory. Alpha and Beta anomers were considered, with all possible combinations of hydroxymethyl rotamer (gg,gt, or tg) and hydroxyl orientation (...

  20. SOURCE ASSESSMENT: PHOSPHATE FERTILIZER INDUSTRY

    EPA Science Inventory

    The report describes a study of air emissions, water effluents, and solid residues resulting from the manufacture of phosphate fertilizers. It includes the production of wet process phosphoric acid, superphosphoric acid, normal superphosphate, triple superphosphate, and ammonium ...

  1. Chemoenzymatic synthesis of polyprenyl phosphates.

    PubMed

    Hartley, Meredith D; Larkin, Angelyn; Imperiali, Barbara

    2008-05-01

    Polyprenyl phosphates, including undecaprenyl phosphate and dolichyl phosphate, are essential intermediates in several important biochemical pathways including N-linked protein glycosylation in eukaryotes and prokaryotes and prokaryotic cell wall biosynthesis. Herein, we describe the evaluation of three potential undecaprenol kinases as agents for the chemoenzymatic synthesis of polyprenyl phosphates. Target enzymes were expressed in crude cell envelope fractions and quantified via the use of luminescent lanthanide-binding tags (LBTs). The Streptococcus mutans diacylglycerol kinase (DGK) was shown to be a very useful agent for polyprenol phosphorylation using ATP as the phosphoryl transfer agent. In addition, the S. mutans DGK can be coupled with two Campylobacter jejuni glycosyltransferases involved in N-linked glycosylation to efficiently biosynthesize the undecaprenyl pyrophosphate-linked disaccharide needed for studies of PglB, the C. jejuni oligosaccharyl transferase. PMID:18374576

  2. Chemoenzymatic synthesis of polyprenyl phosphates

    PubMed Central

    Hartley, Meredith D.; Larkin, Angelyn; Imperiali, Barbara

    2008-01-01

    Polyprenyl phosphates, including undecaprenyl phosphate and dolichyl phosphate, are essential intermediates in several important biochemical pathways including N-linked protein glycosylation in eukaryotes and prokaryotes and prokaryotic cell wall biosynthesis. Herein we describe the evaluation of three potential undecaprenol kinases as agents for the chemoenzymatic synthesis of polyprenyl phosphates. Target enzymes were expressed in crude cell envelope fractions and quantified via the use of luminescent lanthanide binding tags (LBTs). The Streptococcus mutans diacylglycerol kinase (DGK) was shown to be a very useful agent for polyprenol phosphorylation using ATP as the phosphoryl transfer agent. In addition, the S. mutans DGK can be coupled with two Campylobacter jejuni glycosyltransferases involved in N-linked glycosylation, to efficiently biosynthesize the undecaprenyl pyrophosphate-linked disaccharide needed for studies of PglB, the C. jejuni oligosaccharyl transferase. PMID:18374576

  3. Fiber reinforced calcium phosphate cement.

    PubMed

    dos Santos, L A; de Oliveira, L C; da Silva Rigo, E C; Carrodéguas, R G; Boschi, A O; Fonseca de Arruda, A C

    2000-03-01

    The term calcium phosphate cement was introduced by Gruninger et al. (1). This type of cement can be prepared by reacting a calcium phosphate salt with an aqueous solution, which causes it to set by the crossing of the precipitated crystals. These cements offer a series of advantages that allow their use as grafts and substitutes of damaged parts of the bone system. However, these cements have low mechanical strength compared to human bones. This work studied the influence of the use of polyamide fibers in the mechanical properties of a calcium phosphate cement based on alpha-tricalcium phosphate as well as the mechanisms involved in the increase of mechanical strength. The results demonstrate the feasibility of the use of polymeric fibers to increase mechanical strength and the need for coupling agents for the effective performance of the fibers as reinforcement in these materials. PMID:10759644

  4. Triaryl phosphate poisoning in cattle.

    PubMed

    Beck, B E; Wood, C D; Whenham, G R

    1977-03-01

    Clinical signs, pathologic changes and biochemical changes occurred in cattle with natural and experimental triaryl phosphate poisoning. Natural poisoning was caused by triaryl phosphates escaping from a gas pipeline compressor station. The clinical signs were posterior motor paralysis, dyspnea, diarrhea and agalactia. Experimental doses of 1/2-1 gm/kg body weight of these organophosphate compounds caused depression of cholinesterase and axonal degeneration in the spinal cord. PMID:857397

  5. Thermal oxidative degradation studies of phosphate esters.

    PubMed

    Paciorek, K J; Kratzer, R H; Kaufman, J; Nakahara, J H; Christos, T; Hartstein, A M

    1978-08-01

    Five phosphate esters - tri-p-tolyl phosphate, tributyl phosphate, tris(1,3-dichloro-2-propyl)phosphate, tris(2,3-dibromopropyl)phosphate, and tris(2-chloroethyl)phosphate- were subjected to thermal oxidative degradation in air at 370 degrees C. Degradation mechanisms were postulated and the toxic hazards assessed based on the volatiles produced. Tri-p-tolyl phosphate was found to undergo only minimal degradation; the other compounds were decomposed extensively. Butene was the main product formed on tributyl phosphate decomposition; hydrogen halides and halogenated C2- and C3- species were the main products formed by the halogenated phosphate ester. In the case of tris(1,3-dichloro-2-propyl)phosphate acrolein, not hydrogen chloride, presented the major toxic hazard. PMID:696625

  6. Responses to phosphate deprivation in yeast cells.

    PubMed

    Yadav, Kamlesh Kumar; Singh, Neelima; Rajasekharan, Ram

    2016-05-01

    Inorganic phosphate is an essential nutrient because it is required for the biosynthesis of nucleotides, phospholipids and metabolites in energy metabolism. During phosphate starvation, phosphatases play a major role in phosphate acquisition by hydrolyzing phosphorylated macromolecules. In Saccharomyces cerevisiae, PHM8 (YER037W), a lysophosphatidic acid phosphatase, plays an important role in phosphate acquisition by hydrolyzing lysophosphatidic acid and nucleotide monophosphate that results in accumulation of triacylglycerol and nucleotides under phosphate limiting conditions. Under phosphate limiting conditions, it is transcriptionally regulated by Pho4p, a phosphate-responsive transcription factor. In this review, we focus on triacylglycerol metabolism in transcription factors deletion mutants involved in phosphate metabolism and propose a link between phosphate and triacylglycerol metabolism. Deletion of these transcription factors results in an increase in triacylglycerol level. Based on these observations, we suggest that PHM8 is responsible for the increase in triacylglycerol in phosphate metabolising gene deletion mutants. PMID:26615590

  7. Inhibition of calcium oxalate monohydrate growth by citrate and the effect of the background electrolyte

    NASA Astrophysics Data System (ADS)

    Weaver, Matthew L.; Qiu, S. Roger; Hoyer, John R.; Casey, William H.; Nancollas, George H.; De Yoreo, James J.

    2007-08-01

    Pathological mineralization is a common phenomenon in broad range of plants and animals. In humans, kidney stone formation is a well-known example that afflicts approximately 10% of the population. Of the various calcium salt phases that comprise human kidney stones, the primary component is calcium oxalate monohydrate (COM). Citrate, a naturally occurring molecule in the urinary system and a common therapeutic agent for treating stone disease, is a known inhibitor of COM. Understanding the physical mechanisms of citrate inhibition requires quantification of the effects of both background electrolytes and citrate on COM step kinetics. Here we report the results of an in situ AFM study of these effects, in which we measure the effect of the electrolytes LiCl, NaCl, KCl, RbCl, and CsCl, and the dependence of step speed on citrate concentration for a range of COM supersaturations. We find that varying the background electrolyte results in significant differences in the measured step speeds and in step morphology, with KCl clearly producing the smallest impact and NaCl the largest. The kinetic coefficient for the former is nearly three times larger than for the latter, while the steps change from smooth to highly serrated when KCl is changed to NaCl. The results on the dependence of step speed on citrate concentration show that citrate produces a dead zone whose width increases with citrate concentration as well as a continual reduction in kinetic coefficient with increasing citrate level. We relate these results to a molecular-scale view of inhibition that invokes a combination of kink blocking and step pinning. Furthermore, we demonstrate that the classic step-pinning model of Cabrera and Vermilyea (C-V model) does an excellent job of predicting the effect of citrate on COM step kinetics provided the model is reformulated to more realistically account for impurity adsorption, include an expression for the Gibbs-Thomson effect that is correct for all supersaturations, and take into account a reduction in kinetic coefficient through kink blocking. The detailed derivation of this reformulated C-V model is presented and the underlying materials parameters that control its impact are examined. Despite the fact that the basic C-V model was proposed nearly 50 years ago and has seen extensive theoretical treatment, this study represents the first quantitative and molecular scale experimental confirmation for any crystal system.

  8. Bioavailability, food effect and tolerability of S-naproxen betainate sodium salt monohydrate in steady state.

    PubMed

    Marzo, A; Dal Bo, L; Wool, C; Cerutti, R

    1998-09-01

    S-Naproxen betainate sodium salt monohydrate (naproxen-beta Na, CAS 104124-26-7, Aprenin) in 550 mg capsules (corresponding to 327 mg of naproxen) was administered to 24 healthy volunteers (12 males and 12 females) b.i.d. to steady state in order to check its bioavailability, food interaction and tolerability. Plasma concentrations of naproxen were measured by a well validated HPLC method with fluorimetric detection as a morning pre-dose on days 1 to 6 and in timed samples in three different situations, as follows: a) after the morning dose on day 7 in a fasting status, b) after the evening dose and dinner on day 7 and c) after the morning dose of day 8, taken after a high-fat content breakfast. Pharmacokinetic parameters were evaluated from plasma concentrations by non-compartmental analysis to describe the above three situations. The steady state was reached early, namely by the second day of treatment. The extent of absorption did not differ in the three situations tested, whereas the rate of absorption was fastest in fasting conditions, lowest with the evening dose and intermediate after the high-fat content breakfast. The slow absorption rate of the evening dose was attributed to a circadian rhythm and should allow therapeutically active levels early in the morning, when arthritis pain is particularly tedious. In the three situations explored Cmax, Cmin and AUC were associated with CV % values ranging from 11.7 to 17.2%, which are very low and rare in pharmacokinetic trials. This low variability should allow an accurate estimate of the therapeutic effect expected. Tolerability was checked by objective and subjective symptoms, including vital signs, blood/urine biochemical parameters and occult blood in stools, and proved to be very good. From the comparison of these data with those previously published by other authors who have administered 500 mg of naproxen b.i.d., pre-dose concentrations in a steady state proved to be similar, despite the different doses administered, whereas Cmax and AUC obtained in this study were marginally lower. The kind of food interaction was the same as previously described in literature with naproxen. PMID:9793622

  9. Development of an instrument to measure adhesion of calcium oxalate monohydrate to surfaces

    NASA Astrophysics Data System (ADS)

    Habeger, Craig Fredrick

    Calcium oxalate monohydrate (COM) is the primary constituent in kidney stones. COM crystals were synthesized in the laboratory and characterized. Computer calculations of particle shape have been reconciled to observed shapes of COM crystals experimentally synthesized under various conditions. Comparison between the theoretical atomic structures generated by computer calculations are consistent with previously reported atomic layering sequences. Composite mixing rules were used to deconvolute the dielectric constant of COM from a COM/silicone composite. Utilizing the Lichtenecker dielectric mixing model, the value of the static dielectric constant of COM was determined to be 28.9. Optical and dielectric data were then used in the Tabor-Winterton relationship to calculate the Hamaker constant, Asb{131}, of COM particles interacting in water. The Asb{131} for COM as a function of crystallographic habit also was examined. The mean value of Asb{131} for COM was calculated to be 13.7 × 10sp{-21} J at 37sp°C in an aqueous environment. A hydrodynamic method for measuring the adhesion of particles to a surface has been designed for use in the study of kidney stone disease and other pathological biomineralization phenomena. The hydrodynamic force required to displace a particle adhering to a fused quartz substrate was calculated via the Poiseuille equation. The strength necessary to remove 50% of the COM particles adhering to the substrate on the (010) and (101) crystallographic surfaces are 81 and 170 Pa, respectively. The previously determined Hamaker constant and measured values of zeta potential were used to calculate the energy of interaction between a COM particle and the fused quartz substrate which was found to be comparable to experimentally measured values, provided the separation distance was on the order of 20 nm. Using the instrument and technique developed, the adhesion of COM to biologically and non-biologically relevant materials was measured in COM saturated solution and in an artificial urine ion solution. The biologically significant materials were the proteins collagen type I, fibronectin, and MATRIGELsp°ler a mixture of basement membrane proteins. The non-biologically relevant material was polyethyleneimine a positively charged macromolecule used as a control. MATRIGELsp°ler and the positive control, polyethyleneimine, exhibited the highest adhesion to COM crystals.

  10. Oligomeric proanthocyanidins protect against HK-2 cell injury induced by oxalate and calcium oxalate monohydrate crystals.

    PubMed

    Wang, Shuo; Du, Peng; Zhang, Ning; Liu, Jia; Tang, Xingxing; Zhao, Qiang; Yang, Yong

    2016-06-01

    The purpose of the study was to test whether the antioxidants oligomeric proanthocyanidins (OPCs) could provide protection against oxalate and calcium oxalate monohydrate crystals (COM) toxicity in HK-2 cells. Four groups were chosen for the study: negative control group, positive control group (COM + oxalate), OPCs group (OPCs + COM + oxalate), Vit E group (Vit E + COM + oxalate). HK-2 cells were exposed for 4, 8, 12 and 24 h. The activity of HK-2 cell was assessed by MTT. Cellular injury was assessed by activity of Na(+)/K(+) ATP enzyme. Peroxidation level was assessed by malondialdehyde (MDA) content in medium and activity of superoxide dismutase (SOD). Morphological changes of HK-2 cell after exposed for 4 and 12 h in each group were observed under Transmission electron microscope (TEM). The effects of OPCs and VitE on oxalate- and COM-exposed cells were tested. After exposed to oxalate and COM crystals, activity of cells, Na(+)/K(+) ATP enzyme and SOD enzyme showed a significant reduction, and MDA content in medium was significantly increased. OPCs group: the addition of OPCs significantly increased activity of cell, SOD and Na(+)/K(+) ATP enzyme while MDA content was significantly decreased compared with the positive control group. VitE group: compared with the positive control group, activity of HK-2 cell, Na(+)/K(+) ATP enzyme was not significantly changed while SOD activity was restored, and MDA content was significantly decreased after the addition of Vit E. Morphological structure of HK-2 cell was extremely changed as observed under TEM after exposure to high level of COM crystals and oxalate. After the addition of OPCs or Vit E, amounts of cells with vacuoles formed in cytoplasms, karyotheca dissolved and nucleolus disappeared were less than in positive control group. The morphological structure changing in OPCs group was slighter than that in Vit E group. OPCs and vitamin E administration may prevent oxalate- and COM-mediated peroxidative injury, restoring intracellular antioxidant enzyme activity. The protection rendered by OPCs was greater than that of vitamin E. PMID:26446157

  11. Biphasic calcium phosphate in periapical surgery

    PubMed Central

    Suneelkumar, Chinni; Datta, Krithika; Srinivasan, Manali R; Kumar, Sampath T

    2008-01-01

    Calcium phosphate ceramics like hydroxyapatite and β -tricalcium phosphate (β -TCP) possess mineral composition that closely resembles that of the bone. They can be good bone substitutes due to their excellent biocompatibility. Biphasic calcium phosphate is a bone substitute which is a mixture of hydroxyapatite and β -tricalcium phosphate in fixed ratios. Studies have demonstrated the osteoconductive potential of this composition. This paper highlights the clinical use of biphasic calcium phosphate as a bone substitute in periapical surgery. PMID:20142892

  12. Uranium phosphate biomineralization by fungi.

    PubMed

    Liang, Xinjin; Hillier, Stephen; Pendlowski, Helen; Gray, Nia; Ceci, Andrea; Gadd, Geoffrey Michael

    2015-06-01

    Geoactive soil fungi were investigated for phosphatase-mediated uranium precipitation during growth on an organic phosphorus source. Aspergillus niger and Paecilomyces javanicus were grown on modified Czapek-Dox medium amended with glycerol 2-phosphate (G2P) as sole P source and uranium nitrate. Both organisms showed reduced growth on uranium-containing media but were able to extensively precipitate uranium and phosphorus-containing minerals on hyphal surfaces, and these were identified by X-ray powder diffraction as uranyl phosphate species, including potassium uranyl phosphate hydrate (KPUO6 .3H2 O), meta-ankoleite [(K1.7 Ba0.2 )(UO2 )2 (PO4 )2 .6H2 O], uranyl phosphate hydrate [(UO2 )3 (PO4 )2 .4H2 O], meta-ankoleite (K(UO2 )(PO4 ).3H2 O), uramphite (NH4 UO2 PO4 .3H2 O) and chernikovite [(H3 O)2 (UO2 )2 (PO4 )2 .6H2 O]. Some minerals with a morphology similar to bacterial hydrogen uranyl phosphate were detected on A. niger biomass. Geochemical modelling confirmed the complexity of uranium speciation, and the presence of meta-ankoleite, uramphite and uranyl phosphate hydrate between pH 3 and 8 closely matched the experimental data, with potassium as the dominant cation. We have therefore demonstrated that fungi can precipitate U-containing phosphate biominerals when grown with an organic source of P, with the hyphal matrix serving to localize the resultant uranium minerals. The findings throw further light on potential fungal roles in U and P biogeochemistry as well as the application of these mechanisms for element recovery or bioremediation. PMID:25580878

  13. Monodentate coordination by a tripodal ligand system: synthesis and crystal and molecular structure of bis(diisopropyl (1,2-bis(diethylcarbamoyl)ethyl)phosphonate)erbium(III) nitrate monohydrate

    SciTech Connect

    McCabe, D.J.; Duesler, E.N.; Paine, R.T.

    1985-12-18

    Bis(diisopropyl(1,2-bis(diethylcarbamoyl)ethyl)phosphonate)erbium(III) nitrate monohydrate, Er(NO/sub 3/)/sub 3/(i-C/sub 3/H/sub 7/O)/sub 2/P(O)CH-(C(O)N(C/sub 2/H/sub 5/)/sub 2/)(CH/sub 2/C(O)N(C/sub 2/H/sub 5/)/sub 2/))/sub 2/.H/sub 2/O, has been prepared from the trifunctional phosphate ligand and Er(NO/sub 3/)/sub 3/.6H/sub 2/O in ethanol. The complex has been characterized by infrared and NMR spectroscopy and single-crystal X-ray diffraction analysis. The complex was found to crystallize in the monoclinic space group P2/sub 1//n with a = 13.438 (2) A, b = 22.022 (4) A, c = 19.596 (5) A, ..beta.. = 106.21 (2)/sup 0/, Z = 4, V = 5568 (2) A/sup 3/, and rho/sub calcd/ = 1.38 g cm/sup -3/. The structure was solved by heavy-atom techniques. The structure contains an Er(III) ion bonded to the oxygen atom of a water molecule, oxygen atoms of three bidentate nitrate ions, and the phosphoryl oxygen atoms of two of the potentially tripodal ligand (i-C/sub 3/H/sub 7/O)/sub 2/P(O)CH(C(O)N(C/sub 2/H/sub 5/)/sub 2/)(CH/sub 2/C(O)N(C/sub 2/H/sub 5/)/sub 2/). The overall erbium ion coordination number is 9. Two of the four carbonyl oxygen atoms are hydrogen bonded with the coordinated water molecule, while the remaining two carbonyl oxygen atoms, remain uncoordinated. 12 references, 1 figure, 2 tables.

  14. Uranium endowments in phosphate rock.

    PubMed

    Ulrich, Andrea E; Schnug, Ewald; Prasser, Horst-Michael; Frossard, Emmanuel

    2014-04-15

    This study seeks to identify and specify the components that make up the prospects of U recovery from phosphate rock. A systems approach is taken. The assessment includes i) reviewing past recovery experience and lessons learned; ii) identifying factors that determine recovery; and iii) establishing a contemporary evaluation of U endowments in phosphate rock reserves, as well as the available and recoverable amounts from phosphate rock and phosphoric acid production. We find that in the past, recovery did not fulfill its potential and that the breakup of the Soviet Union worsened then-favorable recovery market conditions in the 1990s. We find that an estimated 5.7 million tU may be recoverable from phosphate rock reserves. In 2010, the recoverable tU from phosphate rock and phosphoric acid production may have been 15,000 tU and 11,000 tU, respectively. This could have filled the world U supply-demand gap for nuclear energy production. The results suggest that the U.S., Morocco, Tunisia, and Russia would be particularly well-suited to recover U, taking infrastructural considerations into account. We demonstrate future research needs, as well as sustainability orientations. We conclude that in order to promote investment and production, it seems necessary to establish long-term contracts at guaranteed prices, ensuring profitability for phosphoric acid producers. PMID:24556272

  15. Crystal growth, structural characterization and theoretical investigation on 3,5-dinitrosalicylic acid monohydrate for nonlinear optical applications

    NASA Astrophysics Data System (ADS)

    Mathammal, R.; Sangeetha, K.; Prasad, L. Guru; Jayamani, V.

