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Sample records for sitagliptin phosphate monohydrate

  1. Sitagliptin

    MedlinePlus

    ... because the body does not produce or use insulin normally). Sitagliptin is in a class of medications ... mention any of the following: digoxin (Lanoxicaps, Lanoxin); insulin; and certain oral medications for diabetes including acetohexamide, ...

  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. Improved Chromatographic Separation of Sitagliptin Phosphate and Metformin Hydrochloride.

    PubMed

    Hendy, Moataz S

    2015-12-01

    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

  4. 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

  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. Study of coloration, microbe inhibition during the growth of L-arginine phosphate monohydrate single crystals

    NASA Astrophysics Data System (ADS)

    Li, Aidong; Xu, Chongquan; Li, Aibin; Ming, Naiben

    2000-12-01

    During the growth of L-arginine phosphate monohydrate (LAP) single crystals, the problems of coloration and microbial contamination of the solution were investigated. It was found that the solution coloration can be prevented by conducting crystal growth at temperatures lower than 40°C and by inhibiting microbial growth. Compared to the known microbe inhibitors H 2O 2 and n-hexane, liquid paraffin shows advantages of long durability and convenience of usage for the growth of high-quality LAP single crystals.

  7. 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

  8. 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.

  9. 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.

  10. 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

  11. A theoretical investigation of electric properties of L-arginine phosphate monohydrate including environment polarization effects

    NASA Astrophysics Data System (ADS)

    Fonseca, T. L.; Sabino, J. R.; Castro, M. A.; Georg, H. C.

    2010-10-01

    The dipole moment (μ), linear polarizability (α¯), and first hyperpolarizability (βtot) of the asymmetric unit of L-arginine phosphate (LAP) monohydrate crystal are investigated using the supermolecule approach in combination with an iterative electrostatic polarization scheme. Environment polarization effects are attained by assuring the convergence of the dipole moment of LAP embedded in the polarization field of the surrounding molecules whose atomic sites are treated as point charges. The results obtained show that in the presence of the embedding charges, the value of μ is increased by 9% but the static values of α¯ and βtot are decreased, respectively, by 3% and 13%, as compared with the isolated situation. The MP2/6-311+G(d) model predicts for the in-crystal dipole moment the converged value of 33 D, in good concordance with the available experimental result of 32 D. Our estimates for the converged results of α¯ and βtot are, respectively, 22.51×10-24 and 5.01×10-30 esu. Dispersion effects are found to have a small impact on the nonlinear optical responses of LAP in the visible region. In addition, MP2/6-311G results obtained for βtot by using isolated and embedded LAP dimers show that crystal packing effects have a significant contribution of the electrostatic interactions. Our results suggest that the role of the crystal environment is to minimize the effects of the intermolecular interactions in the electric properties. That is, μ and βtot gain a more additive character in the presence of the field of the embedding charges. This is specially marked for βtot.

  12. Crystal growth, structural and thermal studies of amino acids admixtured L-arginine phosphate monohydrate single crystals

    NASA Astrophysics Data System (ADS)

    Anandan, P.; Saravanan, T.; Parthipan, G.; Kumar, R. Mohan; Bhagavannarayana, G.; Ravi, G.; Jayavel, R.

    2011-05-01

    To study the improved characteristics of L-arginine phosphate monohydrate (LAP) crystals, amino acids mixed LAP crystals have been grown by slow cooling method. Amino acids like glycine, L-alanine, and L-valine have been selected for doping. Optical quality bulk crystals have been harvested after a typical growth period of about twenty days. The effect of amino acids in the crystal lattice and molecular vibrational frequencies of various functional groups in the crystals have been studied using X-ray powder diffraction and Fourier Transform infrared (FTIR) analyses respectively. Thermal behavior of the amino acids mixed LAP crystals have been studied from the TG and DTG analyses. High-resolution X-ray diffraction studies have been carried out to find the crystalline nature. Optical transmission studies have been carried out by UV-vis spectrophotometer. The cut off wavelength is below 240 nm for the grown crystals.

  13. 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

  14. 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

  15. 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.

  16. Isovaline monohydrate.

    PubMed

    Butcher, Ray J; Brewer, Greg; Burton, Aaron S; Dworkin, Jason P

    2013-11-27

    The title compound, C5H11NO2·H2O, is an isomer of the α-amino acid valine that crystallizes from water in its zwitterion form as a monohydrate. It is not one of the 20 proteinogenic amino acids that are used in living systems and differs from the natural amino acids in that it has no α-H atom. The compound exhibits hydrogen bonding between the water mol-ecule and the carboxyl-ate O atoms and an amine H atom. In addition, there are inter-molecular hydrogen-bonding inter-actions between the carboxyl-ate O atoms and amine H atoms. In the crystal, these extensive N-H⋯O and O-H⋯O hydrogen bonds lead to the formation of a three-dimensional network. PMID:24454253

  17. 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.

  18. 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.

  19. Sitagliptin, sitagliptin and metformin, or sitagliptin and amitriptyline attenuate streptozotocin-nicotinamide induced diabetic neuropathy in rats

    PubMed Central

    Sharma, Ashish Kumar; Sharma, Akash; Kumari, Rita; Kishore, Kunal; Sharma, Divya; Srinivasan, Bharthu Parthsarthi; Sharma, Ashok; Singh, Santosh Kumar; Gaur, Samir; Jatav, Vijay Singh; Sharma, Prashant; Srivastava, Varnika; Joshi, Sneha; Joshi, Megha; Dhakad, Prashant Kumar; Kanawat, Davender Singh; Mishra, Akanksha; Sharma, Anil; Singh, Dharmendra; Singh, Ravinder Pal; Chawda, Himmat Singh; Singh, Rambir; Raikwar, Sachin Kumar; Kurmi, Muneem Kumar; Khatri, Pankaj; Agarwal, Ashutosh; Munajjam, Arshee

    2012-01-01

    Diabetic neuropathies are a family of nerve disorders caused by diabetes. Symptoms of the disease include nerve palsy, mononeuropathy, mononeuropathy multiplex, diabetic amyotrophy, painful polyneuropathy, autonomic neuropathy, and thoracoabdominal neuropathy. In this study, type 2 diabetes in rats was induced with nicotinamide-streptozotocin. Drug treatment was initiated on the d 15, with the combination regimen of metformin, pioglitazone and glimipiride or metformin and sitagliptin or sitagliptin, amitriptyline and sitagliptin and led to significantly improved glycemic control, increased grip strength and paw jumping response on d 21, 28 and 35 (P < 0.001). Significant increases in blood protein levels and decreases in urinary protein levels were observed in the animals treated with the different regimens on d 21, 28 and 35 (P < 0.001). Combined treatment of streptozotocin and nicotinamide caused marked degeneration of nerve cells, while administration of metformin and sitagliptin showed tissue regeneration and no body weight gain. In conclusion, treatment with sitagliptin and sitagliptin combined with metformin or amitriptyline results in no body weight gain, but causes an increase in grip strength and pain sensitivity, exhibits neural protection, and reverses the alteration of biochemical parameters in rats with streptozotocin-nicotinamide induced type 2 diabetes. PMID:23554750

  20. Sitagliptin

    MedlinePlus

    ... healthcare providers will talk to you about the best way to manage your diabetes. ... doctor and pharmacist what prescription and nonprescription medications, ... chlorpropamide (Diabinese), glimepiride (Amaryl), glipizide (Glucotrol, ...

  1. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners and Table Sirups § 168.111 Dextrose monohydrate. (a) Dextrose monohydrate is purified and crystallized...

  2. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners and Table Sirups § 168.111 Dextrose monohydrate. (a) Dextrose monohydrate is purified and crystallized...

  3. 21 CFR 168.111 - Dextrose monohydrate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... HUMAN CONSUMPTION SWEETENERS AND TABLE SIRUPS Requirements for Specific Standardized Sweeteners and Table Sirups § 168.111 Dextrose monohydrate. (a) Dextrose monohydrate is purified and crystallized...

  4. 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

  5. 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 (6 mg/kg) produced transient nociceptive effect. Liraglutide (200 µg/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 (6 mg/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

  6. Sitagliptin: Is It Effective in Routine Clinical Practice?

    PubMed Central

    Mohan Dallumal, Rita; Chua, Siew Siang; Wu, David Bin-Chia; Vethakkan, Shireene Ratna

    2015-01-01

    Aim. The present study was conducted to determine the glycaemic effects of sitagliptin in type 2 diabetes patients. Methods. Data was collected from patient medical records of a major teaching hospital in Malaysia, from 2009 to 2012. Glycated hemoglobin (HbA1c) values prior to and up to 12 months after the initiation of sitagliptin were analysed. The change in HbA1c values was accounted for based on a generalized linear model generated using the Generalized Estimating Equations (GEE) method. Results and Discussion. Of the 457 patients, 53.6% were elderly and 81.4% were overweight. The mean HbA1c (standard deviation) before initiation of sitagliptin was 8.5 (1.4)%. This dropped to 7.7 (1.4)%, 3 to 6 months after initiation of sitagliptin, with a mean difference of 0.8% (95% confidence interval (CI): 0.7–1.0; P < 0.001). However, this value increased to 8.0 (1.7)% after 7 to 12 months on sitagliptin (P = 0.002) with a mean difference from baseline of 0.6% (95% CI: 0.4–0.7; P < 0.001). Conclusion. In routine clinical practice, sitagliptin produces a significant reduction in mean HbA1c (0.8%) within the first 6 months of use which corresponds to efficacy data obtained in controlled clinical trials. However, this reduction was lesser, 7 to 12 month later. PMID:26089904

  7. Induction of Energy Expenditure by Sitagliptin Is Dependent on GLP-1 Receptor.

    PubMed

    Goldsmith, Felicia; Keenan, Michael J; Raggio, Anne M; Ye, Xin; Hao, Zheng; Durham, Holiday; Geaghan, James; Jia, Weiping; Martin, Roy J; Ye, Jianping

    2015-01-01

    Sitagliptin (SG) increases serum GLP-1 (Glucagon-like peptide-1) through inhibition of the hormone degradation. Resistant starch (RS) induces GLP-1 expression by stimulating L-cells in the intestine. Sitagliptin and resistant starch may have a synergistic interaction in the induction of GLP-1. This possibility was tested in current study in a mouse model of type 2 diabetes. Hyperglycemia was induced in the diet-induced obese mice by a signal injection of streptozotocin (STZ). Sitagliptin (0.4g/100g diet) was tested in the mice (n = 55) with dietary RS (HAM-RS2) at three dosages (0, 15, or 28g/100g diet). Energy and glucose metabolism were monitored in the evaluation of synergistic activity, and GLP-1 activity was determined in the GLP-1 receptor knockout (KO) mice. In the wild type mice, body weight and adiposity were reduced by sitagliptin, which was enhanced by RS (28g). Serum GLP-1 was induced and energy expenditure was enhanced by sitagliptin. Fasting glucose, insulin, and leptin levels were decreased by sitagliptin. The sitagliptin effects were lost in the KO mice (n = 25) although induction of serum GLP-1 by sitagliptin was even stronger in KO mice. The data suggests that sitagliptin is able to reduce adiposity and insulin resistance through induction of energy expenditure. The effect of sitagliptin is partially enhanced by RS. GLP-1 receptor may regulate serum GLP-1 by facilitating the hormone clearance. PMID:25938560

  8. Fixed-dose combination of sitagliptin and metformin for the treatment of type 2 diabetes

    PubMed Central

    Reynolds, Jonathan K

    2009-01-01

    JanumetTM, a fixed dose combination of sitagliptin/metformin HCL manufactured by Merck Pharmaceuticals, has received US Food and Drug Administration approval for treatment of patients with type 2 diabetes, that are inadequately controlled, either by sitagliptin or metformin alone or together in free-dose combination form. Sitagliptin, an inhibitor of the enzyme DDP-4, assists patients with type 2 diabetes mellitus to achieve glycemic control. It has been shown to be safe and effective at 100 mg daily doses. The effect of giving sitagliptin in combination with metformin is thought to have a complimentary and possibly additive effect on glycemic control. PMID:21437126

  9. Cardioprotective effects of sitagliptin against doxorubicin-induced cardiotoxicity in rats.

    PubMed

    El-Agamy, Dina S; Abo-Haded, Hany M; Elkablawy, Mohamed A

    2016-08-01

    There is a large body of evidence suggesting that inhibitors of dipeptidyl peptidase-4, such as sitagliptin, may exhibit beneficial effects against different inflammatory disorders. This investigation was conducted to elucidate the potential ability of sitagliptin to counteract the injurious effects of doxorubicin in cardiac tissue. Male Wistar rats were pretreated with sitagliptin for 10 days then treated with a single dose of doxorubicin (20 mg/kg, i.p). Electrocardiography, biochemical estimation of serum and tissue markers, and histo- and immunopathological examinations were done. Results have shown that supplementation with sitagliptin resulted in significant improvement of cardiac function with contaminant decrease in serum markers of doxorubicin-induced cardiotoxicity. These results were supported by the histopathological results. Furthermore, a marked protection against oxidative stress was evident through reduction of lipid peroxidation and prevention of reduced glutathione content depletion and superoxide dismutase activity reduction in cardiac tissue of rats pretreated with sitagliptin in combination with doxorubicin. Moreover, sitagliptin ameliorated the activation of nuclear factor kappa-B and the release of inflammatory cytokines, tumour necrosis factor-alpha and nitric oxide. Finally, sitagliptin attenuated doxorubicin-induced increase in the expression of pro-apoptotic protein Bax and in the apoptotic marker, caspase-3. Collectively, these data indicate that sitagliptin pretreatment could alleviate doxorubicin-induced cardiotoxicity via reducing oxidative damage and its subsequent inflammation and apoptosis. PMID:27037281

  10. Effect of ABCB1 polymorphisms and atorvastatin on sitagliptin pharmacokinetics in healthy volunteers

    PubMed Central

    Aquilante, Christina L.; Wempe, Michael F.; Sidhom, Maha S.; Kosmiski, Lisa A.; Predhomme, Julie A.

    2013-01-01

    Objectives The objectives of this study were to determine if ABCB1 polymorphisms are associated with interindividual variability in sitagliptin pharmacokinetics, and if atorvastatin alters the pharmacokinetic disposition of sitagliptin in healthy volunteers. Methods In this open-label, randomized, two-phase crossover study, healthy volunteers were prospectively stratified according to ABCB1 1236/2677/3435 diplotype (n=9, CGC/CGC; n=10, CGC/TTT; and n=10, TTT/TTT). In one phase, participants received a single 100 mg dose of sitagliptin. In the other phase, participants received 40 mg of atorvastatin for five days, with a single 100 mg dose of sitagliptin administered on day 5. A 24 hour pharmacokinetic study followed each sitagliptin dose, and the study phases were separated by a 14-day washout period. Results Sitagliptin pharmacokinetic parameters did not differ significantly between ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotype groups during the monotherapy phase. Atorvastatin administration did not significantly affect sitagliptin pharmacokinetics, with GMRs (90% CIs) for sitagliptin Cmax, AUC0-∞, CLR, and fe of 0.93 (0.86, 1.01), 0.96 (0.91, 1.01), 1.02 (0.93, 1.12), and 0.98 (0.90, 1.06), respectively. Conclusions ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotypes did not influence sitagliptin pharmacokinetics in healthy volunteers. Furthermore, atorvastatin had no effect on the pharmacokinetics of sitagliptin in the setting of ABCB1 CGC/CGC, CGC/TTT, and TTT/TTT diplotypes. PMID:23407853

  11. 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...

  12. 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...

  13. 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...

  14. 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...

  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. Cardiovascular safety of sitagliptin in patients with type 2 diabetes mellitus: a pooled analysis

    PubMed Central

    2013-01-01

    Objective To compare the incidence of cardiovascular events and mortality in patients with type 2 diabetes mellitus treated with sitagliptin or non-sitagliptin comparators. Methods A post hoc assessment of cardiovascular safety in 14,611 patients was performed by pooling data from 25 double-blind studies, which randomised patients at baseline to sitagliptin 100 mg/day or a non-sitagliptin comparator (i.e., non-exposed). Included studies were limited to those at least 12 weeks in duration (range: 12 to 104 weeks). Patient-level data were used in this analysis of major adverse cardiovascular events (MACE) including ischaemic events and cardiovascular deaths. Analyses were performed in three cohorts: the entire 25-study cohort, the cohort from placebo-controlled portions of studies (n=19), and the cohort from studies comparing sitagliptin to a sulphonylurea (n=3). Results In the entire cohort analysis, 78 patients had at least 1 reported MACE-related event, with 40 in the sitagliptin group and 38 in the non-exposed group. The exposure-adjusted incidence rate was 0.65 per 100 patient-years in the sitagliptin group and 0.74 in the non-exposed group (incidence rate ratio = 0.83 [95% confidence interval (CI): 0.53, 1.30]). In the analysis comparing sitagliptin to placebo, the exposure-adjusted incidence rate was 0.80 per 100-patient-years with sitagliptin and 0.76 with placebo (incidence rate ratio = 1.01 [95% CI: 0.55, 1.86]). In the analysis comparing sitagliptin to sulphonylurea, the exposure-adjusted incidence rate was 0.00 per 100 patient-years with sitagliptin and 0.86 with sulphonylurea (incidence rate ratio = 0.00 [95% CI: 0.00, 0.31]). Conclusion A pooled analysis of 25 randomised clinical trials does not indicate that treatment with sitagliptin increases cardiovascular risk in patients with type 2 diabetes mellitus. In a subanalysis, a higher rate of cardiovascular-related events was associated with sulphonylurea relative to sitagliptin. PMID:23286208

  17. Sitagliptin attenuates cardiomyopathy by modulating the JAK/STAT signaling pathway in experimental diabetic rats.

    PubMed

    Al-Rasheed, Nouf M; Al-Rasheed, Nawal M; Hasan, Iman H; Al-Amin, Maha A; Al-Ajmi, Hanaa N; Mahmoud, Ayman M

    2016-01-01

    Sitagliptin, a dipeptidyl peptidase-4 inhibitor, has been reported to promote cardioprotection in diabetic hearts by limiting hyperglycemia and hyperlipidemia. However, little is known about the involvement of the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway modulation in the cardioprotective effects of sitagliptin. The current study aimed to investigate the protective effects of sitagliptin against diabetic cardiomyopathy (DCM), focusing on the modulation of the JAK/STAT pathway. Diabetes was induced by streptozotocin injection, and rats received sitagliptin orally and daily for 90 days. Diabetic rats exhibited hyperglycemia, hyperlipidemia, and a significant increase in heart-to-body weight (HW/BW) ratio. Serum troponin I and creatine kinase MB, cardiac interleukin-6 (IL-6), lipid peroxidation, and nitric oxide levels showed significant increase in diabetic rats. In contrast, both enzymatic and nonenzymatic antioxidant defenses were significantly declined in the heart of diabetic rats. Histopathological study revealed degenerations, increased collagen deposition in the heart of diabetic rats. Sitagliptin alleviated hyperglycemia, hyperlipidemia, HW/BW ratio, histological architecture, oxidative stress, and inflammation, and rejuvenated the antioxidant defenses. In addition, cardiac levels of pJAK2 and pSTAT3 were increased in diabetic rats, an effect which was remarkably decreased after sitagliptin treatment. In conclusion, these results confer an evidence that sitagliptin has great therapeutic potential on DCM through down-regulation of the JAK/STAT signaling pathway. PMID:27418808

  18. Sitagliptin attenuates cardiomyopathy by modulating the JAK/STAT signaling pathway in experimental diabetic rats

    PubMed Central

    Al-Rasheed, Nouf M; Al-Rasheed, Nawal M; Hasan, Iman H; Al-Amin, Maha A; Al-Ajmi, Hanaa N; Mahmoud, Ayman M

    2016-01-01

    Sitagliptin, a dipeptidyl peptidase-4 inhibitor, has been reported to promote cardioprotection in diabetic hearts by limiting hyperglycemia and hyperlipidemia. However, little is known about the involvement of the Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway modulation in the cardioprotective effects of sitagliptin. The current study aimed to investigate the protective effects of sitagliptin against diabetic cardiomyopathy (DCM), focusing on the modulation of the JAK/STAT pathway. Diabetes was induced by streptozotocin injection, and rats received sitagliptin orally and daily for 90 days. Diabetic rats exhibited hyperglycemia, hyperlipidemia, and a significant increase in heart-to-body weight (HW/BW) ratio. Serum troponin I and creatine kinase MB, cardiac interleukin-6 (IL-6), lipid peroxidation, and nitric oxide levels showed significant increase in diabetic rats. In contrast, both enzymatic and nonenzymatic antioxidant defenses were significantly declined in the heart of diabetic rats. Histopathological study revealed degenerations, increased collagen deposition in the heart of diabetic rats. Sitagliptin alleviated hyperglycemia, hyperlipidemia, HW/BW ratio, histological architecture, oxidative stress, and inflammation, and rejuvenated the antioxidant defenses. In addition, cardiac levels of pJAK2 and pSTAT3 were increased in diabetic rats, an effect which was remarkably decreased after sitagliptin treatment. In conclusion, these results confer an evidence that sitagliptin has great therapeutic potential on DCM through down-regulation of the JAK/STAT signaling pathway. PMID:27418808

  19. Sitagliptin After Ischemic Stroke in Type 2 Diabetic Patients: A Nationwide Cohort Study

    PubMed Central

    Chen, Dong-Yi; Wang, Szu-Heng; Mao, Chun-Tai; Tsai, Ming-Lung; Lin, Yu-Sheng; Su, Feng-Chieh; Chou, Chung-Chuan; Wen, Ming-Shien; Wang, Chun-Chieh; Hsieh, I-Chang; Hung, Kuo-Chun; Cherng, Wen-Jin; Chen, Tien-Hsing

    2015-01-01

    Abstract The cerebrovascular safety and efficacy of sitagliptin, a dipeptidyl peptidase-4 inhibitor, in patients with type 2 diabetes mellitus (T2DM) with ischemic stroke remains uncertain. The aim of this study was to assess the efficacy and safety of sitagliptin in patients with T2DM with recent ischemic stroke. We analyzed data from the Taiwan National Health Insurance Research Database between March 1, 2009, and December 31, 2011. Ischemic stroke patients were identified from individuals with T2DM. Patients who received sitagliptin were compared with those who did not to evaluate the cardiovascular safety and efficacy of sitagliptin. The primary outcome was a composite of ischemic stroke, myocardial infarction, or cardiovascular death. A total of 5145 type 2 diabetic patients with ischemic stroke met our inclusion criteria and were followed for up to 2.83 years (mean, 1.17 years). Overall, 1715 patients (33.3%) received sitagliptin and 3430 patients (66.7%) did not. The primary composite outcome occurred in 190 patients in the sitagliptin group (11.1%) and in 370 patients in the comparison group (10.8%) (hazard ratio [HR] = 1.02; 95% confidence interval [CI], 0.85–1.21). Patients treated with sitagliptin had a similar risk of ischemic stroke, hemorrhagic stroke, and all-cause mortality with an HR of 0.95 (95% CI, 0.78–1.16, P = 0.612), 1.07 (95% CI, 0.55–2.11, P = 0.834), and 1.00 (95% CI, 0.82–1.22, P = 0.989), respectively, compared with patients not treated with sitagliptin. Treatment with sitagliptin in type 2 diabetic patients with recent ischemic stroke was not associated with increased or decreased risks of adverse cerebrovascular outcomes. PMID:26181549

  20. 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

  1. 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 57 689 patients (mean age 74 yr) were newly prescribed sitagliptin, and 83 405 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 57 689 patients taking sitagliptin [0.08%] v. 48 of 55 705 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

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

    PubMed

    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

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

    PubMed

    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

  6. 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.

  7. Sitagliptin use and thyroid cancer risk in patients with type 2 diabetes.

    PubMed

    Tseng, Chin-Hsiao

    2016-04-26

    Whether sitagliptin may increase thyroid cancer risk has not been investigated in the Asian populations. This study evaluated the association in Taiwanese patients with newly diagnosed type 2 diabetes from 1999 to 2008 by using the reimbursement database of the National Health Insurance. They should have been followed for at least 6 months after March 1, 2009, the date when sitagliptin was approved for reimbursement. Patients newly treated with sitagliptin (n=58238, "ever users of sitagliptin") or other antidiabetic drugs (n =312853, "never users of sitagliptin") were followed until December 31, 2011. The treatment effect (for ever versus never users, and for tertiles of cumulative duration of therapy) was estimated by Cox regression incorporated with the inverse probability of treatment weighting using propensity score. Results showed that the respective number of incident thyroid cancer in ever users and never users was 28 and 172, with respective incidence of 29.34 and 22.13 per 100,000 person-years. The overall hazard ratio (95% confidence interval) of 1.516 (1.011-2.271) suggested a significantly higher risk associated with sitagliptin use. In tertile analyses, the hazard ratio for the first ( < 6.53 months), second (6.53-14.00 months) and third ( > 14 months) tertile of cumulative duration was 1.995 (1.015-3.919), 2.516 (1.451-4.364) and 0.595 (0.244-1.449), respectively. Analyses after excluding patients with benign thyroid disease and in a subsample matched on baseline characteristics supported the findings in the original sample. In conclusion, sitagliptin use is associated with an increased risk of thyroid cancer, especially during the first year of its treatment. PMID:27029076

  8. Microflora Disturbance during Progression of Glucose Intolerance and Effect of Sitagliptin: An Animal Study

    PubMed Central

    2016-01-01

    Background. Emerging evidences have shown a close interplay between obesity, diabetes, and intestinal flora disturbance. Dipeptidyl peptidase-4 inhibitor, exemplified by sitagliptin, is highly efficacious in treating type 2 diabetes (T2DM), yet little is known if sitagliptin exerts beneficial effects on microbiota associated with obesity and T2DM. We evaluated changes of gut microbiota following the induction of obesity and T2DM in a streptozotocin treated high fat/high carbohydrate fed (HF/HC-STZ) rat model and explored the effect of sitagliptin on gut microbiota for HF/HC-STZ rats. Methods. Sitagliptin was administered via oral gavage to diabetic rats. Fecal DNA extraction and 454 pyrosequencing based on analysis of 16S rRNA genes was utilized to determine the overall structure of microbiota in fecal DNA samples. Results. Results showed that, at the level of phylum, there was higher abundance of Firmicutes and Tenericutes and less abundance of Bacteroidetes in obese rats compared to their lean counterparts. At the level of genus, short-chain fatty acid- (SCFA-) producing bacteria, Blautia, Roseburia, and Clostridium, and probiotics Lactobacillus, Bifidobacterium, and so forth were identified significantly different from each other among conditions. Conclusion. Marked shifts of the gut microbiota structure were observed in the rats during development of glucose intolerance. Intestinal flora changed in the process of glucose intolerance, and treatment of sitagliptin moderately corrected the dysbiosis of microbiota in T2DM.

  9. Comparative effects of vildagliptin and sitagliptin determined by continuous glucose monitoring in patients with type 2 diabetes mellitus.

    PubMed

    Koyanagawa, Naohide; Miyoshi, Hideaki; Ono, Kota; Nakamura, Akinobu; Cho, Kyu Yong; Yamamoto, Kohei; Takano, Yoshinari; Dan-Noura, Midori; Atsumi, Tatsuya

    2016-08-31

    The dipeptidyl peptidase-4 inhibitors vildagliptin and sitagliptin are effective in treating patients with type 2 diabetes mellitus. Patients receiving standard doses of sitagliptin plus insulin may require increased doses of sitagliptin or switching to vildagliptin to improve blood glucose control. This study compared the effects of increasing sitagliptin and switching to vildagliptin in type 2 diabetes patients receiving standard doses of sitagliptin plus insulin. This prospective, randomized, parallel-group comparison trial enrolled 33 type 2 diabetes patients receiving 50 mg sitagliptin once daily plus insulin. Seventeen patients were randomized to 50 mg vildagliptin twice daily, and 16 to 100 mg sitagliptin once daily, and evaluated by continuous glucose monitoring at baseline and after 8 weeks. The primary end-point was the change in mean amplitude of glycemic excursions (MAGE). MAGE decreased from baseline in both the vildagliptin (-13.4 ± 35.7 mg/dL) and sitagliptin (-8.4 ± 24.3 mg/dL) groups, but neither within- nor between-group changes were statistically significant. Similarly, the areas under the curve for blood glucose levels ≥180 mg/dL and <70 mg/dL tended to improve in both groups, but these differences were not statistically significant. In contrast, HbA1c was significantly reduced only in the vildagliptin group, from 7.1 ± 0.6% at baseline to 6.8 ± 0.6% at 8 weeks (p=0.006). Increasing sitagliptin dose and switching to vildagliptin had limited effects in improving MAGE in type 2 diabetic patients treated with standard doses of sitagliptin. PMID:27321385

  10. 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

  11. 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.

  12. 2-Amino­pyrimidinium dihydrogen phosphate monohydrate

    PubMed Central

    Marouani, Houda; Al-Deyab, Salem S.; Rzaigui, Mohamed

    2011-01-01

    In the title compound, C4H6N3 +·H2O4P−·H2O, the pyrimidin­ium ring is essentially planar, with an r.m.s. deviation of 0.0016 Å. In the structure, pairs of symmetry-related anions are connected into centrosymmetric clusters via strong O—H⋯O hydrogen bonds forming six-membered rings with an R 2 2(6) motif. These clusters are inter­connected via water mol­ecules through OW—H⋯O hydrogen bonds, building an infinite layer parallel to the ab plane. Moreover, infinite chains of 2-amino­pyrimidinium cations spread along the a-axis direction. These chains are connected to the inorganic layer through N—H⋯O, C—H⋯O and C—H⋯N hydrogen bonds, which, together with electrostatic and van der Waals inter­actions, contribute to the cohesion and stability of the network in the crystal structure. PMID:21754233

  13. 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

  14. 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

  15. Sitagliptin: a review of its use in patients with type 2 diabetes mellitus.

    PubMed

    Plosker, Greg L

    2014-02-01

    Sitagliptin (Januvia(®), Xelevia™, Glactiv(®), Tesavel(®)) is an orally administered, potent and highly selective inhibitor of dipeptidyl peptidase-4 (DPP-4) and was the first agent of its class to be approved for use in the management of adults with type 2 diabetes. Numerous randomized placebo- or active comparator-controlled trials have demonstrated the efficacy of sitagliptin in terms of improving glycaemic control in patients with type 2 diabetes, including its use as monotherapy, initial combination therapy (usually with fixed-dose combinations of sitagliptin/metformin), or add-on therapy to metformin or to other antihyperglycaemic drugs, with or without metformin. The primary endpoint of the clinical trials was the reduction from baseline in glycosylated haemoglobin (HbA1c), although sitagliptin also showed beneficial effects for other endpoints, such as the proportion of patients who achieved target HbA1c, and reductions from baseline in fasting plasma glucose (FPG) levels and 2-h postprandial glucose (PPG) levels. Sitagliptin was generally well tolerated in clinical trials, had a low risk of hypoglycaemia (although this depends on background therapy) and had a neutral effect on body weight. Despite concerns regarding a possible increased risk of rare pancreatic adverse events (e.g. pancreatitis) with glucagon-like peptide-1 (GLP-1)-based therapies, such as GLP-1 receptor agonists and DPP-4 inhibitors, no causal association has been found; regulators in Europe recently conducted a review of available data, concluding that there is little evidence that these drugs could cause pancreatic inflammation or pancreatic cancer. A similar review is planned in the USA and postmarketing surveillance will continue. Thus, oral sitagliptin is an effective and generally well tolerated treatment option for the management of patients with type 2 diabetes. PMID:24407560

  16. Rare allergic reaction of the kidney: sitagliptin-induced acute tubulointerstitial nephritis.

    PubMed

    Alsaad, Ali A; Dhannoon, Sarah M; Pantin, Sally-Ann L; Porter, Ivan E

    2016-01-01

    A 56-year-old man with a history of diabetes mellitus type-2 and stage-2 chronic kidney disease secondary to diabetic nephropathy presented with an acute deterioration of kidney function. Non-invasive work-up failed to reveal the underlying aetiology for the acute kidney failure. Kidney biopsy revealed acute tubulointerstitial nephritis (ATIN) which was attributed to sitagliptin use. Only few case reports have shown this correlation. Our aim is to alert physicians and other providers of the potential effect of sitagliptin to cause ATIN with this biopsy-proven case. PMID:27436034

  17. PERS&O (PERsistent Sitagliptin treatment & Outcomes): observational retrospective study on cardiovascular risk evolution in patients with type 2 diabetes on persistent sitagliptin treatment

    PubMed Central

    Buonaiuto, Giulia; De Mori, Valentina; Braus, Alessandra; Balini, Annalisa; Berzi, Denise; Carpinteri, Rita; Forloni, Franco; Meregalli, Giancarla

    2016-01-01

    Objectives The UK Prospective Diabetes Study (UKPDS) Risk Engine (RE) provides the best risk estimates available for people with type 2 diabetes (T2D), so it was applied to patients on persistent sitagliptin treatment. Design A ‘real-world’ retrospective, observational, single-center study. Setting The study was performed in a general hospital in Northern Italy in order: (1) to validate UKPDS RE in a cohort of Italian participants with T2D without prespecified diabetes duration, with/without cardiovascular (CV) disease, treated with sitagliptin; (2) to confirm CV risk gender difference; (3) to evaluate the effect on metabolic control and on CV risk evolution obtained by ‘add-on’ persistent sitagliptin treatment. Participants Sitagliptin 100 mg once a day was taken by 462 participants with T2D: 170 of them (males: 106; age: 63.6±8.8; T2D duration: 11.58±7.33; females: 64; age: 65.6±7.95; T2D duration 13.5±7.9) were treated for 48 months with the same dosage. Interventions An analysis of normality was performed both for continuous, and for groups variables on UKPDS RE percentage values, defining the requirement of a base log10 transformation to normalize risk factor values for analysis validation. Results The evaluation of CV risk evolution by gender (t-test) confirmed the expected statistical difference (p<0.0001). Sitagliptin obtained significant results after 12 months, and at the end of the observation, both on metabolic control (expressed by glycated hemoglobin) and on UKPDS RE. Analysis of variance test revealed a significant effect on CV risk after 12 months (p=0.003), and after 48 months (p=0.04). A bivariate correlation analysis revealed a correlation index (r)=0.2 between the two variables (p<0.05). Conclusions These ‘real-world’ data obtained applying UKPDS RE may reflect patients’ and clinicians’ interest in realizing individual CV risk, and its evolution. Sitagliptin-persistent treatment for a medium–long period obtained

  18. Effect of a Dipeptidyl Peptidase-IV Inhibitor, Des-Fluoro-Sitagliptin, on Neointimal Formation after Balloon Injury in Rats

    PubMed Central

    Lim, Soo; Choi, Sung Hee; Shin, Hayley; Cho, Bong Jun; Park, Ho Seon; Ahn, Byung Yong; Kang, Seon Mee; Yoon, Ji Won; Jang, Hak Chul; Kim, Young-Bum; Park, Kyong Soo

    2012-01-01

    Background Recently, it has been suggested that enhancement of incretin effect improves cardiac function. We investigated the effect of a DPP-IV inhibitor, des-fluoro-sitagliptin, in reducing occurrence of restenosis in carotid artery in response to balloon injury and the related mechanisms. Methods and Findings Otsuka Long-Evans Tokushima Fatty rats were grouped into four: control (normal saline) and sitagliptin 100, 250 and 500 mg/kg per day (n = 10 per group). Sitagliptin or normal saline were given orally from 1 week before to 2 weeks after carotid injury. After 3 weeks of treatment, sitagliptin treatment caused a significant and dose-dependent reduction in intima-media ratio (IMR) in obese diabetic rats. This effect was accompanied by improved glucose homeostasis, decreased circulating levels of high-sensitivity C-reactive protein (hsCRP) and increased adiponectin level. Moreover, decreased IMR was correlated significantly with reduced hsCRP, tumor necrosis factor-α and monocyte chemoattractant protein-1 levels and plasminogen activator inhibitor-1 activity. In vitro evidence with vascular smooth muscle cells (VSMCs) demonstrated that proliferation and migration were decreased significantly after sitagliptin treatment. In addition, sitagliptin increased caspase-3 activity and decreased monocyte adhesion and NFκB activation in VSMCs. Conclusions Sitagliptin has protective properties against restenosis after carotid injury and therapeutic implications for treating macrovascular complications of diabetes. PMID:22493727

  19. 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.

  20. 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.

  1. 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

  2. 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

  3. 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 Section 556.625 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  4. 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 Section 556.625 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate....

  5. 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 Section 556.625 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Specific Tolerances for Residues of New Animal Drugs § 556.625 Sodium sulfachloropyrazine monohydrate....

  6. 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 Section 556.625 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... tolerance of zero is established for residues of sodium sulfachloropyrazine monohydrate in the...

  7. 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...

  8. 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...

  9. 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...

  10. Sitagliptin attenuates inflammatory responses in lipopolysaccharide-stimulated cardiomyocytes via nuclear factor-κB pathway inhibition

    PubMed Central

    LIN, CHIEN-HUNG; LIN, CHUNG-CHING

    2016-01-01

    Glucagon-like peptide-1 (GLP-1) and GLP-1 receptors (GLP-1Rs) are responsible for glucose homeostasis, and have been shown to reduce inflammation in preclinical studies. The aim of the present study was to determine whether sitagliptin, an inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), as a GLP-1 receptor agonist, exerts an anti-inflammatory effect on cardiomyoblasts during lipopolysaccharide (LPS) stimulation. Exposure to LPS increased the expression levels of tumor necrosis factor (TNF)-α, interleukin-6 (IL)-6 and IL-1β in H9c2 cells, and also resulted in elevations in cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression and nuclear factor-κB (NF-κB) nuclear translocation. Treatment with the DPP-4 inhibitor sitagliptin dose-dependently downregulated the mRNA levels of IL-6, COX-2 and iNOS in LPS-stimulated H9c2 cells. In addition, sitagliptin inhibited the increased protein expression of IL-6, TNF-α and IL-1β. NF-κB mRNA expression was reduced and its translocation to the nucleus was suppressed by treatment with sitagliptin. The present results demonstrated that sitagliptin exerts a beneficial effect on cardiomyoblasts exposed to LPS by inhibiting expression of inflammatory mediators and suppressing NF-κB activation. These findings indicate that the DPP-4 inhibitor sitagliptin may serve a function in cardiac remodeling attributed to sepsis-induced inflammation. PMID:27284355

  11. Effect of Sitagliptin and Metformin on Prediabetes Progression to Type 2 Diabetes - A Randomized, Double-Blind, Double-Arm, Multicenter Clinical Trial: Protocol for the Sitagliptin and Metformin in PreDiabetes (SiMePreD) Study

    PubMed Central

    2016-01-01

    Background The high prevalence and incidence of type 2 diabetes mellitus (DM), and its associated morbidity and mortality, has prompted growing international interest and effort in the primary prevention of this disease. Primary prevention is possible since type 2 DM is preceded by prediabetes, offering a window opportunity to treat patients, and prevent the emergence of advanced disease. Sitagliptin is an oral dipeptidyl peptidase-IV inhibitor that preserves existing beta cell function and increases beta cell mass. These two effects have been demonstrated both in vitro and in animal studies, and current clinical data show that sitagliptin is safe. Metformin, a biguanide, reduces insulin resistance and inhibits hepatic gluconeogenesis, and has an excellent safety profile. The combination of metformin and sitagliptin, targeting both characteristics of prediabetes (insulin resistance and progressive beta cell degeneration), may potentially slow or halt the progression from prediabetes to type 2 DM. This paper describes the rationale and design of the Sitagliptin and Metformin in PreDiabetes (SiMePreD) study. Objective The aim of this study is to determine the effect of sitagliptin and metformin on progression from prediabetes to type 2 DM. The objectives of the study are to determine the effects of metformin and placebo on glycemic endpoints, the effects of sitagliptin and metformin on glycemic endpoints, the effects of metformin and placebo on incidence of cardiovascular disease and death, and the effects of sitagliptin and metformin on incidence of cardiovascular disease and death. Methods This is a randomized, double-blind, multicenter clinical study that will determine if the combination of metformin and sitagliptin is effective in preventing the progression from prediabetes to type 2 DM. The study will contain two arms (metformin/sitagliptin and metformin/placebo). Primary endpoints include the number of subjects progressing from prediabetes to type 2 DM, the

  12. 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

  13. Combined treatment with sitagliptin and vitamin D in a patient with latent autoimmune diabetes in adults

    PubMed Central

    Rapti, E; Karras, S; Grammatiki, M; Mousiolis, A; Tsekmekidou, X; Potolidis, E; Zebekakis, P; Daniilidis, M

    2016-01-01

    Summary Latent autoimmune diabetes in adults (LADA) is a relatively new type of diabetes with a clinical phenotype of type 2 diabetes (T2D) and an immunological milieu characterized by high titers of islet autoantibodies, resembling the immunological profile of type 1 diabetes (T1D). Herein, we report a case of a young male, diagnosed with LADA based on both clinical presentation and positive anti-glutamic acid decarboxylase antibodies (GAD-abs), which were normalized after combined treatment with a dipeptidyl peptidase-4 inhibitor (DPP-4) (sitagliptin) and cholecalciferol. Learning points Anti-glutamic acid decarboxylase antibodies (GAD-abs) titers in young patients being previously diagnosed as type 2 diabetes (T2D) may help establish the diagnosis of latent autoimmune diabetes in adults (LADA). Sitagliptin administration in patients with LADA might prolong the insulin-free period. Vitamin D administration in patients with LADA might have a protective effect on the progression of the disease. PMID:27252860

  14. Crystal growth of calcium oxalate monohydrate

    NASA Astrophysics Data System (ADS)

    Singh, R. P.; Gaur, S. S.; Sheehan, M. E.; Nancollas, G. H.

    1988-02-01

    The kinetics of crystal growth of calcium oxalate monohydrate has been investigated up to very large extents of growth over a range of supersaturations maintained using the Constant Composition technique. It is suggested that the initial rapid growth of aged seed crystals resulting in marked lattice perfection, reduces the density of growth sites on the crystal surfaces. A method for the preparation of perfected crystallites of calcium oxalate monohydrate through pregrowth of aged crystals has been developed. At large extents of growth with respect to initial seed crystals ( > 200% for aged crystals and 30-60% for pregrown crystals), the rates of crystallization at constant supersaturation undergo marked increases accompanying the formulation of secondary nuclei. These nucleation thresholds depend both upon supersaturation and upon the initial specific surface area of the crystallites and may be important factors in the formation of calcium oxalate stones in vivo. Experiments in whole urine suggest that the kinetics of growth, secondary nucleation, aggregation and cementation of particles may be important factors in kidney stone formation.

  15. Efficacy, Safety and Treatment Satisfaction of Glimepiride vs Sitagliptin in Combination with Metformin in Type 2 Diabetes Mellitus

    PubMed Central

    Kumar, Subodh; Saikia, Dibyajyoti; Kumar, Amish

    2015-01-01

    Introduction Metformin is a preferred drug for starting treatment in type 2 diabetes mellitus. But, eventually most of the patients need additional drug to control blood sugar level. The choice of drug depends upon several factors including patient specific criteria, economical factors and treatment satisfaction. Aim The aim of the present study is to investigate the effects of adding sitagliptin or glimepiride on efficacy, safety and treatment satisfaction in patients with type 2 diabetes mellitus. Materials and Methods It was a retrospective observational study on 50 patients each in sitagliptin and glimepiride group, who are receiving treatment for at least 12 weeks and are stable on respective treatment regimen. Glycated haemoglobin (HBA1c) was the primary measure of efficacy. Safety was assessed by checking weight gain/loss, hypoglycaemia episodes and other laboratory investigations. Patient satisfaction was assessed by Diabetes Treatment Satisfaction Questionnaire. Results The HbA1c level after 12-24 weeks of treatment was not found to be significant compared to each other or from baseline. Compared to baseline fasting plasma glucose & postprandial plasma glucose were lower in glimepiride group. Sitagliptin was associated with less episodes of hypoglycaemia. Weight gain was associated with glimepiride but it was non-significant (p=0.08). Overall treatment satisfaction score were better for sitagliptin but were not statistically significant. Conclusion The efficacy of sitagliptin was comparable. Sitagliptin had superior adverse effect profile with less chances of hypoglycaemia and weight gain. Questionnaire scores were higher for sitagliptin indicating better treatment satisfaction compared to glimepiride. PMID:26816909

  16. 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

  17. Long-term Efficacy and Safety of Sitagliptin in Elderly Patients with Type 2 Diabetes Mellitus.

    PubMed

    Tada, Yuko; Kanazawa, Ippei; Notsu, Masakazu; Tanaka, Ken-Ichiro; Kiyohara, Nobuaki; Sasaki, Motofumi; Sugimoto, Toshitsugu

    2016-01-01

    Objective We herein conducted a retrospective study to evaluate the long-term efficacy and safety of sitagliptin treatment in elderly patients with type 2 diabetes mellitus. Methods We analyzed the changes in glycemic control in 112 Japanese type 2 diabetes patients over 65 years of age treated with 50 mg/day sitagliptin. Hemoglobin A1c (HbA1c) levels, liver and kidney functions, and usage of hypoglycemic agents were recorded for 24 months. Results HbA1c levels were significantly decreased, and the significance of HbA1c reduction was maintained during the observation period [from 7.7±1.1% to 7.2±0.7% (p<0.001) at the end of observational period]. The %change in HbA1c levels was significantly and negatively correlated with the baseline HbA1c levels (r=-0.51, p<0.001), but not with age, duration of diabetes, or the estimated glomerular filtration rate (eGFR). No patient experienced severe hypoglycemia episodes, and aspartate transaminase, alanine transaminase, gamma-glutamyl transpeptidase, and the eGFR remained unchanged. The dose of sulfonylurea was finally decreased in 72% of patients treated with sulfonylurea. Conclusion Sitagliptin treatment continually decreases the HbA1c level for 24 months and is useful to reduce the dose of sulfonylurea in elderly patients with type 2 diabetes. PMID:27181532

  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. 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

  20. 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. PMID:26873580

  1. 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...

  2. 2-Methyl-aspartic acid monohydrate.

    PubMed

    Brewer, Greg; Burton, Aaron S; Dworkin, Jason P; Butcher, Ray J

    2013-11-30

    The title compound, C5H9NO4·H2O, is an isomer of the α-amino acid glutamic acid that crystallizes from water in its zwitterionic form as a monohydrate. It is not one of the 20 proteinogenic α-amino acids that are used in living systems and differs from the natural amino acids in that it has an α-methyl group rather than an α-H atom. In the crystal, an O-H⋯O hydrogen bond is present between the acid and water mol-ecules while extensive N-H⋯O and O-H⋯O hydrogen bonds link the components into a three-dimensional array. PMID:24454270

  3. 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

  4. 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

  5. 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

  6. 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

  7. Cost-effectiveness of Canagliflozin versus Sitagliptin When Added to Metformin and Sulfonylurea in Type 2 Diabetes in Canada.

    PubMed

    Sabapathy, Suthakar; Neslusan, Cheryl; Yoong, Kim; Teschemaker, Anna; Johansen, Pierre; Willis, Michael

    2016-01-01

    BackgroundCanagliflozin, an agent that inhibits sodium glucose co-transporter 2, is approved as add-on to metformin plus sulfonylurea for the treatment of type 2 diabetes in Canada. Canagliflozin offers greater glycemic control, as well as important additional benefits such as weight loss and blood pressure reductions, versus dipeptidyl peptidase-4 inhibitors such as sitagliptin.  ObjectiveThis analysis evaluated the cost-effectiveness of canagliflozin 300 mg and canagliflozin 100 mg versus sitagliptin 100 mg in patients with type 2 diabetes inadequately controlled on metformin plus sulfonylurea from the perspective of the Canadian Agency for Drugs and Technologies in Health. MethodsA 40-year cost-effectiveness analysis was performed using the validated Economic and Health Outcomes Model of Type 2 Diabetes Mellitus (ECHO-T2DM). Patient characteristics, treatment effects, and rates of hypoglycemia and adverse events were sourced from the canagliflozin clinical program. Canada-specific costs and utilities were applied. Sensitivity analyses were conducted using alternative values for key model inputs. ResultsBoth canagliflozin 300 and 100 mg dominated sitagliptin 100 mg over 40 years, providing quality-adjusted life-year gains of 0.31 and 0.28, and cost offsets of $2,217 and $2,560, respectively. Both canagliflozin doses dominated sitagliptin in each of the sensitivity analyses. ConclusionsSimulation results suggested that canagliflozin 300 and 100 mg provided better health outcomes and lower costs than sitagliptin 100 mg as a third-line therapy added-on to metformin and sulfonylurea in patients with type 2 diabetes in Canada. PMID:27463416

  8. The Dipeptidyl Peptidase-4 Inhibitor Sitagliptin Protects against Dyslipidemia-Related Kidney Injury in Apolipoprotein E Knockout Mice

    PubMed Central

    Li, Jingjing; Guan, Meiping; Li, Chenzhong; Lyv, Fuping; Zeng, Yanmei; Zheng, Zongji; Wang, Chengzhi; Xue, Yaoming

    2014-01-01

    The goal of this study was to investigate the possible protective effects of sitagliptin against dyslipidemia-related kidney injury in apolipoprotein E knockout (apoE−/−) mice. Eight-week-old male apoE−/− mice were randomized to receive either a high fat diet (HFD, apoE−/− group) or HFD mixed with sitagliptin (sita + apoE−/− group) for 16 weeks. A control group of age- and gender-matched C57BL/6J mice were fed a HFD. The apoE−/− group exhibited increases in body weight and serum lipid levels in addition to high-density lipoprotein, and increases in 24-h urinary 8-hydroxy-2-deoxyguanosine and albuminuria excretion. Decreased insulin sensitivity was also observed in the apoE−/− group. These mice additionally contained enlargements of the glomerular mesangial matrix area, lipid deposition area, and renal interstitium collagen area. The apoE−/− group also demonstrated down-regulation of phosphorylated AMP-activated protein kinase (AMPK), increases in renal mRNA expression of transforming growth factor-beta 1 (TGF-β1) and fibronectin (FN), and increased protein expression of Akt, TGF-β1, FN and p38/ERK mitogen-activated protein kinase (MAPK). Sitagliptin treatment successfully ameliorated all the deleterious effects of dyslipidemia tested. To our knowledge, this is the first time that sitagliptin has been shown to reverse the renal dysfunction and structural damage induced by dyslipidemia in apoE−/− mice. Our results suggest that the renoprotective mechanism of sitagliptin may be due to a reduction in Akt levels, a restoration of AMPK activity, and inhibition of TGF-β1, FN, and p38/ERK MAPK signaling pathways. PMID:24972137

  9. 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.

  10. 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

  11. Sitagliptin and risk of heart failure hospitalization in patients with type 2 diabetes on dialysis: A population-based cohort study.

    PubMed

    Hung, Yi-Chih; Lin, Che-Chen; Huang, Wei-Lun; Chang, Man-Ping; Chen, Ching-Chu

    2016-01-01

    The incidence of heart failure hospitalization (HHF) after taking sitagliptin in type 2 diabetes (T2DM) patients with end stage renal disease (ESRD) on dialysis is unclear. In this population-based cohort study, we identified individuals with T2DM and ESRD on dialysis who were treated with sitagliptin between 2009 and 2011 and randomly selected a control cohort matched by age, sex, duration of T2DM, hypertension medications, use of statin and aspirin, sulfonylureas, glinides, and insulin usage, atherosclerotic heart disease, congestive heart failure and chronic obstructive pulmonary disease at a 1:4 ratio. Multivariable Cox proportional hazards regression analysis was used to evaluate HHF risk. The overall incidence of HHF was higher in the sitagliptin cohort than in the control cohort (1130 vs. 754 per 10000 person-years; adjusted hazard ratio (HR): 1.52, 95% CI = 1.21-1.90). There was a significant trend towards increased HHF risk associated with increased sitagliptin dose (p for trend < 0.01). Subjects at greater risk of HHF after taking sitagliptin were those without severe hypoglycemia, without ACE inhibitors treatment, with history of heart failure or receiving hemodialysis rather than peritoneal dialysis. In conclusion, use of sitagliptin was associated with an increased risk of HHF in patients with T2DM on dialysis. PMID:27460913

  12. Sitagliptin and risk of heart failure hospitalization in patients with type 2 diabetes on dialysis: A population-based cohort study

    PubMed Central

    Hung, Yi-Chih; Lin, Che-Chen; Huang, Wei-Lun; Chang, Man-Ping; Chen, Ching-Chu

    2016-01-01

    The incidence of heart failure hospitalization (HHF) after taking sitagliptin in type 2 diabetes (T2DM) patients with end stage renal disease (ESRD) on dialysis is unclear. In this population-based cohort study, we identified individuals with T2DM and ESRD on dialysis who were treated with sitagliptin between 2009 and 2011 and randomly selected a control cohort matched by age, sex, duration of T2DM, hypertension medications, use of statin and aspirin, sulfonylureas, glinides, and insulin usage, atherosclerotic heart disease, congestive heart failure and chronic obstructive pulmonary disease at a 1:4 ratio. Multivariable Cox proportional hazards regression analysis was used to evaluate HHF risk. The overall incidence of HHF was higher in the sitagliptin cohort than in the control cohort (1130 vs. 754 per 10000 person-years; adjusted hazard ratio (HR): 1.52, 95% CI = 1.21–1.90). There was a significant trend towards increased HHF risk associated with increased sitagliptin dose (p for trend < 0.01). Subjects at greater risk of HHF after taking sitagliptin were those without severe hypoglycemia, without ACE inhibitors treatment, with history of heart failure or receiving hemodialysis rather than peritoneal dialysis. In conclusion, use of sitagliptin was associated with an increased risk of HHF in patients with T2DM on dialysis. PMID:27460913

  13. 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

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

    PubMed Central

    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

  15. Phosphate salts

    MedlinePlus

    ... taken by mouth or used as enemas. Indigestion. Aluminum phosphate and calcium phosphate are FDA-permitted ingredients ... Phosphate salts containing sodium, potassium, aluminum, or calcium are LIKELY SAFE for most people when taken by mouth short-term, when sodium phosphate is inserted into the ...

  16. The Effect of Sitagliptin on Carotid Artery Atherosclerosis in Type 2 Diabetes: The PROLOGUE Randomized Controlled Trial

    PubMed Central

    Oyama, Jun-ichi; Murohara, Toyoaki; Kitakaze, Masafumi; Ishizu, Tomoko; Sato, Yasunori; Kitagawa, Kazuo; Kamiya, Haruo; Ajioka, Masayoshi; Ishihara, Masaharu; Dai, Kazuoki; Sata, Masataka; Maemura, Koji; Tomiyama, Hirofumi; Higashi, Yukihito; Kaku, Kohei; Matsuhisa, Munehide; Yamashita, Kentaro; Bando, Yasuko K.; Kashihara, Naoki; Ueda, Shinichiro; Inoue, Teruo; Tanaka, Atsushi; Node, Koichi

    2016-01-01

    Background Experimental studies have suggested that dipeptidyl peptidase-4 (DPP-4) inhibitors provide cardiovascular protective effects. We performed a randomized study to evaluate the effects of sitagliptin added on to the conventional therapy compared with conventional therapy alone (diet, exercise, and/or drugs, except for incretin-related agents) on the intima-media thickness (IMT) of the carotid artery, a surrogate marker for the evaluation of atherosclerotic cardiovascular disease, in people with type 2 diabetes mellitus (T2DM). Methods and Findings We used a multicenter PROBE (prospective, randomized, open label, blinded endpoint) design. Individuals aged ≥30 y with T2DM (6.2% ≤ HbA1c < 9.4%) were randomly allocated to receive either sitagliptin (25 to 100 mg/d) or conventional therapy. Carotid ultrasound was performed at participating medical centers, and all parameters were measured in a core laboratory. Of the 463 enrolled participants with T2DM, 442 were included in the primary analysis (sitagliptin group, 222; conventional therapy group, 220). Estimated mean (± standard error) common carotid artery IMT at 24 mo of follow-up in the sitagliptin and conventional therapy groups was 0.827 ± 0.007 mm and 0.837 ± 0.007 mm, respectively, with a mean difference of −0.009 mm (97.2% CI −0.028 to 0.011, p = 0.309). HbA1c level at 24 mo was significantly lower with sitagliptin than with conventional therapy (6.56% ± 0.05% versus 6.72% ± 0.05%, p = 0.008; group mean difference −0.159, 95% CI −0.278 to −0.041). Episodes of serious hypoglycemia were recorded only in the conventional therapy group, and the rate of other adverse events was not different between the two groups. As it was not a placebo-controlled trial and carotid IMT was measured as a surrogate marker of atherosclerosis, there were some limitations of interpretation. Conclusions In the PROLOGUE study, there was no evidence that treatment with sitagliptin had an additional effect on the

  17. A new combination of sitagliptin and furosemide protects against remote myocardial injury induced by renal ischemia/reperfusion in rats.