    2015-06-01

    Organic crystal of 3,5-dinitrosalicylic acid monohydrate has been grown by slow evaporation method at room temperature, using water as solvent. Quantum chemical calculations of energies, geometric structure and vibrational analysis of the title compound are carried out by DFT method with 6-31 + G (d, p) basis set. Both the experimental and theoretical spectra confirm the presence of functional groups. Electric dipole moment, polarizability and the first order hyperpolarizability values have been computed theoretically. The 1H and 13C nuclear magnetic resonance (NMR) chemical shifts of the molecule are calculated by the gauge independent atomic orbital (GIAO) method and compared with the experimental results. The calculated HOMO-LUMO energies confirm the charge transfer within the molecule. Thermodynamic properties (heat capacity, entropy and enthalpy) of the title compound are determined.

  16. Crystal growth and spectroscopic characterization of Aloevera amino acid added lithium sulfate monohydrate: a non-linear optical crystal.

    PubMed

    Manimekalai, R; Antony Joseph, A; Ramachandra Raja, C

    2014-03-25

    Non-linear optical crystals of lithium sulfate monohydrate added with Aloevera amino acid were grown successfully by slow evaporation technique moderately at low cost. Initially the Aloevera amino acid extract was prepared from the 3 years old plant leaves and the amino acids present in that were identified by high performance liquid chromatography. The grown crystal was clear, transparent and they attained the size about 1.3×0.8×0.6 cm(3) within a time span of 20-25 days. The crystal was subjected to Fourier Transform Infrared Spectroscopy, UV-Vis-NIR, thermal and mechanical studies. Proton nuclear magnetic resonance, thin layer chromatography and colorimetric estimation techniques are carried out to confirm and identify the amino acid in the grown crystal. PMID:24316535

  17. [Neuromuscular blocking and respiratory depressing actions of sodium ammonium dimethyl-2-(propano-1,3-dithiosulfate) monohydrate].

    PubMed

    Cao, B J; Chen, Z K; Chi, Z Q

    1990-05-01

    The neuromuscular blocking and respiratory depressing actions of the new insecticide sodium ammonium dimethyl-2-(propano-1,3-dithiosulfate) monohydrate (SCD) were investigated. In peroneal-tibialis anterior nerve-muscle preparations of urethane anesthetized rabbit, SCD 6.5 mg/kg iv completely depressed the indirectly elicited twitch tension but not the directly elicited one. This compound also caused initial potentiation of the indirectly elicited twitch tension. In the partially paralyzed preparations, potentiation of contractions occurred following a brief period of indirectly tetanic stimulation. Nereistoxin but not SCD blocked the indirectly elicited twitch tension of isolated rat diaphragm. The neuromuscular blockade induced by SCD and nereistoxin was antagonized by neostigmine and 4-aminopyridine. SCD and nereistoxin had little or no effect on arterial blood pressure and phrenic nerve discharge of rabbits. The results indicated that SCD-poisoned rabbits died of respiratory paralysis following the neuromuscular blockade. PMID:1965089

  18. Infrared and laser Raman studies of L-phenylalanine L-phenylalaninium perchlorate and bis(DL-phenylalaninium) sulphate monohydrate.

    PubMed

    Rajkumar, Beulah J M; Ramakrishnan, V

    2002-07-01

    Both crystals under study have two phenylalanine groups in the cationic part of the complex. In the L-phenylalanine L-phenylalaninium perchlorate crystal, two phenylalanine groups share one proton and become monoprotonated. In the bis(DL-phenylalaninium) sulphate monohydrate crystal, on the other hand, both the phenylalanine groups are protonated. This leads to several differences in the infrared and Raman spectra of these two crystals. The presence of both the carbonyl and the ionized carboxylic groups has been identified in the perchlorate crystal, while the sulphate crystal has only the carbonyl group. Extensive hydrogen bonding further leads to the shifting of bands due to several stretching and bending modes. It also reduces the Td symmetry of the anions to C2v symmetry causing the degeneracies of several modes to be removed. PMID:12164492

  19. Crystal growth, structural characterization and theoretical investigation on 3,5-dinitrosalicylic acid monohydrate for nonlinear optical applications.

    PubMed

    Mathammal, R; Sangeetha, K; Prasad, L Guru; Jayamani, V

    2015-06-01

    Organic crystal of 3,5-dinitrosalicylic acid monohydrate has been grown by slow evaporation method at room temperature, using water as solvent. Quantum chemical calculations of energies, geometric structure and vibrational analysis of the title compound are carried out by DFT method with 6-31+G (d,p) basis set. Both the experimental and theoretical spectra confirm the presence of functional groups. Electric dipole moment, polarizability and the first order hyperpolarizability values have been computed theoretically. The (1)H and (13)C nuclear magnetic resonance (NMR) chemical shifts of the molecule are calculated by the gauge independent atomic orbital (GIAO) method and compared with the experimental results. The calculated HOMO-LUMO energies confirm the charge transfer within the molecule. Thermodynamic properties (heat capacity, entropy and enthalpy) of the title compound are determined. PMID:25756688

  20. RETRACTED: Crystal growth and spectroscopic characterization of Aloevera amino acid added lithium sulfate monohydrate: A non-linear optical crystal

    NASA Astrophysics Data System (ADS)

    Manimekalai, R.; Antony Joseph, A.; Ramachandra Raja, C.

    2014-03-01

    This article has been retracted: please see Elsevier Policy on Article Withdrawal. This article has been retracted at the request of authors. According to the author we have reported Aloevera Amino Acid added Lithium sulphate monohydrate [AALSMH] crystal is a new nonlinear optical crystal. From the recorded high performance liquid chromatography spectrum, by matching the retention times with the known compounds, the amino acids present in our extract are identified as homocystine, isoleucine, serine, leucine and tyrosine. From the thin layer chromatography and colorimetric estimation techniques, presence of isoleucine was identified and it was also confirmed by NMR spectrum. From the above studies, we came to conclude that AALSMH is new nonlinear optical crystal. After further investigation, lattice parameter values of AALSMH are coinciding with lithium sulphate. Therefore we have decided to withdraw our paper. Sorry for the inconvenience and time spent.

  1. Detergent phosphate bans and eutrophication

    SciTech Connect

    Lee, G.F.; Jones, R.A.

    1986-04-01

    The Vollenweider-OECD eutrophication model has been expanded to approximately 400 lakes. It is possible to make a quantitative prediction of the effects of a detergent phosphate ban and thereby to ascertain the potential benefits of such a ban. In order to assess the effect of a detergent phosphate ban on water quality it is necessary to know the percentage of phosphorus in the domestic waste water that enters the water body, either directly or indirectly, and the percentage of the total phosphorus load that is derived from domestic wastewater. Although detergent phosphate bans generally will not result in an overall improvement to water quality, there may be some situations in which eutrophication-related water quality would be improved by a ban. 8 references, 1 figure, 1 table.

  2. Phosphate corrosion in high-pressure boilers

    SciTech Connect

    Herro, H.M.; Banweg, A.

    1995-12-01

    As operating pressures have increased, the frequency of corrosion-related failures in phosphate-treated boilers has also increased. Congruent phosphate control was derived to prevent the formation of free caustic by feeding orthophosphates to maintain a boiler water sodium-to-phosphate ratio at which theory surmised free caustic could not form. Unfortunately, conventional congruent control did not take into account the interaction of phosphate compounds with deposits and corrosion products, including iron oxides on boiler tube surfaces, and corrosion continued. Phosphate corrosion is the name given to attack involving phosphate compounds having unique wastage morphologies and associated corrosion products and deposits.

  3. Characterisation of 1,3-diammonium propylselenate monohydrate by XRD, FT-IR, FT-Raman, DSC and DFT studies

    NASA Astrophysics Data System (ADS)

    Thirunarayanan, S.; Arjunan, V.; Marchewka, M. K.; Mohan, S.; Atalay, Yusuf

    2016-03-01

    The crystals of 1,3-diammonium propylselenate monohydrate (DAPS) were prepared and characterised X-ray diffraction (XRD), FT-IR, FT-Raman spectroscopy, and DFT/B3LYP methods. It comprises protonated propyl ammonium moieties (diammonium propyl cations), selenate anions and water molecule which are held together by a number of hydrogen bonds and form infinite chains. The XRD data confirm the transfer of two protons from selenic acid to 1,3-diaminopropane molecule. The DAPS complex is stabilised by the presence of O-H···O and N-H···O hydrogen bonds and the electrostatic interactions as well. The N···O and O···O bond distances are 2.82-2.91 and 2.77 Å, respectively. The FT-IR and FT-Raman spectra of 1,3-diammonium propyl selenate monohydrate are recorded and the complete vibrational assignments have been discussed. The geometry is optimised by B3LYP method using 6-311G, 6-311+G and 6-311+G* basis sets and the energy, structural parameters, vibrational frequencies, IR and Raman intensities are determined. Differential scanning colorimetry (DSC) data were also presented to analyse the possibility of the phase transition. Complete natural bonding orbital (NBO) analysis is carried out to analyse the intramolecular electronic interactions and their stabilisation energies. The electrostatic potential of the complex lies in the range +1.902e × 10-2 to -1.902e × 10-2. The limits of total electron density of the complex is +8.43e × 10-2 to -8.43e × 10-2.

  4. Setting constraints on the nature and origin of the two major hydrous sulfates on Mars: Monohydrated and polyhydrated sulfates

    NASA Astrophysics Data System (ADS)

    Wang, Alian; Jolliff, Bradley L.; Liu, Yang; Connor, Kathryn

    2016-04-01

    Monohydrated Mg sulfate (MgSO4·H2O) and polyhydrated sulfate are the most common and abundant hydrous sulfates observed thus far on Mars. They are widely distributed and coexist in many locations. On the basis of results from two new sets of experiments, in combination with past experimental studies and the subsurface salt mineralogy observed at a saline playa (Dalangtan, DLT) in a terrestrial analogue hyperarid region on the Tibet Plateau, we can now set new constraints on the nature and origin of these two major Martian sulfates. Starkeyite (MgSO4·4H2O) is the best candidate for polyhydrated sulfate. MgSO4·H2O in the form of "LH-1w," generated from dehydration of Mg sulfates with high degrees of hydration, is the most likely mineral form for the majority of Martian monohydrated Mg sulfate. Two critical properties of Mg sulfates are responsible for the coexistence of these two phases that have very different degrees of hydration: (1) the metastability of a substructural unit in starkeyite at relatively low temperatures, and (2) catalytic effects attributed to coprecipitated species (sulfates, chlorides, oxides, and hydroxides) from chemically complex brines that help overcome the metastability of starkeyite. The combination of these two properties controls the coexistence of the LH-1w layer and starkeyite layers at many locations on Mars, which sometimes occur in an interbedded stratigraphy. The structural H2O held by these two broadly distributed sulfates represents a large H2O reservoir at the surface and in the shallow subsurface on current Mars.

  5. [Phosphate metabolism and iron deficiency].

    PubMed

    Yokoyama, Keitaro

    2016-02-01

    Autosomal dominant hypophosphatemic rickets(ADHR)is caused by gain-of-function mutations in FGF23 that prevent its proteolytic cleavage. Fibroblast growth factor 23(FGF23)is a hormone that inhibits renal phosphate reabsorption and 1,25-dihydroxyvitamin D biosynthesis. Low iron status plays a role in the pathophysiology of ADHR. Iron deficiency is an environmental trigger that stimulates FGF23 expression and hypophosphatemia in ADHR. It was reported that FGF23 elevation in patients with CKD, who are often iron deficient. In patients with nondialysis-dependent CKD, treatment with ferric citrate hydrate resulted in significant reductions in serum phosphate and FGF23. PMID:26813504

  6. The effects of pre versus post workout supplementation of creatine monohydrate on body composition and strength

    PubMed Central

    2013-01-01

    Background Chronic supplementation with creatine monohydrate has been shown to promote increases in total intramuscular creatine, phosphocreatine, skeletal muscle mass, lean body mass and muscle fiber size. Furthermore, there is robust evidence that muscular strength and power will also increase after supplementing with creatine. However, it is not known if the timing of creatine supplementation will affect the adaptive response to exercise. Thus, the purpose of this investigation was to determine the difference between pre versus post exercise supplementation of creatine on measures of body composition and strength. Methods Nineteen healthy recreational male bodybuilders (mean ± SD; age: 23.1 ± 2.9; height: 166.0 ± 23.2 cm; weight: 80.18 ± 10.43 kg) participated in this study. Subjects were randomly assigned to one of the following groups: PRE-SUPP or POST-SUPP workout supplementation of creatine (5 grams). The PRE-SUPP group consumed 5 grams of creatine immediately before exercise. On the other hand, the POST-SUPP group consumed 5 grams immediately after exercise. Subjects trained on average five days per week for four weeks. Subjects consumed the supplement on the two non-training days at their convenience. Subjects performed a periodized, split-routine, bodybuilding workout five days per week (Chest-shoulders-triceps; Back-biceps, Legs, etc.). Body composition (Bod Pod®) and 1-RM bench press (BP) were determined. Diet logs were collected and analyzed (one random day per week; four total days analyzed). Results 2x2 ANOVA results - There was a significant time effect for fat-free mass (FFM) (F = 19.9; p = 0.001) and BP (F = 18.9; p < 0.001), however, fat mass (FM) and body weight did not reach significance. While there were trends, no significant interactions were found. However, using magnitude-based inference, supplementation with creatine post workout is possibly more beneficial in comparison to pre workout supplementation with regards to FFM, FM and 1-RM BP. The mean change in the PRE-SUPP and POST-SUPP groups for body weight (BW kg), FFM (kg), FM (kg) and 1-RM bench press (kg) were as follows, respectively: Mean ± SD; BW: 0.4 ± 2.2 vs. 0.8 ± 0.9; FFM: 0.9 ± 1.8 vs. 2.0 ± 1.2; FM: -0.1 ± 2.0 vs. −1.2 ± 1.6; Bench Press 1-RM: 6.6 ± 8.2 vs. 7.6 ± 6.1. Qualitative inference represents the likelihood that the true value will have the observed magnitude. Furthermore, there were no differences in caloric or macronutrient intake between the groups. Conclusions Creatine supplementation plus resistance exercise increases fat-free mass and strength. Based on the magnitude inferences it appears that consuming creatine immediately post-workout is superior to pre-workout vis a vis body composition and strength. PMID:23919405

  7. Photorelease of phosphates: Mild methods for protecting phosphate derivatives

    PubMed Central

    Senadheera, Sanjeewa N; Yousef, Abraham L

    2014-01-01

    Summary We have developed a new photoremovable protecting group for caging phosphates in the near UV. Diethyl 2-(4-hydroxy-1-naphthyl)-2-oxoethyl phosphate (14a) quantitatively releases diethyl phosphate upon irradiation in aq MeOH or aq MeCN at 350 nm, with quantum efficiencies ranging from 0.021 to 0.067 depending on the solvent composition. The deprotection reactions originate from the triplet excited state, are robust under ambient conditions and can be carried on to 100% conversion. Similar results were found with diethyl 2-(4-methoxy-1-naphthyl)-2-oxoethyl phosphate (14b), although it was significantly less efficient compared with 14a. A key step in the deprotection reaction in aq MeOH is considered to be a Favorskii rearrangement of the naphthyl ketone motif of 14a,b to naphthylacetate esters 25 and 26. Disruption of the ketone-naphthyl ring conjugation significantly shifts the photoproduct absorption away from the effective incident wavelength for decaging of 14, driving the reaction to completion. The Favorskii rearrangement does not occur in aqueous acetonitrile although diethyl phosphate is released. Other substitution patterns on the naphthyl or quinolin-5-yl core, such as the 2,6-naphthyl 10 or 8-benzyloxyquinolin-5-yl 24 platforms, also do not rearrange by aryl migration upon photolysis and, therefore, do not proceed to completion. The 2,6-naphthyl ketone platform instead remains intact whereas the quinolin-5-yl ketone fragments to a much more complex, highly absorbing reaction mixture that competes for the incident light. PMID:25246963

  8. Phosphate corrosion in high pressure boilers

    SciTech Connect

    Herro, H.M.; Banweg, A.

    1995-12-01

    Phosphate treatments have been used in boilers for more than 70 years. As operating pressures increased, the frequency of corrosion-related failures in phosphate-treated boilers also increased. Many failures were attributed to ``free`` caustic generated by the nonstoichiometric precipitation of various phosphate compounds on boiler surfaces. Congruent control was devised to prevent the formation of free caustic by feeding orthophosphates so as to maintain a boiler water sodium to phosphate ratio in a range where theory surmised free caustic could not form. Unfortunately, conventional congruent control did not take into account the interaction of phosphate compounds with various deposits and corrosion products, including iron oxides on boiler tube surfaces. Corrosion continued to occur even when sodium to phosphate-pH control ranges were maintained according to theory. Phosphate corrosion is the name given to attack involving phosphate compounds having unique wastage morphologies, associated corrosion products and deposits.

  9. Long-Sought Vacuolar Phosphate Transporters Identified.

    PubMed

    Bucher, Marcel; Fabiańska, Izabela

    2016-06-01

    The vacuole is an important subcellular compartment that serves as main phosphate storage in plants among other functions. Three recent studies shed light on the underlying molecular mechanisms for vacuolar phosphate transport that had long remained unknown. PMID:27160805

  10. Contrasting Effects of Water on the Barriers to Decarboxylation of Two Oxalic Acid Monohydrates: A Combined Rotational Spectroscopic and Ab Initio Study.

    PubMed

    Schnitzler, Elijah G; Badran, Courtenay; Jäger, Wolfgang

    2016-04-01

    Using rotational spectroscopy, we have observed two isomers of the monohydrate of oxalic acid, the most abundant dicarboxylic acid in the atmosphere. In the lowest-energy isomer, water hydrogen-bonds to both carboxylic acid groups, and the barrier to decarboxylation decreases. In the second isomer, water bonds to only one carboxylic acid group, and the barrier increases. Though the lower barrier in the former is not unequivocal evidence that water acts as a photocatalyst, the higher barrier in the latter indicates that water acts as an inhibitor in this topology. Oxalic acid is unique among dicarboxylic acids: for the higher homologues calculated, the inhibiting topology of the monohydrate is lowest in energy and most abundant under atmospheric conditions. Consequently, oxalic acid is the only dicarboxylic acid for which single-water catalysis of overtone-induced decarboxylation in the atmosphere is plausible. PMID:26963633

  11. Chemical, modulus and cell attachment studies of reactive calcium phosphate filler-containing fast photo-curing, surface-degrading, polymeric bone adhesives.