    PubMed

    Youssef, Mahmoud I; Mahmoud, Amr A A; Abdelghany, Rasha H

    2015-07-01

    Acute kidney injury (AKI) is associated with high mortality resulting from extra-renal organ damage, particularly the heart. The present study aimed to investigate the protective effect of sitagliptin, a dipeptidyl peptidase-4 (DPP4) inhibitor, against renal and remote cardiac damage induced by ischemia/reperfusion (IR), a leading cause of AKI. In this attempt, we compared the effects of sitagliptin to furosemide, a loop diuretic. Furosemide is commonly used clinically in AKI however, there is a lack of evidence regarding its beneficial effects in AKI. In addition, the combined administration of both drugs was also investigated. Ischemia was induced in anesthetized male Wistar rats by occluding both renal pedicles for 30min followed by reperfusion for 24h. Sitagliptin (5mg kg(-1)), furosemide (245mg kg(-1)) or their combination were administered orally at 5h post-IR and 2h before euthanasia. Administration of sitagliptin or furosemide ameliorated renal and cardiac deterioration induced by renal IR. This was manifested as significant reduction of serum creatinine, urea, cystatin c, creatine kinase-MB, cardiac troponin-I and lactate dehydrogenase (P<0.05). Drug treatment significantly inhibited IR-induced elevation of TNF-α, NF-κB and caspase-3 (P<0.05) in kidney and heart tissue. In addition, they significantly suppressed malondialdehyde, NO and iNOS content, whereas they increased glutathione and antioxidative enzymes activity (P<0.05) in both tissues. Interestingly, a superior protection was observed with the combination compared to the individual drugs. We assume that this combination represents a promising regimen for managing AKI, particularly with the poor clinical outcome obtained with furosemide alone. PMID:25912235

  18. Modeling Sitagliptin Effect on Dipeptidyl Peptidase 4 (DPP4) Activity in Adults with Hematological Malignancies After Umbilical Cord Blood (UCB) Hematopoietic Cell Transplant (HCT)

    PubMed Central

    de Mendizábal, Nieves Vélez; Strother, Robert M.; Farag, Sherif S.; Broxmeyer, Hal E.; Messina-Graham, Steven; Chitnis, Shripad D.; Bies, Robert R.

    2014-01-01

    Background and Objectives Dipeptidyl peptidase-4 (DPP4) inhibition is a potential strategy to increase the engraftment rate of hematopoietic stem/progenitor cells. A recent clinical trial using sitagliptin, a DPP4 inhibitor approved for type 2 diabetes mellitus, has shown to be a promising approach in adults with hematological malignancies after umbilical cord blood (UCB) hematopoietic cell transplant (HCT). Based on data from this clinical trial, a semi-mechanistic model was developed to simultaneously describe DPP4 activity after multiple doses of sitagliptin in subjects with hematological malignancies after a single-unit UCB HCT. Methods The clinical study included 24 patients that received myeloablative conditioning followed by 4 oral sitagliptin 600mg with single-unit UCB HCT. Using a nonlinear mixed effects approach, a semi-mechanistic pharmacokinetic/pharmacodynamic model was developed to describe DPP4 activity from this trial data using NONMEM 7.2. The model was used to drive Monte-Carlo simulations to probe various dosage schedules and the attendant DPP4 response. Results The disposition of sitagliptin in plasma was best described by a 2-compartment model. The relationship between sitagliptin concentration and DPP4 activity was best described by an indirect response model with a negative feedback loop. Simulations showed that twice a day or three times a day dosage schedules were superior to once daily schedule for maximal DPP4 inhibition at the lowest sitagliptin exposure. Conclusion This study provides the first pharmacokinetic/pharmacodynamic model of sitagliptin in the context of HCT, and provides a valuable tool for exploration of optimal dosing regimens, critical for improving time to engraftment in patients after UCB HCT. PMID:24142388

  19. Efficacy and Safety of Sitagliptin Versus Glipizide in Patients With Type 2 Diabetes and Moderate-to-Severe Chronic Renal Insufficiency

    PubMed Central

    Arjona Ferreira, Juan Camilo; Marre, Michel; Barzilai, Nir; Guo, Hua; Golm, Gregory T.; Sisk, Christine McCrary; Kaufman, Keith D.; Goldstein, Barry J.

    2013-01-01

    OBJECTIVE Patients with type 2 diabetes mellitus (T2DM) and chronic kidney disease have an increased risk of micro- and macrovascular disease, but limited options for antihyperglycemic therapy. We compared the efficacy and safety of sitagliptin with glipizide in patients with T2DM and moderate-to-severe chronic renal insufficiency and inadequate glycemic control. RESEARCH DESIGN AND METHODS Patients (n = 426) were randomized 1:1 to sitagliptin (50 mg every day [q.d.] for moderate renal insufficiency and 25 mg q.d. for severe renal insufficiency) or glipizide (2.5 mg q.d., adjusted based on glycemic control to a 10-mg twice a day maximum dose). Randomization was stratified by: 1) renal status (moderate or severe renal insufficiency); 2) history of cardiovascular disease; and 3) history of heart failure. RESULTS At week 54, treatment with sitagliptin was noninferior to treatment with glipizide in A1C change from baseline (−0.8 vs. −0.6%; between-group difference −0.11%; 95% CI −0.29 to 0.06) because the upper bound of the 95% CI was less than the prespecified noninferiority margin of 0.4%. There was a lower incidence of symptomatic hypoglycemia adverse events (AEs) with sitagliptin versus glipizide (6.2 and 17.0%, respectively; P = 0.001) and a decrease in body weight with sitagliptin (−0.6 kg) versus an increase (1.2 kg) with glipizide (difference, −1.8 kg; P < 0.001). The incidence of gastrointestinal AEs was low with both treatments. CONCLUSIONS In patients with T2DM and chronic renal insufficiency, sitagliptin and glipizide provided similar A1C-lowering efficacy. Sitagliptin was generally well-tolerated, with a lower risk of hypoglycemia and weight loss versus weight gain, relative to glipizide. PMID:23248197

  20. 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

  1. 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

  2. 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

  3. Exploration of Sitagliptin as a potential inhibitor for the M1 Alanine aminopeptidase enzyme in Plasmodium falciparum using computational docking

    PubMed Central

    Krishnamoorthy, Mohana; Achary, Anant

    2013-01-01

    Plasmodium falciparum has limited capacity for de novo amino acid synthesis and rely on degradation of host hemoglobin to maintain protein metabolism and synthesis of proteins. M1 alanine aminopeptidase enzyme of the parasite involved in the terminal degradation of host hemoglobin was subjected to in silico screening with low molecular weight protease inhibitors. The km (avg) of the enzyme M1 alanine aminopeptidase for the substrate DL – Alanine β Napthylamide Hydrochloride was estimated as 322.05µM. The molecular interactions between the enzyme and the substrate and the mechanism of enzyme action were analyzed which paved way for inhibition strategies. Among all the inhibitors screened, Sitagliptin was found to be most potent inhibitor with ki of 0.152 µM in its best orientation whereas the ki(avg) was 2.0055 µM. The ki of Sitagliptin is lower than the km of M1 alanine aminopeptidase for the substrate DL – Alanine β Napthylamide Hydrochloride (322.05 µM) and Ki of the known inhibitor Bestatin. Therefore Sitagliptin may serve as a potent competitive inhibitor of the enzyme M1 alanine aminopeptidase of Plasmodium falciparum. PMID:23559748

  4. 2-Hydr-oxy-1-methoxy-anthraquinone monohydrate.

    PubMed

    Liu, Zhi-Meng; Jiao, Yuan-Qi

    2009-01-01

    The title compound, C(15)H(10)O(4)·H(2)O, also known as alizarin 1-methyl ether monohydrate, was isolated from Morinda officinalis How. The anthraquinone ring system is almost planar, the dihedral angle between the two outer benzene rings being 3.07 (4)°. In the crystal structure, O-H⋯O hydrogen bonds link the organic mol-ecules and the water mol-ecules, forming a three-dimensional network. PMID:21582814

  5. 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.

  6. Therapeutic effects of the dipeptidyl peptidase-IV inhibitor, sitagliptin, on non-alcoholic steatohepatitis in FLS-ob/ob male mice.

    PubMed

    Onoyama, Takumi; Koda, Masahiko; Okamoto, Toshiaki; Kishina, Manabu; Matono, Tomomitsu; Sugihara, Takaaki; Murawaki, Yoshikazu

    2015-11-01

    Non-alcoholic steatohepatitis is characterized by hepatic fat accumulation, inflammation and varying degrees of fibrosis. The dipeptidyl peptidase‑IV enzyme is important in glucose metabolism, as well as lipid accumulation, extracellular matrix metabolism and immune stimulation. Furthermore, the enzyme activity of dipeptidyl peptidase‑IV is known to be increased in non‑alcoholic steatohepatitis. Therefore, dipeptidyl peptidase‑IV inhibitors are potential therapeutic agents for non‑alcoholic steatohepatitis. The present study assessed the therapeutic effects of sitagliptin, a dipeptidyl peptidase‑IV inhibitor, on non‑alcoholic steatohepatitis using fatty liver Shionogi‑ob/ob male mice. Sitagliptin (2 mg/kg/day; n=10) or placebo (control; n=10) was orally administered to fatty liver Shionogi‑ob/ob mice for 12 weeks, and hepatic steatosis, fibrosis, inflammation and oxidative stress were assessed in comparison with the controls. Sitagliptin administration reduced body weight and blood glucose levels, and improved hepatic fibrosis. It also inhibited the gene expression levels of fatty acid synthase, transforming growth factor‑β1, tissue inhibitor of metalloproteinases‑1, procollagen‑type 1, tumor necrosis factor‑α, monocyte chemoattractant protein‑1 and enhanced peroxisome proliferator activated receptor‑α. Furthermore, a marked attenuation of hepatic stellate cell activation and Kupffer cells was observed in the sitagliptin group. A decrease in oxidative stress and apoptosis was also observed. Sitagliptin attenuated the progression of hepatic fibrosis by improving lipid metabolism, inflammation and oxidative stress in non-alcoholic steatohepatitis. PMID:26397061

  7. Synthesis, spectral, optical and thermal studies of 1-methyl-2,6-dimethyl-4-hydroxypyridinium chloride monohydrate and bromide monohydrate.

    PubMed

    Dhanuskodi, S; Manivannan, S; Philip, J

    2008-04-01

    Semiorganic 1-methyl-2,6-dimethyl-4-hydroxypyridinium chloride monohydrate (MDMPCl.H(2)O) and bromide monohydrate (MDMPBr.H(2)O) salts have been synthesized. Single crystals of MDMPCl.H(2)O and MDMPBr.H(2)O were grown by the slow evaporation method from aqueous solution at constant temperatures 30 and 32 degrees C respectively. The grown crystals were characterized by elemental analysis, FT-IR and FT-NMR techniques and their molecular structures were elucidated. Thermogravimetric, differential thermal analyses and differential scanning calorimetry reveal the presence of water molecules in the crystal lattices and thermal stabilities. Optical transmittance windows in aqueous solution were found as 300-1100 nm using UV-vis-NIR spectrophotometer. PMID:17709283

  8. 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

  9. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  10. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  11. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  12. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  13. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND... § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications. The...

  14. 21 CFR 524.1610 - Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Orbifloxacin, mometasone furoate monohydrate, and... DOSAGE FORM NEW ANIMAL DRUGS § 524.1610 Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension. (a) Specifications. Each gram of suspension contains 10 milligrams (mg) orbifloxacin,...

  15. Effects of Sitagliptin on Lipid Profiles in Patients With Type 2 Diabetes Mellitus: A Meta-analysis of Randomized Clinical Trials.

    PubMed

    Fan, Minhua; Li, Yuelan; Zhang, Shihong

    2016-01-01

    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

  16. Addition of sitagliptin or metformin to insulin monotherapy improves blood glucose control via different effects on insulin and glucagon secretion in hyperglycemic Japanese patients with type 2 diabetes.

    PubMed

    Otsuka, Yuichiro; Yamaguchi, Suguru; Furukawa, Asami; Kosuda, Minami; Nakazaki, Mitsuhiro; Ishihara, Hisamitsu

    2015-01-01

    This study aimed to explore the effects of the dipeptidyl peptidase-4 inhibitor sitagliptin and the biguanide metformin on the secretion of insulin and glucagon, as well as incretin levels, in Japanese subjects with type 2 diabetes mellitus poorly controlled with insulin monotherapy. This was a single-center, randomized, open-label, parallel group study, enrolling 25 subjects. Eleven patients (hemoglobin A1c [HbA1c] 8.40 ± 0.96%) and 10 patients (8.10 ± 0.54%) on insulin monotherapy completed 12-week treatment with sitagliptin (50 mg) and metformin (750 mg), respectively. Before and after treatment, each subject underwent a meal tolerance test. The plasma glucose, glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), C-peptide, and glucagon responses to a meal challenge were measured. HbA1c reductions were similar in patients treated with sitagliptin (0.76 ± 0.18%) and metformin (0.77 ± 0.17%). In the sitagliptin group, glucose excursion during a meal tolerance test was reduced and accompanied by elevations in active GLP-1 and active GIP concentrations. C-peptide levels were unaltered despite reduced glucose responses, while glucagon responses were significantly suppressed (-7.93 ± 1.95% of baseline). In the metformin group, glucose excursion and incretin responses were unaltered. C-peptide levels were slightly increased but glucagon responses were unchanged. Our data indicate that sitagliptin and metformin exert different effects on islet hormone secretion in Japanese type 2 diabetic patients on insulin monotherapy. A glucagon suppressing effect of sitagliptin could be one of the factors improving blood glucose control in patients inadequately controlled with insulin therapy. PMID:25328079

  17. 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

  18. The dipeptidyl peptidase-4 inhibitor sitagliptin suppresses mouse colon tumorigenesis in type 2 diabetic mice.

    PubMed

    Yorifuji, Naoki; Inoue, Takuya; Iguchi, Munetaka; Fujiwara, Kaori; Kakimoto, Kazuki; Nouda, Sadaharu; Okada, Toshihiko; Kawakami, Ken; Abe, Yosuke; Takeuchi, Toshihisa; Higuchi, Kazuhide

    2016-02-01

    Patients with type 2 diabetes mellitus are known to have an increased risk of colorectal neoplasia. Dipeptidyl peptidase-4 (DPP-4) inhibitors have been used as a new therapeutic tool for type 2 diabetes. Since the substrates for DPP-4 include intestinotrophic hormones and chemokines such as GLP-2 and stromal cell-derived factor-1 (SDF-1), which are associated with tumor progression, DPP-4 inhibitors may increase the risk of colorectal tumors. However, the influence of DPP-4 inhibitors on colorectal neoplasia in patients with type 2 diabetes remains unknown. In the present study, we show that long-term administration of a DPP-4 inhibitor, sitagliptin (STG), suppressed colon carcinogenesis in leptin-deficient (ob/ob) C57BL/6J mice. Colonic mucosal concentrations of glucagon‑like peptide-1 (GLP-1) and GLP-2 were significantly elevated in the ob/ob mice. However, mucosal GLP concentrations and the plasma level of SDF-1 were not affected by the administration of STG. Real‑time PCR analysis revealed that colonic mucosal IL-6 mRNA expression, which was significantly upregulated in the ob/ob mice, was significantly suppressed by the long-term administration of STG. These results suggest that a DPP-4 inhibitor may suppress colon carcinogenesis in mice with type 2 diabetes in a GLP-independent manner. Since DPP-4 has multiple biological functions, further studies analyzing other factors related to colon carcinogenesis are needed. PMID:26573958

  19. 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

  20. Prediction of the effect on antihyperglycaemic action of sitagliptin by plasma active form glucagon-like peptide-1

    PubMed Central

    Kushiyama, Akifumi; Kikuchi, Takako; Tanaka, Kentaro; Tahara, Tazu; Takao, Toshiko; Onishi, Yukiko; Yoshida, Yoko; Kawazu, Shoji; Iwamoto, Yasuhiko

    2016-01-01

    AIM: To investigate whether active glucagon-like peptide-1 (GLP-1) is a prediction Factor of Effect of sitagliptin on patients with type 2 diabetes mellitus (GLP-1 FEST:UMIN000010645). METHODS: Seventy-six patients with type 2 diabetes, who had insufficient glycemic control [Hemoglobin A1c (HbA1c) ≥ 7%] in spite of treatment with metformin and/or sulfonylurea, were included in the investigation. Patients were divided into three groups by tertiles of fasting plasma active GLP-1 level, before the administration of 50 mg sitagliptin. RESULTS: At baseline, body mass index, serum UA, insulin and HOMA-IR were higher in the high active GLP-1 group than in the other two groups. The high active GLP-1 group did not show any decline of HbA1c (7.6% ± 1.4% to 7.5% ± 1.5%), whereas the middle and low groups indicated significant decline of HbA1c (7.4 ± 0.7 to 6.8 ± 0.6 and 7.4 ± 1.2 to 6.9 ± 1.3, respectively) during six months. Only the low and middle groups showed a significant increment of active GLP-1, C-peptide level, a decreased log and proinsulin/insulin ratio after administration. In logistic analysis, the low or middle group is a significant explanatory variable for an HbA1c decrease of ≥ 0.5%, and its odds ratio is 4.5 (1.40-17.6) (P = 0.01) against the high active GLP-1 group. This remains independent when adjusted for HbA1c level before administration, patients’ medical history, medications, insulin secretion and insulin resistance. CONCLUSION: Plasma fasting active GLP-1 is an independent predictive marker for the efficacy of dipeptidyl peptidase 4 inhibitor sitagliptin. PMID:27326345

  1. Reinvestigation of growth of urea thiosemicarbazone monohydrate crystal

    NASA Astrophysics Data System (ADS)

    Srinivasan, Bikshandarkoil R.; Raghavaiah, Pallepogu; Nadkarni, V. S.

    2013-08-01

    The reaction of urea with thiosemicarbazide in 1:1 mole ratio in aqueous solution does not result in the formation of urea thiosemicarbazone monohydrate crystal, as reported by Hanumantharao, Kalainathan and Bhagavannarayana [Spectrochim. Acta A91 (2012) 345-351]. A reinvestigation of the reported reaction reveals that the crystal obtained is the starting material namely thiosemicarbazide, which has been unambiguously confirmed with the aid of infrared and 1H NMR spectra and single crystal X-ray structure determination. Analysis of 1H NMR spectrum reveals that thiosemicarbazide exhibits thione-thiol tautomerism in solution. In contrast, thiosemicarbazide exists as the thione tautomer in the solid state.

  2. Management of dyslipidemia and hyperglycemia with a fixed-dose combination of sitagliptin and simvastatin

    PubMed Central

    Steinberg, Helmut; Anderson, Matt S; Musliner, Thomas; Hanson, Mary E; Engel, Samuel S

    2013-01-01

    The risk of death due to heart disease and stroke is up to four times higher in individuals with diabetes compared to individuals without diabetes. Most guidelines that address treatment of dyslipidemia in patients with diabetes consider diabetes a cardiovascular disease (CVD) “risk equivalent” and recommend intensive treatment of dyslipidemia for the purpose of CVD prevention. Statins (3-hydroxy 3-methylglutaryl coenzyme A reductase [HMG-CoA reductase] inhibitors) are first-line agents in achieving lipid goals as an adjunct to diet and exercise and should be used in most patients. In addition to lipid management and blood pressure control, glycemic control is a basic component in the management of diabetes. Glycemic control is achieved by combining diabetes self-management education, diet and exercise, and, where required, antihyperglycemic agents (OHAs). Persistence and adherence to therapy are critical in achieving recommended treatment goals. However, overall compliance with concomitantly prescribed OHAs and statins is low in patients with type 2 diabetes. Fixed-dose combination (FDC) therapies have been shown to improve adherence by reducing pill burden, the complexity of treatment regimen, and, potentially, cost. Based on the available evidence regarding the pharmacokinetics and the efficacy and safety profiles of each component drug, the sitagliptin/simvastatin FDC may provide a rational and well-tolerated approach to achieving better adherence to multiple-drug therapy and improved lipid lowering and glycemic control, with consequent reduction in cardiovascular risk, diabetic microvascular disease, and mortality in diabetic patients for whom treatment with both compounds is appropriate. PMID:23761972

  3. 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

  4. Diabetic Nephropathy Amelioration by a Low-Dose Sitagliptin in an Animal Model of Type 2 Diabetes (Zucker Diabetic Fatty Rat)

    PubMed Central

    Mega, Cristina; Teixeira de Lemos, Edite; Vala, Helena; Fernandes, Rosa; Oliveira, Jorge; Mascarenhas-Melo, Filipa; Teixeira, Frederico; Reis, Flávio

    2011-01-01

    This study was performed to assess the effect of chronic low-dose sitagliptin, a dipeptidyl peptidase 4 inhibitor, on metabolic profile and on renal lesions aggravation in a rat model of type-2 diabetic nephropathy, the Zucker diabetic fatty (ZDF) rat. Diabetic and obese ZDF (fa/fa) rats and their controls ZDF (+/+) were treated for 6 weeks with vehicle (control) or sitagliptin (10 mg/kg/bw). Blood/serum glucose, HbA1c, insulin, Total-c, TGs, urea, and creatinine were assessed, as well as kidney glomerular and tubulointerstitial lesions (interstitial fibrosis/tubular atrophy), using a semiquantitative rating from 0 (absent/normal) to 3 (severe and extensive damage). Vascular lesions were scored from 0–2. Sitagliptin in the diabetic rats promoted an amelioration of glycemia, HbA1c, Total-c, and TGs, accompanied by a partial prevention of insulinopenia. Furthermore, together with urea increment prevention, renal lesions were ameliorated in the diabetic rats, including glomerular, tubulointerstitial, and vascular lesions, accompanied by reduced lipid peroxidation. In conclusion, chronic low-dose sitagliptin treatment was able to ameliorate diabetic nephropathy, which might represent a key step forward in the management of T2DM and this serious complication. PMID:22203828

  5. 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

  6. 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

  7. 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

  8. Safety and Efficacy of Sitagliptin-Metformin in Fixed Combination for the Treatment of Type 2 Diabetes Mellitus

    PubMed Central

    Ballav, Chitrabhanu; Gough, Stephen C.L.

    2013-01-01

    The biguanide, metformin, is considered first-line treatment for type 2 diabetes. Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor acts through the incretin pathway and has a glucose dependent mode of action. The complementary hypoglycemic properties of these drugs make fixed dose combination treatment an attractive prospect. Evidence from recent clinical trials suggests a beneficial effect of the combination on efficacy, demonstrated by significant improvement of hemoglobin A1c (HbA1c), fasting and postprandial glucose levels. The fixed dose combination is likely to have greater patient tolerability compared with monotherapy with either agent because of low rates of hypoglycemia, weight neutrality, and lower rates of side effects. High acquisition cost and paucity of long-term safety data are, however, potential barriers to their wider use. An overview of the pharmacology and clinical outcomes from recent trials of the metformin-sitagliptin combination and how the combination could fit into the type 2 diabetes treatment algorithm is presented in this review. PMID:24031162

  9. 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

  10. Linagliptin but not Sitagliptin inhibited transforming growth factor-β2-induced endothelial DPP-4 activity and the endothelial-mesenchymal transition.

    PubMed

    Shi, Sen; Kanasaki, Keizo; Koya, Daisuke

    2016-02-26

    Dipeptidyl peptidase (DPP)-4 plays an important role in endothelial cell biology. We have shown that the DPP-4 inhibitor Linagliptin can inhibit the endothelial-mesenchymal transition (EndMT) and ameliorate diabetic kidney fibrosis associated with the suppression of DPP-4 protein levels via the induction of miR-29. The current study demonstrated that such effects of Linagliptin on endothelial cell profibrotic programs were drug-specific but not class effects. In the cell-free system, both Linagliptin and Sitagliptin inhibited recombinant DPP-4 activity in a concentration-dependent manner. Linagliptin can inhibit all of the following: DPP-4 activity and protein level, integrin β1 protein levels, EndMT, and DPP-4 3'UTR activity; Sitagliptin, however, inhibited none of these in the current study. Additionally, TGF-β2 induced both the induction of VEGF-R1 and the suppression of VEGF-R2 levels in endothelial cells, and both were inhibited by Linagliptin but not by Sitagliptin. miR-29, the miR that negatively regulates the 3'UTR of DPP-4 mRNA, was suppressed by TGF-β2 and restored by Linagliptin but not by Sitagliptin. Following the overexpression of pCMV-DPP-4-GFP and pCMV6-Myc-DPP-4 in endothelial cells, the proximity of Myc-DPP-4 and DPP-4-GFP was suppressed by Linagliptin but not by Sitagliptin, suggesting that only Linagliptin inhibited the homo-dimer formation of DPP-4 in endothelial cells; this difference in activity between the two gliptins could explain their diverse effects on endothelial cell biology. In conclusion, each of the DPP-4 inhibitors may have unique drug-specific effects. PMID:26826382

  11. Miglitol administered before breakfast increased plasma active glucagon-like peptide-1 (GLP-1) levels after lunch in patients with type 2 diabetes treated with sitagliptin.

    PubMed

    Aoki, Kazutaka; Kamiyama, Hiroshi; Yoshimura, Kouichiro; Shibuya, Makoto; Masuda, Kiyomi; Terauchi, Yasuo

    2012-06-01

    We recently reported that the administration of miglitol alone just before breakfast improved postprandial hyperglycemia and increased active glucagon-like peptide-1 (GLP-1) levels after lunch in men without diabetes. Miglitol and dipeptidyl peptidase-4 inhibitors, such as sitagliptin, enhance plasma active GLP-1 concentrations via different mechanisms; therefore, combined therapy with these agents was more effective than monotherapy. In this study, we compared the effectiveness of the administration of miglitol alone just before breakfast on the plasma glucose, serum insulin and glucagon, and plasma incretin levels in sitagliptin-treated patients with type 2 diabetes. We measured the plasma glucose, serum insulin and glucagon, plasma active GLP-1, and total glucose-dependent insulinotropic polypeptide levels before breakfast, at 120 min after breakfast, before lunch, and 60 and 120 min after lunch in patients with diabetes who are receiving sitagliptin. This trial was performed for the following 2 days on each subject (Day 1: no miglitol, Day 2: miglitol alone [50 mg] administered just before breakfast). The area under the curve (AUC) of the plasma glucose levels after lunch in the miglitol-treated group tended to be lower than that in the miglitol-untreated group, but the difference was not statistically significant. Miglitol alone administered at breakfast increased the AUC of the active plasma GLP-1 levels after lunch in sitagliptin-treated patients with diabetes. Our results suggest that the once-daily administration of miglitol as a "GLP-1 enhancer" in combination with sitagliptin was effective for the treatment for patients with diabetes. PMID:21898126

  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 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

  14. 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

  15. 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.

  16. Hydrothermal crystallization of α-alumina monohydrate in the presence of copper ions

    NASA Astrophysics Data System (ADS)

    Brown, N.

    1989-09-01

    The effect of copper ions on the hydrothermal crystallization of α-alumina monohydrate (A1OOH, mineral name boehmite), following oxidation of the organic carbon compounds in sodium aluminate solution of the Bayer process, has been examined using scanning electron microscopy and particle size analyses. The initial effect of the copper ions on the homogeneously nucleated α-alumina monohydrate is to inhibit crystal growth on the (001) faces and direct the growth process to the prismatic faces of the rhombic or diamond shaped crystals. At low copper levels (up to 0.1 wt% in α-alumina monohydrate), this leads to the formation of plate-like crystals up to 25 μm in size which can intergrow and develop into particles with an average size of up to 100 μm. The size and structure of the μ-alumina monohydrate particles, however, depend on the amount of copper present and increasing copper levels (up to 1.0 wt%) lead progressively to a decrease in average particle size of α-alumina monohydrate to about 10 μm and the formation of more rounded oblong-shaped particles having a compact sheaf-like structure. Copper-containing α-alumina monohydrate particles of this size and form can be readily recovered from the oxidized liquor and recycled in the industrial process.