    PubMed

    Abou Neel, E A; Palmer, G; Knowles, J C; Salih, V; Young, A M

    2010-07-01

    The initial structure, setting and degradation processes of a poly(lactide-co-propylene glycol-co-lactide) dimethacrylate adhesive filled with 50, 60 or 70 wt.% reactive calcium phosphates (monocalcium phosphate monohydrate (MCPM)/beta-tricalcium phosphate (beta-TCP)) have been assessed using nuclear magnetic resonance, Fourier transform infrared spectroscopy, Raman, X-ray powder diffraction and gravimetric studies. Filler incorporation reduced the rapid light-activated monomer polymerization rates slightly, but not the final levels. Upon immersion in water for 24h, the set composite mass and volume increased due to water sorption. This promoted initial soluble MCPM loss from the composite surfaces, but also its reaction and monetite precipitation within the specimen bulk. After 48 h, composite gravimetric and chemical studies were consistent with surface erosion of polymer with reacted/remaining filler. The filled formulations exhibited more rapid early water sorption and subsequent surface erosion than the unfilled polymer. Calcium and phosphate release profiles and solution pH measurements confirmed early loss of surface MCPM with protons from polymer degradation products. At later times, the slower release of monetite/beta-TCP buffered composite storage solutions at approximately 5 instead of 3.2 for the unfilled polymer. Incorporation of filler increased both the early and later time material modulus. At intermediate times this effect was lost, presumably as a result of enhanced water sorption. The early modulus values obtained fell within the range reported for cancellous bone. Despite surface degradation, initial human mesenchymal cell attachment to both composites and polymer could be comparable with a non-degrading positive Thermanox control. These studies indicate that the filled formulations may be good candidates for bone repair. Release of calcium and phosphate ions provides components essential for such repair. PMID:20085828

  12. Why nature really chose phosphate.

    PubMed

    Kamerlin, Shina C L; Sharma, Pankaz K; Prasad, Ram B; Warshel, Arieh

    2013-02-01

    Phosphoryl transfer plays key roles in signaling, energy transduction, protein synthesis, and maintaining the integrity of the genetic material. On the surface, it would appear to be a simple nucleophile displacement reaction. However, this simplicity is deceptive, as, even in aqueous solution, the low-lying d-orbitals on the phosphorus atom allow for eight distinct mechanistic possibilities, before even introducing the complexities of the enzyme catalyzed reactions. To further complicate matters, while powerful, traditional experimental techniques such as the use of linear free-energy relationships (LFER) or measuring isotope effects cannot make unique distinctions between different potential mechanisms. A quarter of a century has passed since Westheimer wrote his seminal review, 'Why Nature Chose Phosphate' (Science 235 (1987), 1173), and a lot has changed in the field since then. The present review revisits this biologically crucial issue, exploring both relevant enzymatic systems as well as the corresponding chemistry in aqueous solution, and demonstrating that the only way key questions in this field are likely to be resolved is through careful theoretical studies (which of course should be able to reproduce all relevant experimental data). Finally, we demonstrate that the reason that nature really chose phosphate is due to interplay between two counteracting effects: on the one hand, phosphates are negatively charged and the resulting charge-charge repulsion with the attacking nucleophile contributes to the very high barrier for hydrolysis, making phosphate esters among the most inert compounds known. However, biology is not only about reducing the barrier to unfavorable chemical reactions. That is, the same charge-charge repulsion that makes phosphate ester hydrolysis so unfavorable also makes it possible to regulate, by exploiting the electrostatics. This means that phosphate ester hydrolysis can not only be turned on, but also be turned off, by fine tuning the electrostatic environment and the present review demonstrates numerous examples where this is the case. Without this capacity for regulation, it would be impossible to have for instance a signaling or metabolic cascade, where the action of each participant is determined by the fine-tuned activity of the previous piece in the production line. This makes phosphate esters the ideal compounds to facilitate life as we know it. PMID:23318152

  13. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Ferric phosphate. 184.1301 Section 184.1301 Food... Specific Substances Affirmed as GRAS § 184.1301 Ferric phosphate. (a) Ferric phosphate (ferric orthophosphate, iron (III) phosphate, FePO4·xH2O, CAS Reg. No. 10045-86-0) is an odorless, yellowish-white...

  14. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Ferric phosphate. 184.1301 Section 184.1301 Food... Specific Substances Affirmed as GRAS § 184.1301 Ferric phosphate. (a) Ferric phosphate (ferric orthophosphate, iron (III) phosphate, FePO4·xH2O, CAS Reg. No. 10045-86-0) is an odorless, yellowish-white...

  15. Isolated monohydrates of a model peptide chain: effect of a first water molecule on the secondary structure of a capped phenylalanine.

    PubMed

    Biswal, Himansu S; Loquais, Yohan; Tardivel, Benjamin; Gloaguen, Eric; Mons, Michel

    2011-03-23

    The formation of monohydrates of capped phenylalanine model peptides, CH(3)-CO-Phe-NH(2) and CH(3)-CO-Phe-NH-CH(3), in a supersonic expansion has been investigated using laser spectroscopy and quantum chemistry methods. Conformational distributions of the monohydrates have been revealed by IR/UV double-resonance spectroscopy and their structures assigned by comparison with DFT-D calculations. A careful analysis of the final hydrate distribution together with a detailed theoretical investigation of the potential energy surface of the monohydrates demonstrates that solvation occurs from the conformational distribution of the isolated peptide monomers. The distribution of the monohydrates appears to be strongly dependent on both the initial monomer conformation (extended or folded backbone) and the solvation site initially occupied by the water molecule. The solvation processes taking place during the cooling can be categorized as follows: (a) solvation without significant structural changes of the peptide, (b) solvation inducing significant distortions of the backbone but retaining the secondary structure, and (c) solvation triggering backbone isomerizations, leading to a modification of the peptide secondary structure. It is observed that solvation by a single water molecule can fold a β-strand into a γ-turn structure (type c) or induce a significant opening of a γ-turn characterized by an elongated C(7) hydrogen bond (type b). These structural changes can be considered as a first step toward the polyproline II condensed-phase structure, illustrating the role played by the very first water molecule in the solvation process. PMID:21361380

  16. Sintering of calcium phosphate bioceramics.

    PubMed

    Champion, E

    2013-04-01

    Calcium phosphate ceramics have become of prime importance for biological applications in the field of bone tissue engineering. This paper reviews the sintering behaviour of these bioceramics. Conventional pressureless sintering of hydroxyapatite, Ca10(PO4)6(OH)2, a reference compound, has been extensively studied. Its physico-chemistry is detailed. It can be seen as a competition between two thermally activated phenomena that proceed by solid-state diffusion of matter: densification and grain growth. Usually, the objective is to promote the first and prevent the second. Literature data are analysed from sintering maps (i.e. grain growth vs. densification). Sintering trajectories of hydroxyapatite produced by conventional pressureless sintering and non-conventional techniques, including two-step sintering, liquid phase sintering, hot pressing, hot isostatic pressing, ultrahigh pressure, microwave and spark plasma sintering, are presented. Whatever the sintering technique may be, grain growth occurs mainly during the last step of sintering, when the relative bulk density reaches 95% of the maximum value. Though often considered very advantageous, most assisted sintering techniques do not appear very superior to conventional pressureless sintering. Sintering of tricalcium phosphate or biphasic calcium phosphates is also discussed. The chemical composition of calcium phosphate influences the behaviour. Similarly, ionic substitutions in hydroxyapatite or in tricalcium phosphate create lattice defects that modify the sintering rate. Depending on their nature, they can either accelerate or slow down the sintering rate. The thermal stability of compounds at the sintering temperature must also be taken into account. Controlled atmospheres may be required to prevent thermal decomposition, and flash sintering techniques, which allow consolidation at low temperature, can be helpful. PMID:23212081

  17. Phosphate based oil well cements

    NASA Astrophysics Data System (ADS)

    Natarajan, Ramkumar

    The main application of the cement in an oil well is to stabilize the steel casing in the borehole and protect it from corrosion. The cement is pumped through the borehole and is pushed upwards through the annulus between the casing and the formation. The cement will be exposed to temperature and pressure gradients of the borehole. Modified Portland cement that is being used presently has several shortcomings for borehole sealant. The setting of the Portland cement in permafrost regions is poor because the water in it will freeze even before the cement sets and because of high porosity and calcium oxide, a major ingredient it gets easily affected by the down hole gases such as carbon dioxide. The concept of phosphate bonded cements was born out of considerable work at Argonne National Laboratory (ANL) on their use in stabilization of radioactive and hazardous wastes. Novel cements were synthesized by an acid base reaction between a metal oxide and acid phosphate solution. The major objective of this research is to develop phosphate based oil well cements. We have used thermodynamics along with solution chemistry principles to select calcined magnesium oxide as candidate metal oxide for temperatures up to 200°F (93.3°C) and alumina for temperatures greater than 200°F (93.3°C). Solution chemistry helped us in selecting mono potassium phosphate as the acid component for temperatures less than 200°F (93.3°C) and phosphoric acid solution greater than 200°F (93.3°C). These phosphate cements have performance superior to common Portland well cements in providing suitable thickening time, better mechanical and physical properties.

  18. 21 CFR 582.1217 - Calcium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Calcium phosphate. 582.1217 Section 582.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  19. 21 CFR 582.5217 - Calcium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Calcium phosphate. 582.5217 Section 582.5217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  20. 21 CFR 582.1217 - Calcium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Calcium phosphate. 582.1217 Section 582.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  1. 21 CFR 582.5217 - Calcium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Calcium phosphate. 582.5217 Section 582.5217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  2. 21 CFR 182.8217 - Calcium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Calcium phosphate. 182.8217 Section 182.8217 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  3. 21 CFR 182.8217 - Calcium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Calcium phosphate. 182.8217 Section 182.8217 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  4. 21 CFR 582.5217 - Calcium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Calcium phosphate. 582.5217 Section 582.5217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  5. 21 CFR 582.1217 - Calcium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Calcium phosphate. 582.1217 Section 582.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  6. 21 CFR 182.8217 - Calcium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Calcium phosphate. 182.8217 Section 182.8217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8217 Calcium phosphate. (a) Product. Calcium phosphate...

  7. 21 CFR 182.6778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Sodium phosphate. 182.6778 Section 182.6778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  8. 21 CFR 182.8778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Sodium phosphate. 182.8778 Section 182.8778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  9. 21 CFR 582.6778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium phosphate. 582.6778 Section 582.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use....

  10. 21 CFR 182.1778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Sodium phosphate. 182.1778 Section 182.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  11. 21 CFR 582.1778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Sodium phosphate. 582.1778 Section 582.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  12. 21 CFR 182.8778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Sodium phosphate. 182.8778 Section 182.8778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  13. 21 CFR 582.6778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Sodium phosphate. 582.6778 Section 582.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use....

  14. 21 CFR 582.5778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium phosphate. 582.5778 Section 582.5778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  15. 21 CFR 182.6778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Sodium phosphate. 182.6778 Section 182.6778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  16. 21 CFR 582.1778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Sodium phosphate. 582.1778 Section 582.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  17. 21 CFR 582.5778 - Sodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Sodium phosphate. 582.5778 Section 582.5778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  18. 21 CFR 182.1778 - Sodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Sodium phosphate. 182.1778 Section 182.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  19. 21 CFR 582.5217 - Calcium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Calcium phosphate. 582.5217 Section 582.5217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  20. 21 CFR 182.8217 - Calcium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Calcium phosphate. 182.8217 Section 182.8217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  1. 21 CFR 182.6290 - Disodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Disodium phosphate. 182.6290 Section 182.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is generally recognized...

  2. 21 CFR 182.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Dipotassium phosphate. 182.6285 Section 182.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  3. 21 CFR 582.6290 - Disodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Disodium phosphate. 582.6290 Section 582.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Disodium phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is...

  4. 21 CFR 182.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Dipotassium phosphate. 182.6285 Section 182.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  5. 21 CFR 582.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Dipotassium phosphate. 582.6285 Section 582.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  6. 21 CFR 582.5301 - Ferric phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ferric phosphate. 582.5301 Section 582.5301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5301 Ferric phosphate. (a) Product. Ferric phosphate. (b) Conditions of use....

  7. 21 CFR 582.5217 - Calcium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Calcium phosphate. 582.5217 Section 582.5217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  8. 21 CFR 182.1217 - Calcium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Calcium phosphate. 182.1217 Section 182.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  9. 21 CFR 182.1217 - Calcium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Calcium phosphate. 182.1217 Section 182.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic)....

  10. 21 CFR 182.6290 - Disodium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Disodium phosphate. 182.6290 Section 182.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is generally recognized...

  11. 21 CFR 182.8217 - Calcium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Calcium phosphate. 182.8217 Section 182.8217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  12. 21 CFR 582.6290 - Disodium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Disodium phosphate. 582.6290 Section 582.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Disodium phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is...

  13. 21 CFR 582.5301 - Ferric phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ferric phosphate. 582.5301 Section 582.5301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5301 Ferric phosphate. (a) Product. Ferric phosphate. (b) Conditions of use....

  14. 21 CFR 582.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Dipotassium phosphate. 582.6285 Section 582.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  15. 40 CFR 721.5995 - Polyalkyl phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Polyalkyl phosphate. 721.5995 Section... Substances § 721.5995 Polyalkyl phosphate. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified generically as a polyalkyl phosphate (PMN P-95-1772)...

  16. 21 CFR 582.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Dipotassium phosphate. 582.6285 Section 582.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  17. 21 CFR 582.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Dipotassium phosphate. 582.6285 Section 582.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  18. 21 CFR 582.6290 - Disodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Disodium phosphate. 582.6290 Section 582.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Disodium phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is...

  19. 21 CFR 182.6290 - Disodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Disodium phosphate. 182.6290 Section 182.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is generally recognized...

  20. 21 CFR 582.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Dipotassium phosphate. 582.6285 Section 582.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  1. 21 CFR 182.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Dipotassium phosphate. 182.6285 Section 182.6285...) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6285 Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is generally recognized as safe when used...

  2. 21 CFR 182.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Dipotassium phosphate. 182.6285 Section 182.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  3. 21 CFR 182.6285 - Dipotassium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Dipotassium phosphate. 182.6285 Section 182.6285 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD... Dipotassium phosphate. (a) Product. Dipotassium phosphate. (b) Conditions of use. This substance is...

  4. 21 CFR 582.5301 - Ferric phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ferric phosphate. 582.5301 Section 582.5301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5301 Ferric phosphate. (a) Product. Ferric phosphate. (b) Conditions of use....

  5. 21 CFR 582.5301 - Ferric phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ferric phosphate. 582.5301 Section 582.5301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5301 Ferric phosphate. (a) Product. Ferric phosphate. (b) Conditions of use....

  6. 21 CFR 582.1141 - Ammonium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ammonium phosphate. 582.1141 Section 582.1141 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1141 Ammonium phosphate. (a) Product. Ammonium phosphate (mono- and dibasic). (b)...

  7. 21 CFR 582.6290 - Disodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Disodium phosphate. 582.6290 Section 582.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Disodium phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is...

  8. 21 CFR 582.6290 - Disodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Disodium phosphate. 582.6290 Section 582.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Disodium phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is...

  9. 21 CFR 582.5301 - Ferric phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Ferric phosphate. 582.5301 Section 582.5301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5301 Ferric phosphate. (a) Product. Ferric phosphate. (b) Conditions of use....

  10. 21 CFR 182.6290 - Disodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Disodium phosphate. 182.6290 Section 182.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... phosphate. (a) Product. Disodium phosphate. (b) Conditions of use. This substance is generally recognized...

  11. 21 CFR 182.1778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Sodium phosphate. 182.1778 Section 182.1778 Food... GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This substance is...

  12. 21 CFR 182.6778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Sodium phosphate. 182.6778 Section 182.6778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  13. 21 CFR 182.1778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Sodium phosphate. 182.1778 Section 182.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  14. 21 CFR 582.1778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Sodium phosphate. 582.1778 Section 582.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  15. 21 CFR 582.1778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Sodium phosphate. 582.1778 Section 582.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  16. 21 CFR 582.6778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Sodium phosphate. 582.6778 Section 582.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use....

  17. 21 CFR 582.5778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Sodium phosphate. 582.5778 Section 582.5778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  18. 21 CFR 582.5778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Sodium phosphate. 582.5778 Section 582.5778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  19. 21 CFR 582.5778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Sodium phosphate. 582.5778 Section 582.5778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  20. 21 CFR 182.8778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Sodium phosphate. 182.8778 Section 182.8778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  1. 21 CFR 582.6778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Sodium phosphate. 582.6778 Section 582.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use....

  2. 21 CFR 182.8778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Sodium phosphate. 182.8778 Section 182.8778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8778 Sodium phosphate. (a) Product. Sodium phosphate (mono-,...

  3. 21 CFR 182.8778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Sodium phosphate. 182.8778 Section 182.8778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients § 182.8778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  4. 21 CFR 182.1778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Sodium phosphate. 182.1778 Section 182.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Substances § 182.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  5. 21 CFR 182.6778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Sodium phosphate. 182.6778 Section 182.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6778 Sodium phosphate. (a) Product. Sodium phosphate...

  6. 21 CFR 582.6778 - Sodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Sodium phosphate. 582.6778 Section 582.6778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use....

  7. 21 CFR 182.6778 - Sodium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Sodium phosphate. 182.6778 Section 182.6778 Food... HUMAN CONSUMPTION (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This...

  8. 21 CFR 582.1778 - Sodium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Sodium phosphate. 582.1778 Section 582.1778 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Additives § 582.1778 Sodium phosphate. (a) Product. Sodium phosphate (mono-, di-, and tribasic)....

  9. 21 CFR 582.5434 - Magnesium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Magnesium phosphate. 582.5434 Section 582.5434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5434 Magnesium phosphate. (a) Product. Magnesium phosphate (di- and tribasic)....

  10. 21 CFR 582.5434 - Magnesium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Magnesium phosphate. 582.5434 Section 582.5434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5434 Magnesium phosphate. (a) Product. Magnesium phosphate (di- and tribasic)....

  11. 21 CFR 582.5434 - Magnesium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Magnesium phosphate. 582.5434 Section 582.5434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5434 Magnesium phosphate. (a) Product. Magnesium phosphate (di- and tribasic)....

  12. 21 CFR 582.5434 - Magnesium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Magnesium phosphate. 582.5434 Section 582.5434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5434 Magnesium phosphate. (a) Product. Magnesium phosphate (di- and tribasic)....

  13. 21 CFR 582.5434 - Magnesium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Magnesium phosphate. 582.5434 Section 582.5434 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL... Supplements 1 § 582.5434 Magnesium phosphate. (a) Product. Magnesium phosphate (di- and tribasic)....

  14. Phosphatidylinositol 4-phosphate and phosphatidylinositol 3-phosphate regulate phagolysosome biogenesis.

    PubMed

    Jeschke, Andreas; Zehethofer, Nicole; Lindner, Buko; Krupp, Jessica; Schwudke, Dominik; Haneburger, Ina; Jovic, Marko; Backer, Jonathan M; Balla, Tamas; Hilbi, Hubert; Haas, Albert

    2015-04-14

    Professional phagocytic cells ingest microbial intruders by engulfing them into phagosomes, which subsequently mature into microbicidal phagolysosomes. Phagosome maturation requires sequential fusion of the phagosome with early endosomes, late endosomes, and lysosomes. Although various phosphoinositides (PIPs) have been detected on phagosomes, it remained unclear which PIPs actually govern phagosome maturation. Here, we analyzed the involvement of PIPs in fusion of phagosomes with various endocytic compartments and identified phosphatidylinositol 4-phosphate [PI(4)P], phosphatidylinositol 3-phosphate [PI(3)P], and the lipid kinases that generate these PIPs, as mediators of phagosome-lysosome fusion. Phagosome-early endosome fusion required PI(3)P, yet did not depend on PI(4)P. Thus, PI(3)P regulates phagosome maturation at early and late stages, whereas PI(4)P is selectively required late in the pathway. PMID:25825728

  15. Nucleation reduction strategy of BaNH{4}MgHPO{4} (barium ammonium magnesium hydrogen phosphate, in vitro approach-1) crystals grown in silica gel medium and its characterization studies

    NASA Astrophysics Data System (ADS)

    Suresh, P.; Kanchana, G.; Sundaramoorthi, P.

    2009-02-01

    Kidney stones consist of various organic, inorganic and semi-organic compounds. Mineral oxalate monohydrate and di-hydrate is the main inorganic constituent of kidney stones. However, the mechanisms for the formation of crystal mineral oxalate are not clearly understood. In this field of study there are many hypothesis including nucleation, crystal growth and or aggregation of formation of AOMH (ammonium oxalate monohydrate) and AODH (ammonium oxalate di-hydrate) crystals. The effect of some urinary species such as ammonium oxalates, calcium, citrate, proteins and trace mineral elements have been previously reported by the author. The kidney stone constituents are grown in the kidney environments, the sodium meta silica gel medium (SMS) provides the necessary growth simulation (in vitro). In the artificial urinary stone growth process, growth parameters within the different chemical environments are identified. The author has reported the growth of urinary crystals such as CHP, SHP, BHP and AHP. In the present study, BaNH{4}MgHPO{4} (barium ammonium magnesium hydrogen phosphate) crystals have been grown in three different growth faces to attain the total nucleation reductions. As an extension of this research, many characterization studies have been carried out and the results are reported.

  16. [Regulatory mechanism of circulating inorganic phosphate].

    PubMed

    Michigami, Toshimi

    2016-02-01

    Circulating level of phosphate is altered by age and diet, and is also controlled by several hormones such as parathyroid hormone(PTH), 1,25-dihydroxyvitamin D[1,25(OH)2D]and fibroblast growth factor 23(FGF23). The main function of PTH and 1,25(OH)2D is maintaining calcium homeostasis, while FGF23 plays a central role in phosphate metabolism. PTH suppresses phosphate reabsorption in the proximal tubules to increase the renal phosphate wasting, while 1,25(OH)2D facilitates the intestinal phosphate absorption. FGF23 increases the renal phosphate wasting and reduces the production of 1,25(OH)2D. Of note, these hormones mutually regulate one another. The production of FGF23 is also regulated by various local factors. The mechanism for sensing the phosphate availability still remains unknown, and further investigation is required. PMID:26813498

  17. The Biogeochemistry of Phosphate Mineral Dissolution

    NASA Astrophysics Data System (ADS)

    Buis, P. F.