  17. 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.

  18. 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

  19. 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

  20. Direct Catalytic Asymmetric Mannich Reaction with Dithiomalonates as Excellent Mannich Donors: Organocatalytic Synthesis of (R)-Sitagliptin.

    PubMed

    Bae, Han Yong; Kim, Mun Jong; Sim, Jae Hun; Song, Choong Eui

    2016-08-26

    In this study, dithiomalonates (DTMs) were demonstrated to be exceptionally efficient Mannich donors in terms of reactivity and stereoselectivity in cinchona-based-squaramide-catalyzed enantioselective Mannich reactions of diverse imines or α-amidosulfones as imine surrogates. Owing to the superior reactivity of DTMs as compared to conventional malonates, the catalyst loading could be reduced to 0.1 mol % without the erosion of enantioselectivity (up to 99 % ee). Furthermore, by the use of a DTM, even some highly challenging primary alkyl α-amidosulfones were smoothly converted into the desired adducts with excellent enantioselectivity (up to 97 % ee), whereas the use of a malonate or monothiomalonate resulted in no reaction under identical conditions. The synthetic utility of the chiral Mannich adducts obtained from primary alkyl substrates was highlighted by the organocatalytic, coupling-reagent-free synthesis of the antidiabetic drug (-)-(R)-sitagliptin. PMID:27486059

  1. 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.

  2. Cost-utility of albiglutide versus insulin lispro, insulin glargine, and sitagliptin for the treatment of type 2 diabetes in the US.

    PubMed

    Bruhn, David; Martin, Alan A; Tavares, Ruben; Hunt, Barnaby; Pollock, Richard F

    2016-07-01

    Objective To compare the cost-utility of the glucagon-like peptide-1 receptor agonist albiglutide with those of insulin lispro (both in combination with insulin glargine), insulin glargine, and the dipeptidyl peptidase-4 inhibitor sitagliptin, representing treatments along the type 2 diabetes treatment continuum. Methods The Centre for Outcomes Research and Effectiveness (CORE) Diabetes Model was used for the cost-utility analysis. Data from three Phase 3 clinical trials (HARMONY 6, HARMONY 4, and HARMONY 3) evaluating albiglutide for the treatment of patients with type 2 diabetes were used for the baseline characteristics and treatment effects. Utilities and costs were derived from published sources. Results Albiglutide treatment was associated with an improvement in mean quality-adjusted life expectancy of 0.099, 0.033, and 0.101 years when compared with insulin lispro, insulin glargine, and sitagliptin, respectively. Over the 50-year time horizon, mean total costs in the albiglutide arm were $4332, $2597, and $2223 more than in the other respective treatments. These costs resulted in an incremental cost-utility ratio of $43,541, $79,166, and $22,094 per quality-adjusted life-year (QALY) gained for albiglutide vs insulin lispro, insulin glargine, and sitagliptin, respectively. At a willingness-to-pay threshold of $50,000 per QALY gained, there was a 53.0%, 41.5%, and 67.5% probability of albiglutide being cost-effective compared with the other respective treatments. Limitations This analysis was an extrapolation over a 50-year time horizon based on relatively short-term data obtained during clinical trials. It does not take into account potential differences between the respective treatments in adherence and persistence that can influence both effects and costs. Conclusions Albiglutide represents a reasonable treatment option for patients with type 2 diabetes based on its cost-utility, relative to insulin lispro, insulin glargine, and sitagliptin. PMID:26882484

  3. Adding of Sitagliptin on Insulin Therapy Effectively and Safely Reduces a Hemoglobin A1c Level and Glucose Fluctuation in Japanese Patients with Type 2 Diabetes

    PubMed Central

    Tajiri, Yuji; Kawano, Seiko; Hirao, Saori; Oshige, Tamami; Iwata, Shinpei; Ono, Yasuhiro; Inada, Chizuko; Akashi, Tomoyuki; Hayashi, Hideki; Tojikubo, Masayuki; Yamada, Kentaro

    2014-01-01

    Aims. Efficacy and safety of DPP-4 inhibitor, sitagliptin, add-on therapy to insulin were investigated in Japanese patients with type 2 diabetes. Subjects and Methods. Two hundred and sixteen patients (126 men, 65 ± 12 years old, BMI 24.9 ± 4.5, means ± S.D.) who had been treated by insulin alone or insulin combined with other oral hypoglycemic agents (OHAs) were recruited, and sitagliptin was added for 3 months. Results. HbA1c was significantly decreased after 3 months of add-on therapy as a whole (8.56 ± 1.50% to 7.88 ± 1.25%, P < 0.0001). Body weight did not change and insulin dosage was significantly (P < 0.0001) decreased for 3 months. Furthermore, day-to-day glucose variability was significantly reduced (18.3 ± 9.1 to 16.1 ± 8.1%, P < 0.05). In stepwise multiple regression analysis on ΔHbA1c as an outcome variable, the higher baseline HbA1c value and a preserved CPR were selected as significant predictive variables. Fifteen patients complained of mild hypoglycemia without any assistance during 3 months of sitagliptin add-on, while no severe hypoglycemic episode was reported. Conclusions. Add-on of sitagliptin to ongoing insulin therapy effectively reduced either HbA1c level or glucose fluctuation and could be a practical and well-tolerated alternative to treat Japanese patients with type 2 diabetes who had been inadequately controlled by insulin with or without other OHAs.

  4. 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

  5. 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

  6. Growth, spectral, optical, thermal, crystallization perfection and nonlinear optical studies of novel nonlinear optical crystal—Urea thiosemicarbazone monohydrate

    NASA Astrophysics Data System (ADS)

    Hanumantharao, Redrothu; Kalainathan, S.; Bhagavannarayana, G.

    2012-06-01

    Single crystals of organic nonlinear material urea thiosemicarbazone monohydrate (UTM) have been grown by slow evaporation method. The grown crystals were characterized by single crystal X-ray diffraction analysis reveals that sample crystallized in triclinic system with noncentrosymmetric space group P1. Powder XRD pattern confirmed that grown crystal posses highly crystalline nature. FTIR spectrum was recorded to identify the presence of functional groups and molecular structure was confirmed by 1H NMR spectrum. Material confirmation of title compound has been performed by using mass spectroscopic analysis. Elemental composition of grown crystal was confirmed by energy-dispersive spectrometry (EDS). To study the crystalline perfection of the grown crystals, high-resolution X-ray diffraction (HR-XRD) study was carried out. Thermogravimetric and differential thermal analyses were employed to understand the thermal and physio-chemical stability of the synthesized compound. UV-Vis-NIR spectrum revealed the transmission properties of the crystal specimen. Relative SHG efficiency is measured by Kurtz and Perry method and found to about 0.89 times that of standard potassium dihydrogen phosphate (KDP) crystals.

  7. 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.

  8. Determination of Cephalexin Monohydrate in Pharmaceutical Dosage Form by Stability-Indicating RP-UFLC and UV Spectroscopic Methods

    PubMed Central

    Panda, Sagar Suman; Ravi Kumar, Bera V. V.; Dash, Rabisankar; Mohanta, Ganeswar

    2013-01-01

    An ultra-fast liquid chromatographic method and two UV spectroscopic methods were developed for the determination of cephalexin monohydrate in pharmaceutical dosage forms. Isocratic separation was performed on an Enable C18G column (250 mm × 4.6 mm i.d., 5 μm) using methanol:0.01 M TBAHS (50:50, v/v) as the mobile phase at a flow rate of 1.0 ml/min. The PDA detection wavelength was set at 254 nm. The UV spectroscopic method was performed at 261 nm and at 256–266 nm for the AUC method using a phosphate buffer (pH=5.5). The linearity was observed over a concentration range of 1.0–120 μg/ml for UFLC and both of the UV spectroscopic methods (correlation coefficient=0.999). The developed methods were validated according to ICH guidelines. The relative standard deviation values for the intraday and interday precision studies were < 2%, and the accuracy was > 99% for all of the three methods. The developed methods were used successfully for the determination of cephalexin in dry syrup formulation. PMID:24482771

  9. 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.

  10. Dissolution kinetics of single crystals of alpha-lactose monohydrate.

    PubMed

    Raghavan, S L; Ristic, R I; Sheen, D B; Sherwood, J N

    2002-10-01

    The dissolution kinetics of alpha-lactose monohydrate (alphaLM) single crystals were studied by a flow-cell method at different undersaturations. Linear dissolution profiles were obtained as a function of time for all the faces except the (010) face. The dissolution rates, obtained from these profiles, were anisotropic and varied considerably with undersaturation. At low undersaturations (0-2%), the order of dissolution rate was (110) > (100) > (011) = (110) > (010). This order changed with increasing undersaturation (>5%) to (011) > (100) > (110) > (110) > (010). In alphaLM crystals in which lattice strain was induced by synchrotron X-irradiation, the rates of dissolution of all faces increased with increasing strain. The increase was less significant for the (011) faces than for the remainder. Under this constraint, the (010) face became the fastest dissolving one and the [011]face became the slowest one. The results of all experiments are explained on the basis that although dislocations may act as initiating dissolution centers at very low undersaturations, these sources rapidly give way to two-dimensional nucleation of randomly distributed dissolution sites as the undersaturation is increased. Under these conditions, which better reflect the normal dissolution processes of materials, bulk lattice strain plays the most significant role in defining the dissolution rate. The results show a potential route to the controlled engineering of the dissolution behavior of crystalline materials. PMID:12226843

  11. 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.

  12. Scientific facts behind creatine monohydrate as sport nutrition supplement.

    PubMed

    Silber, M L

    1999-09-01

    Currently, strong efforts are being made toward demonstrating possible risks of using pure creatine monohydrate (Cr.H2O). In this article, scientific facts and considerations are presented, which support such concern. A further attempt is made to pursue the concept of possible risks of uncontrolled supplementation in athletes with pure Cr.H2O. The problem is viewed from the scientific evidence that a highly conservative mechanism of homeostatic feed-back inhibitory self-regulation of Cr biosynthesis in the body has been evolutionary developed. It is shown that numerous features characteristic to Cr biosynthesis, metabolism, and regulation allow to interpret its stimulatory action in the body as endocrine hormone-like. Based on this assumption, a practical approach for detecting altered links in Cr metabolism and biosynthesis under conditions of pure Cr.H2O overdosing, is suggested. Strategic considerations regarding early diagnosis, prognosis, and correction of the down-regulated endogenous Cr biosynthesis in athletes on continuous pure Cr.H2O supplementation, are discussed. As a high efficient and safe alternative to pure Cr.H2O, a complex nutrition supplement formula for elite athletes is proposed, which exploits natural alpha-ketoglutarate as a vehicle for delivering exogenous low molecular biologically-active compounds, including Cr. PMID:10573658

  13. 9-O-Ethyl­berberrubinium iodide monohydrate

    PubMed Central

    Grundt, Peter; Pernat, Jennifer; Krivogorsky, Bogdana; Halverson, Melanie A.; Berry, Steven M.

    2010-01-01

    In the title compound (systematic name: 9-eth­oxy-10-meth­oxy-5,6-dihydro-1,3-dioxolo[4,5-g]isoquinolino­[3,2-a]isoquin­olin-7-ium iodide monohydrate), 2C21H20NO4 +·2I−·H2O, two independent mol­ecules pack in the unit cell, where interactions between the molecules are stabilized by weak inter­molecular π–π stacking inter­actions [centroid–centroid distances in the range 3.571 (4) to 3.815 (4)Å]. Inter­molecular C—H⋯O inter­actions are also observed. The iodide anions are disordered with occupancy ratios of 0.94 (1):0.06 (1) and 0.91 (1):0.09 (1). The cationic molecule is planar in structure with a small torsion resulting from the dihydropyridine ring. PMID:21587567

  14. Effects on whole saliva of chewing gums containing calcium phosphates.

    PubMed

    Chow, L C; Takagi, S; Shern, R J; Chow, T H; Takagi, K K; Sieck, B A

    1994-01-01

    To evaluate chewing gums as a vehicle to increase salivary mineral saturation levels and enhance salivation, monocalcium phosphate monohydrate (MCPM) and an equimolar mixture of tetracalcium phosphate (TTCP) with dicalcium phosphate anhydrous (DCPA) were chosen as experimental chewing gum additives. Each of eight subjects chewed a commercial sugarless bubble gum (control) for 16 min or the same gum to which 5 wt% of MCPM or the TTCP-DCPM mixture had been added. The saliva samples collected every 2 min were analyzed for weight, pH, and total calcium (Ca) and phosphate (P) concentrations. Both experimental gums were found to increase significantly the Ca and P concentrations of saliva during the 16-minute period even more than with a previously evaluated gum that contained dicalcium phosphate dihydrate. The degree of saturation of tooth mineral was significantly increased by both experimental gums, with the greater increase being produced by the TTCP-DCPA gum. The MCPM gum produced a significantly greater saliva flow and a lower salivary pH than did the control and TTCP-DCPA gums. The results suggest that the experimental gums may be useful for promoting remineralization in general and for inducing salivation in xerostomic patients. PMID:8294615

  15. 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.

  16. 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

  17. Sitagliptin/Metformin Versus Insulin Glargine Combined With Metformin in Obese Subjects With Newly Diagnosed Type 2 Diabetes.

    PubMed

    Ji, Ming; Xia, Libin; Cao, Jingzhu; Zou, Dajin

    2016-03-01

    To compare the therapeutic effects of different regimens in Chinese obese type 2 diabetic mellitus (T2DM) patients. From October 2013 to July 2014, a total of 166 T2DM outpatients who attended the Shanghai Changhai Hospital and the Yijishan Hospital of Wannan Medical College were randomly assigned into an experimental sitagliptin/metformin combined with low caloric diet group (n = 115) and an insulin glargine combined with metformin control group (n = 51). Inclusion criteria were body mass index (BMI) ≥ 25 kg/m and diagnosed with T2DM with glycosylated hemoglobin (glycated hemoglobin A1C [HbA1c]) >9%. Main outcome parameters were fasting plasma glucose, postprandial plasma glucose, BMI, HbA1c, fasting C-peptide, 2-h postprandial C-peptide, triglyceride (TG), total cholesterol (TC), high-density cholesterol (HDL-C), and low-density cholesterol (LDL-C), which were determined by the 75 g steamed-bun meal tolerance test before and 4, 8, 12, and 24 weeks after the treatment started. Treatment costs and life quality were also assessed. BMI, HbA1C, TG, TC, and LDL were significantly more reduced (P < 0.000) and HbA1c significantly better improved in the experimental group than in the control group (<6.5% in 24 [20.87%] vs 2 [3.92%], P < 0.001; <7% in 65 [56.52%] vs 12 [23.53%], P < 0.001). Quality of life scores in the experimental group increased more than in the control group (P < 0.001). The costs for the experimental group medication were less than for other regimens. For obese T2DM patients diagnosed with a glycosylated hemoglobin level >9%, oral sitagliptin/metformin combined with a low caloric diet effectively and economically maintained glycemic control and significantly improved life quality. PMID:26986104

  18. Sitagliptin/Metformin Versus Insulin Glargine Combined With Metformin in Obese Subjects With Newly Diagnosed Type 2 Diabetes

    PubMed Central

    Ji, Ming; Xia, Libin; Cao, Jingzhu; Zou, Dajin

    2016-01-01

    Abstract To compare the therapeutic effects of different regimens in Chinese obese type 2 diabetic mellitus (T2DM) patients. From October 2013 to July 2014, a total of 166 T2DM outpatients who attended the Shanghai Changhai Hospital and the Yijishan Hospital of Wannan Medical College were randomly assigned into an experimental sitagliptin/metformin combined with low caloric diet group (n = 115) and an insulin glargine combined with metformin control group (n = 51). Inclusion criteria were body mass index (BMI) ≥ 25 kg/m2 and diagnosed with T2DM with glycosylated hemoglobin (glycated hemoglobin A1C [HbA1c]) >9%. Main outcome parameters were fasting plasma glucose, postprandial plasma glucose, BMI, HbA1c, fasting C-peptide, 2-h postprandial C-peptide, triglyceride (TG), total cholesterol (TC), high-density cholesterol (HDL-C), and low-density cholesterol (LDL-C), which were determined by the 75 g steamed-bun meal tolerance test before and 4, 8, 12, and 24 weeks after the treatment started. Treatment costs and life quality were also assessed. BMI, HbA1C, TG, TC, and LDL were significantly more reduced (P < 0.000) and HbA1c significantly better improved in the experimental group than in the control group (<6.5% in 24 [20.87%] vs 2 [3.92%], P < 0.001; <7% in 65 [56.52%] vs 12 [23.53%], P < 0.001). Quality of life scores in the experimental group increased more than in the control group (P < 0.001). The costs for the experimental group medication were less than for other regimens. For obese T2DM patients diagnosed with a glycosylated hemoglobin level >9%, oral sitagliptin/metformin combined with a low caloric diet effectively and economically maintained glycemic control and significantly improved life quality. PMID:26986104

  19. 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.

  20. 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.

  1. 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

  2. 75 FR 16346 - Ophthalmic and Topical Dosage Form New Animal Drugs; Orbifloxacin, Mometasone Furoate Monohydrate...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-04-01

    ... orbifloxacin, mometasone furoate monohydrate, and posaconazole for the treatment of otitis externa in dogs... of otitis externa in dogs associated with susceptible strains of yeast (Malassezia pachydermatis) and... posaconazole. (b) Sponsor. See No. 000061 in Sec. 510.600(c) of this chapter. (c) Conditions of use in...

  3. Negative Linear Compressibility in Organic Mineral Ammonium Oxalate Monohydrate with Hydrogen Bonding Wine-Rack Motifs.

    PubMed

    Qiao, Yuancun; Wang, Kai; Yuan, Hongsheng; Yang, Ke; Zou, Bo

    2015-07-16

    Negative linear compressibility (NLC) is a relatively uncommon phenomenon and rarely studied in organic systems. Here we provide the direct evidence of the persistent NLC in organic mineral ammonium oxalate monohydrate under high pressure using synchrotron X-ray powder diffraction, Raman spectroscopy and density functional theory (DFT) calculation. Synchrotron X-ray powder diffraction measurement reveals that ammonium oxalate monohydrate shows both positive and negative linear compressibility along b-axis before 11.5 GPa. The red shift of the external Raman modes and abnormal changes of several selected internal modes in high-pressure Raman spectra further confirmed the NLC. DFT calculations demonstrate that the N-H···O hydrogen bonding "wine-rack" motifs result in the NLC along b-axis in ammonium oxalate monohydrate. We anticipate the high-pressure study of ammonium oxalate monohydrate may represent a promising strategy for accelerating the pace of exploitation and improvement of NLC materials especially in organic systems. PMID:26266859

  4. 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.

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

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Orbifloxacin, mometasone furoate monohydrate, and posaconazole suspension. 524.1610 Section 524.1610 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS OPHTHALMIC AND TOPICAL DOSAGE FORM NEW ANIMAL DRUGS...

  6. 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

  7. Comparison of GLP-1 Analogues versus Sitagliptin in the Management of Type 2 Diabetes: Systematic Review and Meta-Analysis of Head-to-Head Studies

    PubMed Central

    Wang, Tiansheng; Gou, Zhuoyue; Wang, Fei; Ma, Manling; Zhai, Suo-di

    2014-01-01

    Background Incretin–based therapies which include glucagon-like peptide-1 (GLP-1) receptor agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors are recommended by several practice guidelines as second-line agents for add-on therapy to metformin in patients with type 2 diabetes (T2DM) who do not achieve glycemic control with metformin plus lifestyle interventions alone. The purpose of this study is to perform a systematic review with meta-analysis of existing head to head studies to compare the efficacy and safety of GLP-1 analogues with DPP-4 inhibitors. Methods We performed a systematic review and meta-analysis of head-to-head studies to compare GLP-1 analogues with DPP-4 inhibitors in the management of type 2 diabetes. A random effects model was selected to perform the meta-analyses, results were expressed as weighted mean differences for continuous outcomes and relative risks for dichotomous outcomes, both with 95% confidence intervals, and with I2 values and P values as markers of heterogeneity. Results Four head-to-head randomized controlled studies with 1755 patients were included. Compared to sitagliptin, GLP-1 analogues are more effective in reducing HbA1C (weight mean difference −0.41%, 95% CI −0.51 to −0.31) and body weight (weight mean difference −1.55 kg, 95% CI −1.98 to −1.12). Conversely, GLP-1 analogues are associated with a higher incidence of gastrointestinal adverse events compared to sitagliptin: nausea (relative risk 3.14, 95% CI 2.15 to 4.59), vomiting (relative risk 2.60, 95% CI 1.48 to 4.56), diarrhea (relative risk 1.82, 95% CI 1.24 to 2.69), and constipation (relative risk 2.50, 95% CI 1.33 to 4.70). Conclusions The result of this meta-analysis demonstrates that compared to sitagliptin, GLP-1 analogues are more effective for glycemic control and weight loss, but have similar efficacy in reducing blood pressure and lipid parameters, however, GLP-1 analogues are associated with a higher incidence of gastrointestinal adverse

  8. 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

  9. 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

  10. 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

  11. 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

  12. 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.

  13. 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.

  14. [In vitro effect of Hordeum vulgare on the crystallization of calcium oxalate monohydrate (whewellite)].

    PubMed

    Djaroud, Samira; Harrache, Djamila; Amar, Amina

    2012-01-01

    The recommended conservative treatment of hyperoxaluria is mainly based on hyperhydration and ingestion of inhibitors of crystallization. In accordance with this context, the aim of this study was to determine the in vitro effect of Hordeum vulgare on calcium oxalate crystallization oxalo-dependent. The crystallization of calcium oxalate monohydrate in supersaturated aqueous solution at 37 °C, was followed in a model turbidimetric continuous in a closed system. The proposed model is very good reproducibility (CV < 10%), crystallization was monitored continuously in the presence of Hordeum vulgare at different concentrations (0.0625 to 1 g/L). The comparison of turbidimetric parameters, that characterize the growth stage of monohydrated oxalate calcium crystals and observation of the crystals obtained at the end of crystallization into scanning electron microscopy, have been able to demonstrate the inducing effect of Hordeum vulgare to 0.0625 g/L and a slight inhibitory effect at the others concentrations. PMID:23207820

  15. Growth and characterization of Cu (II) doped negatively soluble lithium sulfate monohydrate crystals

    NASA Astrophysics Data System (ADS)

    Boopathi, K.; Ramasamy, P.; Bhagavannarayana, G.

    2014-01-01

    Single crystals of pure and Cu (II) doped negatively soluble lithium sulfate monohydrate have been grown by slow evaporation solution technique. In the present work, to improve the crystalline quality of lithium sulfate monohydrate crystal, metal dopant was incorporated into the pure crystals. The as grown crystals are clear, transparent and the sizes of the crystals were up to 18×12×3 mm3 and 50×15×5 mm3. The presence of metal dopant has been confirmed by energy dispersive spectroscopy, atomic absorption spectroscopy analysis. Single crystal and powder X-ray diffraction studies were carried out to ascertain lattice parameters and identify different phase nature. Optical transmission spectrum of the grown crystals was recorded. FT-IR and thermal analysis were carried out to investigate the functional group and thermal behavior of the grown crystals respectively. The grown crystal was subjected to Vickers micro hardness, HRXRD, piezoelectric, laser damage threshold measurements and second harmonic generation efficiency studies.

  16. 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.

  17. 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

  18. Theoretical calculation of zero field splitting parameters of Cr3+ doped ammonium oxalate monohydrate

    NASA Astrophysics Data System (ADS)

    Kripal, Ram; Yadav, Awadhesh Kumar

    2015-06-01

    Zero field splitting parameters (ZFSPs) D and E of Cr3+ ion doped ammonium oxalate monohydrate (AOM) are calculated with formula using the superposition model. The theoretically calculated ZFSPs for Cr3+ in AOM crystal are compared with the experimental value obtained by electron paramagnetic resonance (EPR). Theoretical ZFSPs are in good agreement with the experimental ones. The energy band positions of optical absorption spectra of Cr3+ in AOM crystal calculated with CFA package are in good match with the experimental values.

  19. Influence of storage condition on properties of MCC II-based pellets with theophylline-monohydrate.

    PubMed

    Krueger, Cornelia; Thommes, Markus; Kleinebudde, Peter

    2014-10-01

    Microcrystalline cellulose II (MCC II(1)) is a polymorph of commonly used MCC I; in 2010 it was introduced as new pelletization aid in wet-extrusion/spheronization leading to fast disintegrating pellets. Previous investigations suggested that the storage of the resulting pellets affect the disintegration behavior, the non-hygroscopic substance chloramphenicol that showed no polymorphism or hydrate formation due to relative humidity was used for the investigations. Therefore, theophylline-monohydrate that can dehydrate during storage, but also during manufacturing and drying was used for this study to confirm the results of the previous study and give a more detailed overview of the influence of recrystallization of theophylline monohydrate on disintegration. Storage recommendations should be derived. MCC II-based pellets were prepared of binary mixtures containing 10%, 20% or 50% MCCII as pelletization aid and theophylline-monohydrate as API. These pellets were stored at different relative humidity (0-97%rH; 20°C); the influence on their disintegration and drug release was investigated. The storage conditions had an impact on pellet disintegration. Low relative humidities (⩽ 40%rH) led to a conversion of the monohydrate to the anhydrous form. Newly grown crystals formed a kind of network around the pellet and inhibited the disintegration. High relative humidity (>80%rh) affected the disintegration caused by changes in the MCCII as already seen in the previous study. Due to the changed disintegration behavior also the drug release and release kinetic changed. Therefore, for theophylline containing pellets a storage humidity of 55%rH to 80%rH (20°C) is recommended. All in all, these investigations substantiate the knowledge of MCCII-based pellets providing a better basis for adequate storage conditions of MCCII based pellets. PMID:24950003

  20. Peptides of Matrix Gla Protein Inhibit Nucleation and Growth of Hydroxyapatite and Calcium Oxalate Monohydrate Crystals

    PubMed Central

    Goiko, Maria; Dierolf, Joshua; Gleberzon, Jared S.; Liao, Yinyin; Grohe, Bernd; Goldberg, Harvey A.; de Bruyn, John R.; Hunter, Graeme K.

    2013-01-01

    Matrix Gla protein (MGP) is a phosphorylated and γ-carboxylated protein that has been shown to prevent the deposition of hydroxyapatite crystals in the walls of blood vessels. MGP is also expressed in kidney and may inhibit the formation of kidney stones, which mainly consist of another crystalline phase, calcium oxalate monohydrate. To determine the mechanism by which MGP prevents soft-tissue calcification, we have synthesized peptides corresponding to the phosphorylated and γ-carboxylated sequences of human MGP in both post-translationally modified and non-modified forms. The effects of these peptides on hydroxyapatite formation and calcium oxalate crystallization were quantified using dynamic light scattering and scanning electron microscopy, respectively. Peptides YGlapS (MGP1-14: YγEpSHEpSMEpSYELNP), YEpS (YEpSHEpSMEpSYELNP), YGlaS (YγESHESMESYELNP) and SK-Gla (MGP43-56: SKPVHγELNRγEACDD) inhibited formation of hydroxyapatite in order of potency YGlapS > YEpS > YGlaS > SK-Gla. The effects of YGlapS, YEpS and YGlaS on hydroxyapatite formation were on both crystal nucleation and growth; the effect of SK-Gla was on nucleation. YGlapS and YEpS significantly inhibited the growth of calcium oxalate monohydrate crystals, while simultaneously promoting the formation of calcium oxalate dihydrate. The effects of these phosphopeptides on calcium oxalate monohydrate formation were on growth of crystals rather than nucleation. We have shown that the use of dynamic light scattering allows inhibitors of hydroxyapatite nucleation and growth to be distinguished. We have also demonstrated for the first time that MGP peptides inhibit the formation of calcium oxalate monohydrate. Based on the latter finding, we propose that MGP function not only to prevent blood-vessel calcification but also to inhibit stone formation in kidney. PMID:24265810

  1. 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.

  2. Structural, thermal and optical characterization of an organic NLO material—Benzaldehyde thiosemicarbazone monohydrate single crystals

    NASA Astrophysics Data System (ADS)

    Santhakumari, R.; Ramamurthi, K.

    2011-02-01

    Single crystals of the organic NLO material, benzaldehyde thiosemicarbazone (BTSC) monohydrate, were grown by slow evaporation method. Solubility of BTSC monohydrate was determined in ethanol at different temperatures. The grown crystals were characterized by single crystal X-ray diffraction analysis to determine the cell parameters and by FT-IR technique to study the presence of the functional groups. Thermogravimetric and differential thermal analyses reveal the thermal stability of the crystal. UV-vis-NIR spectrum shows excellent transmission in the region of 200-1100 nm. Theoretical calculations were carried out to determine the linear optical constants such as extinction coefficient and refractive index. Further the optical nonlinearities of BTSC have been investigated by Z-scan technique with He-Ne laser radiation of wavelength 632.8 nm. Mechanical properties of the grown crystal were studied using Vickers microhardness tester. Second harmonic generation efficiency of the powdered BTSC monohydrate was tested using Nd:YAG laser and it is found to be ˜5.3 times that of potassium dihydrogen orthophosphate.

  3. Structural, thermal and optical characterization of an organic NLO material--benzaldehyde thiosemicarbazone monohydrate single crystals.

    PubMed

    Santhakumari, R; Ramamurthi, K

    2011-02-01

    Single crystals of the organic NLO material, benzaldehyde thiosemicarbazone (BTSC) monohydrate, were grown by slow evaporation method. Solubility of BTSC monohydrate was determined in ethanol at different temperatures. The grown crystals were characterized by single crystal X-ray diffraction analysis to determine the cell parameters and by FT-IR technique to study the presence of the functional groups. Thermogravimetric and differential thermal analyses reveal the thermal stability of the crystal. UV-vis-NIR spectrum shows excellent transmission in the region of 200-1100 nm. Theoretical calculations were carried out to determine the linear optical constants such as extinction coefficient and refractive index. Further the optical nonlinearities of BTSC have been investigated by Z-scan technique with He-Ne laser radiation of wavelength 632.8 nm. Mechanical properties of the grown crystal were studied using Vickers microhardness tester. Second harmonic generation efficiency of the powdered BTSC monohydrate was tested using Nd:YAG laser and it is found to be ∼5.3 times that of potassium dihydrogen orthophosphate. PMID:21186136

  4. A novel quantification method of pantaprazole sodium monohydrate in sesquihydrate by thermogravimetric analyzer.

    PubMed

    Reddy, V Ranga; Rajmohan, M Anantha; Shilpa, R Laxmi; Raut, Dilip M; Naveenkumar, Kolla; Suryanarayana, M V; Mathad, Vijayavitthal T

    2007-04-11

    To demonstrate the applicability of thermogravimetric analyzer as a tool for the quantification of pantaprazole sodium monohydrate in sesquihydrate, studies have been conducted. Thermal analysis (DSC, TGA) crystallographic (PXRD) and spectroscopic techniques (FT-IR) were used for the characterization of the polymorphs. Thermogravimetric analysis (TGA) analysis was explored by high-resolution dynamic (Hi-Res-dynamic) and high-resolution modulated (Hi-Res-modulated) test procedures to quantify the hydrate polymorphic mixtures. The two polymorphic forms exhibited significant differences and good resolution in the second derivative thermogram generated by Hi-Res-modulated test procedure. Thus, the TGA with Hi-Res-modulated test procedure was considered for the quantification of monohydrate in sesquihydrate. The calibration plot was constructed from the known mixtures of two polymorphs by plotting the peak area of the second derivative thermogram against the weight percent of monohydrate. Using this novel approach, 1 wt% limit of detection (LOD) was achieved. The polymorphic purity results, obtained by TGA in Hi-Res-modulated test procedure were found to be in good agreement with the results predicted by FT-IR and was comparable with the actual values of the known polymorphic mixtures. The Hi-Res-modulated TGA technique is very simple and easy to perform the analysis. PMID:17317068

  5. 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.

  6. 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

  7. 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

  8. Glucose-6-phosphate dehydrogenase

    MedlinePlus

    ... this page: //medlineplus.gov/ency/article/003671.htm Glucose-6-phosphate dehydrogenase test To use the sharing features on this page, please enable JavaScript. Glucose-6-phosphate dehydrogenase (G6PD) is a type of ...

  9. Chloroquine Phosphate Oral

    MedlinePlus

    ... allergic to chloroquine phosphate, chloroquine hydrochloride (Aralen HCl), hydroxychloroquine (Plaquenil), or any other drugs.tell your doctor ... taking chloroquine phosphate, chloroquine hydrochloride (Aralen HCl), or hydroxychloroquine (Plaquenil).tell your doctor if you are pregnant ...

  10. Chloroquine Phosphate Oral

    MedlinePlus

    ... allergic to chloroquine phosphate, chloroquine hydrochloride (Aralen HCl), hydroxychloroquine (Plaquenil), or any other drugs.tell your doctor and ... taking chloroquine phosphate, chloroquine hydrochloride (Aralen HCl), or hydroxychloroquine (Plaquenil).tell your doctor if you are pregnant ...

  11. 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.

  12. 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

  13. Mechanisms of Glucose Lowering of Dipeptidyl Peptidase-4 Inhibitor Sitagliptin When Used Alone or With Metformin in Type 2 Diabetes

    PubMed Central

    Solis-Herrera, Carolina; Triplitt, Curtis; Garduno-Garcia, Jose de Jesús; Adams, John; DeFronzo, Ralph A.; Cersosimo, Eugenio

    2013-01-01

    OBJECTIVE To assess glucose-lowering mechanisms of sitagliptin (S), metformin (M), and the two combined (M+S). RESEARCH DESIGN AND METHODS We randomized 16 patients with type 2 diabetes mellitus (T2DM) to four 6-week treatments with placebo (P), M, S, and M+S. After each period, subjects received a 6-h meal tolerance test (MTT) with [14C]glucose to calculate glucose kinetics. Fasting plasma glucose (FPG), fasting plasma insulin, C-peptide (insulin secretory rate [ISR]), fasting plasma glucagon, and bioactive glucagon-like peptide (GLP-1) and gastrointestinal insulinotropic peptide (GIP) were measured. RESULTS FPG decreased from P, 160 ± 4 to M, 150 ± 4; S, 154 ± 4; and M+S, 125 ± 3 mg/dL. Mean post-MTT plasma glucose decreased from P, 207 ± 5 to M, 191 ± 4; S, 195 ± 4; and M+S, 161 ± 3 mg/dL (P < 0.01). The increase in mean post-MTT plasma insulin and in ISR was similar in P, M, and S and slightly greater in M+S. Fasting plasma glucagon was equal (∼65–75 pg/mL) with all treatments, but there was a significant drop during the initial 120 min with S 24% and M+S 34% (both P < 0.05) vs. P 17% and M 16%. Fasting and mean post-MTT plasma bioactive GLP-1 were higher (P < 0.01) after S and M+S vs. M and P. Basal endogenous glucose production (EGP) fell from P 2.0 ± 0.1 to S 1.8 ± 0.1 mg/kg ⋅ min, M 1.8 ± 0.2 mg/kg ⋅ min (both P < 0.05 vs. P), and M+S 1.5 ± 0.1 mg/kg ⋅ min (P < 0.01 vs. P). Although the EGP slope of decline was faster in M and M+S vs. S, all had comparable greater post-MTT EGP inhibition vs. P (P < 0.05). CONCLUSIONS M+S combined produce additive effects to 1) reduce FPG and postmeal plasma glucose, 2) augment GLP-1 secretion and β-cell function, 3) decrease plasma glucagon, and 4) inhibit fasting and postmeal EGP compared with M or S monotherapy. PMID:23579178

  14. Carcinogenicity and chronic toxicity of hydrazine monohydrate in rats and mice by two-year drinking water treatment.

    PubMed

    Matsumoto, Michiharu; Kano, Hirokazu; Suzuki, Masaaki; Katagiri, Taku; Umeda, Yumi; Fukushima, Shoji

    2016-04-01

    The carcinogenicity and chronic toxicity of hydrazine monohydrate was examined by administrating hydrazine monohydrate in drinking water to groups of 50 F344/DuCrj rats and 50 Crj:BDF1 mice of both sexes for two years. The drinking water concentration of hydrazine monohydrate was 0, 20, 40 or 80 ppm (wt/wt) for male and female rats and male mice; and 0, 40, 80 or 160 ppm for female mice. Survival rates of each group of males and females rats and mice were similar to the respective controls, except female rats administered 80 ppm. Two-year administration of hydrazine monohydrate produced an increase in the incidences of hepatocellular adenomas and carcinomas in rats of both sexes along with hepatic foci. In mice, the incidences of hepatocellular adenomas and carcinomas were increased in females, and significantly increased incidences of hepatocellular adenomas in females administered 160 ppm were observed. Thus, hydrazine monohydrate is carcinogenic in two species, rats and mice. Additionally, non-neoplastic renal lesions in rats and mice and non-neoplastic nasal lesions in mice were observed. PMID:26774757

  15. Sitagliptin/metformin fixed-dose combination in type 2 diabetes mellitus: an evidence-based review of its place in therapy.

    PubMed

    Hayes, Jennifer; Anderson, Rosie; Stephens, Jeffrey W

    2016-01-01

    Type 2 diabetes mellitus is a progressive disease associated with significant morbidity and mortality. There is good evidence showing that intensive glycemic control reduces the development and progression of complications. In order to achieve glycemic targets, patients often require a combination of oral therapy and/or insulin in addition to lifestyle modification. Unfortunately, many of the traditional therapies for type 2 diabetes are associated with weight gain and hypoglycemia, resulting in poor compliance and subsequent worsening of glycemic control. The dipeptidyl peptidase-4 inhibitor sitagliptin is a therapy for type 2 diabetes and is available as a fixed-dose combination with metformin. Phase III clinical trials have demonstrated beneficial effects on glycemic control and minimal untoward effects with this combination. In this article, we provide an overview of the pharmacology, efficacy, and safety and examine the role of this combination within current practice. PMID:27486305

  16. Sitagliptin/metformin fixed-dose combination in type 2 diabetes mellitus: an evidence-based review of its place in therapy

    PubMed Central

    Hayes, Jennifer; Anderson, Rosie; Stephens, Jeffrey W

    2016-01-01

    Type 2 diabetes mellitus is a progressive disease associated with significant morbidity and mortality. There is good evidence showing that intensive glycemic control reduces the development and progression of complications. In order to achieve glycemic targets, patients often require a combination of oral therapy and/or insulin in addition to lifestyle modification. Unfortunately, many of the traditional therapies for type 2 diabetes are associated with weight gain and hypoglycemia, resulting in poor compliance and subsequent worsening of glycemic control. The dipeptidyl peptidase-4 inhibitor sitagliptin is a therapy for type 2 diabetes and is available as a fixed-dose combination with metformin. Phase III clinical trials have demonstrated beneficial effects on glycemic control and minimal untoward effects with this combination. In this article, we provide an overview of the pharmacology, efficacy, and safety and examine the role of this combination within current practice. PMID:27486305

  17. 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

  18. 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

  19. 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

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

    NASA Astrophysics Data System (ADS)

    Ahmed, A. Ben; 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 12 12 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 μ, the polarizability α and the hyperpolarizability β 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 β value revealing microscopic second-order NLO behavior.

  1. 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

  2. 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.

  3. Growth and characterization of L-histidine cadmium chloride monohydrate a semiorganic nonlinear optical crystals

    NASA Astrophysics Data System (ADS)

    Chandrasekaran, J.; Ilayabarathi, P.; Maadeswaran, P.; Mohamed Kutty, P.; Pari, S.

    2012-04-01

    L-histidine cadmium chloride monohydrate (LHCCM), a semiorganic nonlinear optical material was grown from aqueous solution by slow solvent evaporation method at room temperature. The LHCCM crystals were characterized by X-ray powder diffraction analysis. The presence of functional groups was identified through fourier transform infrared spectroscopy. Thermogravimetric and differential thermal analysis confirms that the crystal is stable up to 277 °C. The dielectric constant was studied as a function of frequency for various temperatures. The mechanical properties of the grown crystals have been studied using Vickers microhardness tester. The second harmonic generation behavior of LHCCM crystal was tested by modified Kurtz-Perry powder technique.

  4. Growth of high quality bulk size single crystals of inverted solubility lithium sulphate monohydrate

    NASA Astrophysics Data System (ADS)

    Silambarasan, A.; Rajesh, P.; Ramasamy, P.

    2015-06-01

    The paper summarizes the processes of growing large lithium sulfate monohydrate (LSMH) single crystals. We have established a procedure to grow high quality bulk size single crystals of inverted solubility LSMH by a newly developed unidirectional crystallization technique called the Sankeranarayenan - Ramasamy (SR) method. The convective flow of crystal growth processes from solution and the conditions of growing crystals of various aspects were discussed. Good quality LSMH single crystal is grown of the size 20 mmX80 mm without cracks, localized-defects and inclusions. The as-grown crystals are suitable for piezoelectric and nonlinear optical applications.

  5. Structural and vibrational properties of betainium perchlorate monohydrate crystal and character of its hydrogen bonds

    NASA Astrophysics Data System (ADS)

    Ilczyszyn, Marek; Godzisz, Dorota; Ilczyszyn, Maria M.

    2002-06-01

    Betainium perchlorate monohydrate crystal ((CH 3) 3NCH 2COOH)(ClO 4)·H 2O) undergoes a continuous (second order) phase transition at ca. 180 K. X-ray data and vibrational spectroscopy studies at different temperatures are used for description of the phase transition mechanism, as well as of hydrogen bonds formed by water in this molecular system. Perturbation of monomer water by various surroundings (water vapour, low-temperature matrices, solvents, betaine-acid crystals) and properties of triple hydrogen bonds to water oxygen atom are discussed.

  6. 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.

  7. Growth of high quality bulk size single crystals of inverted solubility lithium sulphate monohydrate

    SciTech Connect

    Silambarasan, A.; Rajesh, P. Ramasamy, P.

    2015-06-24

    The paper summarizes the processes of growing large lithium sulfate monohydrate (LSMH) single crystals. We have established a procedure to grow high quality bulk size single crystals of inverted solubility LSMH by a newly developed unidirectional crystallization technique called the Sankeranarayenan - Ramasamy (SR) method. The convective flow of crystal growth processes from solution and the conditions of growing crystals of various aspects were discussed. Good quality LSMH single crystal is grown of the size 20 mmX80 mm without cracks, localized-defects and inclusions. The as-grown crystals are suitable for piezoelectric and nonlinear optical applications.

  8. 4-Oxocyclohexanecarboxylic acid: hydrogen bonding in the monohydrate of a delta-keto acid.

    PubMed

    Barcon, Alan; Brunskill, Andrew P J; Thompson, Hugh W; Lalancette, Roger A

    2004-02-01

    The title monohydrate, C(7)H(10)O(3).H(2)O, aggregates as a complex hydrogen-bonding network, in which the water molecule accepts a hydrogen bond from the carboxyl group of one molecule and donates hydrogen bonds to ketone and carboxyl C=O functions in two additional molecules, yielding a sheet-like structure of parallel ribbons. The keto acid adopts a chiral conformation through rotation of the carboxyl group by 62.50 (15) degrees relative to the plane defined by its point of attachment and the ketone C and O atoms. Two C-H.O close contacts exist in the structure. PMID:14767139

  9. 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

  10. 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.

  11. 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.

  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. 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)

  14. 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

  15. The impact of material attributes and process parameters on the micronisation of lactose monohydrate.

    PubMed

    Shariare, M H; de Matas, M; York, P; Shao, Q

    2011-04-15

    Dry powder inhalers (DPIs), which are important medicines for drug delivery to the lungs, require drug particles in the respirable size range of 1-6 μm for optimal lung deposition. Drugs administered by the oral route also derive benefit from particles in this size range owing to their large surface area to volume ratio, which provides potential for rapid dissolution. Micronisation used in the production of particles, however often leads to heterogeneous product containing mechanically activated surfaces with amorphous content. This study was therefore carried out to evaluate the effect of particle properties of three grades of lactose monohydrate, with sizes above and below the brittle-ductile transition (dcrit) and their interaction with process variables on the quality of micronised material. Following an experimental design, the impact of three factors (grinding pressure, injector pressure and feed rate) on the particulate attributes of micronised powders produced from the different size grades was assessed. Processing conditions were shown to be important determinants of powder properties only for the coarsest starting material. Ultrafine material was achieved by processing finer grade feed stock below dcrit. However the resultant product was more crystalline and transformed on heating to the anhydrous state with markedly reduced onset temperature with lower energy surfaces than powders produced from larger sized starting material. Thus the propensity for micronisation of lactose monohydrate can be altered through control of starting materials and optimal settings for process variables. PMID:21295125

  16. High pressure ionic and molecular crystals of ammonia monohydrate within density functional theory.

    PubMed

    Griffiths, Gareth I G; Misquitta, Alston J; Fortes, A Dominic; Pickard, Chris J; Needs, Richard J

    2012-08-14

    A combination of first-principles density functional theory calculations and a search over structures is used to predict the stability of a proton-transfer modification of ammonia monohydrate with space group P4∕nmm. The phase diagram is calculated with the Perdew-Burke-Ernzerhof (PBE) density functional, and the effects of a semi-empirical dispersion correction, zero point motion, and finite temperature are investigated. Comparison with MP2 and coupled cluster calculations shows that the PBE functional over-stabilizes proton transfer phases because too much electronic charge moves with the proton. This over-binding is partially corrected by using the PBE0 hybrid exchange-correlation functional, which increases the enthalpy of P4∕nmm by about 0.6 eV per formula unit relative to phase I of ammonia monohydrate and shifts the transition to the proton transfer phase from the PBE pressure of 2.8 GPa to about 10 GPa. This is consistent with experiment as proton transfer phases have not been observed at pressures up to ∼9 GPa, while higher pressures have not yet been explored experimentally. PMID:22897292

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

    PubMed

    Bouchet, Aude; Schütz, Markus; Dopfer, Otto

    2016-01-18

    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

  18. 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...

  19. 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.

  20. 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

  1. 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

  2. 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

  3. 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

  4. Dry powder aerosols generated by standardized entrainment tubes from drug blends with lactose monohydrate: 2. Ipratropium bromide monohydrate and fluticasone propionate.

    PubMed

    Xu, Zhen; Mansour, Heidi M; Mulder, Tako; McLean, Richard; Langridge, John; Hickey, Anthony J

    2010-08-01

    The objectives of this study were: systematic investigation of dry powder aerosol performance using standardized entrainment tubes (SETs) and lactose-based formulations with two model drugs; mechanistic evaluation of performance data by powder aerosol deaggregation equation (PADE). The drugs (IPB and FP) were prepared in sieved and milled lactose carriers (2% w/w). Aerosol studies were performed using SETs (shear stresses tau(s) = 0.624-13.143 N/m(2)) by twin-stage liquid impinger, operated at 60 L/min. PADE was applied for formulation screening. Excellent correlation was observed when PADE was adopted correlating FPF to tau(s). Higher tau(s) corresponded to higher FPF values followed by a plateau representing invariance of FPF with increasing tau(s). The R(2) values for PADE linear regression were 0.9905-0.9999. Performance described in terms of the maximum FPF (FPF(max): 15.0-37.6%) resulted in a rank order of ML-B/IPB > ML-A/IPB > SV-A/IPB > SV-B/IPB > ML-B/FP > ML-A/FP > SV-B/FP > SV-A/FP. The performance of IPB was superior to FP in all formulations. The difference in lactose monohydrate carriers was less pronounced for the FPF in IPB than in FP formulations. The novel PADE offers a robust method for evaluating aerodynamic performance of dry powder formulations within a defined tau(s) range. PMID:20222025

  5. 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.

  6. 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

  7. Modelling of calcium phosphates

    NASA Astrophysics Data System (ADS)

    Calderin Hidalgo, Lazaro Juan

    This work is a contribution to a large scale joint experimental and theoretical effort to understand the biological properties of silicon doped calcium phosphates undertaken by Queen's University and Millenium Biologix Corp. We have modeled calcium phosphates and silicon doped calcium phosphates in close relation to experiment in order to study possible location of silicon in the lattice. Density functional theory has been used to study the structural and dynamical properties of small systems of calcium phosphates to gain preliminary information on phosphates and the performance of the theoretical methods. The same methods were used to investigate structural and electronic properties of larger scale calcium phosphate systems, while a classical shell model was developed to investigate the dynamical properties of such large and complex systems. In the context of the shell model a method was devised to calculate the dynamical matrix corrected for the long range Coulomb interaction in the long wave length limit. It was necessary also to develop a theoretical expression for the dielectric function in the context of the shell model. Infrared spectra and thermal parameters were calculated based on these methods. We also propose some directions for future research.

  8. A new crystalline phase of L-alpha-dipalmitoyl phosphatidylcholine monohydrate.

    PubMed Central

    Fringeli, U P

    1981-01-01

    A new phase transition of L-alpha-dipalmitoyl phosphatidylcholine (DPPC) monohydrate from the "biaxial" phase to a crystalline phase (C phase) has been found at 71 degrees C by means of infrared attenuated total reflection (IR-ATR) spectroscopy. The transition is characterized by drastic conformational changes in the glycerophosphorylcholine moiety, which led on the one hand to an alignment of the turn near the ester group in the hydrocarbon chain at glycerol C(2) position. On the other hand a uniform conformation of the glycerophosphorylcholine moiety is found to be typical for the C phase, in contrast to nonuniform head group conformations of DPPC in other regions of the DPPC/water phase diagram investigated so far. Images FIGURE 2 FIGURE 3 FIGURE 4 FIGURE 5 FIGURE 6 FIGURE 8 PMID:6894555

  9. Growth of negative solubility lithium sulfate monohydrate crystal by slow evaporation and Sankaranarayanan-Ramasamy method

    NASA Astrophysics Data System (ADS)

    Boopathi, K.; Rajesh, P.; Ramasamy, P.

    2012-04-01

    Single crystals of negatively soluble lithium sulfate monohydrate (LSMH) have been grown by conventional and Sankaranarayanan-Ramasamy (SR) methods. A negatively soluble material has been grown for the first time by the SR method. The size of the grown crystal is 40 mm length and 15 mm diameter. The solubility of the material has been found at different temperatures. The grown crystals were subjected to high resolution X-ray diffraction studies, UV-vis analysis, dielectric measurements, Vickers micro-hardness, piezoelectric measurements, laser damage threshold and second harmonic generation studies. Crystalline perfection of the grown crystals was analyzed using HRXRD. The grown crystals were found to be transparent in the entire visible region. The SR method grown crystal has higher hardness, lower dielectric loss, higher piezoelectric charge coefficient and higher laser stability compared to the conventional method grown crystal. The powder Kurtz method confirms that LSMH has SHG efficiency.

  10. Investigations on the growth and characterization of L-citrulline oxalate monohydrate single crystal

    NASA Astrophysics Data System (ADS)

    Sreevalsa, V. G.; Jayalekshmi, S.

    2011-06-01

    New single crystals of L-citrulline oxalate (LCO) monohydrate are grown from aqueous solution by slow evaporation technique. Structure and morphology of the grown crystals are identified by single crystal XRD. The compound crystallizes in the orthorhombic structure with space group P2 12 12 1, having cell parameters, a=5.208(5) Å, b=9.829(5) Å and c=23.879(5) Å. Powder X-ray diffraction data is used for the assignment of the hkl values. The chemical composition of the synthesized crystals is verified by CHN analysis. Functional groups present in the sample are identified by Fourier transform infra red (FT-IR) and FT-Raman spectral analysis. The second harmonic signal generated by the crystal using pulsed Nd: YAG Laser is confirmed by the emission of green radiation, showing that the crystal is a potential candidate for nonlinear optical studies.

  11. 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.

  12. (+)-Gibberellin C: hydrogen-bonding pattern of the monohydrate of a non-racemic pentacyclic diterpenoid.

    PubMed

    Thompson, H W; Brunskill, A P; Lalancette, R A

    2000-12-01

    In the monohydrate of the title compound, (+)-2beta, 4aalpha-dihydroxy-1,7-dimethyl-8-oxo-4bbeta,7alpha- gibbane-1alpha, 10beta-dicarboxylic acid-1,4a-lactone, C(19)H(24)O(6).H(2)O, intermolecular hydrogen bonding progresses helically along b from carboxyl to ketone [O...O = 2.694 (5) A]. The carboxyl and lactone carbonyl groups in translationally related molecules within a helix both accept hydrogen bonds from the same water of hydration. The oxygen of this water in turn accepts a hydrogen bond from the hydroxyl group of a third screw-related molecule in an adjacent counterdirectionally oriented helix, yielding a complex three-dimensional hydrogen-bonding array. Intermolecular O...H-C close contacts were found to the carboxyl and lactone carbonyls, the hydroxyl, and the water. PMID:11119009

  13. 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.

  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. 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. Crystal structures of manganese and cobalt dichloride monohydrate and deuteration effects on magnetic behavior.

    PubMed

    Pagola, S; Trowell, K T; Havas, K C; Reed, Z D; Chan, D G; Van Dongen, M J; DeFotis, G C

    2013-12-01

    This work reports the long sought crystal structures of the title members of the intriguing series of 3d transition metal dichloride monohydrates. The double chain structure which results from rearrangement of the well-known pseudo-octahedral coordination geometry and single chains in the corresponding metal chloride dihydrate is extremely unusual. MnCl2·H2O and CoCl2·H2O each crystallize in orthorhombic space group Pnma with Z = 4 and lattice parameters a = 9.0339(1), 8.8207(3); b = 3.68751(5), 3.5435(1); c = 11.5385(2), 11.2944(4) all in Å and for Mn, Co, respectively. Results are reported also for both fully deuterated systems; the structures remain the same with lattice parameter changes typically much less than 0.1%. Various magnetic properties of MnCl2·D2O and CoCl2·D2O are reported. For the latter, there are no apparent differences, qualitatively or quantitatively, from the previously measured properties of CoCl2·H2O. Interestingly, for the former some differences with respect to MnCl2·H2O are apparent, principally a lower Tmax = 3.10(10) K about which a broad antiferromagnetic maximum is centered, and a larger value χmax = 0.336(3) emu/mol. However, antiferromagnetic ordering appears to occur at essentially the same 2.18(2) K. Results of fits to susceptibilities of MnCl2·D2O and CoCl2·D2O are compared with those obtained before for MnCl2·H2O and CoCl2·H2O. Structural considerations serve to rationalize the physical properties, especially the lower dimensional magnetism of monohydrates. PMID:24251931

  17. Glucose-6-phosphate isomerase.

    PubMed

    Achari, A; Marshall, S E; Muirhead, H; Palmieri, R H; Noltmann, E A

    1981-06-26

    Glucose-6-phosphate isomerase (EC 5.3.1.9) is a dimeric enzyme of molecular mass 132000 which catalyses the interconversion of D-glucose-6-phosphate and D-fructose-6-phosphate. The crystal structure of the enzyme from pig muscle has been determined at a nominal resolution of 2.6 A. The structure is of the alpha/beta type. Each subunit consists of two domains and the active site is in both the domain interface and the subunit interface (P.J. Shaw & H. Muirhead (1976), FEBS Lett. 65, 50-55). Each subunit contains 13 methionine residues so that cyanogen bromide cleavage will produce 14 fragments, most of which have been identified and at least partly purified. Sequence information is given for about one-third of the molecule from 5 cyanogen bromide fragments. One of the sequences includes a modified lysine residue. Modification of this residue leads to a parallel loss of enzymatic activity. A tentative fit of two of the peptides to the electron density map has been made. It seems possible that glucose-6-phosphate isomerase, triose phosphate isomerase and pyruvate kinase all contain a histidine and a glutamate residue at the active site. PMID:6115414

  18. Structural and vibrational spectral investigations of melaminium maleate monohydrate by FTIR, FT-Raman and quantum chemical calculations

    NASA Astrophysics Data System (ADS)

    Arjunan, V.; Kalaivani, M.; Marchewka, M. K.; Mohan, S.