    2002-12-01

    It has been found that different microorganisms dissolve phosphate minerals in soil to supply needed phosphorus. The growth of various bacteria and fungi, when not supplied with necessary phosphorus in lab tests, have shown some of these microorganisms to secrete weak acids, dissolving phosphate minerals to various degrees. This study attempted to evaluate such solubilities. Aspergillium niger, a common fungi, was grown in a liquid media for a two day period, filtered, and then added to finely ground samples of the phosphate minerals apatite, variscite, and lazulite. The filtrates were tested for pH and phosphate concentrations before and after addition of the minerals. Initial results indicate pH of the filtrates has a direct correlation with phosphate concentrations. The different phosphate minerals showed different solubilities in the filtrates. Collophane, an amorphous variant of apatite also tested, showed a significantly greater phosphate concentration in the filtrate than the crystalline apatite sample.

  18. Effects of Complementary Creatine Monohydrate and Physical Training on Inflammatory and Endothelial Dysfunction Markers Among Heart Failure Patients

    PubMed Central

    Hemati, Farajollah; Rahmani, Asghar; Asadollahi, Khairollah; Soleimannejad, Koroush; Khalighi, Zahra

    2016-01-01

    Background: Previous studies have reported endothelial dysfunction and inflammatory cytokine in heart failure patients (HF). Objectives: The purpose of this study was to determine the effects of creatine monohydrate and exercise on inflammatory and endothelial dysfunction markers among HF patients. Patients and Methods: One hundred patients were prospectively randomized into two groups: Intervention group which received 5 grams/day creatine monohydrate and exercised for 8 weeks; and control group which did not receive any interventions. Interleukine-6 (IL-6), high sensitivity C reactive protein (hs-CRP), P-selectin, intercellular adhesion molecule-1 (ICAM-1), and vascular cell adhesion molecule 1 (VCAM-1) were measured at the start and end of the study for both groups. Results: In total, 100 patients including 50 controls and 50 intervention group (54% male, mean EF of 34.2 ± 10.5% and 52% male, mean EF of 35.6 ± 12.7%, respectively) were analyzed. The serum levels of hs-CRP and IL-6 increased at the end of the study in the control group compared to the baseline, (7.5 ± 1.5 mg/L vs. 6.9 ± 1.3 mg/L, P < 0.05 and 3.0 ± 0.75 ng/L vs. 2.55 ± 0.9 ng/L, P < 0.05, respectively). However, compared to the baseline, the level of both markers decreased at the end of the study in the intervention group (6.3 ± 1.6 mg/L vs.7.5 ± 1.5 mg/L, P < 0.05 and 2.1 ± 0.8 ng/L vs.2.5 ± 0.5 ng/L, P < 0.05). Also, P-selectin and ICAM-1 levels increased at the end of study (56.9 ± 1.8 ng/L vs. 51.9 ± 1.5 ng/L, P < 0.05 and 368.1 ± 25.4 µg/L vs. 353.1 ± 10.4 µg/L, P < 0.05 respectively). Inversely, the levels of these markers decreased in the intervention group, at the end of study (49.7 ± 1.9 ng/l vs. 51.4 ± 2.1 ng/l, P < 0.05 and 342.7 ± 16.5 µg/l vs. 350.4 ± 14.7 µg/l, P < 0.05, respectively). VCAM-1 level was not decreased significantly at the end of the study in the intervention group (570.5 ± 78.4 µg/L vs. 575.3 ± 86.5 µg/L, P > 0.05). Conclusions: Combination of creatine monohydrate and exercise attenuated inflammation and endothelial dysfunction markers among heart failure patients.

  19. Calcium phosphate in catheter encrustation.

    PubMed

    Cox, A J; Harries, J E; Hukins, D W; Kennedy, A P; Sutton, T M

    1987-02-01

    Encrusted catheters from nine female patients were the source of samples of deposits which were examined by X-ray diffraction, atomic absorption spectroscopy, infra-red spectroscopy and extended X-ray absorption fine structure (EXAFS) spectroscopy. In eight samples the only crystalline phase which could be clearly distinguished by X-ray diffraction was ammonium magnesium orthophosphate hexahydrate, NH4MgPO4 X 6H2O, which occurs naturally as the mineral struvite. However, atomic absorption spectroscopy revealed an appreciable concentration of calcium in all samples. Calcium phosphates have previously been detected in catheter deposits. Infra-red and EXAFS spectra were consistent with the calcium phosphate being present as a poorly crystalline hydroxyapatite. Thus the deposits appear to consist of a mixture of crystalline struvite and a form of hydroxyapatite which is not fully crystalline. PMID:3030487

  20. Glucose-6-Phosphate Dehydrogenase Deficiency.

    PubMed

    Luzzatto, Lucio; Nannelli, Caterina; Notaro, Rosario

    2016-04-01

    G6PD is a housekeeping gene expressed in all cells. Glucose-6-phosphate dehydrogenase (G6PD) is part of the pentose phosphate pathway, and its main physiologic role is to provide NADPH. G6PD deficiency, one of the commonest inherited enzyme abnormalities in humans, arises through one of many possible mutations, most of which reduce the stability of the enzyme and its level as red cells age. G6PD-deficient persons are mostly asymptomatic, but they can develop severe jaundice during the neonatal period and acute hemolytic anemia when they ingest fava beans or when they are exposed to certain infections or drugs. G6PD deficiency is a global health issue. PMID:27040960

  1. Combination therapy with sitagliptin and lansoprazole in patients with recent-onset type 1 diabetes (REPAIR-T1D): 12-month results of a multicentre, randomised, placebo-controlled, phase 2 trial

    PubMed Central

    Griffin, Kurt J; Thompson, Paul A; Gottschalk, Michael; Kyllo, Jennifer H; Rabinovitch, Alex

    2014-01-01

    Summary Background Type 1 diabetes results from autoimmune destruction of pancreatic β cells. Findings from preclinical studies suggest that dipeptidyl peptidase-4 inhibitors and proton-pump inhibitors might enhance β-cell survival and regeneration. We postulated that sitagliptin and lansoprazole would preserve β-cell function in patients with recent-onset type 1 diabetes. Methods We did a double-blind, placebo-controlled, phase 2 trial (REPAIR-T1D). Participants aged 11–36 years, diagnosed with type 1 diabetes within the past 6 months were recruited from Sanford Health Systems (Sioux Falls, SD, USA; Fargo, ND, USA), Children's Hospitals and Clinics of Minnesota (St Paul, MN, USA), and Rady Children's Hospital (San Diego, CA, USA). Participants were randomly assigned (2:1) to receive oral sitagliptin (100 mg for participants ≥18 years, 50 mg for those <18 years) and lansoprazole (60 mg for participants ≥18 years, 30 mg for those <18 years) or matched placebo for 12 months. Randomisation was done by a blocked randomisation process (blocks of three and six), with separate streams for younger (<18 years) and older (≥18 years) participants, and males and females. All participants and personnel remained masked until after the completion of the final 12 month visit, at which time data were unmasked to the analysis team. The primary endpoint was C-peptide response to a mixed meal challenge at 12 months measured as 2 h area under curve. Analysis was by intention to treat. This trial is registered with ClinicalTrials.gov, number NCT01155284. Findings Between Sept 21, 2010, and May 29, 2012, 46 participants were randomly assigned to the treatment group and 22 to the placebo group; of whom 40 participants in the treatment group and 18 in the placebo group completed the 12-month treatment. At 12 months, the mean change in C-peptide area under curve was −229 pmol/L (95% CI −316 to −142) for the treatment group and −253 pmol/L (−383 to −123) for the placebo group; this difference was not significant (p=0·77). No adverse or serious adverse events were probably or definitely related to the study treatment. Interpretation Although the expected change in the primary endpoint was not achieved, not all participants had increases in glucagon-like peptide-1 and gastrin concentrations that were expected with treatment. Although participants did not have adverse events related to study drugs, the study is not powered to address safety definitively. Further trials including these drugs might be warranted, but should be designed to ensure appropriate selection of participants and increases in these intermediary hormones. Funding Sanford Research and JDRF. PMID:24997559

  2. Microstructural disassembly of calcium phosphates.

    PubMed

    Wang, Haibo; Lee, Jong-Kook; Moursi, Amr M; Anderson, David; Winnard, Phillip; Powell, Heather; Lannutti, John

    2004-01-01

    Microstructural factors may play a role in the osseointegration of calcium phosphates. In this paper, direct microstructural interactions between crystalline calcium phosphates and the biological milieu are reported. Degradation via exposure to osteoblast culture closely resembles in vivo interactions with subcutaneous tissues in a bovine model at early time periods. That these interactions were common to both experiments constitutes one of the few known examples of in vitro-in vivo correspondence. Interestingly, the degradation of phase pure hydroxyapatite (HA) in vitro was more rapid than that of biphasic HA in vivo. In both cases, grain extraction/pullout was frequently observed. This suggests a connection to smaller-scale observations of epitaxial CHA nucleation and growth on pre-existing HA grains. A microstructure in which the grain boundary is dissolving/corroding can apparently be disassembled by forces transmitted through biological structures. These observations are distinct from those of simple non-biological solutions and prove that biological environments can interact with the material beneath the ceramic-cell/ceramic-tissue interface. Many often ignored microstructural factors-grain size, shape, grain boundary strength and the presence of impurity phases-may in fact control degradation. We also suggest that even relatively modest initial grain sizes will, in combination with the mild/absent foreign body response to calcium phosphates, result in lengthy in vivo particle resistence. PMID:14661250

  3. Real-time analysis of diaquat dibromide monohydrate in water with a SERS-based integrated microdroplet sensor

    NASA Astrophysics Data System (ADS)

    Gao, Rongke; Choi, Namhyun; Chang, Soo-Ik; Lee, Eun Kyu; Choo, Jaebum

    2014-07-01

    We report the fast and sensitive trace analysis of diaquat dibromide monohydrate (DQ) in water using a surface-enhanced Raman scattering (SERS)-based microdroplet sensor. This sensor is composed of two compartments: the first one is for droplet generation for fresh silver nanoparticle (AgNP) synthesis and the second for droplet merging for SERS detection. Silver ions were nucleated and grown to large size AgNPs in droplets, and then each droplet was synchronously merged with another droplet containing DQ for SERS detection. This two-phase liquid-liquid segmented flow system prevented memory effects caused by the precipitation of nanoparticle aggregates on channel walls because the aqueous droplets were isolated by a continuous oil phase. The limit of detection (LOD) of DQ in water was determined to be below 5 nM, which satisfies the maximum contaminant level defined by the United States EPA. This method was also validated successfully in DQ-spiked tap water. The SERS-based integrated sensing system is expected to be useful as an in-the-field sensing platform for fast and reproducible trace analysis of environmental pollutants in water.We report the fast and sensitive trace analysis of diaquat dibromide monohydrate (DQ) in water using a surface-enhanced Raman scattering (SERS)-based microdroplet sensor. This sensor is composed of two compartments: the first one is for droplet generation for fresh silver nanoparticle (AgNP) synthesis and the second for droplet merging for SERS detection. Silver ions were nucleated and grown to large size AgNPs in droplets, and then each droplet was synchronously merged with another droplet containing DQ for SERS detection. This two-phase liquid-liquid segmented flow system prevented memory effects caused by the precipitation of nanoparticle aggregates on channel walls because the aqueous droplets were isolated by a continuous oil phase. The limit of detection (LOD) of DQ in water was determined to be below 5 nM, which satisfies the maximum contaminant level defined by the United States EPA. This method was also validated successfully in DQ-spiked tap water. The SERS-based integrated sensing system is expected to be useful as an in-the-field sensing platform for fast and reproducible trace analysis of environmental pollutants in water. Electronic supplementary information (ESI) available. See DOI: 10.1039/c4nr01269k

  4. Crystal structure of zwitterionic 3-(2-hy­droxy-2-phospho­nato-2-phosphono­eth­yl)imidazo[1,2-a]pyridin-1-ium monohydrate (minodronic acid monohydrate): a redetermination

    PubMed Central

    Airoldi, Annalisa; Bettoni, Piergiorgio; Donnola, Monica; Calestani, Gianluca; Rizzoli, Corrado

    2015-01-01

    In a previous study, the X-ray structure of the title compound, C9H12N2O7P2·H2O, was reported [Takeuchi et al., (1998 ▸). Chem. Pharm. Bull. 46, 1703–1709], but neither atomic coordinates nor details of the geometry were published. The structure has been redetermined with high precision as its detailed knowledge is essential to elucidate the presumed polymorphism of minodronic acid monohydrate at room temperature. The mol­ecule crystallizes in a zwitterionic form with cationic imidazolium[1,2a]pyridine and anionic phospho­nate groups. The dihedral angle formed by the planes of the pyridine and imidazole rings is 3.55 (9)°. A short intra­molecular C—H⋯O contact is present. In the crystal, mol­ecules are linked by O—H⋯O, N—H⋯O and C—H⋯O hydrogen bonds and π–π inter­actions [centroid-to-centroid distance = 3.5822 (11) Å], forming a three-dimensional structure. PMID:25705449

  5. A vacuolar phosphate transporter essential for phosphate homeostasis in Arabidopsis.

    PubMed

    Liu, Jinlong; Yang, Lei; Luan, Mingda; Wang, Yuan; Zhang, Chi; Zhang, Bin; Shi, Jisen; Zhao, Fu-Geng; Lan, Wenzhi; Luan, Sheng

    2015-11-24

    Inorganic phosphate (Pi) is stored in the vacuole, allowing plants to adapt to variable Pi availability in the soil. The transporters that mediate Pi sequestration into vacuole remain unknown, however. Here we report the functional characterization of Vacuolar Phosphate Transporter 1 (VPT1), an SPX domain protein that transports Pi into the vacuole in Arabidopsis. The vpt1 mutant plants were stunted and consistently retained less Pi than wild type plants, especially when grown in medium containing high levels of Pi. In seedlings, VPT1 was expressed primarily in younger tissues under normal conditions, but was strongly induced by high-Pi conditions in older tissues, suggesting that VPT1 functions in Pi storage in young tissues and in detoxification of high Pi in older tissues. As a result, disruption of VPT1 rendered plants hypersensitive to both low-Pi and high-Pi conditions, reducing the adaptability of plants to changing Pi availability. Patch-clamp analysis of isolated vacuoles showed that the Pi influx current was severely reduced in vpt1 compared with wild type plants. When ectopically expressed in Nicotiana benthamiana mesophyll cells, VPT1 mediates vacuolar influx of anions, including Pi, SO4(2-), NO3(-), Cl(-), and malate with Pi as that preferred anion. The VPT1-mediated Pi current amplitude was dependent on cytosolic phosphate concentration. Single-channel analysis showed that the open probability of VPT1 was increased with the increase in transtonoplast potential. We conclude that VPT1 is a transporter responsible for vacuolar Pi storage and is essential for Pi adaptation in Arabidopsis. PMID:26554016

  6. A novel L-arginine salt nonlinear optical crystal: L-arginine p-nitrobenzoate monohydrate (LANB)

    NASA Astrophysics Data System (ADS)

    Wang, L.; Zhang, G. H.; Liu, X. T.; Wang, L. N.; Wang, X. Q.; Zhu, L. Y.; Xu, D.

    2014-01-01

    A novel L-arginine salt nonlinear optical single crystal, L-arginine p-nitrobenzoate monohydrate (LANB) has been grown by slow cooling method from aqueous solution. Its solubility at different temperatures in water was measured. The grown crystal was characterized by the elemental analyses, X-ray single crystal and powder diffractions, Fourier transform infrared and Raman spectra. The structure analysis revealed that LANB belongs to the monoclinic crystallographic system, space group P21, with unit cell parameters: a = 8.566(3), b = 5.817(2), c = 17.131(7) , ? = 101.223(5), Z = 2 and V = 837.2(6) 3. The proton and carbon configurations of L-arginine were confirmed through 1H NMR and 13C NMR spectra analyses. The linear and nonlinear optical properties of LANB crystal were studied by the use of transmission spectrum and second harmonic generation (SHG). The thermal properties were investigated by using thermo gravimetric (TG) and differential thermal analysis (DTA).

  7. Growth, crystalline perfection, optical, thermal, laser damage threshold and electrical characterization of melaminium levulinate monohydrate single crystal

    NASA Astrophysics Data System (ADS)

    Sivakumar, N.; Kanagathara, N.; Bhagavannarayana, G.; Kalainathan, S.; Anbalagan, G.

    2015-09-01

    Equimolar amounts of melamine and levulinic acid results an organic crystal of melaminium levulinate monohydrate (MLM) at room temperature. MLM belongs to a monoclinic crystal structure having P21/c space group which was confirmed by single crystal X-ray diffraction study. Functional groups present in the MLM crystal were identified by FT-IR spectral study. HRXRD study dictates the quality of MLM crystal. UV-visble spectrum of MLM reveals the lower cut-off wavelength of 293 nm with 55% optical transparency and optical band gap was found to be 4.20 eV for the prominent plane (1 0 -1). Refractive indices for the three axes of MLM crystal were found to be nx=2.6, ny=2.4 and nz=2.2 respectively. Further the thermal stability and melting point of MLM crystal were investigated by TG/DTA study. Dielectric permittivity tensor components were estimated for the planes (1 0 -1), (0 1 0) and (1 1 1) respectively. The thermal conductivity of the crystal by Wiedemann-Franz law was found to be 5.99×10-11 W/mK at 70 °C. LDT value (2.84 GW/cm2) of MLM was estimated for laser optical device applications.

  8. Synthesis, structure, crystal growth and characterization of a novel semiorganic nonlinear optical l-proline lithium bromide monohydrate single crystal.

    PubMed

    Sathiskumar, S; Balakrishnan, T; Ramamurthi, K; Thamotharan, S

    2015-03-01

    l-Proline lithium bromide monohydrate (LPLBM), a promising semiorganic nonlinear optical material, was synthesized and single crystals of LPLBM were grown from solution by slow evaporation technique. Single crystal X-ray structure solution reveals that the grown crystal belongs to monoclinic system with space group P21. Presence of various functional groups was identified by FT-IR and FT-Raman spectral analyses. UV-Vis-NIR spectroscopic study shows that the LPLBM crystal possesses 90% of transmittance in the range of 250-1100nm. Vickers microhardness values, the dielectric constant and dielectric loss of the LPLBM crystal were reported. Elemental analysis by energy dispersive X-ray analysis shows the presence of carbon, nitrogen, oxygen and bromine. The surface morphology of the crystal was investigated using scanning electron microscopic study. The thermal stability of the LPLBM crystal was studied from TGA and DSC analysis. Second harmonic generation efficiency of the LPLBM crystal measured by Kurtz and Perry powder technique using Nd:YAG laser is about 0.3 times that of urea. PMID:25498813

  9. Experimental and theoretical investigations of non-centrosymmetric 8-hydroxyquinolinium dibenzoyl-(L)-tartrate methanol monohydrate single crystal

    SciTech Connect

    Sudharsana, N.; Krishnakumar, V.; Nagalakshmi, R.

    2015-01-15

    Graphical abstract: ORTEP diagram of HQDBT. - Highlights: • Single crystal XRD and NMR studies confirm the formation of the title compound. • SHG efficiency was found to be 0.6 times that of KDP. • First-order hyperpolarizability (β) was calculated using HF and B3LYP methods. - Abstract: A novel 8-hydroxyquinolinium dibenzoyl-(L)-tartrate methanol monohydrate crystal has been grown by slow evaporation technique. The single crystal X-ray diffraction analysis has been done for the title compound and is found to crystallize in orthorhombic space group P2{sub 1}2{sub 1}2{sub 1}. The optical absorption cut-off wavelength is found to be 440 nm. The vibrational analysis has been carried out to assess the functional groups present in the title compound. The molecular structure of the title compound has been confirmed by nuclear magnetic resonance spectroscopy. Thermogravimetric, differential scanning calorimetric and differential thermal analyses reveal the melting point and thermal stability of the title compound. The second harmonic generation efficiency is confirmed by Kurtz–Perry powder technique. Further quantum chemical calculations are performed using Gaussian 03 software.

  10. Crystal structure of cis-2-(2-carb-oxy-cyclo-prop-yl)glycine (CCG-III) monohydrate.

    PubMed

    Lindeman, Sergey; Wallock, Nathaniel J; Donaldson, William A

    2015-07-01

    The title compound, C6H9NO4·H2O [systematic name: (αR,1R,2S)-rel-α-amino-2-carb-oxy-cyclo-propane-acetic acid monohydrate], crystallizes with two organic mol-ecules and two water mol-ecules in the asymmetric unit. The space group is P21 and the organic mol-ecules are enanti-omers, thus this is an example of a 'false conglomerate' with two mol-ecules of opposite handedness in the asymmetric unit (r.m.s. overlay fit = 0.056 Å for one mol-ecule and its inverted partner). Each mol-ecule exists as a zwitterion, with proton transfer from the amino acid carb-oxy-lic acid group to the amine group. In the crystal, the components are linked by N-H⋯O and O-H⋯O hydrogen bonds, generating (100) sheets. Conformationally restricted glutamate analogs are of inter-est due to their selective activation of different glutamate receptors, and the naturally occurring (+)-CCG-III is an inhibitor of glutamate uptake and the key geometrical parameters are discussed. PMID:26279882

  11. Renal papillary calcification and the development of calcium oxalate monohydrate papillary renal calculi: a case series study

    PubMed Central

    2013-01-01

    Background The objective of this study is to determine in a case series (four patients) how calcified deposits in renal papillae are associated with the development of calcium oxalate monohydrate (COM) papillary calculi. Methods From the recently collected papillary calculi, we evaluated retrospectively patients, subjected to retrograde ureteroscopy, with COM papillary lithiasis. Results The COM papillary calculi were found to result from subepithelial injury. Many of these lesions underwent calcification by hydroxyapatite (HAP), with calculus morphology and the amount of HAP in the concave zone dependent on the location of the calcified injury. Most of these HAP deposits grew, eroding the epithelium covering the renal papillae, coming into contact with urine and starting the development of COM calculi. Subepithelial HAP plaques may alter the epithelium covering the papillae, resulting in the deposit of COM crystals directly onto the epithelium. Tissue calcification depends on a pre-existing injury, the continuation of this process is due to modulators and/or crystallization inhibitors deficiency. Conclusions Since calculus morphology and the amount of detected HAP are dependent on the location and widespread of calcified injury, all types of papillary COM calculi can be found in the same patient. All patients had subepithelial calcifications, with fewer papillary calculi, demonstrating that some subepithelial calcifications did not further evolve and were reabsorbed. A high number of subepithelial calcifications increases the likelihood that some will be transformed into COM papillary calculi. PMID:23497010

  12. High-throughput platform for design and screening of peptides as inhibitors of calcium oxalate monohydrate crystallization

    NASA Astrophysics Data System (ADS)

    Farmanesh, Sahar; Chung, Jihae; Chandra, Divya; Sosa, Ricardo D.; Karande, Pankaj; Rimer, Jeffrey D.

    2013-06-01

    Crystal growth modifiers present a versatile tool for controlling crystal shape and size. Our work described here focuses on the design and screening of short peptides as inhibitors of calcium oxalate monohydrate (COM) crystals using high-throughput approaches. We designed a small library of 13 peptides containing Ala and Asp amino acids arranged in varying sequences that mimic ubiquitous motifs in natural calcium-binding proteins. Peptides were screened using a quick assay to measure their efficacy for inhibiting COM crystallization. Our results show that subtle variations in the placement of Ala and Asp residues in the peptide sequence can have a profound effect on their inhibition potential. We were able to discover peptide sequences that inhibit COM crystallization more effectively than some of the well-known COM inhibitors, such as citrate. Our results also demonstrate that peptides can be engineered to bind to specific faces of COM crystals. Peptide sequences identified in this work are promising candidates for further development as therapies for biomineral-related diseases, such as kidney stone disease. Collectively, our work establishes new paradigms for the design, synthesis, and screening of peptides for controlling crystal habit with the potential to impact a variety of fields, including drug discovery, advanced materials, catalysis and separations.

  13. 2-(4-Hy­droxy­phen­yl)-1H-benzimidazol-3-ium chloride monohydrate

    PubMed Central

    González-Padilla, Jazmin E.; Rosales-Hernández, Martha Cecila; Padilla-Martínez, Itzia I.; García-Báez, Efren V.; Rojas-Lima, Susana

    2013-01-01

    The title mol­ecular salt, C13H11N2O+·Cl−·H2O, crystallizes as a monohydrate. In the cation, the phenol and benzimidazole rings are almost coplanar, making a dihedral angle of 3.18 (4)°. The chloride anion and benzimidazole cation are linked by two N+—H⋯Cl− hydrogen bonds, forming chains propagating along [010]. These chains are linked through O—H⋯Cl hydrogen bonds involving the water mol­ecule and the chloride anion, which form a diamond core, giving rise to the formation of two-dimensional networks lying parallel to (10-2). Two π–π inter­actions involving the imidazolium ring with the benzene and phenol rings [centroid–centroid distances = 3.859 (3) and 3.602 (3) Å, respectively], contribute to this second dimension. A strong O—H⋯O hydrogen bond involving the water mol­ecule and the phenol substituent on the benzimidazole unit links the networks, forming a three-dimensional structure. PMID:24427105

  14. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

    PubMed Central

    Herbertz, Stephan; Sawyer, J Scott; Stauber, Anja J; Gueorguieva, Ivelina; Driscoll, Kyla E; Estrem, Shawn T; Cleverly, Ann L; Desaiah, Durisala; Guba, Susan C; Benhadji, Karim A; Slapak, Christopher A; Lahn, Michael M

    2015-01-01

    Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks of cancer, including tumor proliferation, invasion and metastasis, inflammation, angiogenesis, and escape of immune surveillance. There are several pharmacological approaches to block TGF-β signaling, such as monoclonal antibodies, vaccines, antisense oligonucleotides, and small molecule inhibitors. Galunisertib (LY2157299 monohydrate) is an oral small molecule inhibitor of the TGF-β receptor I kinase that specifically downregulates the phosphorylation of SMAD2, abrogating activation of the canonical pathway. Furthermore, galunisertib has antitumor activity in tumor-bearing animal models such as breast, colon, lung cancers, and hepatocellular carcinoma. Continuous long-term exposure to galunisertib caused cardiac toxicities in animals requiring adoption of a pharmacokinetic/pharmacodynamic-based dosing strategy to allow further development. The use of such a pharmacokinetic/pharmacodynamic model defined a therapeutic window with an appropriate safety profile that enabled the clinical investigation of galunisertib. These efforts resulted in an intermittent dosing regimen (14 days on/14 days off, on a 28-day cycle) of galunisertib for all ongoing trials. Galunisertib is being investigated either as monotherapy or in combination with standard antitumor regimens (including nivolumab) in patients with cancer with high unmet medical needs such as glioblastoma, pancreatic cancer, and hepatocellular carcinoma. The present review summarizes the past and current experiences with different pharmacological treatments that enabled galunisertib to be investigated in patients. PMID:26309397

  15. Application of Calcium Phosphate Materials in Dentistry

    PubMed Central

    Al-Sanabani, Jabr S.; Al-Sanabani, Fadhel A.

    2013-01-01

    Calcium phosphate materials are similar to bone in composition and in having bioactive and osteoconductive properties. Calcium phosphate materials in different forms, as cements, composites, and coatings, are used in many medical and dental applications. This paper reviews the applications of these materials in dentistry. It presents a brief history, dental applications, and methods for improving their mechanical properties. Notable research is highlighted regarding (1) application of calcium phosphate into various fields in dentistry; (2) improving mechanical properties of calcium phosphate; (3) biomimetic process and functionally graded materials. This paper deals with most common types of the calcium phosphate materials such as hydroxyapatite and tricalcium phosphate which are currently used in dental and medical fields. PMID:23878541

  16. Inherited Disorders of Calcium and Phosphate Metabolism

    PubMed Central

    Gattineni, Jyothsna

    2014-01-01

    Purpose of Review Inherited disorders of calcium and phosphate homeostasis have variable presentation and can cause significant morbidity. Understanding the mode of inheritance and pathophysiology of these conditions will help in the diagnosis and early institution of therapy. Recent Findings Identification of genetic mutations in human subjects and animal models has advanced our understanding of many inherited disorders of calcium and phosphate regulation. Identification of mutations of CaSR also has improved our understanding of hypocalcemic and hypercalcemic conditions. Mutations of Fgf23, Klotho and phosphate transporter genes have been identified as causes for disorders of phosphate metabolism. Summary Calcium and phosphate homeostasis is tightly regulated in a narrow range due to their vital role in many biological processes. Inherited disorders of calcium and phosphate metabolism though uncommon can have severe morbidity. Genetic counseling of the affected families is an important part of the follow up of these patients. PMID:24553630

  17. Phosphate-limited culture of Azotobacter vinelandii.

    PubMed Central

    Tsai, J C; Aladegbami, S L; Vela, G R

    1979-01-01

    Batch cultures of Azotobacter vinelandii grown in phosphate-deficient media were compared with control cultures grown in phosphate-sufficient media. Phosphate limitation was assessed by total cell yield and by growth kinetics. Although cell protein, nucleic acids, and early growth rate were unaffected by phosphate deficiency, cell wall structure, oxygen uptake, and cell viability were significantly affected. Also, phosphate-limited cells contained much larger amounts of poly-beta-hydroxybutyric acid but lower adenylate nucleotide energy charge than did control cells. The ratio of adenosine 5'-triphosphate to adenosine 5'-diphosphate was much lower in phosphate-deficient cells. The data indicate a substrate saving choice of three metabolic pathways available to this organism under different growth conditions. Images PMID:457614

  18. Solid titration of octacalcium phosphate.

    PubMed

    Pan, H-B; Darvell, B W

    2009-01-01

    Octacalcium phosphate (OCP) is of considerable importance as a precursor in the formation of dental enamel and an intermediate phase in the precipitation of hydroxyapatite (HAp) in bone. However, agreement is poor on the solubility product (pK(sp)), possibly due to the formation of the more stable phase HAp. The system was investigated using solid titration, which has shown reliability in work on HAp and related fluoride minerals, with OCP in 100 mM KCl at 37.0 +/- 0.1 degrees C. The constitution of the end point precipitate was determined by X-ray diffraction and selected-electron area diffraction; the particle morphology and elements present were examined by high-resolution field emission scanning, transmission electron microscopy and energy-dispersive X-ray analysis. The titration curve for OCP was found for pH approximately 3.4-7.4. The precipitate was HAp at pH 3.6 and 4.5; no residual OCP or other phase was detected. Dicalcium phosphate dihydrate (DCPD) was then found to form at pH 3.6 on further addition of OCP titrant after equilibrium had been achieved, possibly due to easier nucleation at lower pH. However, markedly crystalline HAp was formed in equilibrium for OCP titration with HAp seeding, verifying HAp as the more stable phase. A solubility isotherm for OCP was not obtained as HAp appears to be less soluble in the pH range studied. This adds weight to the view that HAp may be the most stable phase of all calcium phosphates, with further doubt being cast on DCPD being the most stable phase below pH 4.2. However, metastable DCPD may form in an Ostwald succession, depending on supersaturation and nucleation conditions. PMID:19556792

  19. Symbiotic phosphate transport in arbuscular mycorrhizas.

    PubMed

    Karandashov, Vladimir; Bucher, Marcel

    2005-01-01

    Arbuscular mycorrhizal fungi colonize the root systems of most land plants and modulate plant growth by enhancing the availability of nutrients, mainly phosphorus, for plant nutrition. Recently identified genes encoding mycorrhiza-specific plant phosphate transporters have enabled fundamental problems in arbuscular mycorrhizal symbiosis research to be addressed. Because phosphate transport is a key feature of this symbiosis, the study of phosphate transport mechanisms and their gene regulation will further our understanding of the intimate interaction between the two symbiotic partners. PMID:15642520

  20. Mineral induced formation of sugar phosphates

    NASA Technical Reports Server (NTRS)

    Pitsch, S.; Eschenmoser, A.; Gedulin, B.; Hui, S.; Arrhenius, G.

    1995-01-01

    Glycolaldehyde phosphate, sorbed from highly dilute, weakly alkaline solution into the interlayer of common expanding sheet structure metal hydroxide minerals, condenses extensively to racemic aldotetrose-2, 4-diphophates, and aldohexose-2, 4, 6-triphosphates. The reaction proceeds mainly through racemic erythrose-2, 4-phosphate, and terminates with a large fraction of racemic altrose-2, 4, 6-phosphate. In the absence of an inductive mineral phase, no detectable homogeneous reaction takes place in the concentration- and pH range used. The reactant glycolaldehyde phosphate is practically completely sorbed within an hour from solutions with concentrations as low as 50 micron; the half-time for conversion to hexose phosphates is of the order of two days at room temperature and pH 9.5. Total production of sugar phosphates in the mineral interlayer is largely independent of the glycolaldehyde phosphate concentration in the external solution, but is determined by the total amount of GAP offered for sorption up to the capacity of the mineral. In the presence of equimolar amounts of rac-glyceraldehyde-2-phosphate, but under otherwise similar conditions, aldopentose-2, 4, -diphosphates also form, but only as a small fraction of the hexose-2, 4, 6-phosphates.

  1. Low temperature ultrasonic attenuation in phosphate glasses

    SciTech Connect

    Keppens, V.; Laermans, C.; Sales, Brian C; Boatner, Lynn A

    2011-01-01

    Ultrasonic attenuation measurements on phosphate glasses with different chain lengths, lead metaphosphate and lead-indium phosphate, have been carried out at low temperatures (0.3 10 K) and high frequencies (100 160 MHz). The materials investigated are lead metaphosphate (average chain length > 15) and lead indium phosphate (average chain length = 3). Both materials have the typical glasslike behavior, explained by the presence of tunneling states (TS). A detailed analysis reveals that the density of states of these TS is significantly lower in the lead metaphosphate glass compared to the lead indium glass. This difference can be related to the difference in length of the phosphate tetrahedra chains.

  2. Next generation calcium phosphate-based biomaterials

    PubMed Central

    LC, Chow

    2009-01-01

    It has been close to a century since calcium phosphate materials were first used as bone graft substitutes. Numerous studies conducted in the last two decades have produced a wealth of information on the chemistry, in vitro properties, and biological characteristics of granular calcium phosphates and calcium phosphate cement biomaterials. An in depth analysis of several key areas of calcium phosphate cement properties is presented with the aim of developing strategies that could lead to break-through improvements in the functional efficacies of these materials. PMID:19280963

  3. Preparation of porous lanthanum phosphate with templates

    SciTech Connect

    Onoda, Hiroaki; Ishima, Yuya; Takenaka, Atsushi; Tanaka, Isao

    2009-08-05

    Malonic acid, propionic acid, glycine, n-butylamine, and urea were added to the preparation of lanthanum phosphate from lanthanum nitrate and phosphoric acid solutions. All additives were taken into lanthanum phosphate particles. The additives that have a basic site were easy to contain in precipitates. The addition of templates improved the specific surface area of lanthanum phosphate. The amount of pore, with radius smaller than 4 nm, increased with the addition of templates. The remained additives had influence on the acidic properties of lanthanum phosphate.

  4. Spectroscopic studies of lithium phosphate, lead phosphate and zinc phosphate glasses containing TiO2: Effect of gamma irradiation

    NASA Astrophysics Data System (ADS)

    Ghoneim, N. A.; Abdelghany, A. M.; Abo-Naf, S. M.; Moustafa, F. A.; ElBadry, Kh. M.

    2013-03-01

    Pristine lithium phosphate, lead phosphate and zinc phosphate glasses and glasses of the same compositions containing TiO2 (0.25 → 2.5%) were prepared. UV-visible and infrared absorption spectra of the prepared samples were measured before and after gamma irradiation. Optical spectra of these prepared glasses reveal strong UV absorption bands which are attributed to the presence of trace iron impurities in lithium and zinc phosphate glasses while the broad UV bands in lead phosphate glasses were related to absorption of both trace iron impurities and divalent lead ions. The TiO2-containing glasses reveal an extra two visible bands at about 550-580 and 680-740 nm due to the transitions 2B2g → 2B1g and 2B2g → 2A1g of distorted octahedral Ti3+ ions. The effects of gamma irradiation reveal variations, extended in the UV-visible region in the lithium phosphate while with lead phosphate and zinc phosphate samples the variations are restricted to UV spectra. The response to gamma irradiation on optical absorption has been analyzed for both the sharing of all glass constituents including trace iron impurities. Lead and zinc phosphate glasses reveal only induced UV bands from photochemical effect of trace iron impurities while lithium phosphate shows extra induced visible band due to positive holes. The effects of gamma irradiation on the IR spectra are limited to a slight decrease of the intensities for some IR bands. The IR spectra are observed to be slightly affected by the increase of TiO2 indicating the stability of the main phosphate network units and the shielding behavior of titanium ions.

  5. The Plastidic Pentose Phosphate Translocator Represents a Link between the Cytosolic and the Plastidic Pentose Phosphate Pathways in Plants1

    PubMed Central

    Eicks, Michael; Maurino, Vernica; Knappe, Silke; Flgge, Ulf-Ingo; Fischer, Karsten

    2002-01-01

    Plastids are the site of the reductive and the oxidative pentose phosphate pathways, which both generate pentose phosphates as intermediates. A plastidic transporter from Arabidopsis has been identified that is able to transport, in exchange with inorganic phosphate or triose phosphates, xylulose 5-phosphate (Xul-5-P) and, to a lesser extent, also ribulose 5-phosphate, but does not accept ribose 5-phosphate or hexose phosphates as substrates. Under physiological conditions, Xul-5-P would be the preferred substrate. Therefore, the translocator was named Xul-5-P/phosphate translocator (XPT). The XPT shares only approximately 35% to 40% sequence identity with members of both the triose phosphate translocator and the phosphoenolpyruvate/phosphate translocator classes, but a higher identity of approximately 50% to glucose 6-phosphate/phosphate translocators. Therefore, it represents a fourth group of plastidic phosphate translocators. Database analysis revealed that plant cells contain, in addition to enzymes of the oxidative branch of the oxidative pentose phosphate pathway, ribose 5-phosphate isomerase and ribulose 5-phosphate epimerase in both the cytosol and the plastids, whereas the transketolase and transaldolase converting the produced pentose phosphates to triose phosphates and hexose phosphates are probably solely confined to plastids. It is assumed that the XPT function is to provide the plastidic pentose phosphate pathways with cytosolic carbon skeletons in the form of Xul-5-P, especially under conditions of a high demand for intermediates of the cycles. PMID:11842155

  6. The SLC37 family of sugar-phosphate/phosphate exchangers.

    PubMed

    Chou, Janice Y; Mansfield, Brian C

    2014-01-01

    The SLC37 family members are endoplasmic reticulum (ER)-associated sugar-phosphate/phosphate (P(i)) exchangers. Three of the four members, SLC37A1, SLC37A2, and SLC37A4, function as Pi-linked glucose-6-phosphate (G6P) antiporters catalyzing G6P:P(i) and P(i):P(i) exchanges. The activity of SLC37A3 is unknown. SLC37A4, better known as the G6P transporter (G6PT), has been extensively characterized, functionally and structurally, and is the best characterized family member. G6PT contains 10 transmembrane helices with both N and C termini facing the cytoplasm. The primary in vivo function of the G6PT protein is to translocate G6P from the cytoplasm into the ER lumen where it couples with either the liver/kidney/intestine-restricted glucose-6-phosphatase-α (G6Pase-α or G6PC) or the ubiquitously expressed G6Pase-β (or G6PC3) to hydrolyze G6P to glucose and P(i). The G6PT/G6Pase-α complex maintains interprandial glucose homeostasis, and the G6PT/G6Pase-β complex maintains neutrophil energy homeostasis and functionality. G6PT is highly selective for G6P and is competitively inhibited by cholorogenic acid and its derivatives. Neither SLC37A1 nor SLC37A2 can couple functionally with G6Pase-α or G6Pase-β, and the antiporter activities of SLC37A1 or SLC37A2 are not inhibited by cholorogenic acid. Deficiencies in G6PT cause glycogen storage disease type Ib (GSD-Ib), a metabolic and immune disorder. To date, 91 separate SLC37A4 mutations, including 39 missense mutations, have been identified in GSD-Ib patients. Characterization of missense mutations has yielded valuable information on functionally important residues in the G6PT protein. The biological roles of the other SLC37 proteins remain to be determined and deficiencies have not yet been correlated to diseases. PMID:24745989

  7. Con: Phosphate binders in chronic kidney disease.

    PubMed

    Kestenbaum, Bryan

    2016-02-01

    Phosphate binders are prescribed to chronic kidney disease (CKD) patients based on associations of serum phosphate concentrations with mortality and calcification, experimental evidence for direct calcifying effects of phosphate on vascular smooth muscle tissue and the central importance of phosphate retention in CKD-mineral and bone disorder (CKD-MBD). Current knowledge regarding phosphate metabolism in CKD provides important insight into disease mechanisms and supports future clinical trials of phosphate binders in CKD patients to determine the impact of these medications on clinically relevant outcomes.The risks and benefits of phosphate binders cannot be inferred from association studies of serum phosphate concentrations, which are inconsistent and subject to confounding, animal-experimental data, which are based on conditions that differ from human disease, or physiological arguments, which are limited to known regulatory factors. Many interventions that targeted biochemical pathways suggested by association studies and suspected biological importance have yielded null or harmful results. Clinical trials of phosphate binders are of high clinical and scientific importance to nephrology. Demonstration of reduced rates of clinical disease in such trials could lead to important health benefits for CKD patients, whereas negative results would refocus efforts to understand and treat CKD-MBD. Clinical trials that employ highly practical or 'pragmatic' designs represent an optimal approach for determining the safety and effectiveness of phosphate binders in real-world settings. Absent clinical trial data, observational studies of phosphate binders in large CKD populations could provide important information regarding the benefits, risks and/or unintended side effects of these medications. PMID:26681747

  8. Antifeedant, larvicidal and growth inhibitory effects of ononitol monohydrate isolated from Cassia tora L. against Helicoverpa armigera (Hub.) and Spodoptera litura (Fab.) (Lepidoptera: Noctuidae).