    2013-04-01

    The structural investigations of the molecular complex of melamine with maleic acid, namely melaminium maleate monohydrate have been carried out by quantum chemical methods in addition to FTIR, FT-Raman and far-infrared spectral studies. The quantum chemical studies were performed with DFT (B3LYP) method using 6-31G**, cc-pVDZ and 6-311++G** basis sets to determine the energy, structural and thermodynamic parameters of melaminium maleate monohydrate. The hydrogen atom from maleic acid was transferred to the melamine molecule giving the singly protonated melaminium cation. The ability of ions to form spontaneous three-dimensional structure through weak Osbnd H⋯O and Nsbnd H⋯O hydrogen bonds shows notable vibrational effects.

  19. 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

  20. 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.

  1. Fundamentals of phosphate transfer.

    PubMed

    Kirby, Anthony J; Nome, Faruk

    2015-07-21

    Historically, the chemistry of phosphate transfer-a class of reactions fundamental to the chemistry of Life-has been discussed almost exclusively in terms of the nucleophile and the leaving group. Reactivity always depends significantly on both factors; but recent results for reactions of phosphate triesters have shown that it can also depend strongly on the nature of the nonleaving or "spectator" groups. The extreme stabilities of fully ionised mono- and dialkyl phosphate esters can be seen as extensions of the same effect, with one or two triester OR groups replaced by O(-). Our chosen lead reaction is hydrolysis-phosphate transfer to water: because water is the medium in which biological chemistry takes place; because the half-life of a system in water is an accepted basic index of stability; and because the typical mechanisms of hydrolysis, with solvent H2O providing specific molecules to act as nucleophiles and as general acids or bases, are models for reactions involving better nucleophiles and stronger general species catalysts. Not least those available in enzyme active sites. Alkyl monoester dianions compete with alkyl diester monoanions for the slowest estimated rates of spontaneous hydrolysis. High stability at physiological pH is a vital factor in the biological roles of organic phosphates, but a significant limitation for experimental investigations. Almost all kinetic measurements of phosphate transfer reactions involving mono- and diesters have been followed by UV-visible spectroscopy using activated systems, conveniently compounds with good leaving groups. (A "good leaving group" OR* is electron-withdrawing, and can be displaced to generate an anion R*O(-) in water near pH 7.) Reactivities at normal temperatures of P-O-alkyl derivatives-better models for typical biological substrates-have typically had to be estimated: by extended extrapolation from linear free energy relationships, or from rate measurements at high temperatures. Calculation is free

  2. 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

  3. 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

  4. Synthesis, Characterization, and Intercalation of Vanadyl Phosphate Modified with Manganese

    NASA Astrophysics Data System (ADS)

    Richtrová, Klára; Votinský, Jiří; Kalousová, Jaroslava; Beneš, Ludvík.; Zima, Vítěslav

    1995-05-01

    A yellow-brown crystalline solid, stable in air and having a variable composition of [Mn(H 2O] x(VO) 1- xPO 4 · 2H 2O (0 ≤ x ≤ 0.25), has been prepared by the reaction of solid V 2O 5 with a bolling aqueous solution of H 3PO 4 and KMnO 4. The elementary cell of this compound is tetragonal (space symmetry group either P4/ n or P 4/ nmm) with the following parameters for x = 0.25: a = 0.62034 nm, c = 1.3814 nm, V = 0.51359 nm 3, Z = 4, Mr = 199.44, Dcalc = 2.492 g/cm 3, and Dexp = 2.52 g/cm 3. The magnetic behavior of this substance indicates the presence of manganese atoms at the oxidation level of III. The paramagnetic centers formed by the Mn III atoms are not markedly magnetically coupled. The structure of the compound is probably derived from the original layered lattice of vanadyl phosphate hydrate VOPO 4 · 2H 2O by replacement of at most one quarter of the vanadyl groups (V VO) 3+ by [Mn III(H 2O)] 3+ groups. Upon being heated, the substance forms a monohydrate at first, then the anhydrous salt forms, and finally the water coordinated with manganese atoms escapes. The compound can be intercalated with foreign molecules and ions in the same way as vanadyl phosphate, and the results of intercalation experiments with methanol, ethanol, 1-propanol, l-butanol, 1-butylamine, 1-octylamine, formic acid, acetic acid, and pyridine, as well as those of oxidation-reduction intercalation with a solution of sodium iodide in acetone, are presented. The experimental conditions of the intercalations are described. The layered complexes formed have been identified by powder X-ray structure analysis, thermogravimetry, differential thermal analysis, and infrared absorption spectroscopy.

  5. 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

  6. 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.

  7. 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

  8. Factors affecting crystallization, dispersion, and aggregation of calcium oxalate monohydrate in various urinary environments

    NASA Astrophysics Data System (ADS)

    Christmas, Kimberly Gail

    The mechanisms for the formation of kidney stones are not well understood. One possible mechanism is the formation of aggregates in the nephron tubules of the kidneys. However, altering the urinary environment may be a method to help prevent the recurrence of the formation of kidney stones. The primary inorganic constituent found in kidney stones of North American patients is calcium oxalate monohydrate (COM). In this research, studies on the effect of mixing rate on COM precipitation showed that rapid mixing compared to slow mixing produced smaller particle sizes and a narrower particle size distribution due to the more uniform supersaturation level. The findings are consistent with the general contention that mixing directly influences nucleation rate while mixing rate has relatively little influence over rate of growth in precipitation processes. Screening and central composite experimental designs are used to determine the effect of various factors on the aggregation and dispersion characteristics of previously grown calcium oxalate monohydrate (COM) crystals in artificial urinary environments of controlled variables. The variables examined are pH, calcium, oxalate, pyrophosphate, citrate, and protein concentrations in ultrapure water and artificial urine. Optical density measurements, zeta potential analysis, particle size analyzer, optical microscopy, AFM force measurements, protein adsorption, and ions and small molecule adsorption have been used to assess the state of aggregation and dispersion of the COM crystals and to elucidate the mechanisms involved in such a complex system. The data indicate that our model protein, mucin, acts as a dispersant. This is attributed to steric hindrance resulting from the adsorbed mucoprotein. Oxalate, however, promotes aggregation. Interesting interactions between protein and oxalate along with protein and citrate are observed. Such interactions (synergistic or antagonistic) are found to depend on the concentrations of

  9. 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

  10. A review of glycemic efficacy of liraglutide once daily in achieving glycated hemoglobin targets compared with exenatide twice daily, or sitagliptin once daily in the treatment of type 2 diabetes.

    PubMed

    Alshali, Khalid Z; Karawagh, Abdullah M

    2016-08-01

    Incretin-based therapies such as glucagon-like peptide-1 (GLP-1) receptor agonists (RA) and dipeptidyl peptidase-4 (DPP-4) inhibitors have gained prominence in recent years for the treatment of type 2 diabetes (T2D). Such therapies offer the potential to stimulate endogenous insulin activity in proportion to circulating glucose levels; thereby, lowering the risk of hypoglycemic episodes. The synthetic GLP-1 RA exenatide, the human GLP-1 RA liraglutide, and the DPP-4 inhibitor sitagliptin are the first agents in their respective classes to be approved for the treatment of T2D and their efficacy and safety has been studied extensively in clinical trials. This article reviewed the efficacy of liraglutide once daily in achieving clinical guidelines-recommended glycated hemoglobin A1c levels in patients with T2D compared with exenatide twice daily, or sitagliptin once daily, based on published literature, with an aim to elucidate the preferred choice of incretin-related therapy in treating uncontrolled T2D. PMID:27464858

  11. 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...

  12. FT-IR, FT-Raman spectra and DFT calculations of melaminium perchlorate monohydrate

    NASA Astrophysics Data System (ADS)

    Kanagathara, N.; Marchewka, M. K.; Drozd, M.; Renganathan, N. G.; Gunasekaran, S.; Anbalagan, G.

    2013-08-01

    Melaminium perchlorate monohydrate (MPM), an organic material has been synthesized by slow solvent evaporation method at room temperature. Powder X-ray diffraction analysis confirms that MPM crystal belongs to triclinic system with space group P-1. FTIR and FT Raman spectra are recorded at room temperature. Functional group assignment has been made for the melaminium cations and perchlorate anions. Vibrational spectra have also been discussed on the basis of quantum chemical density functional theory (DFT) calculations using Firefly (PC GAMESS) version 7.1 G. Vibrational frequencies are calculated and scaled values are compared with experimental values. The assignment of the bands has been made on the basis of the calculated PED. The Mulliken charges, HOMO-LUMO orbital energies are analyzed directly from Firefly program log files and graphically illustrated. HOMO-LUMO energy gap and other related molecular properties are also calculated. The theoretically constructed FT-IR and FT-Raman spectra of MPM coincide with the experimental one. The chemical structure of the compound has been established by 1H and 13C NMR spectra. No detectable signal was observed during powder test for second harmonic generation.

  13. Structural, Hirshfeld surface and spectroscopic studies of the noncentrosymmetric 1-ethylpiperazinediium pentachloroantimonate (III) monohydrate

    NASA Astrophysics Data System (ADS)

    Soudani, S.; Zeller, M.; Jelsch, C.; Lefebvre, F.; Ben Nasr, Cherif

    2016-08-01

    1-Ethylpiperazinediium pentachloroantimonate (III) monohydrate, C6H16N2SbCl5·H2O, has been synthesized by the reaction of antimony trioxide (Sb2O3) and 1-ethylpiperazine in an aqueous solution of hydrochloric acid. The structure crystallizes in orthorhombic system, in the non-centrosymmetric space group Pca21 and consists of isolated [C6H16N2]2+ cations, square pyramidal [SbCl5]2- anions and lattice water molecules. Osbnd H⋯Cl hydrogen bonds link the [SbCl5]2- anions and water molecules to form double chains stretching along the [101] direction. The chains in turn are linked to the organic cations via Nsbnd H⋯Cl, Csbnd H⋯Cl, Csbnd H⋯O and Nsbnd H⋯O hydrogen bonds to form a three-dimensional network. This structure presents an example of a general square pyramidal complex ion containing a stereo-chemically active lone pair of electrons. Solid state 13C and 15N CP-MAS NMR spectra are in agreement with the X-ray structure, and vibrational absorption bands were identified by infrared spectroscopy. DFT calculations allowed the attribution of the NMR peaks and IR absorption bands. The interactions variability of the two independent cations and ten chloride atoms is analyzed via Hirshfeld surface analysis.

  14. 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

  15. 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

  16. 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].

  17. 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.

  18. 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.

  19. 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

  20. Mebendazole mesylate monohydrate: a new route to improve the solubility of mebendazole polymorphs.

    PubMed

    de Paula, Karina; Camí, Gerardo E; Brusau, Elena V; Narda, Griselda E; Ellena, Javier

    2013-10-01

    Mebendazole mesylate monohydrate, a new stable salt of mebendazole (MBZ), has been synthesized and fully characterized. It was obtained from recrystallization of MBZ forms A, B, or C in diverse solvents with the addition of methyl sulfonic acid solution. The crystal packing is first organized as a two-dimensional array consisting of rows of alternating MBZ molecules linked to columns of mesylate ions by hydrogen bonds. The three-dimensional structure is further developed by classical intermolecular interactions involving water molecules. In addition, nonclassical contacts are also found. The vibrational behavior is consistent with the crystal structure, the most important functional groups showing shifts to lower or higher frequencies in relation to the MBZ polymorphs. Thermal analysis indicates that the compound is stable up to 50°C. Decomposition occurs in five steps. Solubility studies show that the title compound presents a significant higher performance than polymorph C. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3528-3538, 2013. PMID:23897162

  1. (-)-Dioxosantadienic acid: hydrogen-bonding patterns in a bicyclic sesquiterpenoid keto acid and its monohydrate.

    PubMed

    Brunskill, A P; Lalancette, R A; Thompson, H W

    2001-09-01

    The anhydrous form, (I), of the title compound, (-)-2-(1,2,3,4,4a,7-hexahydro-4a,8-dimethyl-1,7-dioxo-2-naphthyl)propionic acid, C(15)H(18)O(4), derived from a naturally occurring sesquiterpenoid, has two molecules in the asymmetric unit, (I) and (I'), differing in the conformations of the saturated ring and the carboxyl group. The compound aggregates as carboxyl-to-ketone hydrogen-bonding catemers [O.O = 2.776 (3) and 2.775 (3) A]. Two crystallographically independent sets of single-strand hydrogen-bonding helices with opposite end-to-end orientation pass through the cell in the b direction, one consisting exclusively of molecules of (I) and the other entirely of (I'). Three C-H.O=C close contacts are found in (I). The monohydrate, C(15)H(18)O(4).H(2)O, (II), with two molecules of (I) plus two water molecules in its asymmetric unit, forms a complex three-dimensional hydrogen-bonding network including acid-to-water, water-to-acid, water-to-ketone, water-to-water and acid-to-acid hydrogen bonds, plus three C-H.O=C close contacts. In both (I) and (II), only the ketone remote from the acid is involved in hydrogen bonding. PMID:11588376

  2. 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

  3. 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.

  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. Deuterated vs Normal Hydrogen Magnetism of M (Mn,Co) Dichloride Monohydrate, and Crystal Structure

    NASA Astrophysics Data System (ADS)

    Pagola, S.; Trowell, K. T.; Havas, K. C.; Reed, Z. D.; Chan, D. G.; Defotis, G. C.

    2011-03-01

    Presented here are susceptibility data for fully deuterated forms of the title materials, and comparison with normal hydrogen forms. Also shown is the first structure determination for any monohydrate compound, for the Mn system with the simplest magnetic behavior to analyze. Interesting similarities and contrasts appear relative to normal hydrogen analogs. For the Co system the location of an enhanced susceptibility maximum, and its magnitude, match very well those of the normal hydrogen form. The deuterated Mn material shows a similar very broad susceptibility maximum as normal material, implying low-dimensional (probably d=1) magnetism, and with indication of a transition somewhat below T(max), presumably due to weak interchain interactions. But, the location of the maximum is at significantly lower temperature than in normal material, and the size is larger; both findings suggest a weaker intrachain interaction. Yet, the apparent transition, near 2.17 K, differs hardly at all in location from that in the normal material. The crystal structure determination for the normal Mn system provides the first evidence of a structural reason for the low dimensional magnetism observed, in that somewhat isolated magnetic chains are apparent.

  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. 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.

  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. Dysregulation of phosphate metabolism and conditions associated with phosphate toxicity

    PubMed Central

    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

  10. Silver(I)-Catalyzed Three-Component Reaction of Propargylic Alcohols, Carbon Dioxide and Monohydric Alcohols: Thermodynamically Feasible Access to β-Oxopropyl Carbonates.

    PubMed

    Zhou, Zhi-Hua; Song, Qing-Wen; Xie, Jia-Ning; Ma, Ran; He, Liang-Nian

    2016-07-20

    A silver(I)-catalyzed three-component reaction of propargylic alcohols, CO2 , and monohydric alcohols was successfully developed for the synthesis of β-oxopropyl carbonates. As such, a series of β-oxopropyl carbonates were exclusively produced in excellent yields (up to 98 %), even under atmospheric pressure of CO2 . The silver catalyst works efficiently for both the carboxylative cyclization of propargylic alcohols with CO2 and subsequent transesterification of α-alkylidene cyclic carbonates with monohydric alcohols; thus this tandem process performs smoothly under mild conditions. This work provides a versatile and thermodynamically favorable approach to dissymmetric dialkyl carbonates. PMID:27237704

  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. Comparison of the crystal structures of the potent anticancer and anti-angiogenic agent regorafenib and its monohydrate.

    PubMed

    Sun, Meng Ying; Wu, Su Xiang; Zhou, Xin Bo; Gu, Jian Ming; Hu, Xiu Rong

    2016-04-01

    Regorafenib {systematic name: 4-[4-({[4-chloro-3-(trifluoromethy)phenyl]carbamoyl}amino)-3-fluorophenoxy]-1-methylpyridine-2-carboxamide}, C21H15ClF4N4O3, is a potent anticancer and anti-angiogenic agent that possesses various activities on the VEGFR, PDGFR, raf and/or flt-3 kinase signaling molecules. The compound has been crystallized as polymorphic form I and as the monohydrate, C21H15ClF4N4O3·H2O. The regorafenib molecule consists of biarylurea and pyridine-2-carboxamide units linked by an ether group. A comparison of both forms shows that they differ in the relative orientation of the biarylurea and pyridine-2-carboxamide units, due to different rotations around the ether group, as measured by the C-O-C bond angles [119.5 (3)° in regorafenib and 116.10 (15)° in the monohydrate]. Meanwhile, the conformational differences are reflected in different hydrogen-bond networks. Polymorphic form I contains two intermolecular N-H...O hydrogen bonds, which link the regorafenib molecules into an infinite molecular chain along the b axis. In the monohydrate, the presence of the solvent water molecule results in more abundant hydrogen bonds. The water molecules act as donors and acceptors, forming N-H...O and O-H...O hydrogen-bond interactions. Thus, R4(2)(28) ring motifs are formed, which are fused to form continuous spiral ring motifs along the a axis. The (trifluoromethyl)phenyl rings protrude on the outside of these motifs and interdigitate with those of adjacent ring motifs, thereby forming columns populated by halogen atoms. PMID:27045179

  13. 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.

  14. H+ ion implantation on L-arginine monohydrobromide monohydrate single crystal for tuning electro-optical properties

    NASA Astrophysics Data System (ADS)

    Sangeetha, K.; Babu, R. Ramesh; Kumar, Praveen; Bhagavannarayana, G.; Ramamurthi, K.

    2011-03-01

    A nonlinear optical single crystal, l-arginine monohydrobromide monohydrate (LAHBr), has been implanted with 100 keV H+ ions at different ion fluences ranging from 1012 to 1015 ions/cm2 to study the property changes after implantation. Crystalline perfection of the pristine and implanted LAHBr crystals was analyzed using high-resolution X-ray diffraction. The refractive index, birefringence, mechanical stability, dielectric constant and optical absorption bands induced by color centers of the implanted crystals were studied at different ion fluences and compared with pristine LAHBr single crystals.

  15. Effect of H + ion implantation on structural, morphological, optical and dielectric properties of L-arginine monohydrochloride monohydrate single crystals

    NASA Astrophysics Data System (ADS)

    Sangeetha, K.; Babu, R. Ramesh; Kumar, P.; Bhagvannarayana, G.; Ramamurthi, K.

    2011-06-01

    L-arginine monohydrochloride monohydrate (LAHCl) single crystals have been implanted with 100 keV H + ions at different ion fluence ranging from 10 12 to 10 15 ions/cm 2. Implanted LAHCl single crystals have been investigated for property changes. Crystal surface and crystalline perfection of the pristine and implanted crystals were analyzed by atomic force microscope and high-resolution X-ray diffraction studies, respectively. Optical absorption bands induced by colour centers, refractive index and birefringence, mechanical stability and dielectric constant of implanted crystals were studied at different ion fluence and compared with that of pristine LAHCl single crystal.

  16. 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.

  17. 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

  18. Comparison of creatine monohydrate and carbohydrate supplementation on repeated jump height performance.

    PubMed

    Koenig, Chad A; Benardot, Dan; Cody, Mildred; Thompson, Walter R

    2008-07-01

    Creatine monohydrate (CrMH) supplementation aids the ability to maintain performance during repeated bouts of high-intensity exercise, including jump performance. However, carbohydrate supplementation may also provide similar benefits and is less expensive. This study compared the effects of an energy-free placebo, 2 different caloric concentrations of carbohydrate drinks, and a CrMH supplement on repeated jump heights. Sixty active males (mean age, 22 +/- 3.2 years) performed 2 sets of countermovement static jump height tests (10 jumps over 60 seconds) separated by 5 days to determine the differential effects of the placebo, carbohydrate, and CrMH on jump height sustainability over 10 jumps. Subjects were randomly assigned to groups (15 subjects per group) to receive daily doses (x5 days) of carbohydrate drinks containing 100 or 250 kilocalories (kcal), a 25-g CrMH supplement, or an energy-free placebo. After 5 days, the CrMH group experienced a significant weight gain (+1.52; +/-0.89 kg, p < 0.01), while the other groups did not. The 2 levels of carbohydrate and CrMH supplements were all significantly better at sustaining jump height than the energy-free placebo over the final 3-4 jumps. The 250-kcal carbohydrate-supplemented group experienced a level of benefit (p < 0.01) that was at least equal to that of the CrMH group (p < 0.05), suggesting that the higher dose of carbohydrate was as effective as CrMH in maintaining repeated bouts of high-intensity activity as measured by repeated static jumps. Given the equivalent performance improvement and the absence of weight gain, the carbohydrate supplementation could be considered the preferred option for weight-conscious power athletes involved in activities that require repeated- motion high-intensity activities. PMID:18545204

  19. Formation of interconnected macropores in apatitic calcium phosphate bone cement with the use of an effervescent additive.

    PubMed

    Hesaraki, S; Moztarzadeh, F; Sharifi, D

    2007-10-01

    Calcium phosphate cements (CPCs) can be considered as good candidate for bone tissue engineering because they can be resorbed and take part in the bone remodeling process. Several efforts have been made into improve the resorption rate of the calcium phosphate cement by introducing macropores to the cement matrix. In this investigation a simple and effective method has been presented based on the addition of various amounts of an effervescent agent to the calcium phosphate cement components. The effervescent agent was a mixture of sodium hydrogen carbonate, NaHCO(3) (that was added to the powder phase), and citric acid monohydrate, C(6)H(8)O(7).H(2)O (that was dissolved in the liquid phase). The obtained macroporous samples were characterized by Fourier transform infrared spectrometer, X-ray diffraction, and scanning electron microscopy techniques at 4 h after setting and 3 days after soaking in a special simulated body fluid solution named Hank's balanced salt solution. Mercury intrusion porosimetry was also employed for characterizing the pore volume and pore size distribution in the cement structure. Results showed that the rate of conversion of staring reactant to the apatite phase and the apatite chemistry were significantly changed by using the additive in the cement components. Also both the pore volume and pore size were changed by varying both the amount of effervescent additive and the powder to liquid ratio. PMID:17380498

  20. 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.

  1. Solution properties and taste behavior of lactose monohydrate in aqueous ascorbic acid solutions at different temperatures: Volumetric and rheological approach.

    PubMed

    Sarkar, Abhijit; Sinha, Biswajit

    2016-11-15

    The densities and viscosities of lactose monohydrate in aqueous ascorbic acid solutions with several molal concentrations m=(0.00-0.08)molkg(-1) of ascorbic acid were determined at T=(298.15-318.15)K and pressure p=101kPa. Using experimental data apparent molar volume (ϕV), standard partial molar volume (ϕV(0)), the slope (SV(∗)), apparent specific volumes (ϕVsp), standard isobaric partial molar expansibility (ϕE(0)) and its temperature dependence [Formula: see text] the viscosity B-coefficient and solvation number (Sn) were determined. Viscosity B-coefficients were further employed to obtain the free energies of activation of viscous flow per mole of the solvents (Δμ1(0≠)) and of the solute (Δμ2(0≠)). Effects of molality, solute structure and temperature and taste behavior were analyzed in terms of solute-solute and solute-solvent interactions; results revealed that the solutions are characterized predominantly by solute-solvent interactions and lactose monohydrate behaves as a long-range structure maker. PMID:27283672

  2. 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.

  3. Structural and vibrational spectral investigations of melaminium glutarate monohydrate by FTIR, FT-Raman and DFT methods.

    PubMed

    Arjunan, V; Marchewka, M K; Raj, Arushma; Yang, Haifeng; Mohan, S

    2015-01-25

    Melaminium glutarate monohydrate has been synthesised and FTIR and FT-Raman spectral investigations are carried out. The molecular geometry and vibrational frequencies of melaminium glutarate monohydrate in the ground state have been determined by using B3LYP method with 6-31++G(**), 6-31++G and cc-pVDZ basis sets. The stability of the system, inter molecular hydrogen bonding and the electron donor-acceptor interactions of the complex have been investigated by using natural bonding orbital analysis. It reveals that the N-H⋯O and O-H⋯O intermolecular interactions significantly influence crystal packing of this molecular complex. The glutarate anion forms hydrogen bonds to the melaminium cation as the proton donor of the type N-H⋯O with a distance (N⋯O)=2.51 Å. It is also linked by other hydrogen bonds to the water molecule of the type O-H⋯O with (O⋯O)=2.82 Å and to the amino (NH2) group of melaminium cation of the type N-H⋯O with (N⋯O)=2.82 Å as the proton acceptor. The electrostatic potential of the complex is in the range +1.892e×10(-2) to -1.892e×10(-2). The limits of total electron density of the complex is +6.679e×10(-2) to -6.679e×10(-2). PMID:25123944

  4. 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.

  5. 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 (...

  6. Effects of Epothilone A in Combination with the Antidiabetic Drugs Metformin and Sitagliptin in HepG2 Human Hepatocellular Cancer Cells: Role of Transcriptional Factors NF-κB and p53.

    PubMed

    Rogalska, Aneta; Sliwinska, Agnieszka; Kasznicki, Jacek; Drzewoski, Jozef; Marczak, Agnieszka

    2016-01-01

    Type 2 diabetes mellitus patients are at increased risk of many forms of malignancies, especially of the pancreas, colon and hepatocellular cancer. Unfortunately, little is known of the possible interaction between antidiabetic drugs and anticancer agents. The present study investigates the influence of metformin (MET) and sitagliptin (SITA) on the in vitro anticancer activity of the microtubule depolymerization inhibitor agent epothilone A (EpoA). Hepatocellular liver carcinoma cell line (HepG2) viability and apoptosis were determined by the MTT test and by double staining with PO-PRO-1 and 7-aminoactinomycin D, respectively, after treatment with EpoA, metformin or sitagliptin. The levels of nuclear factor NF-κB and p53 were evaluated in the presence and absence of inhibitors. While EpoA and MET inhibited HepG2 cell proliferation, SITA did not. EpoA and SITA induced higher p53 levels than MET. All tested drugs increased the level of NF-κB. Only MET enhanced the proapoptotic effect of EpoA. The EpoA+MET combination evoked the highest cytotoxic effect on HepG2 cells and led to apoptosis independent of p53, decreasing the level of NF-κB. These findings support the link between NF-κB and p53 in the modulation of apoptotic effects in HepG2 cells treated by EpoA. Our studies indicate that the combination of EpoA and MET applied in subtoxic doses has a stronger cytotoxic effect on liver cancer cells than each of the compounds alone. The therapeutic advantages of the combination of EpoA with MET may be valuable in the treatment of patients with diabetes mellitus type 2 (T2DM) and liver cancer. PMID:27039825

  7. 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

  8. Sphingosine 1-phosphate signalling.

    PubMed

    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

  9. Templated, layered manganese phosphate

    DOEpatents

    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.

  10. 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.

  11. 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

  12. 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

  13. 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

  14. 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...

  15. 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...

  16. 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

  17. 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

  18. 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 ...

  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. 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.

  1. Synthesis, growth, and characterization of bis (potassium) 2,4-dinitrophenolate monohydrate (BPDNP): a new third harmonic generation material

    NASA Astrophysics Data System (ADS)

    Sathishkumar, K.; Chandrasekaran, J.; Babu, B.; Sathish, Clastin I.; Matsushita, Yoshitaka

    2015-06-01

    Novel semi-organic single crystals of bis (potassium) 2,4-dinitrophenolate monohydrate were grown by slow evaporation technique at room temperature. Single-crystal XRD confirms that the crystal belongs to monoclinic system with space group C2/c. 1H NMR and 13C NMR studies were conducted for the crystal. In order to know the purity, LC-MS studies were also conducted for the crystal. Functional groups present in the synthesized compound were confirmed by FT-IR analysis. UV-Vis studies show that the crystal has a lower cutoff wave length at 461 nm. Dielectric studies were carried out to study the charge transport mechanism in the crystal. Photoconductivity study exhibits the positive photoconductivity nature of the grown crystal. Nonlinear absorption coefficient ( β), nonlinear refraction ( n 2), and third-order susceptibility ( χ (3)) were also evaluated for the grown crystal.

  2. 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.

  3. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... ferric chloride or ferric citrate. (b) The ingredient meets the specifications of the Food Chemicals... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Ferric phosphate. 184.1301 Section 184.1301 Food... GRAS § 184.1301 Ferric phosphate. (a) Ferric phosphate (ferric orthophosphate, iron (III) phosphate,...