    PubMed

    Baskar, Kathirvelu; Ignacimuthu, Savarimuthu

    2012-07-01

    Ononitol monohydrate isolated from the ethyl acetate extract of Cassia tora L. using column chromatography was evaluated for its antifeedant, larvicidal and growth inhibitory activities against Helicoverpa armigera and Spodoptera litura at different concentrations of 125, 250, 500 and 1000 ppm. Leaf disc no-choice method was used for the bioassay. The compound showed significant antifeedant, larvicidal and pupicidal activities against H. armigera and S. litura. The compound also prolonged the larval-pupal duration of the insect at all the tested concentrations. The activities were concentration dependent for both the insects. Ononitol could be used as an agent to prepare botanical new pesticidal formulations. PMID:22436590

  9. 21 CFR 182.6290 - Disodium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Disodium phosphate. 182.6290 Section 182.6290 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Sequestrants 1 § 182.6290 Disodium phosphate. (a) Product. Disodium...

  10. 21 CFR 137.175 - Phosphated flour.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... requirements of this section allowance is made for the added monocalcium phosphate. ... label declaration of ingredients, prescribed for flour by § 137.105, except that: (a) Monocalcium phosphate is added in a quantity not less than 0.25 percent and not more than 0.75 percent of the weight...

  11. 21 CFR 137.175 - Phosphated flour.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... requirements of this section allowance is made for the added monocalcium phosphate. ... label declaration of ingredients, prescribed for flour by § 137.105, except that: (a) Monocalcium phosphate is added in a quantity not less than 0.25 percent and not more than 0.75 percent of the weight...

  12. 21 CFR 137.175 - Phosphated flour.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... requirements of this section allowance is made for the added monocalcium phosphate. ... label declaration of ingredients, prescribed for flour by § 137.105, except that: (a) Monocalcium phosphate is added in a quantity not less than 0.25 percent and not more than 0.75 percent of the weight...

  13. 21 CFR 137.175 - Phosphated flour.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... requirements of this section allowance is made for the added monocalcium phosphate. ... label declaration of ingredients, prescribed for flour by § 137.105, except that: (a) Monocalcium phosphate is added in a quantity not less than 0.25 percent and not more than 0.75 percent of the weight...

  14. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Ferric phosphate. 184.1301 Section 184.1301 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DIRECT FOOD SUBSTANCES AFFIRMED AS GENERALLY RECOGNIZED AS SAFE Listing of Specific Substances Affirmed as GRAS § 184.1301 Ferric phosphate. (a)...

  15. 21 CFR 573.320 - Diammonium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS FOOD ADDITIVES PERMITTED IN FEED AND DRINKING WATER OF ANIMALS Food Additive Listing § 573.320 Diammonium phosphate. The food additive diammonium phosphate may be safely used in ruminant feed in accordance with the following prescribed conditions: (a) The food additive is...

  16. 21 CFR 573.320 - Diammonium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS FOOD ADDITIVES PERMITTED IN FEED AND DRINKING WATER OF ANIMALS Food Additive Listing § 573.320 Diammonium phosphate. The food additive diammonium phosphate may be safely used in ruminant feed in accordance with the following prescribed conditions: (a) The food additive is...

  17. 21 CFR 573.320 - Diammonium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... DRUGS, FEEDS, AND RELATED PRODUCTS FOOD ADDITIVES PERMITTED IN FEED AND DRINKING WATER OF ANIMALS Food Additive Listing § 573.320 Diammonium phosphate. The food additive diammonium phosphate may be safely used in ruminant feed in accordance with the following prescribed conditions: (a) The food additive is...

  18. 21 CFR 182.1217 - Calcium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Calcium phosphate. 182.1217 Section 182.1217 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SUBSTANCES GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1217 Calcium phosphate. (a)...

  19. Creatine Monohydrate and Conjugated Linoleic Acid Improve Strength and Body Composition Following Resistance Exercise in Older Adults

    PubMed Central

    Tarnopolsky, Mark; Zimmer, Andrew; Paikin, Jeremy; Safdar, Adeel; Aboud, Alissa; Pearce, Erin; Roy, Brian; Doherty, Timothy

    2007-01-01

    Aging is associated with lower muscle mass and an increase in body fat. We examined whether creatine monohydrate (CrM) and conjugated linoleic acid (CLA) could enhance strength gains and improve body composition (i.e., increase fat-free mass (FFM); decrease body fat) following resistance exercise training in older adults (>65 y). Men (N = 19) and women (N = 20) completed six months of resistance exercise training with CrM (5g/d)+CLA (6g/d) or placebo with randomized, double blind, allocation. Outcomes included: strength and muscular endurance, functional tasks, body composition (DEXA scan), blood tests (lipids, liver function, CK, glucose, systemic inflammation markers (IL-6, C-reactive protein)), urinary markers of compliance (creatine/creatinine), oxidative stress (8-OH-2dG, 8-isoP) and bone resorption (Ν-telopeptides). Exercise training improved all measurements of functional capacity (P<0.05) and strength (P<0.001), with greater improvement for the CrM+CLA group in most measurements of muscular endurance, isokinetic knee extension strength, FFM, and lower fat mass (P<0.05). Plasma creatinine (P<0.05), but not creatinine clearance, increased for CrM+CLA, with no changes in serum CK activity or liver function tests. Together, this data confirms that supervised resistance exercise training is safe and effective for increasing strength in older adults and that a combination of CrM and CLA can enhance some of the beneficial effects of training over a six-month period. Trial Registration. ClinicalTrials.gov NCT00473902 PMID:17912368

  20. FTIR, HATR and FT-Raman studies on the anhydrous and monohydrate species of maltose in aqueous solution.

    PubMed

    Iramain, Maximiliano Alberto; Davies, Lilian; Brandán, Silvia Antonia

    2016-06-16

    The structures of α- and β-maltose anhydrous and their corresponding monohydrated species were studied combining the FT-IR, FT-Raman and HATR spectra with DFT calculations. The four structures were optimized in gas and aqueous solution by using the hybrid B3LYP/6-31G* method. The self-consistent force field (SCRF) calculations together with the polarized continuum (PCM) model were used to study the systems in solution while the solvation energies were computed using the solvation model (SM). The calculated structural and vibrational properties could explain the anomerization of maltose in solution, as was reported in the literature while the natural bond orbital (NBO) analyses for those species support clearly the mutarotation equilibria between both forms in solution, evidencing the anhydrous forms the equilibrium: α (45%) ⇔ β (55%), similar to that experimentally reported at 20 °C. Bands of all the species observed in the vibrational spectra support the presence of the anomeric species of maltose in solution while the presence of dimeric species justify the intense IR bands observed in the higher wavenumbers region. The similar gap values for maltose and lactose probably justify that these sugars are reducing sugars while the high values in sucrose could explain that it is a non-reducing sugar. On the other hand, the sweeteners cyclamate and saccharine are most reactive in solution than the sugars maltose, lactose and sucrose, as expected due to their ionic characteristics. The predicted vibrational spectra for the four species of maltose show reasonable concordances with the corresponding experimental ones. The f(δC-O-C) force constants of the glycosidic bonds follow the tendency: maltose > lactose > sucrose. PMID:27131126

  1. Onset and duration of action of nasal sprays in seasonal allergic rhinitis patients: olopatadine hydrochloride versus mometasone furoate monohydrate.

    PubMed

    Patel, Deepen; Garadi, Rekha; Brubaker, Michael; Conroy, J Peter; Kaji, Yoshiko; Crenshaw, Krista; Whitling, Anna; Wall, G Michael

    2007-01-01

    Rapid relief of symptoms should be one of the primary goals of treatment for allergic rhinitis (AR). The onset and duration of action of olopatadine hydrochloride nasal spray, 665 mcg (OLO; Patanese), for seasonal AR (SAR) was evaluated in this study. This study was performed to determine the onset and duration of action of OLO compared with placebo spray, with mometasone furoate monohydrate, 50 mcg (MM; Nasonex), as a reference standard. This was a single center, single-dose, randomized, double-blinded parallel-group environmental exposure chamber study. Patients were primed at two 2-hour priming visits. Eligible patients were randomized to OLO, placebo spray, or MM, 2 sprays/nostril. Allergy symptoms (sneezing, runny, itchy, and stuffy nose) were rated by patients at 16 time points during 12 hours after dosing and patient satisfaction was assessed at 4 and 12 hours postdose. Safety was assessed by a review of adverse events, cardiovascular and nasal examination parameters. Four hundred twenty-five adult patients were randomized. OLO was superior to placebo spray in reducing total nasal symptoms (TNSS) within 30 minutes after dosing and maintained superiority for at least 12 hours (p < 0.05). The onset of MM was not observed until 150 minutes postdose and was smaller in magnitude compared with OLO. OLO was superior to both placebo spray (p < 0.0001) and MM (p < 0.05) in patient satisfaction. Treatment was well-tolerated with no safety concerns. OLO is superior to placebo spray and MM in reducing allergy symptoms; OLO has a rapid onset of action and a duration of effect of at least 12 hours. PMID:18034980

  2. EGCG decreases binding of calcium oxalate monohydrate crystals onto renal tubular cells via decreased surface expression of alpha-enolase.

    PubMed

    Kanlaya, Rattiyaporn; Singhto, Nilubon; Thongboonkerd, Visith

    2016-06-01

    Crystal retention on tubular cell surface inside renal tubules is considered as the earliest and crucial step for kidney stone formation. Therapeutics targeting this step would cease the development of kidney stone. This study thus aimed to investigate the potential role of epigallocatechin-3-gallate (EGCG), a major antioxidant found in green tea leaves, in the reduction of calcium oxalate monohydrate (COM) crystal binding onto renal tubular cells. Pretreatment of the cells with EGCG for up to 6 h significantly diminished crystal-binding capability in a dose-dependent manner. Indirect immunofluorescence assay without and with cell permeabilization followed by laser-scanning confocal microscopy revealed that EGCG significantly reduced surface expression of alpha-enolase, whereas its intracellular level was increased. Western blot analysis confirmed such contradictory changes in membrane and cytosolic fractions of EGCG-treated cells, whereas the total level in whole cell lysate remained unchanged. Moreover, overexpression of surface alpha-enolase and enhancement of cell-crystal adhesion induced by 10 mM sodium oxalate were completely abolished by EGCG. Taken together, these data indicate that EGCG decreases binding of COM crystals onto renal tubular cells by decreasing the surface expression of alpha-enolase via re-localization or inhibition of alpha-enolase shuttling from the cytoplasm to the plasma membrane. These findings may also explain the effects of EGCG in reducing COM crystal deposition in previous animal models of kidney stone disease. Thus, EGCG may be useful for the prevention of new or recurrent stone formation. PMID:26898643

  3. Phosphate rock resources of the United States

    USGS Publications Warehouse

    Cathcart, James Bachelder; Sheldon, Richard Porter; Gulbrandsen, Robert A.

    1984-01-01

    In 1980, the United States produced about 54 million tons of phosphate rock, or about 40 percent of the world's production, of which a substantial amount was exported, both as phosphate rock and as chemical fertilizer. During the last decade, predictions have been made that easily ruinable, low-cost reserves of phosphate rock would be exhausted, and that by the end of this century, instead of being a major exporter of phosphate rock, the United States might become a net importer. Most analysts today, however, think that exports will indeed decline in the next one or two decades, but that resources of phosphate are sufficient to supply domestic needs for a long time into the future. What will happen in the future depends on the actual availability of low-cost phosphate rock reserves in the United States and in the world. A realistic understanding of future phosphate rock reserves is dependent on an accurate assessment, now, of national phosphate rock resources. Many different estimates of resources exist; none of them alike. The detailed analysis of past resource estimates presented in this report indicates that the estimates differ more in what is being estimated than in how much is thought to exist. The phosphate rock resource classification used herein is based on the two fundamental aspects of a mineral resource(l) the degree of certainty of existence and (2) the feasibility of economic recovery. The comparison of past estimates (including all available company data), combined with the writers' personal knowledge, indicates that 17 billion metric tons of identified, recoverable phosphate rock exist in the United States, of which about 7 billion metric tons are thought to be economic or marginally economic. The remaining 10 billion metric tons, mostly in the Northwestern phosphate district of Idaho, are considered to be subeconomic, ruinable when some increase in the price of phosphate occurs. More than 16 billion metric tons probably exist in the southeastern Coastal Plain phosphate province, principally in Florida and North Carolina and offshore in the shallow Atlantic Ocean from North Carolina to southern Florida. This resource is considered to be hypothetical because it is based on geologic inference combined with sparse drilling data. Total resources of phosphate rock in the United States are sufficient to supply domestic demands for the foreseeable future, provided that drilling is done to confirm hypothetical resources and the chemistry of the deposits is determined. Mining and beneficiation techniques will have to be modified or improved, and new techniques will have to be developed so that these deposits can be profitably exploited.

  4. Apparent phosphate retrieval system in Bacillus cereus.

    PubMed Central

    Guddal, P H; Johansen, T; Schulstad, K; Little, C

    1989-01-01

    Bacillus cereus secretes three different phospholipases C. We studied the effect of Pi levels in the growth medium on the production of these exoenzymes. Production of both phosphatidylcholine-preferring phospholipase C and sphingomyelinase C was repressed by Pi in the growth medium, whereas production of phosphatidylinositol phospholipase C was unaffected. We also found that B. cereus secretes a phosphate-repressed alkaline phosphatase activity. Together with a previously reported highly efficient, active uptake system for Pi, these three phosphate-repressed exoenzyme activities seem to be part of a phosphate retrieval mechanism that operates under growth-limiting concentrations of Pi. In natural soil systems, which are the natural habitats of B. cereus, the scarcity of Pi is the major growth-limiting factor. A phosphate-repressed metalloprotease activity was also detected in culture supernatants of B. cereus. It is unclear whether this exoenzyme activity also participates in the proposed phosphate-scavenging system. PMID:2507529

  5. Phosphate Translocator of Isolated Guard-Cell Chloroplasts from Pisum sativum L. Transports Glucose-6-Phosphate.

    PubMed Central

    Overlach, S.; Diekmann, W.; Raschke, K.

    1993-01-01

    Chloroplasts were isolated from ruptured guard-cell protoplasts of the Argenteum mutant of Pisum sativum L. and purified by centrifugation through a Percoll layer. The combined volume of the intact plastids and the uptake of phosphate were determined by silicone oil-filtering centrifugation, using tritiated water and [14C]sorbitol as membrane-permeating and nonpermeating markers and [32P]phosphate as tracer for phosphate. The affinities of the phosphate translocator for organic phosphates were assessed by competition with inorganic phosphate. The affinities for dihydroxyacetone phosphate, 3-phosphoglycerate (PGA), and phosphoenolpyruvate were in the same order as those reported for mesophyll chloroplasts of several species. However, the guard-cell phosphate translocator had an affinity for glucose-6-phosphate that was as high as that for PGA. Guard-cell chloroplasts share this property with amyloplasts from the root of pea (H.W. Heldt, U.I. Flugge, S. Borchert [1991] Plant Physiol 95: 341-343). An ability to import glucose-6-phosphate enables guard-cell chloroplasts to synthesize starch despite the reported absence of a fructose-1,6-bisphosphatase activity in the plastids, which would be required if only C3 phosphates could enter through the translocator. PMID:12231774

  6. Phosphate Biomineralization of Cambrian Microorganisms

    NASA Technical Reports Server (NTRS)

    McKay, David S.; Rozanov, Alexei Yu.; Hoover, Richard B.; Westall, Frances

    1998-01-01

    As part of a long term study of biological markers (biomarkers), we are documenting a variety of features which reflect the previous presence of living organisms. As we study meteorites and samples returned from Mars, our main clue to recognizing possible microbial material may be the presence of biomarkers rather than the organisms themselves. One class of biomarkers consists of biominerals which have either been precipitated directly by microorganisms, or whose precipitation has been influenced by the organisms. Such microbe-mediated mineral formation may include important clues to the size, shape, and environment of the microorganisms. The process of fossilization or mineralization can cause major changes in morphologies and textures of the original organisms. The study of fossilized terrestrial organisms can help provide insight into the interpretation of mineral biomarkers. This paper describes the results of investigations of microfossils in Cambrian phosphate-rich rocks (phosphorites) that were found in Khubsugul, Northern Mongolia.

  7. Effect of Creatine Monohydrate Supplementation on Various Hematological and Serum Biochemical Parameters of Male Albino Mice following Neonatal Hypoxia-Ischemia Encephalopathy

    PubMed Central

    Nazir, Nabia; Gillani, Quratulane; Akbar, Atif

    2013-01-01

    Background. Present study was designed to report the effect of 2% creatine monohydrate supplementation for 8, 12 and 15 weeks on hematology and serum biochemical profile of male albino mouse following hypoxic ischemic insult on postnatal day 10. Methods. 66 Blood samples (2% creatine monohydrate supplemented (N = 34) and unsupplemented (N = 32)) were analyzed for various hematological (blood glucose, packed cell volume, total WBC count, total RBC count) and serum biochemical parameters (cholesterol, AST, ALT, HDL, LDL, total protein, triglycerides). Results. ALT had higher concentrations in mice feeding on normal diet for 8 (P > 0.01) and 12 weeks (P > 0.01) following asphyxia and in 12 weeks treatment without asphyxia (P = 0.006) when compared with the creatine supplemented mice. LDL (P = 0.011) and cholesterol (P > 0.01) had higher concentrations in mice on normal diet for 12 weeks following hypoxia ischemia. Cholesterol (P > 0.01) in 12 and glucose (P = 0.006) in 15 week treatment group had significantly lower concentrations in creatine supplemented male albino mice when compared with untreated group following hxpoic-ischemic insult. Conclusion. We concluded that creatine supplementation following hypoxic ischemic insult helps in maintain the normal blood chemistry. PMID:24170981

  8. Genotoxicity evaluation of benzene, di(2-ethylhexyl) phthalate, and trisodium ethylenediamine tetraacetic acid monohydrate using a combined rat comet/micronucleus assays.

    PubMed

    Kitamoto, Sachiko; Matsuyama, Ryoko; Uematsu, Yasuaki; Ogata, Keiko; Ota, Mika; Yamada, Toru; Miyata, Kaori; Kimura, Juki; Funabashi, Hitoshi; Saito, Koichi

    2015-07-01

    As a part of the Japanese Center for the Validation of Alternative Methods (JaCVAM)-initiative international validation study of the in vivo alkaline comet assay (comet assay), we examined DNA damage in the liver, stomach, and bone marrow of rats dosed orally three times with up to 2000 mg/kg of benzene, di(2-ethylhexyl) phthalate, and trisodium ethylenediamine tetraacetic acid monohydrate. All three compounds gave negative results in the liver and stomach. In addition, a bone marrow comet and micronucleus analysis revealed that benzene, but not di(2-ethylhexyl) phthalate or trisodium ethylenediamine tetraacetic acid monohydrate induced a significant increase in the median % tail DNA and micronucleated polychromatic erythrocytes, compared with the respective concurrent vehicle control. These results were in good agreement with the previously reported genotoxicity findings for each compound. The present study has shown that combining the micronucleus test with the comet assay and carrying out these analyses simultaneously is effective in clarifying the mechanism of action of genotoxic compounds such as benzene. PMID:26212304

  9. Salicylanilide diethyl phosphates as cholinesterases inhibitors.

    PubMed

    Krátký, Martin; Štěpánková, Šárka; Vorčáková, Katarína; Vinšová, Jarmila

    2015-02-01

    Based on the presence of dialkyl phosphate moiety, we evaluated twenty-seven salicylanilide diethyl phosphates (diethyl [2-(phenylcarbamoyl)phenyl] phosphates) for the inhibition of acetylcholinesterase (AChE) from electric eel (Electrophorus electricus L.) and butyrylcholinesterase (BChE) from equine serum. Ellman's spectrophotometric method was used. The inhibitory activity (expressed as IC50 values) was compared with that of the established drugs galantamine and rivastigmine. Salicylanilide diethyl phosphates showed significant activity against both cholinesterases with IC50 values from 0.903 to 86.3 μM. IC50s for BChE were comparatively lower than those obtained for AChE. All of the investigated compounds showed higher inhibition of AChE than rivastigmine, and six of them inhibited BChE more effectively than both rivastigmine and galantamine. In general, derivatives of 4-chlorosalicylic acid showed enhanced activity when compared to derivatives of 5-halogenated salicylic acids, especially against BChE. The most effective inhibitor of AChE was O-{5-chloro-2-[(3-bromophenyl)carbamoyl]phenyl} O,O-diethyl phosphate with IC50 of 35.4 μM, which is also one of the most potent inhibitors of BChE. O-{5-Chloro-2-[(3,4-dichlorophenyl)carbamoyl]phenyl} O,O-diethyl phosphate exhibited in vitro the strongest inhibition of BChE (0.90 μM). Salicylanilide diethyl phosphates act as pseudo-irreversible cholinesterases inhibitors. PMID:25462625

  10. FGF23 and Phosphate Wasting Disorders

    PubMed Central

    Huang, Xianglan; Jiang, Yan; Xia, Weibo

    2013-01-01

    A decade ago, only two hormones, parathyroid hormone and 1,25(OH)2D, were widely recognized to directly affect phosphate homeostasis. Since the discovery of fibroblast growth factor 23 (FGF23) in 2000 (1), our understanding of the mechanisms of phosphate homeostasis and of bone mineralization has grown exponentially. FGF23 is the link between intestine, bone, and kidney together in phosphate regulation. However, we still do not know the complex mechanism of phosphate homeostasis and bone mineralization. The physiological role of FGF23 is to regulate serum phosphate. Secreted mainly by osteocytes and osteoblasts in the skeleton (2,3), it modulates kidney handling of phosphate reabsorption and calcitriol production. Genetic and acquired abnormalities in FGF23 structure and metabolism cause conditions of either hyper-FGF23 or hypo-FGF23. Hyper-FGF23 is related to hypophosphatemia, while hypo-FGF23 is related to hyperphosphatemia. Both hyper-FGF23 and hypo-FGF23 are detrimental to humans. In this review, we will discuss the pathophysiology of FGF23 and hyper-FGF23 related renal phosphate wasting disorders (4). PMID:26273497

  11. Are Polyphosphates or Phosphate Esters Prebiotic Reagents?

    NASA Technical Reports Server (NTRS)

    Keefe, Anthony D.; Miller, Stanley L.

    1995-01-01

    It is widely held that there was a phosphate compound in prebiotic chemistry that played the role of adenosine triphosphate and that the first living organisms had ribose-phosphate in the backbone of their genetic material. However, there are no known efficient prebiotic synthesis of high-energy phosphates or phosphate esters. We review the occurrence of phosphates in nature, the efficiency of the volcanic synthesis of P4O10, the efficiency of polyphosphate synthesis by heating phosphate minerals under geological conditions, and the use of high-energy organic compounds such as cyanamide or hydrogen cyanide. These are shown to be inefficient processes especially when the hydrolysis of the polyphosphates is taken into account. For example, if a whole atmosphere of methane or carbon monoxide were converted to cyanide which somehow synthesized polyphosphates quantitatively, the polyphosphate concentration in the ocean would still have been insignificant. We also attempted to find more efficient high-energy polymerizing agents by spark discharge syntheses, but without success. There may still be undiscovered robust prebiotic syntheses of polyphosphates, or mechanisms for concentrating them, but we conclude that phosphate esters may not have been constituents of the first genetic material. Phosphoanhydrides are also unlikely as prebiotic energy sources.

  12. Levels of Phosphate Esters in Spirodela

    PubMed Central

    Bieleski, R. L.

    1968-01-01

    The duckweed Spirodela oligorrhiza was grown in sterile nutrient solutions that contained 1 mm phosphate-32P at various specific activities. In solutions with activities higher than 2 μc per μmole per ml, plant growth was inhibited after a time, and the physical appearance of the plants was affected. The critical level of radiation, at which growth was first affected, corresponded to 5 kilorads. Plants were grown for 9 days (5 generations) in a culture solution containing phosphate at 0.5 μc per μmole per ml (radiation load approx 0.5 kilorads) so that all phosphorus-containing materials in the tissue became uniformly labeled. The various radioactive compounds were extracted, chromatographed, identified, and their radioactivity was measured. From this radioactivity plus the specific activity of the supplied phosphate, the amount of each compound was calculated. The data constitute a complete balance-sheet for phosphorus in a plant tissue. The identity of 98% of the phosphorus in the tissue was determined. Inorganic phosphate (32,700 mμmoles/g fr wt) was the predominant phosphorus-containing compound; RNA (5100 mμmoles P/g fr wt) was the main organic phosphate; phosphatidyl choline (1600 mμmoles/g fr wt) was the main phospholipid, and glucose-6-phosphate (500 mμmoles/g fr wt) the main acid-soluble phosphate ester. Amounts of other phosphorus compounds are given. Images PMID:16656910

  13. Fibroblast growth factor-23 relationship to dietary phosphate and renal phosphate handling in healthy young men.

    PubMed

    Ferrari, Serge L; Bonjour, Jean-Philippe; Rizzoli, René

    2005-03-01

    The renal handling of inorganic phosphate (Pi) is controlled not only by PTH, but also by hitherto undetermined mechanisms dependent on phosphate intake. Recently, fibroblast growth factor (FGF)-23 was identified as a novel phosphaturic factor in tumor-induced osteomalacia and autosomal-dominant hypophosphatemic rickets. We hypothesized that phosphate intake could influence FGF-23 concomitantly to the changes in renal Pi handling. Twenty-nine healthy males were subjected to a 5-d low-phosphate diet and a phosphate binder, followed by a high-phosphate diet including supplements. Concomitant modifications in calcium intake allowed minimizing PTH changes in response to dietary phosphate. Serum FGF-23 levels significantly decreased on the low-phosphate diet, then increased with the oral phosphate load. Changes in FGF-23 were positively correlated with changes in 24-h urinary Pi excretion and negatively correlated with changes in the maximal tubular reabsorption of Pi and 1,25(OH)(2)D(3) (calcitriol), whereas PTH was not. In multivariate analysis, changes in FGF-23 remained the most significantly correlated to changes in 1,25(OH)(2)D(3) and maximal tubular reabsorption of Pi. Moreover, FGF-23 was positively correlated to serum osteocalcin, a marker of osteoblastic activity. In summary, FGF-23 was inversely related to renal Pi transport and serum calcitriol levels in healthy young men. These data suggest that FGF-23 may be implicated in the physiological regulation of Pi homeostasis in response to dietary phosphate changes, independent of PTH. PMID:15613425

  14. Aquatic Toxicity Assessment of Phosphate Compounds

    PubMed Central

    Kim, Eunju; Yoo, Sunkyoung; Ro, Hee-Young; Han, Hye-Jin; Baek, Yong-Wook; Eom, Ig-Chun; Kim, Pilje; Choi, Kyunghee

    2013-01-01

    Objectives Tricalcium phosphate and calcium hydrogenorthophosphate are high production volume chemicals, mainly used as foodstuff additives, pharmaceuticals, lubricants, synthetic resin, and disinfectants. Phosphate has the potential to cause increased algal growth leading to eutrophication in the aquatic environment. However, there is no adequate information available on risk assessment or acute and chronic toxicity. The aim of this research is to evaluate the toxic potential of phosphate compounds in the aquatic environment. Methods An aquatic toxicity test of phosphate was conducted, and its physico-chemical properties were obtained from a database recommended in the Organization for Economic Cooperation and Development (OECD) guidance manual. An ecotoxicity test using fish, Daphnia, and algae was conducted by the good laboratory practice facility according to the OECD TG guidelines for testing of chemicals, to secure reliable data. Results The results of the ecotoxicity tests of tricalcium phosphate and calcium hydrogenorthophosphate are as follows: In an acute toxicity test with Oryzias latipes, 96 hr 50% lethal concentration (LC50) was >100 (measured:>2.14) mg/L and >100 (measured: >13.5) mg/L, respectively. In the Daphnia test, 48 hr 50% effective concentration (EC50) was >100 (measured: >5.35) mg/L and >100 (measured: >2.9) mg/L, respectively. In a growth inhibition test with Pseudokirchneriella subcapitata, 72 hr EC50 was >100 (measured: >1.56) mg/L and >100 (measured: >4.4) mg/L, respectively. Conclusions Based on the results of the ecotoxicity test of phosphate using fish, Daphnia, and algae, L(E)C50 was above 100 mg/L (nominal), indicating no toxicity. In general, the total phosphorus concentration including phosphate in rivers and lakes reaches levels of several ppm, suggesting that phosphate has no toxic effects. However, excessive inflow of phosphate into aquatic ecosystems has the potential to cause eutrophication due to algal growth. PMID:23440935

  15. BISMUTH PHOSPHATE CARRIER PROCESS FOR Pu RECOVERY

    DOEpatents

    Finzel, T.G.

    1959-02-01

    An improvement in the bismuth phosphate carrier precipitation process for recovering plutonium is described. It has been found that a more granular and more easily filterable carrier precipitiite is formed if the addition of the bismuth and phosphate ions is effected by first adding 9/10 of the bismuth ions necessary, then slowly adding all of the source of the phosphate ions to be incorporated in the precipitate, while digesting at 75 C and afterwards incorporating the remainder of the total bismuth ions necessary

  16. Phosphate-bonded calcium aluminate cements

    DOEpatents

    Sugama, Toshifumi

    1993-01-01

    A method is described for making a rapid-setting phosphate-bonded cementitious material. A powdered aluminous cement is mixed with an aqueous solution of ammonium phosphate. The mixture is allowed to set to form an amorphous cementitious material which also may be hydrothermally treated at a temperature of from about 120.degree. C. to about 300.degree. C. to form a crystal-containing phosphate-bonded material. Also described are the cementitious products of this method and the cement composition which includes aluminous cement and ammonium polyphosphate.

  17. Phosphate-bonded calcium aluminate cements

    DOEpatents

    Sugama, T.

    1993-09-21

    A method is described for making a rapid-setting phosphate-bonded cementitious material. A powdered aluminous cement is mixed with an aqueous solution of ammonium phosphate. The mixture is allowed to set to form an amorphous cementitious material which also may be hydrothermally treated at a temperature of from about 120 C to about 300 C to form a crystal-containing phosphate-bonded material. Also described are the cementitious products of this method and the cement composition which includes aluminous cement and ammonium polyphosphate. 10 figures.

  18. Improved phosphate clearances with polycarbonate membranes.

    PubMed

    Fleming, L W; Hudson, S W; Stewart, W K

    1982-01-01

    Clearance studies of urea, creatinine and inorganic phosphate have been carried out using polycarbonate dialysers on 20 occasions in two patients undergoing routine maintenance haemodialysis. Clearances were calculated using plasma concentrations and both measured blood flow and calculated plasma flow. Urea and creatinine clearances were comparable to those obtained with cellulose-based dialysers, but phosphate clearances were relatively increased, averaging over 70% of urea clearances. All clearances were reduced as TMP values increased, a feature at variance with the usual situation with cellulose membranes. Polycarbonate dialysers have the advantage of higher relative phosphate clearances in addition to the other advantages claimed for them. PMID:7182087

  19. [Adsorption of Phosphate by Lanthanum Hydroxide/Natural Zeolite Composites from Low Concentration Phosphate Solution].

    PubMed

    Lin, Jian-wei; Wang, Hong; Zhan, Yan-hui; Chen, Dong-mei

    2016-01-15

    A series of composites of lanthanum hydroxide/natural zeolite ( La( OH) 3/NZ composites) were prepared by co-precipitation method, and these composites were used as adsorbents to remove phosphate from aqueous solution. The phosphate adsorption capacities of different composites prepared with different precipitated pH values were compared in batch mode. The adsorption characteristics of phosphate from aqueous solution on the La(OH)3/NZ composite prepared with the precipitated pH value of 11 was investigated using batch experiments. The results showed that the La(OH)3/NZ composite prepared with the precipitated pH values of 5-7 and 13 had a low adsorption capacity for phosphate in aqueous solution, while the La( OH) 3/NZ composites prepared with the precipitated pH values of 9-12 exhibited much higher phosphate adsorption capacity. The phosphate adsorption capacity of the La (OH)3/NZ composite increased with the increase of the precipitated pH value from 9 to 11, but remained basically unchanged with the increase of the precipitated pH value from 11 to 12. The equilibrium adsorption data of phosphate from aqueous solution on the La ( OH ) 3/NZ composite prepared with the precipitated pH value of 11 could be described by the Langmuir isotherm model with the predicted maximum phosphate adsorption of 44 mg x g(-1) (phosphate solution pH 7 and 30 degrees C). The kinetic data of phosphate adsorption from low concentration phosphate solution on the La(OH)3/NZ composite prepared with the precipitated pH value of 11 well followed a pseudo-second-order model. The presence of Cl- and SO4(2-) in low concentration phosphate solution had no negative effect on phosphate adsorption onto the La(OH)3/NZ composite prepared with the precipitated pH value of 11, while the presence of HCO3- slightly inhibited the adsorption of phosphate. Coexisting humic acid had a negative effect on the adsorption of phosphate at low concentration on the La(OH)3/NZ composite prepared with the precipitated pH value of 11. The mechanism for phosphate adsorption onto the La(OH)3/NZ composite prepared with the precipitated pH value of 11 was explained by the ligand exchange process. Results of this work indicate that the La(OH)3/NZ composite prepared with the precipitated pH value of 11 is a promising adsorbent material for the removal of low concentration phosphate from water/wastewater. PMID:27078960

  20. Glucose-6-phosphate dehydrogenase deficiency.

    PubMed

    Cappellini, M D; Fiorelli, G

    2008-01-01

    Glucose-6-phosphate dehydrogenase (G6PD) deficiency is the most common human enzyme defect, being present in more than 400 million people worldwide. The global distribution of this disorder is remarkably similar to that of malaria, lending support to the so-called malaria protection hypothesis. G6PD deficiency is an X-linked, hereditary genetic defect due to mutations in the G6PD gene, which cause functional variants with many biochemical and clinical phenotypes. About 140 mutations have been described: most are single base changes, leading to aminoacid substitutions. The most frequent clinical manifestations of G6PD deficiency are neonatal jaundice, and acute haemolytic anaemia, which is usually triggered by an exogenous agent. Some G6PD variants cause chronic haemolysis, leading to congenital non-spherocytic haemolytic anaemia. The most effective management of G6PD deficiency is to prevent haemolysis by avoiding oxidative stress. Screening programmes for the disorder are undertaken, depending on the prevalence of G6PD deficiency in a particular community. PMID:18177777

  1. Micro-mechanical model of calcium oxalate monohydrate aggregation in supersaturated solutions: Effect of crystal form and seed concentration

    NASA Astrophysics Data System (ADS)

    Pitt, K.; Mitchell, G. P.; Ray, A.; Heywood, B. R.; Hounslow, M. J.

    2012-12-01

    In this paper we report crystal growth and aggregation behaviour for calcium oxalate monohydrate (COM) in a stirred tank for two differing seed types - rounded and well defined - at various seed loadings. Initially we used our previously developed model [1] to study the growth and aggregation. In this model a dimensionless strength, termed the Mumtaz number, has been formulated, which accounts for the effects of stirring, supersaturation and particle size on the aggregation rate of COM. Subtle differences in growth and aggregation rates were observed between the two populations of crystals; the model was unable to describe this behaviour. These differences were attributed to their different surface characteristics. Growth and aggregation kinetic parameters were also seen to be highly dependent on seed loading. This is attributed to poisoning by an unknown trace impurity, the effect of which is dependent on seed loading. This has led to the development of a new model to account for both surface characteristics and the presence of a trace impurity that adsorbs onto the surface of crystals pinning growth steps. At low seeds loadings, surface coverage by the impurity is higher and so growth rates are reduced. These results are very well described by an extension of the approach of Weaver et al. [2]. We use Liew et al.'s [1] model to represent aggregation by a collision efficiency that depends on a modified Mumtaz number. This model requires the determination of a simple group of parameters that we term the 'aggregation tendency'. The relationship between aggregation tendency and growth rate constant suggests that aggregation is in fact controlled by the growth rate of some high-energy facets not expressed macroscopically. The fact that aggregation tendency increases with surface coverage of impurity further suggests that the presence of impurity gives rise to longer or more numerous linear features along which initial contact between crystals takes place. The combined growth and aggregation models are capable of describing all the experiments reported here for both seed types and over a range of seed loadings.

  2. Effect of dietary creatine monohydrate supplementation on muscle lipid peroxidation and antioxidant capacity of transported broilers in summer.

    PubMed

    Wang, X F; Zhu, X D; Li, Y J; Liu, Y; Li, J L; Gao, F; Zhou, G H; Zhang, L

    2015-11-01

    This experiment was to evaluate the effect of dietary supplementation with creatine monohydrate (CMH) during the finishing period on the muscle lipid peroxidation and antioxidant capacity of broilers that experienced transport stress in summer. A total of 320 male Arbor Acres broilers (28 d in age) were randomly allotted to 3 dietary treatments including a basal control diet without additional CMH (160 birds), or with 600 (80 birds) or 1,200 mg/kg (80 birds) CMH for 14 d. On the morning of d 42, after an 8-h fast, the birds fed the basal diets were divided into 2 equal groups, and all birds in the 4 groups of 80 birds were transported according to the following protocols: 1) a 0.75-h transport of birds on basal diets (as a lower-stress control group), 2) a 3-h transport of birds on basal diets, 3) a 3-h transport of birds on 600 or 4) 1,200 mg/kg CMH supplementation diets. The results showed that the 3-h transport decreased the concentration of creatine (Cr) in both the pectoralis major (PM) and the tibialis anterior (TA) muscles, increased the concentration of phosphocreatine (PCr) and PCr/Cr ratio in PM muscle, and elevated the concentrations of thiobarbituric acid-reactive substances and the activities of total superoxide dismutase and glutathione peroxidase in both the PM and TA muscles of birds (P < 0.05). In addition, transport also upregulated mRNA expression of avian uncoupling protein and heat shock protein 70 in both the PM and TA muscles, as well as avian peroxisome proliferator-activated receptor γ coactivator-1α in the TA muscle (P < 0.05). Dietary supplementation with 1,200 mg/kg CMH increased the concentrations of Cr and PCr in PM muscle, and Cr in TA muscle than those in the 3-h transport group (P < 0.05). However, contrary to our hypothesis, dietary CMH did not alter the measured parameters in relation to muscle lipid peroxidation and antioxidant capacity affected by 3-h transport (P > 0.05). These results indicate that dietary CMH supplementation does not provide any significant protection via directly scavenging free radicals or increased antioxidant capacity of transported broilers. PMID:26371332

  3. The oxygen isotopic composition of phosphate in Elkhorn Slough, California: A tracer for phosphate sources

    NASA Astrophysics Data System (ADS)

    McLaughlin, Karen; Cade-Menun, Barbara J.; Paytan, Adina

    2006-11-01

    Elkhorn Slough, a small seasonal estuary in central California, has been subjected to increased nutrient loading from agricultural and other non-point sources. However, because nutrients do not behave conservatively, tracing nutrient sources and cycling in ecosystems like Elkhorn Slough has been difficult to assess. This is particularly true of phosphorus (P), which has only one stable isotope and cannot be used as an isotopic tracer. However, isotopic fractionation of oxygen in phosphate at surface water temperatures only occurs as a result of enzyme-mediated, biochemical reactions. Thus, if phosphate demand is low relative to input and is not heavily cycled within the ecosystem, the ?18O of phosphate will reflect the isotopic composition of phosphate sources to the system. We utilized the ?18O of dissolved inorganic phosphate (DIP) within the main channel of the slough and nearby Moss Landing Harbor and the ?18O of reactive phosphate from sediment and soil samples collected within the watershed to understand phosphate sources and cycling within Elkhorn Slough. Trends in the ?18O of DIP were seasonally consistent with high values near the mouth reflecting oceanic phosphate (19.1-20.3), dropping to a minimum value near Hummingbird Island in the central slough (point source, 14.1-14.4), and increasing again near the head of the slough, reflecting fertilizer input (18.9-19.3). Reactive phosphate ?18O values extracted from sediments and soils in the watershed range from 10.6 in a drainage ditch to 22.3 in creek sediments near agriculture fields. The wide range in phosphate ?18O values reflects the variations in land use and application of different fertilizers in this agriculturally dominated landscape. These data suggest that phosphate ?18O can be an effective tool for identifying P sources and understanding phosphate dynamics in estuarine ecosystems.

  4. Enzyme activity in dialkyl phosphate ionic liquids

    SciTech Connect

    Thomas, M.F.; Dunn, J.; Li, L.-L.; Handley-Pendleton, J. M.; van der lelie, D.; Wishart, J. F.