  4. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... reaction of sodium phosphate with ferric chloride or ferric citrate. (b) The ingredient meets the... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Ferric phosphate. 184.1301 Section 184.1301 Food... Specific Substances Affirmed as GRAS § 184.1301 Ferric phosphate. (a) Ferric phosphate...

  5. 21 CFR 184.1301 - Ferric phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... reaction of sodium phosphate with ferric chloride or ferric citrate. (b) The ingredient meets the... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Ferric phosphate. 184.1301 Section 184.1301 Food... Specific Substances Affirmed as GRAS § 184.1301 Ferric phosphate. (a) Ferric phosphate...

  6. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Erythromycin phosphate. 520.823 Section 520.823... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.823 Erythromycin phosphate. (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance...

  7. 21 CFR 520.823 - Erythromycin phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Erythromycin phosphate. 520.823 Section 520.823... DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.823 Erythromycin phosphate. (a) Specifications. Erythromycin phosphate is the phosphate salt of the antibiotic substance...

  8. 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.

  9. Structures of protonated thymine and uracil and their monohydrated gas-phase ions from ultraviolet action spectroscopy and theory.

    PubMed

    Pedersen, Sara Øvad; Byskov, Camilla Skinnerup; Turecek, Frantisek; Brøndsted Nielsen, Steen

    2014-06-19

    The strong UV chromophores thymine (Thy) and uracil (Ura) have identical heteroaromatic rings that only differ by one methyl substituent. While their photophysics has been elucidated in detail, the effect on the excited states of base protonation and single water molecules is less explored. Here we report gas-phase absorption spectra of ThyH(+) and UraH(+) and monohydrated ions and demonstrate that the substituent is not only responsible for spectral shifts but also influences the tautomer distribution, being different for bare and monohydrated ions. Spectra interpretation is aided by calculations of geometrical structures and transition energies. The lowest free-energy tautomer (denoted 178, enol-enol form) accounts for 230-280 nm (ThyH(+)) and 225-270 nm (UraH(+)) bands. ThyH(+) hardly absorbs above 300 nm, whereas a discernible band is measured for UraH(+) (275-320 nm), ascribed to the second lowest free-energy tautomer (138, enol-keto form) comprising a few percent of the UraH(+) population at room temperature. Band widths are similar to those measured of cold ions in support of very short excited-state lifetimes. Attachment of a single water increases the abundance of 138 relative to 178, 138 now clearly present for ThyH(+). 138 resembles more the tautomer present in aqueous solution than 178 does, and 138 may indeed be a relevant transition structure. The band of ThyH(+)(178) is unchanged, that of UraH(+)(178) is nearly unchanged, and that of UraH(+)(138) blue-shifts by about 10 nm. In stark contrast to protonated adenine, more than one solvating water molecule is required to re-establish the absorption of ThyH(+) and UraH(+) in aqueous solution. PMID:24874819

  10. 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.

  11. 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

  12. 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

  13. 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

  14. 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

  15. 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

  16. A study of the piezoelectric resonance in metal organic NLO single crystals: Sodium D-isoascorbate monohydrate and Lithium L-ascorbate dihydrate

    NASA Astrophysics Data System (ADS)

    Saripalli, Ravi Kiran; Raghavendra Rao, K.; Sanath Kumar, R.; Bhat, H. L.; Elizabeth, Suja

    2016-05-01

    Large single crystals of Sodium D-isoacsorbate monohydrate and Lithium L-ascorbate dehydrate were grown using solution growth technique. Dielectric constant and dielectric loss were monitored as a function of frequency at different temperatures. These are typically characterized by strong resonance peaks. The piezoelectric coefficients d31, elastic coefficient (S11) and electromechanical coupling coefficient (k31) were estimated by resonance-antiresonance method. The temperature dependence of the resonance-peaks frequencies was studied.

  17. 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

  18. 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

  19. 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.

  20. [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

  1. 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

  2. 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

  3. Genetics Home Reference: glucose phosphate isomerase deficiency

    MedlinePlus

    ... Me Understand Genetics Home Health Conditions GPI deficiency glucose phosphate isomerase deficiency Enable Javascript to view the ... boxes. Download PDF Open All Close All Description Glucose phosphate isomerase (GPI) deficiency is an inherited disorder ...

  4. Phosphate bonding to goethite and pyrolusite surfaces

    USGS Publications Warehouse

    Weiner, Eugene R.; Goldberg, M.C.; Boymel, P.M.

    1984-01-01

    Fourier transform infrared (FTIR) spectra were obtained from pure and phosphated goethite (??-FeOOH), and pyrolusite (MnO2). The nature of the phosphate-surface bond was determined to be binuclear for goethite and bidentate for pyrolusite.

  5. 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

  6. Crystal structure of zwitterionic 3-(2-hy-droxy-2-phospho-nato-2-phosphono-eth-yl)imidazo[1,2-a]pyridin-1-ium monohydrate (minodronic acid monohydrate): a redetermination.

    PubMed

    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 mol-ecule crystallizes in a zwitterionic form with cationic imidazolium[1,2a]pyridine and anionic phospho-nate groups. The dihedral angle formed by the planes of the pyridine and imidazole rings is 3.55 (9)°. A short intra-molecular C-H⋯O contact is present. In the crystal, mol-ecules are linked by O-H⋯O, N-H⋯O and C-H⋯O hydrogen bonds and π-π inter-actions [centroid-to-centroid distance = 3.5822 (11) Å], forming a three-dimensional structure. PMID:25705449

  7. 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...

  8. 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...

  9. 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)....

  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 182.6285 - 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...

  12. 21 CFR 582.1217 - 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. 582.1217 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)....

  13. 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)....

  14. 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...

  15. 21 CFR 582.1217 - 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. 582.1217 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)....

  16. 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...

  17. 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...

  18. 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)....

  19. 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)...

  20. 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...

  1. 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...

  2. 21 CFR 582.1141 - Ammonium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 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)...

  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 582.1141 - Ammonium phosphate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 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)...

  5. 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)....

  6. Urea phosphate as granular or fluid fertilizers

    SciTech Connect

    Blouin, G.M.

    1984-01-01

    Studies are being conducted of the production and agronomic characteristics of the phosphoric acid-urea adduct, urea phosphate, and of the various granular and fluid fertilizers that can be produced from it. Flowsheets are given for the production of urea phosphate. Characteristics of unpurified and purified urea phosphate are also given. (DLC)

  7. 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...

  8. 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...

  9. 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)....

  10. 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)....

  11. 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....

  12. 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...

  13. 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)....

  14. 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...

  15. 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)....

  16. 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....

  17. 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)....

  18. 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...

  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, 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-,...

  1. 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)....

  2. 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...

  3. 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....

  4. 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...

  5. 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)....

  6. 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....

  7. 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...

  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, 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)....

  12. 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...

  13. 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...

  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 582.5778 - 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)....

  16. 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)....

  17. 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)....

  18. 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)...

  19. 21 CFR 182.1217 - 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. 182.1217 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)....

  20. 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...

  1. 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)....

  2. 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...

  3. 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)....

  4. 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)....

  5. 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...

  6. 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)....

  7. 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...

  8. 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...

  9. 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)....

  10. 21 CFR 582.1141 - Ammonium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 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)...

  11. 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...

  12. 21 CFR 582.1141 - Ammonium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 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)...

  13. 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...

  14. 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...

  15. 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...

  16. 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)....

  17. 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... GENERALLY RECOGNIZED AS SAFE Multiple Purpose GRAS Food Substances § 182.1217 Calcium phosphate. (a) Product. Calcium phosphate (mono-, di-, and tribasic). (b) Conditions of use. This substance is...

  18. 21 CFR 182.1217 - 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. 182.1217 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)....

  19. 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...

  20. 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...

  1. 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.

  2. Quantification of residual crystallinity in ball milled commercially sourced lactose monohydrate by thermo-analytical techniques and terahertz spectroscopy.

    PubMed

    Smith, Geoff; Hussain, Amjad; Bukhari, Nadeem Irfan; Ermolina, Irina

    2015-05-01

    The quantification of crystallinity is necessary in order to be able to control the milling process. The use of thermal analysis for this assessment presents certain challenges, particularly in the case of crystal hydrates. In this study, the residual crystallinity on ball milling of lactose monohydrate (LMH), for periods up to 90min, was evaluated by thermo-analytical techniques (TGA, DSC) and terahertz spectroscopy (THz). In general, the results from one of the DSC analysis and the THz measurements agree showing a monotonous decrease in relative residual crystallinity with milling time (∼80% reduction after 60min milling) and a slight increase at the 90min time point. However, the estimates from TGA and two other methods of analyzing DSC curve do not agree with the former techniques and show variability with significantly higher estimates for crystallinity. It was concluded that, the thermal techniques require more complex treatment of the data in the evaluation of changes in crystallinity of a milled material (in particular to account for the de-vitrification and mutarotation of the material that inevitably occurs during the measurement cycle) while the analysis of THz data is more straightforward, with the measurement having no impact on the native state of the material. PMID:25784570

  3. N′-[(E)-2-Hy­droxy-5-iodo­benzyl­idene]furan-2-carbohydrazide monohydrate

    PubMed Central

    Bikas, Rahman; Anarjan, Parisa Mahboubi; Ng, Seik Weng; Tiekink, Edward R. T.

    2012-01-01

    The organic mol­ecule of the title monohydrate, C12H9IN2O3·H2O, features a disordered furyl ring with the major component [site occupancy = 0.575 (18)] having the carbonyl O and furyl O atoms syn, and the other conformation having these atoms anti. The mol­ecule is slightly twisted with the dihedral angle between the benzene and furyl rings being 10.3 (6)° (major component). An intra­molecular O—H⋯N(imine) hydrogen bond is formed. In the crystal, the water mol­ecule accepts a hydrogen bond from an amine H atom, and forms two O—H⋯O(carbon­yl) hydrogen bonds, thereby linking three different carbohydrazide mol­ecules. The result is a supra­molecular layer parallel to (001). The closest contacts between layers are of the type I⋯I, at a distance of 3.6986 (6) Å. PMID:22347029

  4. 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.

  5. Characterizing radiation-induced oxidation of DNA by way of the monohydrated guanine-cytosine radical cation.

    PubMed

    Jaeger, Heather M; Schaefer, Henry F

    2009-06-11

    The interaction of one water molecule with the guanine-cytosine radical cation has been studied with ab initio and density functional methods in order to help elucidate the nature of oxidized aqueous DNA. The theoretical spin density of [GC]*(+) reveals that the radical center is localized on guanine. The adiabatic ionization potential lowers from 7.63 to 6.71 eV in concurrence with the formation of the Watson-Crick base pair and hydration by one water molecule. A natural bond orbital analysis of partial charges shows that approximately 80% of the positive charge persists on guanine upon hydration and formation of the Watson-Crick base pair with cytosine. Hydration energies were computed with second-order Z-averaged perturbation theory (ZAPT2) using the aug-cc-pVDZ basis set at 11 stationary points on the B3LYP/DZP++ potential energy surface. The hydration energy at the global minimum is 14.2 kcal mol(-1). The lowest energy structures correspond to hydration near the glycosidic bond sites. Structural changes in the Watson-Crick base pair are predominantly seen for monohydration in the groove regions of double-helix DNA. PMID:19445496

  6. 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

  7. 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) Å, β = 101.223(5)°, Z = 2 and V = 837.2(6) Å3. 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).

  8. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway.

    PubMed

    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

  9. Herbal extracts of Tribulus terrestris and Bergenia ligulata inhibit growth of calcium oxalate monohydrate crystals in vitro

    NASA Astrophysics Data System (ADS)

    Joshi, V. S.; Parekh, B. B.; Joshi, M. J.; Vaidya, A. B.

    2005-02-01

    A large number of people in this world are suffering from urinary stone problem. Calcium oxalate monohydrate (COM) and calcium oxalate dihydrate (COD) containing stones (calculi) are commonly found. In the present study, COM crystals were grown by a double diffusion gel growth technique using U-tubes. The gel was prepared from hydrated sodium metasilicate solution. The gel framework acts like a three-dimensional crucible in which the crystal nuclei are delicately held in the position of their formation, and nutrients are supplied for the growth. This technique can be utilized as a simplified screening static model to study the growth, inhibition and dissolution of urinary stones in vitro. The action of putative litholytic medicinal plants, Tribulus terrestris Linn. ( T.t) and Bergenia ligulata Linn. ( B.l.), has been studied in the growth of COM crystals. Tribulus terrestris and Bergenia ligulata are commonly used as herbal medicines for urinary calculi in India. To verify the inhibitive effect, aqueous extracts of Tribulus terrestris and Bergenia ligulata were added along with the supernatant solutions. The growth was measured and compared, with and without the aqueous extracts. Inhibition of COM crystal growth was observed in the herbal extracts. Maximum inhibition was observed in Bergenia ligulata followed by Tribulus terrestris. The results are discussed.

  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. A dual approach to study the electro-optical properties of a noncentrosymmetric L-asparagine monohydrate.

    PubMed

    Shkir, Mohd; Muhammad, Shabbir; AlFaify, S; Irfan, Ahmad; Yahia, I S

    2015-02-25

    In this work we reports the experimental and theoretical investigation on an organic noncentrosymmetric monohydrated L-asparagine (LAM) molecule. LAM single crystals were grown in specially designed beaker for the first time. Structural confirmation was done by identifying the vibrational modes using IR and FT-Raman spectroscopic studies. The ultra violet-visible-near infrared absorbance, diffuse reflectance spectra were recorded in the spectral range 190-2500 nm. The optical transparency was calculated and found to be ∼80%. Its optical band gap was calculated found to be ∼5.100 eV. Density functional theory (DFT) was employed to optimize the molecular geometry of LAM using B3LYP/6-31G(∗) basis set of theory. The HOMO-LUMO energy gap of 6.047 eV and transition energy of 176 nm (f0=0.024) have been found in semi-quantitative agreement with our experimental results. The dipole moment, polarizability and first hyperpolarizability were calculated at the same level of theory. The obtained results reveals that the titled compound can be a decent contender for nonlinear applications. PMID:25238181

  12. Synthesis, structure, spectral, thermal and first-order molecular hyperpolarizability of 4-benzoylpyridine isonicotinyl hydrazone monohydrate single crystals.

    PubMed

    Meenatchi, V; Muthu, K; Rajasekar, M; Meenakshisundaram, S P

    2014-04-24

    Single crystals of 4-benzoylpyridine isonicotinyl hydrazone monohydrate were grown by slow evaporation solution growth technique from ethanol at room temperature. It belongs to triclinic system with space group P1¯ and the cell parameters are, a=8.9250(2) Å, b=9.1540(2) Å, c=10.87500(10) Å and V=797.88(3) Å(3). Powder XRD closely resembles with that of simulated pattern from single crystal XRD. The characteristic functional groups present in the molecule are confirmed by FT-IR and FT-Raman analyses. The crystal is transparent in the visible region having a lower optical cut-off at ∼420 nm and the band gap energies are estimated by the application of Kubelka-Munk algorithm. Thermal analysis by TG/DTA indicates the stability of the material. The scanning electron microscopy studies reveal the surface morphology of the as-grown crystal. Mass spectrometry provides information pertaining to the structure and molecular weight of the compound. Theoretical calculations were performed using Hartree-Fock method with 6-31G(d,p) as the basis set for to derive the optimized geometry, dipole moment and first-order molecular hyperpolarizality (β) values. PMID:24508881

  13. Growth, spectral, optical, thermal, and mechanical behaviour of an organic single crystal: Quinolinium 2-carboxy 6-nitrophthalate monohydrate

    NASA Astrophysics Data System (ADS)

    Mohana, J.; Ahila, G.; Bharathi, M. Divya; Anbalagan, G.

    2016-09-01

    Organic single crystals of quinolinium 2-carboxy 6-nitrophthalate monohydrate (QN) were grown by slow evaporation solution growth technique using ethanol and water as a mixed solvent. X-ray powder diffraction analysis revealed that the crystal belongs to the monoclinic crystal system with space group of P21/c. The functional groups present in the crystallized material confirmed its molecular structure. The optical transparency range and the lower cutoff wavelength were identified from the UV-vis spectrum. The optical constants were determined by UV-visible transmission spectrum at normal incidence, measured over the 200-700 nm spectral range. The dispersion of the refractive index was discussed in terms of the single-oscillator Wemple and DiDomenico model. The calculated HOMO and LUMO energies show that the charge transfer occur within the molecule. Electronic excitation properties were discussed within the framework of two level model on the basis of an orbital analysis. The nonlinear optical absorption coefficient (β) and nonlinear refraction (n2) of QN was measured by Z-scan technique and reported here. Thermal stability of QN was determined using TGA/DSC curves. Vicker's microhardness studies were carried out on the (1 1 ̅0) plane to understand the mechanical properties of the grown crystal. The microhardness measurements showed a Vickers hardness value as 18.4 kg/mm2 which is comparable to well-known organic crystal, urea.

  14. 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.

  15. Synthesis, growth, crystal structure and characterization of a new organic NLO crystal: L-Lysine 4-nitrophenolate monohydrate (LLPNP)

    NASA Astrophysics Data System (ADS)

    Mahadevan, M.; Magesh, M.; Ramachandran, K.; Anandan, P.; Arivanandhan, M.; Hayakawa, Y.

    2014-09-01

    L-Lysine 4-nitrophenolate monohydrate (LLPNP) has been synthesized and grown by solution growth method at room temperature using deionised water as a solvent. The crystal structure of the materials was solved by single crystal X-ray diffraction analysis and it was found that the material has orthorhombic system. The crystallinity of the grown crystals was studied by the powder X-ray diffraction analysis. Molecular structure of the grown crystal was investigated by 1H NMR spectroscopy. The various functional groups of the sample were identified by Fourier transform infrared and Fourier transform-Raman spectroscopic analyses. Thermal stability of the grown crystal has been studied by Thermogravimetric and Differential thermal (TG&DTA) analysis. The optical absorption of the grown crystals has been ascertained by UV-Vis-NIR absorption studies. Second harmonic generation (SHG) efficiency of the material has been determined by Kurtz and Perry technique and the efficiency was found to be 4.45 and 1.4 times greater than that of standard KDP and urea samples, respectively.

  16. Crystal structure, thermal analysis and IR spectrometric investigation of the tris(2,6-diaminopyridinium) hydrogen sulfate sulfate monohydrate

    NASA Astrophysics Data System (ADS)

    Saïd, Salem; Elleuch, Slim; Ślepokura, Katarzyna; Lis, Tadeusz; Naïli, Houcine

    2016-06-01

    The crystals of new inorganic-organic hybrid material tris(2,6-diaminopyridinium) hydrogen sulfate sulfate monohydrate (C5H8N3)3(HSO4)(SO4)·H2O, were grown by slow evaporation technique in aqueous solution. The title compound has been prepared and characterized by X-ray diffraction, IR spectroscopy and thermal analysis. The complex crystallizes in the triclinic system, space group P 1 bar , with the following cell parameters a = 8.051(3)Å, b = 10.646(4)Å, c = 14.138(6)Å, α = 73.23(3)°, β = 79.28(3)°, γ = 82.28(3)°, V = 1135.8(8)Å3 and Z = 2, T = 100 K. The crystal is built up from hydrogen sulfate anions HSO4-, sulfate anions SO42-, protonated cations (C5H8N3)+ and water molecules. In this compound, hydrogen bonding and π⋯π interactions play crucial roles in forming interesting structural patterns. Thermal analysis indicates that (C5H8N3)3(HSO4)(SO4)·H2O does not experience any structural phase transition in the temperature range measured from 25 to 700 °C. Therefore, the properties of the new phase are inconsistent with the characteristic features of the superprotonic family M3H(SO4)2.

  17. 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

  18. 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.

  19. Studies on semi-organic non linear optical single crystal: Lithium formate monohydrate (HCO2LiṡH2O)

    NASA Astrophysics Data System (ADS)

    Joseph Daniel, D.; Ramasamy, P.

    2014-03-01

    A semi-organic nonlinear optical single crystal, of lithium formate monohydrate (LFMH), has been grown by slow evaporation solution growth technique. The single crystal XRD analysis confirms that the crystal belongs to the orthorhombic system with non-centrosymmetric space group Pbn21. Powder X-ray diffraction analysis was carried out for the grown crystal in the 2θ range 20-80°. The crystalline perfection was analyzed by high-resolution X-ray diffraction (HRXRD) and found that the quality of the grown single crystal is quite good. The UV-Vis spectrum shows that it has a good transmittance in the entire visible region with the lower cut-off wavelength at 240 nm. The presence of the functional groups was confirmed by using FT-IR spectral analysis. The thermal characteristics of LFMH were analyzed by thermogravimetric (TGA) and differential thermal analysis (DTA) and differential scanning calorimetry (DSC). Dielectric studies have been carried out for the grown crystal at different frequencies from 100 Hz to 5 MHz. Both dielectric constant and dielectric loss values are found to decrease with increasing frequency. The mechanical behavior of the grown crystal was studied using Vickers microhardness tester. Nonlinear optical characteristics of LFMH have been studied using Q-switched Nd:YAG laser (λ = 1064 nm). The second harmonic generation conversion efficiency of LFMH is 0.9 times that of standard KDP crystal. The laser damage threshold value of LFMH is found to be 1.5 GW/cm2.

  20. Synthesis, structure, crystal growth and characterization of a novel semiorganic nonlinear optical L-proline lithium bromide monohydrate single crystal

    NASA Astrophysics Data System (ADS)

    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 250-1100 nm. 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.

  1. Nonradiative Decay Dynamics of METHYL-4-HYDROXYCINNAMATE and its Monohydrated Complex Revealed by Picosecond Pump-Probe Spectroscopy

    NASA Astrophysics Data System (ADS)

    Ebata, T.; Shimada, D.; Kusaka, R.; Inokuchi, Y.; Ehara, M.

    2012-06-01

    The lifetimes of methyl 4-hydroxycinnamate (OMpCA) and its mono-hydrated complex (OMpCA-H_2O) in the S_1 state have been measured by picosecond pump-probe spectroscopy in a supersonic beam. For OMpCA, the lifetime of the S_1 - S_0 origin is 8 - 9 ps. On the other hand, the lifetime of OMpCA-H_2O complex at the origin is 930 ps, which is 100 times longer than that. Furthermore, in the complex the S_1 lifetime shows rapid decrease at an energy of 200 cm-1 above the origin and becomes as short as 9 ps at 500 cm-1. Theoretical calculations with symmetry-adapted cluster-configuration interaction (SAC-CI) method suggest that in OMpCA, the trans - cis isomerization occurs smoothly without a barrier on the S_1surface, while in OMpCA-H_2O complex, there exists a barrier along the isomerization coordinate. The calculated barrier height of OMpCA-H_2O is in good agreement with that estimated from the lifetime measurements.

  2. Phosphatidylinositol 4-phosphate and phosphatidylinositol 3-phosphate regulate phagolysosome biogenesis

    PubMed Central

    Jeschke, Andreas; Zehethofer, Nicole; Lindner, Buko; Krupp, Jessica; Schwudke, Dominik; Haneburger, Ina; Jovic, Marko; Backer, Jonathan M.; Balla, Tamas; Hilbi, Hubert; Haas, Albert

    2015-01-01

    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

  3. [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

  4. Phosphate uptake kinetics by Acinetobacter isolates.

    PubMed

    Pauli, A S; Kaitala, S

    1997-02-01

    Acinetobacter isolates from activated sludge treatment plants of forest industry were used as model organisms for polyphosphate accumulating bacteria to study excess phosphate uptake by the overplus phenomenon as well as luxury uptake of phosphate during growth. The initial, rapid phosphate uptake by the phosphorus-starved Acinetobacter isolates (the overplus phenomenon) followed the Michaelis-Menten model (maximum initial phosphate uptake rate 29 mg P g(-1) dry mass (DM) h(-1), half-saturation constant for excess phosphate uptake 17 mg P L(-1)). During the rapid uptake no growth was observed, but most cells contained polyphosphate granules. Also growth and luxury uptake of phosphate could be modeled with the Michaelis-Menten equation (maximum phosphate uptake rate 3.7-12 mg P g(-1) DM h(-1), half-saturation constant for growth 0.47-6.0 mg P L(-1), maximum specific growth rate 0.15-0.55 h(-1)). PMID:18633985

  5. 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

  6. About Calcium Phosphate Cements (CPC)

    NASA Astrophysics Data System (ADS)

    Piñera, Silvia; Piña, Cristina

    2006-09-01

    Calcium phosphate cements (CPC) are used in orthopaedic surgery as bone substitution and fixation of metallic implants, showing advantages with respect to other materials like polymeric cements or ceramic blocks also used for bone repair. For example, they are easy to shape and fill bone defects, react at low temperature and their setting product is hydroxyapatite, mineral from it's composed the inorganic part of the bone, resulting a bioabsorbable material that can be replaced by new bone. Nevertheless there are still some complications like their low absorption rate, inyectability, setting times and their low strength that limits their use to only non load bearing applications. In this work we present a brief resume of some investigations that has been proposed to solve some of these problems, like the addition of phosphates solutions or seeds to increase the reaction rate, or fibers and hard particles to produce a composite material.

  7. 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

  8. Bioavailable dietary phosphate, a mediator of cardiovascular disease, may be decreased with plant-based diets, phosphate binders, niacin, and avoidance of phosphate additives.

    PubMed

    McCarty, Mark F; DiNicolantonio, James J

    2014-01-01

    Increased fasting serum phosphate within the normal physiological range has been linked to increased cardiovascular risk in prospective epidemiology; increased production of fibroblast growth factor 23, and direct vascular effects of phosphate, may mediate this risk. Although dietary phosphate intake does not clearly influence fasting serum phosphate in individuals with normal renal function, increased phosphate intake can provoke a rise in fibroblast growth factor 23, and in diurnal phosphate levels, and hence may adversely influence vascular health. Dietary phosphate absorption can be moderated by emphasizing plant-based dietary choices (which provide phosphate in less bioavailable forms); avoidance of processed foods containing inorganic phosphate food additives; and by ingestion of phosphate-binder drugs, magnesium supplements, or niacin, which precipitate phosphate or suppress its gastrointestinal absorption. The propensity of dietary phosphate to promote vascular calcification may be opposed by optimal intakes of magnesium, vitamin K, and vitamin D; the latter should also counter the tendency of phosphate to elevate parathyroid hormone. PMID:24984987

  9. The comparison of approaches to the solid-state NMR-based structural refinement of vitamin B1 hydrochloride and of its monohydrate

    NASA Astrophysics Data System (ADS)

    Czernek, Jiří; Pawlak, Tomasz; Potrzebowski, Marek J.; Brus, Jiří

    2013-01-01

    The 13C and 15N CPMAS SSNMR measurements were accompanied by the proper theoretical description of the solid-phase environment, as provided by the density functional theory in the pseudopotential plane-wave scheme, and employed in refining the atomic coordinates of the crystal structures of thiamine chloride hydrochloride and of its monohydrate. Thus, using the DFT functionals PBE, PW91 and RPBE, the SSNMR-consistent solid-phase structures of these compounds are derived from the geometrical optimization, which is followed by an assessment of the fits of the GIPAW-predicted values of the chemical shielding parameters to their experimental counterparts.

  10. N-(2,6-Dimethyl­anilino)-5,6-dihydro-4H-1,3-thia­zin-3-ium chloride monohydrate

    PubMed Central

    Veidis, Mikelis V.; Orola, Liana; Arajs, Reinis

    2008-01-01

    In the title compound, alternatively called xylazine hydro­chloride monohydrate, C12H17N2S+·Cl−·H2O, the six-membered thia­zine ring is in a half-chair conformation. In the crystal structure, six component centrosymmetric clusters are formed via inter­molecular O—H⋯Cl, N—H⋯O and N—H⋯Cl hydrogen bonds involving xylazine cations, chloride anions and water mol­ecules. PMID:21202581

  11. A vacuolar phosphate transporter essential for phosphate homeostasis in Arabidopsis

    PubMed Central

    Liu, Jinlong; Yang, Lei; Luan, Mingda; Wang, Yuan; Zhang, Chi; Zhang, Bin; Shi, Jisen; Zhao, Fu-Geng; Lan, Wenzhi; Luan, Sheng

    2015-01-01

    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, SO42−, 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

  12. 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

  13. A randomized controlled trial of liraglutide versus insulin detemir plus sitagliptin: Effective switch from intensive insulin therapy to the once-daily injection in patients with well-controlled type 2 diabetes.