    2011-12-01

    The activity of four metagenomic enzymes and an enzyme cloned from the straw mushroom, Volvariellavolvacea were studied in the following ionic liquids, 1,3-dimethylimidazolium dimethyl phosphate, [mmim][dmp], 1-ethyl-3-methylimidazolium dimethyl phosphate, [emim][dmp], 1-ethyl-3-methylimidazolium diethyl phosphate, [emim][dep] and 1-ethyl-3-methylimidazolium acetate, [emim][OAc]. Activity was determined by analyzing the hydrolysis of para-nitrobenzene carbohydrate derivatives. In general, the enzymes were most active in the dimethyl phosphate ionic liquids, followed by acetate. Generally speaking, activity decreased sharply for concentrations of [emim][dep] above 10% v/v, while the other ionic liquids showed less impact on activity up to 20% v/v.

  5. Airborne radioactivity surveys for phosphate in Florida

    USGS Publications Warehouse

    Moxham, Robert M.

    1953-01-01

    Airborne radioactivity surveys totalling 5,600 traverse miles were made in ten areas in Florida, which were thought to be geologically favorable for the occurrence of uraniferous phosphate deposits. Abnormal radioactivity was recorded in eight of the ten areas surveyed. The anomalies are located in Bradford, Clay, Columbia, DeSoto, Dixie, Lake, Marion, Orange, Sumter, Taylor, and Union Counties. Two of the anomalies were investigated briefly on the ground. One resulted from a deposit of river-pebble phosphate in the Peace River valley; samples of the river pebble contain an average of 0.013 percent equivalent uranium. The other anomaly resulted from outcrops of leached phosphate rock containing as much as 0.016 percent equivalent uranium. Several anomalies in other areas were recorded at or near localities where phosphate deposits have been reported to occur.

  6. Airborne radioactivity surveys for phosphate in Florida

    USGS Publications Warehouse

    Moxham, Robert M.

    1954-01-01

    Airborne radioactivity surveys totaling 5, 600 traverse miles were made in 10 areas in Florida, which were thought to be geologically favorable for deposits of uraniferous phosphate. Abnormal radioactivity was recorded in 8 of the 10 areas surveyed. The anomalies are located in Bradford, Clay, Columbia, DeSoto, Dixie, Lake, Marion, Orange, Sumter, Taylor, and Union Counties. Two of the anomalies were investigated briefly on the ground. One resulted from a deposit of river-pebble phosphate in the Peace River valley; the river-pebble samples contain an average of 0.013 percent equivalent uranium. The other anomaly resulted from outcrops of leached phosphatic rock containing as much as 0. 016 percent equivalent uranium. Several anomalies in other areas were recorded at or near localities where phosphate deposits have been reported.

  7. Using phosphate supplementation to reverse hypophosphatemia and phosphate depletion in neurological disease and disturbance.

    PubMed

    Håglin, Lena

    2016-06-01

    Hypophosphatemia (HP) with or without intracellular depletion of inorganic phosphate (Pi) and adenosine triphosphate has been associated with central and peripheral nervous system complications and can be observed in various diseases and conditions related to respiratory alkalosis, alcoholism (alcohol withdrawal), diabetic ketoacidosis, malnutrition, obesity, and parenteral and enteral nutrition. In addition, HP may explain serious muscular, neurological, and haematological disorders and may cause peripheral neuropathy with paresthesias and metabolic encephalopathy, resulting in confusion and seizures. The neuropathy may be improved quickly after proper phosphate replacement. Phosphate depletion has been corrected using potassium-phosphate infusion, a treatment that can restore consciousness. In severe ataxia and tetra paresis, complete recovery can occur after adequate replacement of phosphate. Patients with multiple risk factors, often with a chronic disease and severe HP that contribute to phosphate depletion, are at risk for neurologic alterations. To predict both risk and optimal phosphate replenishment requires assessing the nutritional status and risk for re-feeding hypophosphatemia. The strategy for correcting HP depends on the severity of the underlying disease and the goal for re-establishing a phosphate balance to limit the consequences of phosphate depletion. PMID:25909152

  8. Isolation of phosphate-solubilizing fungus and its application in solubilization of rock phosphates.

    PubMed

    Wu, Yingben; He, Yuelin; Yin, Hongmei; Chen, Wei; Wang, Zhen; Xu, Lijuan; Zhang, Aiqun

    2012-12-01

    Microorganisms have been obtained to improve the agronomic value of rock phosphates (RPs), but the phosphorus solubilizing rate by these approaches is very slow. It is important to explore a high-efficient phosphate-solubilizing approach with a kind of microorganisms. This study aimed to isolate a high-efficient level of phosphate-solubilizing fungus from rhizosphere soil samples phosphate mines (Liuyang County, Hunan province, China) and apply it in solubilization of RPs. The experiments were carried out by the conventional methodology for morphological and biochemical fungus characterization and the analysis of 18s rRNA sequence. Then the effects of time, temperature, initial pH, phosphorus (P) sources, RPs concentration, shaking speed and silver ion on the content of soluble P released by this isolate were investigated. The results showed this isolate was identified as Galactomyces geotrichum P14 (P14) in GeneBank and the maximum amount of soluble P was 1252.13 mg L(-1) within 40 h in a modified phosphate growth agar's medium (without agar) where contained tricalcium phosphate (TCP) as sole phosphate source. At the same time, it could release phosphate and solubilize various rock phosphates. The isolated fungus can convert RPs from insoluble form into plant available form and therefore it hold great potential for biofertilizers to enhance soil fertility and promote plant growth. PMID:24261118

  9. Phosphate rock costs, prices and resources interaction.

    PubMed

    Mew, M C

    2016-01-15

    This article gives the author's views and opinions as someone who has spent his working life analyzing the international phosphate sector as an independent consultant. His career spanned two price hike events in the mid-1970's and in 2008, both of which sparked considerable popular and academic interest concerning adequacy of phosphate rock resources, the impact of rising mining costs and the ability of mankind to feed future populations. An analysis of phosphate rock production costs derived from two major industry studies performed in 1983 and 2013 shows that in nominal terms, global average cash production costs increased by 27% to $38 per tonne fob mine in the 30 year period. In real terms, the global average cost of production has fallen. Despite the lack of upward pressure from increasing costs, phosphate rock market prices have shown two major spikes in the 30 years to 2013, with periods of less volatility in between. These price spike events can be seen to be related to the escalating investment cost required by new mine capacity, and as such can be expected to be repeated in future. As such, phosphate rock price volatility is likely to have more impact on food prices than rising phosphate rock production costs. However, as mining costs rise, recycling of P will also become increasingly driven by economics rather than legislation. PMID:26412420

  10. Amorphous calcium (ortho)phosphates.

    PubMed

    Dorozhkin, Sergey V

    2010-12-01

    Amorphous calcium phosphates (ACPs) represent a unique class of biomedically relevant calcium orthophosphate salts, having variable chemical but essentially identical glass-like physical properties, in which there is neither translational nor orientational long-range ordering of the atomic positions. Normally, ACPs are the first solid phases, precipitated after a rapid mixing of aqueous solutions containing ions of Ca(2+) and PO₄³⁻; however, other production techniques are known. Interestingly, ACPs prepared by wet-chemical techniques were found to have a relatively constant chemical composition over a relatively wide range of preparation conditions, which suggests the presence of a well-defined local structural unit, presumably with the structure of Ca₉(PO₄)₆ - so-called Posner cluster. However, the presence of similar clusters in ACPs produced by other techniques remains uncertain. All ACPs are thermodynamically unstable compounds and, unless stored in dry conditions or doped by stabilizers, spontaneously tend to transform to crystalline calcium orthophosphates, mainly to calcium apatites. This solution instability of ACPs and their easy transformation to crystalline phases are of a great biological relevance. Specifically, the initiating role ACPs play in matrix vesicle biomineralization raises the importance of ACPs from a mere laboratory curiosity to that of a key intermediate in skeletal calcification. In addition, due to significant chemical and structural similarities with calcified mammalian tissues, as well as excellent biocompatibility and bioresorbability, all types of ACPs are very promising candidates for the manufacture of artificial bone grafts. This review summarizes the current knowledge on the occurrence, preparation, composition, structure, major properties and biomedical applications of ACPs. To assist readers in looking for the specific details on ACPs, a great number of references have been collected and systematized. PMID:20609395

  11. Phosphate separation and recovery from wastewater by novel electrodialysis.

    PubMed

    Zhang, Yang; Desmidt, Evelyn; Van Looveren, Arnaud; Pinoy, Luc; Meesschaert, Boudewijn; Van der Bruggen, Bart

    2013-06-01

    Stimulated by the depletion of phosphate resources, phosphate recovery systems have been studied in recent years. The use of struvite reactors has proven to be an effective phosphate recovery process. However, the struvite reactor effluent still consists of an excessive amount of phosphate that cannot be recovered nor can be directly discharged. In this study, selectrodialysis (SED) was used to improve the efficiency of phosphate recovery from a struvite reactor: SED was implemented in such a way that phosphate from the effluent of an USAB (upflow anaerobic sludge blanket) reactor was transferred to the recycled effluent of a struvite reactor. Prior to the experiments, synthetic water with chloride and phosphate was used to characterize the efficiency of SED for phosphate separation. Results indicate that SED was successful in concentrating phosphate from the feed stream. The initial current efficiency reached 72%, with a satisfying (9 mmol L(-1)) phosphate concentration. In the experiments with the anaerobic effluent as the phosphate source for enrichment of the effluent of the struvite reactor, the phosphate flux was 16 mmol m(-2) h(-1). A cost evaluation shows that 1 kWh electricity can produce 60 g of phosphate by using a full scale stack, with a desalination rate of 95% on the feed wastewater. Finally, a struvite precipitation experiment shows that 93% of phosphate can be recovered. Thus, an integrated SED-struvite reactor process can be used to improve phosphate recovery from wastewater. PMID:23651001

  12. Ureolytic phosphate precipitation from anaerobic effluents.

    PubMed

    Desmidt, E; Verstraete, W; Dick, J; Meesschaert, B D; Carballa, M

    2009-01-01

    In this work, the elimination of phosphate from industrial anaerobic effluents was evaluated at lab-scale. For that purpose, the ureolytic method previously developed for the precipitation of Ca(2 + ) from wastewater as calcite was adapted for the precipitation of phosphate as struvite. In the first part of the study, computer simulations using MAPLE and PHREEQC were performed to model phosphate precipitation from wastewater as struvite. The results obtained showed that relative high concentrations of ammonium and magnesium are needed to precipitate phosphate as struvite. The total molar concentrations ratio of Mg(2 + ):PO(4) (3-)-P:NH(4) (+) required to decrease PO(4) (3-)-P concentrations from 20 to 6 mg PO(4) (3-)-P/l at pH 8.4-8.5 was estimated on 4.6:1:8. In the second part of the study, lab-scale experiments with either synthetic wastewater or the anaerobic effluent from a vegetable processing industry were carried out in batch and continuous mode. Overall, the continuous operation at a hydraulic retention time (HRT) of 2.4 h and an added molar concentration [Mg(2 + )]:[PO(4) (3-)-P]:[NH(4) (+)] ratio of 1.6:1:2.3 resulted in a constant pH value in the reactor (around 8.5) and an efficient phosphate removal (>90%) to residual levels of 1-2 mg PO(4) (3-)-P/l. Different operational conditions, such as the initial phosphate concentration, HRT and the use of CaCl(2) or MgO instead of MgCl(2), were analysed and the performance of the reactor was satisfactory under a broad range of them. Yet, overall, optimal results (higher phosphate removal) were obtained with MgCl(2). PMID:19474493

  13. Two isostructural carbamates: the o-tolyl N-(pyridin-3-yl)carbamate and 2-bromo­phenyl N-(pyridin-3-yl)carbamate monohydrates

    PubMed Central

    Mocilac, Pavle; Gallagher, John F.

    2015-01-01

    The title carbamate monohydrates, C13H12N2O2·H2O and C12H9BrN2O2·H2O, form isomorphous crystals that are isostructural in their primary hydrogen-bonding modes. In both carbamates, the primary hydrogen bonding and aggregation involves cyclic amide–water–pyridine moieties as (N—H⋯O—H⋯N)2 dimers about inversion centres [as R 4 4(14) rings], where the participation of strong hydrogen-bonding donors and acceptors is maximized. The remaining water–carbonyl O—H⋯O=C inter­action extends the aggregation into two-dimensional planar sheets that stack parallel to the (100) plane. The Br derivative does not participate in halogen bonding. A weak intra­molecular C—H⋯O hydrogen bond is observed in each compound. PMID:26594512

  14. Cationic cobaltammine as anion receptor: Synthesis, characterization, single crystal X-ray structure and packing analysis of hexaamminecobalt(III) chloride ( R, R)-tartrate monohydrate

    NASA Astrophysics Data System (ADS)

    Bala, Ritu; Sharma, Raj Pal; Venugopalan, Paloth; Harrison, William T. A.

    2007-03-01

    In an effort to utilize the [Co(NH 3) 6] 3+ cation as a new anion receptor (binding agent) for dihydroxy dicarboxylate anion i.e., tartrate, orange single crystals of hexaamminecobalt(III) chloride ( R, R)-tartrate monohydrate, [Co(NH 3) 6]Cl(C 4H 4O 6)·H 2O, were obtained by reacting hexaamminecobalt(III) chloride with potassium-sodium tartrate tetrahydrate in a 1:1 molar ratio in hot water. The single crystal X-ray structure determination of [Co(NH 3) 6]Cl(C 4H 4O 6)·H 2O revealed that a distinctive network of hydrogen bonding interactions (N-H⋯O, N-H⋯Cl -, O-H⋯O) stabilize the crystal lattice. This is the first complex salt of hexaamminecobalt(III) with dihydroxy dicarboxylate anion i.e., tartrate.

  15. Crystal structures of tiotropium bromide and its monohydrate in view of combined solid-state nuclear magnetic resonance and gauge-including projector-augmented wave studies.

    PubMed

    Pindelska, Edyta; Szeleszczuk, Lukasz; Pisklak, Dariusz Maciej; Majka, Zbigniew; Kolodziejski, Waclaw

    2015-07-01

    Tiotropium bromide is an anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease. The crystal structures of this compound and its monohydrate have been previously solved and published. However, in this paper, we showed that those structures contain some major errors. Our methodology based on combination of the solid-state nuclear magnetic resonance (NMR) spectroscopy and quantum mechanical gauge-including projector-augmented wave (GIPAW) calculations of NMR shielding constants enabled us to correct those errors and obtain reliable structures of the studied compounds. It has been proved that such approach can be used not only to perform the structural analysis of a drug substance and to identify its polymorphs, but also to verify and optimize already existing crystal structures. PMID:25981387

  16. Crystal structure of (2E)-1-(1-benzo-furan-2-yl)-3-(2-bromo-phen-yl)prop-2-en-1-one monohydrate.

    PubMed

    Satheeshchandra, S; Shetty, Nandakumar

    2015-11-01

    The title compound, C17H11BrO2·H2O, crystallizes as a monohydrate in the chiral ortho-rhom-bic space group P212121, and has non-linear optical (NLO) properties. The mol-ecule has an E conformation about the C=C bond and is relatively planar with the benzo-furan and bromo-phenyl rings being inclined to one another by 10.60 (14)°. In the crystal, the water mol-ecule is linked to the organic mol-ecule by O-H⋯O hydrogen bonds, forming an R (2) 2(7) ring motif while C-H⋯O hydrogen bonds lead to the formation of helices along the b-axis direction. PMID:26594555

  17. Structural characterization, phase transition and dielectric properties of 4-cyanopyridynium perchlorate monohydrate: [(4-CNC 5H 4NH)][ClO 4]·H 2O

    NASA Astrophysics Data System (ADS)

    Czupiński, O.; Wojtaś, M.; Pietraszko, A.; Jakubas, R.

    2007-01-01

    Crystal structure of 4-cyanopyridynium perchlorate monohydrate ([(4-CNC 5H 4NH)][ClO 4]·H 2O) has been determined at 293 and 240 K as orthorhombic space group, Pnma and monoclinic space group, P2 1/ c, respectively, by means of single crystal X-ray diffraction. At room temperature the perchlorate anion reveals significant disorder, which is realized by the splitting of two oxygen atoms into four sites. DSC, dilatometric and dielectric spectroscopy techniques show that the crystal undergoes phase transition at 286/288 K (on cooling/heating scans). [(4-CNC 5H 4NH)][ClO 4]·H 2O appears to be an insulator with relatively high activation energy of the order of 100 kJ/mol. The phase transition in the title crystal is believed to be related to the dynamics of the perchlorate anion.

  18. Natural bond orbital analysis, electronic structure, non-linear properties and vibrational spectral analysis of L-histidinium bromide monohydrate: a density functional theory.

    PubMed

    Sajan, D; Joseph, Lynnette; Vijayan, N; Karabacak, M

    2011-10-15

    The spectroscopic properties of the crystallized nonlinear optical molecule L-histidinium bromide monohydrate (abbreviated as L-HBr-mh) have been recorded and analyzed by FT-IR, FT-Raman and UV techniques. The equilibrium geometry, vibrational wavenumbers and the first order hyperpolarizability of the crystal were calculated with the help of density functional theory computations. The optimized geometric bond lengths and bond angles obtained by using DFT (B3LYP/6-311++G(d,p)) show good agreement with the experimental data. The complete assignments of fundamental vibrations were performed on the basis of the total energy distribution (TED) of the vibrational modes, calculated with scaled quantum mechanics (SQM) method. The natural bond orbital (NBO) analysis confirms the occurrence of strong intra and intermolecular N-H⋯O hydrogen bonding. PMID:21775197

  19. Brain perfusion and permeability in patients with advanced, refractory glioblastoma treated with lomustine and the transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate

    PubMed Central

    SEPULVEDA-SANCHEZ, JUAN; RAMOS, ANA; HILARIO, AMAYA; DE VELASCO, GUILLERMO; CASTELLANO, DANIEL; GARCIA DE LA TORRE, MARTA; RODON, JORDI; LAHN, MICHAEL F.

    2015-01-01

    Transforming growth factor-β (TGF-β) signaling is associated with tumor progression and vascularization in malignant glioma. In the present study, magnetic resonance imaging was used to evaluate changes in the size and vascularity of glioblastomas in 12 patients who were treated with lomustine and the novel inhibitor of TGF-β signaling, LY2157299 monohydrate. A response in tumor size was observed in 2 of the 12 patients; in 1 of these 2 patients, a reduction in vascular permeability and perfusion was also detected. The effect was observed following 4 cycles of treatment (~3 months). Changes in vascularity have not previously been attributed to treatment with lomustine; therefore, the effect may be associated with LY2157299 treatment. LY2157299 does not appear to have an anti-angiogenic effect when combined with lomustine, and hence may have a different mechanism of action profile compared with anti-angiogenic drugs. PMID:26137087

  20. Analysis of Altered MicroRNA Expression Profiles in Proximal Renal Tubular Cells in Response to Calcium Oxalate Monohydrate Crystal Adhesion: Implications for Kidney Stone Disease

    PubMed Central

    Wang, Bohan; Wu, Bolin; Liu, Jun; Yao, Weimin; Xia, Ding; Li, Lu; Chen, Zhiqiang; Ye, Zhangqun; Yu, Xiao

    2014-01-01

    Background Calcium oxalate monohydrate (COM) is the major crystalline component in kidney stones and its adhesion to renal tubular cells leads to tubular injury. However, COM-induced toxic effects in renal tubular cells remain ambiguous. MicroRNAs (miRNAs) play an important role in gene regulation at the posttranscriptional levels. Objective The present study aimed to assess the potential changes in microRNAs of proximal renal tubular cells in response to the adhesion of calcium oxalate monohydrate (COM) crystals. Methodology Lactate dehydrogenase (LDH) activity and DAPI staining were used to measure the toxic effects of HK-2 cells exposed to COM crystals. MicroRNA microarray and mRNA microarray were applied to evaluate the expression of HK-2 cells exposed to COM crystals. Quantitative real-time PCR (qRT-PCR) technology was used to validate the microarray results. Target prediction, Gene Ontology (GO) analysis and pathway analysis were applied to predict the potential roles of microRNAs in biological processes. Principal Findings Our study showed that COM crystals significantly altered the global expression profile of miRNAs in vitro. After 24 h treatment with a dose (1 mmol/L), 25 miRNAs were differentially expressed with a more than 1.5-fold change, of these miRNAs, 16 were up-regulated and 9 were down-regulated. A majority of these differentially expressed miRNAs were associated with cell death, mitochondrion and metabolic process. Target prediction and GO analysis suggested that these differentially expressed miRNAs potentially targeted many genes which were related to apoptosis, regulation of metabolic process, intracellular signaling cascade, insulin signaling pathway and type 2 diabetes. Conclusion Our study provides new insights into the role of miRNAs in the pathogenesis associated with nephrolithiasis. PMID:24983625