    PubMed

    Inoue, Yuichiro; Nakamura, Akinobu; Kondo, Yoshinobu; Hamano, Kumiko; Satoh, Shinobu; Terauchi, Yasuo

    2015-07-01

    This study aimed to compare the efficacy and safety of liraglutide versus insulin detemir plus sitagliptin in Japanese patients with type 2 diabetes treated with a basal-bolus insulin regimen. In this multicenter, open-label trial, 90 patients whose diabetes had been controlled well or moderately (glycated hemoglobin [HbA1c ] ≤ 7.3%) with basal-bolus insulin regimen were randomly assigned to a liraglutide group or a detemir group and were followed up for 24 weeks. The primary end point was HbA1c change from baseline to 24 weeks. Of the 90 enrolled patients, 82 completed this trial. At 24 weeks, the mean changes in HbA1c from baseline were 0.1% ± 0.9% versus 0.3% ± 0.8% in the liraglutide versus detemir groups, respectively (P = .46). The "overall" satisfaction score for the Diabetes Treatment Satisfaction Questionnaire changed from 25.2 ± 7.4 to 29.9 ± 5.3 (P < .001) and from 26.4 ± 6.1 to 28.3 ± 6.4 (P = .12) in the liraglutide and detemir groups, respectively. Although the mean change difference in HbA1c between both groups was not significant, switching from a basal-bolus insulin regimen to liraglutide once daily improved patient satisfaction levels without loss of glycemic control. PMID:25677642

  14. 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

  15. 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

  16. Dry powder aerosols generated by standardized entrainment tubes from drug blends with lactose monohydrate: 1. Albuterol sulfate and disodium cromoglycate.

    PubMed

    Xu, Zhen; Mansour, Heidi M; Mulder, Tako; McLean, Richard; Langridge, John; Hickey, Anthony J

    2010-08-01

    The major objective of this study was: discriminatory assessment of dry powder aerosol performance using standardized entrainment tubes (SETs) and lactose-based formulations with two model drugs. Drug/lactose interactive physical mixtures (2%w/w) were prepared. Their properties were measured: solid-state characterization of phase behavior and molecular interactions by differential scanning calorimetry and X-ray powder diffraction; particle morphology and size by scanning electron microscopy and laser diffraction; aerosol generation by SETs and characterization by twin-stage liquid impinger and Andersen cascade impactor operated at 60 L/min. The fine particle fraction (FPF) was correlated with SET shear stress (tau(s)), using a novel powder aerosol deaggregation equation (PADE). Drug particles were <5 microm in volume diameter with narrow unimodal distribution (Span <1). The lowest shear SET (tau(s) = 0.624 N/m(2)) gave a higher emitted dose (ED approximately 84-93%) and lower FPF (FPF(6.4) approximately 7-25%). In contrast, the highest shear SET (tau(s) = 13.143 N/m(2)) gave a lower ED (ED approximately 75-89%) and higher FPF (FPF(6.4) approximately 15-46%). The performance of disodium cromoglycate was superior to albuterol sulfate at given tau(s), as was milled with respect to sieved lactose monohydrate. Excellent correlation was observed (R(2) approximately 0.9804-0.9998) when pulmonary drug particle release from the surface of lactose carriers was interpreted by PADE linear regression for dry powder formulation evaluation and performance prediction. PMID:20198688

  17. Insight into biological phosphate recovery from sewage.

    PubMed

    Ye, Yuanyao; Ngo, Huu Hao; Guo, Wenshan; Liu, Yiwen; Zhang, Xinbo; Guo, Jianbo; Ni, Bing-Jie; Chang, Soon Woong; Nguyen, Dinh Duc

    2016-10-01

    The world's increasing population means that more food production is required. A more sustainable supply of fertilizers mainly consisting of phosphate is needed. Due to the rising consumption of scarce resources and limited natural supply of phosphate, the recovery of phosphate and their re-use has potentially high market value. Sewage has high potential to recover a large amount of phosphate in a circular economy approach. This paper focuses on utilization of biological process integrated with various subsequent processes to concentrate and recycle phosphate which are derived from liquid and sludge phases. The phosphate accumulation and recovery are discussed in terms of mechanism and governing parameters, recovery efficiency, application at plant-scale and economy. PMID:27434305

  18. 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

  19. 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

  20. Mineral induced formation of sugar phosphates

    NASA Astrophysics Data System (ADS)

    Pitsch, S.; Eschenmoser, A.; Gedulin, B.; Hui, S.; Arrhenius, G.

    1995-08-01

    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-diphosphates 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 µm; 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. 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.

  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. 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.

  4. 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

  5. Phosphate transporters and their function.

    PubMed

    Biber, Jürg; Hernando, Nati; Forster, Ian

    2013-01-01

    Plasma phosphate concentration is maintained within a relatively narrow range by control of renal reabsorption of filtered inorganic phosphate (P(i)). P(i) reabsorption is a transcellular process that occurs along the proximal tubule. P(i) flux at the apical (luminal) brush border membrane represents the rate-limiting step and is mediated by three Na(+)-dependent P(i) cotransporters (members of the SLC34 and SLC20 families). The putative proteins responsible for basolateral P(i) flux have not been identified. The transport mechanism of the two kidney-specific SLC34 proteins (NaPi-IIa and NaPi-IIc) and of the ubiquitously expressed SLC20 protein (PiT-2) has been studied by heterologous expression to reveal important differences in kinetics, stoichiometry, and substrate specificity. Studies on the regulation of the abundance of the respective proteins highlight significant differences in the temporal responses to various hormonal and nonhormonal factors that can influence P(i) homeostasis. The phenotypes of mice deficient in NaPi-IIa and NaPi-IIc indicate that NaPi-IIa is responsible for most P(i) renal reabsorption. In contrast, in the human kidney, NaPi-IIc appears to have a relatively greater role. The physiological relevance of PiT-2 to P(i) reabsorption remains to be elucidated. PMID:23398154

  6. Zirconium Phosphate Supported MOF Nanoplatelets.

    PubMed

    Kan, Yuwei; Clearfield, Abraham

    2016-06-01

    We report a rare example of the preparation of HKUST-1 metal-organic framework nanoplatelets through a step-by-step seeding procedure. Sodium ion exchanged zirconium phosphate, NaZrP, nanoplatelets were judiciously selected as support for layer-by-layer (LBL) assembly of Cu(II) and benzene-1,3,5-tricarboxylic acid (H3BTC) linkers. The first layer of Cu(II) is attached to the surface of zirconium phosphate through covalent interaction. The successive LBL growth of HKUST-1 film is then realized by soaking the NaZrP nanoplatelets in ethanolic solutions of cupric acetate and H3BTC, respectively. The amount of assembled HKUST-1 can be readily controlled by varying the number of growth cycles, which was characterized by powder X-ray diffraction and gas adsorption analyses. The successful construction of HKUST-1 on NaZrP was also supported by its catalytic performance for the oxidation of cyclohexene. PMID:27175935

  7. The SLC37 Family of Sugar-Phosphate/Phosphate Exchangers

    PubMed Central

    Chou, Janice Y.; Mansfield, Brian C.

    2014-01-01

    The SLC37 family members are endoplasmic reticulum (ER)-associated sugar-phosphate/phosphate (Pi) exchangers. Three of the four members, SLC37A1, SLC37A2, and SLC37A4, function as Pi-linked glucose-6-phosphate (G6P) antiporters catalyzing G6P:Pi and Pi:Pi 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 Pi. The G6PT/G6Pase-α complex maintains interprandial glucose homeostasis, and the G6PT/G6Pase-β complex maintains neutro-phil 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

  8. 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 DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5301 Ferric phosphate....

  9. 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 DRUGS, FEEDS, AND RELATED PRODUCTS SUBSTANCES GENERALLY RECOGNIZED AS SAFE Nutrients and/or Dietary Supplements 1 § 582.5217 Calcium phosphate....

  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 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...

  15. Drug-pyridoxal phosphate interactions.

    PubMed

    Ebadi, M; Gessert, C F; Al-Sayegh, A

    1982-01-01

    phosphate. Some interesting relationships are pointed out between vitamin B6, picolinic acid, and zinc. It is postulated that the intestinal absorption of zinc is facilitated by picolinic acid, a metabolite of tryptophan. The derivation of picolinic acid from tryptophan depends on the action of the enzyme kynureninase, which is dependent on pyridoxal phosphate; therefore, the adequate absorption of zinc is indirectly dependent on an adequate supply of vitamin B6. The formation of pyridoxal phosphate, on the other hand, appears to be indirectly dependent on Zn2++ which activates pyridoxal kinase.(ABSTRACT TRUNCATED AT 400 WORDS) PMID:6087425

  16. 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

  17. Expanding the structural landscape of niclosamide: a high Z' polymorph, two new solvates and monohydrate H(A).

    PubMed

    Sovago, Ioana; Bond, Andrew D

    2015-05-01

    Three new crystalline phases are reported for the drug niclosamide [5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide], C13H8Cl2N2O4. A new high-Z' polymorph (denoted Form II) is described, with four molecules in the asymmetric unit in the space group P2/n. The structure exhibits pseudosymmetry, including local translations and screw-type operations. The niclosamide molecules are linked by O-H...O hydrogen bonds into chains, and the chains are packed so that the molecules form face-to-face (stacking) and end-to-end interactions within layers perpendicular to the chains. There are two different layer arrangements, giving a structure that is relatively complex. In the acetone and acetonitrile solvates, the incorporated solvent molecules accept hydrogen bonds from the OH groups of niclosamide, and the niclosamide molecules are stacked in a face-to-face manner. In the acetone solvate, C13H8Cl2N2O4·C3H6O, V-shaped arrangements are formed in which the nitrobenzene ends of the niclosamide molecules are brought into face-to-face contact. In the acetonitrile solvate, C13H8Cl2N2O4·CH3CN, stacking occurs by translation along a short axis (ca 3.8 Å) and the crystals are frequently observed to be twinned by twofold rotation around that axis. The acetonitrile molecules occupy channels in the structure. A complete structure is provided for niclosamide monohydrate, C13H8Cl2N2O4·H2O, polymorph HA, obtained by Rietveld refinement against laboratory powder X-ray diffraction data. It has been suggested that this compound is related to the methanol solvate of niclosamide [Harriss, Wilson & Radosevljevic Evans (2014). Acta Cryst. C70, 758-763], but it is found that the two are not fully isostructural: they contain isostructural two-dimensional layers, but the layers are arranged differently in the two structures. This suggests that HA may have the potential for polytypism, and features in the Rietveld difference curve indicate that a polytype fully isostructural with the

  18. 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

  19. 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

  20. Phosphate transport and arsenate resistance in the cyanobacterium Anabaena variabilis

    SciTech Connect

    Thiel, T.

    1988-03-01

    Cells of the cyanobacterium Anabaena variabilis starved for phosphate for 3 days took up phosphate at about 100 times the rate of unstarved cells.Kinetic data suggested that a new transport system had been induced by starvation for phosphate. The inducible phosphate transport system was quickly repressed by addition of P/sub i/. Phosphate-starved cells were more sensitive to the toxic effects of arsenate than were unstarved cells, but phosphate could alleviate some of the toxicity. Arsenate was a noncompetitive inhibitor of phosphate transport; however, the apparent K/sub i/ values were high, particularly for phosphate-replete cells. Preincubation of phosphate-starved cells with arsenate caused subsequent inhibition of phosphate transport, suggesting that intracellular arsenate inhibited phosphate transport. This effect was not seen in phosphate-replete cells.

  1. Nanoporous sorbent material as an oral phosphate binder and for aqueous phosphate, chromate, and arsenate removal

    PubMed Central

    Sangvanich, Thanapon; Ngamcherdtrakul, Worapol; Lee, Richard; Morry, Jingga; Castro, David; Fryxell, Glen E.; Yantasee, Wassana

    2014-01-01

    Phosphate removal is both biologically and environmentally important. Biologically, hyperphosphatemia is a critical condition in end-stage chronic kidney disease patients. Patients with hyperphosphatemia are treated long-term with oral phosphate binders to prevent phosphate absorption to the body by capturing phosphate in the gastrointestinal (GI) tract followed by fecal excretion. Environmentally, phosphate levels in natural water resources must be regulated according to limits set forth by the US Environmental Protection Agency. By utilizing nanotechnology and ligand design, we developed a new material to overcome limitations of traditional sorbent materials such as low phosphate binding capacity, slow binding kinetics, and negative interference by other anions. A phosphate binder based on iron-ethylenediamine on nanoporous silica (Fe-EDA-SAMMS) has been optimized for substrates and Fe(III) deposition methods. The Fe-EDA-SAMMS material had a 4-fold increase in phosphate binding capacity and a broader operating pH window compared to other reports. The material had a faster phosphate binding rate and was significantly less affected by other anions than Sevelamer HCl, the gold standard oral phosphate binder, and AG® 1-X8, a commercially available anion exchanger. It had less cytotoxicity to Caco-2 cells than lanthanum carbonate, another prescribed oral phosphate binder. The Fe-EDA-SAMMS also had high capacity for arsenate and chromate, two of the most toxic anions in natural water. PMID:25554735

  2. 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.

  3. 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

  4. 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.

  5. 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

  6. 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

  7. 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.

  8. 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.

  9. [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

  10. Preparation, crystal structure, vibrational spectral and density functional studies of bis (4-nitrophenol)-2,4,6-triamino-1,3,5-triazine monohydrate

    NASA Astrophysics Data System (ADS)

    Kanagathara, N.; Marchewka, M. K.; Drozd, M.; Renganathan, N. G.; Gunasekaran, S.; Anbalagan, G.

    2013-10-01

    An organic-organic salt, bis (4-nitrophenol) 2,4,6-triamino 1,3,5-triazine monohydrate (BNPM) has been prepared by slow evaporation technique at room temperature. Single crystal X-ray diffraction analysis reveals that the compound crystallizes in triclinic system with centrosymmetric space group P-1. IR and Raman spectra of BNPM have been recorded and analyzed. The study has been extended to confocal Raman spectral analysis. Band assignments have been made for the melamine and p-nitrophenol molecules. Vibrational spectra have also been discussed on the basis of quantum chemical density functional theory calculations using Firefly (PC GAMESS) Version 7.1 G. Vibrational frequencies are calculated and scaled values are compared with the experimental one. The Mulliken charges, HOMO-LUMO orbital energies are calculated and analyzed. The chemical structure of the compound was established by 1H NMR and 13C NMR spectra.

  11. 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.

  12. Thermodynamic study of binary system Propafenone Hydrocloride with Metoprolol Tartrate: solid-liquid equilibrium and compatibility with α-lactose monohydrate and corn starch.

    PubMed

    Marinescu, Daniela-Crina; Pincu, Elena; Meltzer, Viorica

    2013-05-20

    Solid-liquid equilibrium (SLE) for binary mixture of Propafenone Hydrocloride (PP) with Metoprolol Tartrate (MT) was investigated using differential scanning calorimetry (DSC) and corresponding activity coefficients were calculated. Simple eutectic behavior for this system was observed. The excess thermodynamic functions: G(E) and S(E) for the pre-, post-, and eutectic composition have been obtained using the computed activity coefficients data of the eutectic phase with their excess chemical potentials μi(E) (i=1, 2). The experimental solid-liquid phase temperatures were compared with predictions obtained from available eutectic equilibrium models. The results indicate non-ideality in this mixture. Also, the compatibility of each component and their eutectic mixture with usual excipients was investigated, and the DSC experiments indicate possible weak interactions with α-lactose monohydrate and compatibility with corn starch. The results obtained were confirmed by FT-IR measurements. PMID:23545398

  13. 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

  14. Intramolecular charge delocalization and nonlinear optical properties of push-pull chromophore 1-(4-N,N-dimethylaminopyridinium) acetic acid bromide monohydrate from vibrational spectra.

    PubMed

    John, C Jesintha; Amalanathan, M; Sajan, D; Lakshmi, K Udaya; Joe, I Hubert

    2011-01-01

    FT-Raman and FT-IR spectra of the nonlinear optical crystal 1-(4-N,N-dimethylaminopyridinium) acetic acid bromide monohydrate have been recorded and analyzed. The equilibrium geometry, vibrational wavenumbers and the first order hyperpolarizability of the crystal have been calculated with the help of density functional theory computations. The assignments of the vibrational spectra have been carried out with the help of Scaled Quantum Mechanic force field theory. Optimized geometry gives the charge transfer interaction of the pyridine ring and the amino group in the electron-donor side of the nonlinear optic chromophore. Electron-phonon coupling and O-H⋯O interactions in making the molecule nonlinear optical active have been analyzed based on the vibrational spectral features. The Natural Bond Orbital analysis confirms the occurrence of strong intermolecular O-H⋯O hydrogen bonding. PMID:21036101

  15. 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

  16. Two isostructural carbamates: the o-tolyl N-(pyridin-3-yl)carbamate and 2-bromo-phenyl N-(pyridin-3-yl)carbamate monohydrates.

    PubMed

    Mocilac, Pavle; Gallagher, John F

    2015-11-01

    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 inter-action 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 intra-molecular C-H⋯O hydrogen bond is observed in each compound. PMID:26594512

  17. 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

  18. Librational modes of the water molecules in barium and strontium halide monohydrates, MX 2 · 1H 2O (M = Ba, Sr; X = Cl, Br, I)

    NASA Astrophysics Data System (ADS)

    Lutz, H. D.; Christian, H.

    1983-09-01

    The IR and Raman spectra of the isotypic alkaline earth halide monohydrates, MX 2 · 1H 2O, with M = Sr, Ba and X = Cl, Br, I, and of deuterated samples are presented for the range 200-700 cm -1 and discussed in terms of normal modes, assignment, coupling, correlation with structure data, and temperature dependence of both the H 2O (D 2O) and the HDO librational modes. The normal modes of the out-of-plane librations of HDO molecules are of the wagging and twisting type rather than H and D out-of-plane vibrations [4], at least for water molecules with C2v or nearly C2v symmetry. Thus the observed H 2O/HDO isotopic shifts can be used as a criterion for assigning the H 2O librations. The librational modes of the halide monohydrates (with tetrahedrally coordinated water oxygen atoms) are found in the order ν Rγ ≫ ν Rt ≫ ν Rr. The intensities of the IR and Raman spectra are in the order Rγ ≫ Rr ≫ Rt (or ˜ Rt in the case of strongly distorted H 2O molecules) and Rt ≫ Rr ≫ Rγ, respectively. Correlations of the H 2O librational modes with structural or bonding data are restricted by frequency shifts due to vibrational coupling and by the fact that the oxygen and the hydrogen atoms of the water molecules are generally affected in a different manner by bond interactions. However, in the case of the twisting vibrations, there are clear correlations with both the size of the metal ions, i.e. increase of ν Rt with decreasing size, and the intermolecular bonding of the hydrogen atoms, as shown by the OH stretching frequencies, i.e. increase of ν Rt with decreasing ν OH.

  19. Phosphate stimulates CFTR Cl- channels.

    PubMed Central

    Carson, M R; Travis, S M; Winter, M C; Sheppard, D N; Welsh, M J

    1994-01-01

    Cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channels appear to be regulated by hydrolysis of ATP and are inhibited by a product of hydrolysis, ADP. We assessed the effect of the other product of hydrolysis, inorganic phosphate (P(i)), on CFTR Cl- channel activity using the excised inside-out configuration of the patch-clamp technique. Millimolar concentrations of P(i) caused a dose-dependent stimulation of CFTR Cl- channel activity. Single-channel analysis demonstrated that the increase in macroscopic current was due to an increase in single-channel open-state probability (po) and not single-channel conductance. Kinetic modeling of the effect of P(i) using a linear three-state model indicated that the effect on po was predominantly the result of an increase in the rate at which the channel passed from the long closed state to the bursting state. P(i) also potentiated activity of channels studied in the presence of 10 mM ATP and stimulated Cl- currents in CFTR mutants lacking much of the R domain. Binding studies with a photoactivatable ATP analog indicated that Pi decreased the amount of bound nucleotide. These results suggest that P(i) increased CFTR Cl- channel activity by stimulating a rate-limiting step in channel opening that may occur by an interaction of P(i) at one or both nucleotide-binding domains. Images FIGURE 8 PMID:7532021

  20. Phosphate Oxygen Isotopes as a Tracer for Sources and Cycling of Phosphate in San Francisco Bay

    NASA Astrophysics Data System (ADS)

    McLaughlin, K.; Paytan, A.; Kendall, C.; Silva, S.

    2004-12-01

    Phosphorous is an essential macro-nutrient for primary productivity, but tracing sources and cycling of P in marine systems has been difficult to assess because P has only one stable isotope and can not be used as an isotopic tracer. Recently a new technique (McLaughlin et al., 2004) has been developed to track sources and cycling of phosphate in aquatic systems. This approach takes advantage of the strong P-O bond in phosphate, which is resistant to inorganic hydrolysis. The exchange of oxygen isotopes therein only occurs due to intracellular biological cycling. Because the d18O of phosphate will largely be determined by the isotopic composition of the water in which it is being recycled and because the isotopic composition of rivers and oceans is significantly different, the d18O of phosphate may be used as a tracer for different sources of phosphate to an estuarine system which is not phosphate limited. Consequently, the d18O of phosphate may be useful for quantifying the mixing of different sources of phosphate in estuarine systems. We applied this method to enhance our understanding of P sources and cycling in the San Francisco Bay. To this end we conducted four sampling transects from Coyote Creek in the South Bay to the Sacramento and San Joaquin Rivers in the North between October 2002 and August 2004. Phosphate d18O ranged from 10.1 to 20.1 per mil, with highest values at the Golden Gate and lowest at the San Joaquin River. Most of the Bay samples showed strong positive correlations with salinity, water d18O, and the inverse of phosphate concentration, suggesting a simple two-component mixing of oceanic and riverine sources. These data suggest that phosphate d18O can be an effective tool for identifying P point sources and understanding phosphate dynamics in the ecosystem.

  1. 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 δ18O of phosphate will reflect the isotopic composition of phosphate sources to the system. We utilized the δ18O of dissolved inorganic phosphate (DIP) within the main channel of the slough and nearby Moss Landing Harbor and the δ18O of reactive phosphate from sediment and soil samples collected within the watershed to understand phosphate sources and cycling within Elkhorn Slough. Trends in the δ18O 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 δ18O 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 δ18O values reflects the variations in land use and application of different fertilizers in this agriculturally dominated landscape. These data suggest that phosphate δ18O can be an effective tool for identifying P sources and understanding phosphate dynamics in estuarine ecosystems.

  2. Issues of natural radioactivity in phosphates

    SciTech Connect

    Schnug, E.; Haneklaus, S.; Schnier, C.; Scholten, L.C.

    1996-12-31

    The fertilization of phosphorus (P) fertilizers is essential in agricultural production, but phosphates contain in dependence on their origin different amounts of trace elements. The problem of cadmium (Cd) loads and other heavy metals is well known. However, only a limited number of investigations examined the contamination of phosphates with the two heaviest metals, uranium (U) and thorium (Th), which are radioactive. Also potassium (K) is lightly radioactive. Measurements are done n the radioactivity content of phosphates, P fertilizers and soils. The radiation doses to workers and public as well as possible contamination of soils from phosphate rock or fertilizer caused by these elements or their daughter products is of interest with regard to radiation protection. The use of P fertilizers is necessary for a sustainable agriculture, but it involves radioactive contamination of soils. The consequences of the use of P fertilizers is discussed, also with regard to existing and proposed legislation. 11 refs., 2 figs., 7 tabs.

  3. Enzyme activity in dialkyl phosphate ionic liquids.

    PubMed

    Thomas, Marie F; Li, Luen-Luen; Handley-Pendleton, Jocelyn M; van der Lelie, Daniel; Dunn, John J; Wishart, James F

    2011-12-01

    The activity of four metagenomic enzymes and an enzyme cloned from the straw mushroom, Volvariella volvacea 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. PMID:22001053

  4. Do osteocytes contribute to phosphate homeostasis?

    PubMed

    Feng, Jian Q; Ye, Ling; Schiavi, Susan

    2009-07-01

    Osteocytes, the terminally differentiated cell of the osteoblast lineage, account for over 90% of all bone cells. Due to their relative inaccessibility within mineralized matrix, little is known regarding their specific functions in comparison to the well studied surface bone cells, osteoblasts and osteoclasts. Furthermore, bone is often viewed as a mineral reservoir that passively releases calcium and phosphate in response to hormones secreted from remote organs. Noncollagenous matrix proteins produced in osteocytes, such as dentin matrix protein 1 (DMP1), have also been viewed as inert scaffolds for calcium-phosphate deposition. Recent discoveries of new genetic mutations in human diseases and development of genetically engineered animal models challenge these classic paradigms, suggesting that the osteocyte plays an active role in both mineralization and total systemic phosphate regulation. In this review, we will focus on roles of osteocytes in mineralization and particularly in phosphate regulation via the DMP1- FGF23 pathway. PMID:19448536

  5. 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.

  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. 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.

  8. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 179, which is incorporated by reference. Magnesium phosphate, tribasic, meets the specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 180, which...

  9. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 179, which is incorporated by reference. Magnesium phosphate, tribasic, meets the specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 180, which...

  10. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... phosphoric acid. (b) Magnesium phosphate, dibasic, meets the specifications of the Food Chemicals Codex, 3d... specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 180, which is incorporated by reference. Copies...

  11. 21 CFR 184.1434 - Magnesium phosphate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 179, which is incorporated by reference. Magnesium phosphate, tribasic, meets the specifications of the Food Chemicals Codex, 3d Ed. (1981), p. 180, which...

  12. Product inhibition of potato tuber pyrophosphate:fructose-6-phosphate phosphotransferase by phosphate and pyrophosphate.

    PubMed

    Stitt, M

    1989-02-01

    The product inhibition of potato (Solanum tuberosum) tuber pyrophosphate:fructose-6-phosphate phosphotransferase by inorganic pyrophosphate and inorganic phosphate has been studied. The binding of substrates for the forward (glycolytic) and the reverse (gluconeogenic) reaction is random order, and occurs with only weak competition between the substrate pair fructose-6-phosphate and pyrophosphate, and between the substrate pair fructose-1,6-bisphosphate and phosphate. Pyrophosphate is a powerful inhibitor of the reverse reaction, acting competitively to fructose-1,6-biphosphate and noncompetitively to phosphate. At the concentrations needed for catalysis of the reverse reaction, phosphate inhibits the forward reaction in a largely noncompetitive mode with respect to both fructose-6-phosphate and pyrophosphate. At higher concentrations, phosphate inhibits both the forward and the reverse reaction by decreasing the affinity for fructose-2,6-bisphosphate and thus, for the other three substrates. These results allow a model to be proposed, which describes the interactions between the substrates at the catalytic site. They also suggest the enzyme may be regulated in vivo by changes of the relation between metabolites and phosphate and could act as a means of controlling the cytosolic pyrophosphate concentration. PMID:16666593

  13. 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

  14. 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

  15. Redetermnation of lagochiline monohydrate

    PubMed Central

    Ibragimov, Aziz; Dolimov, Davron; Talipov, Samat; Izotova, Lidiya; Zainutdinov, Umardjon

    2010-01-01

    In the title compound, C20H36O5·H2O, previously studied by film methods [Vorontsova et al. (1975 ▶). Izvest. USSR Ser. Chem. 2, 338–343], the H atoms have been located and the absolute structure (seven stereogenic centres) established. An intra­molecular O—H⋯O hydrogen bond generates an S(6) ring. In the crystal, mol­ecules are linked by O—H⋯O hydrogen bonds, forming a three-dimensional network. PMID:21579472

  16. Disorders of phosphate homeostasis and tissue mineralisation.

    PubMed

    Bergwitz, Clemens; Jüppner, Harald

    2009-01-01

    Phosphate is absorbed from the diet in the gut, stored as hydroxyapatite in the skeleton, and excreted with the urine. The balance between these compartments determines the circulating phosphate concentration. Fibroblast growth factor 23 (FGF23) has recently been discovered and is part of a previously unrecognised hormonal bone-kidney axis. Phosphate-regulating gene with homologies to endopeptidases on the X chromosome, and dentin matrix protein 1 regulate the expression of FGF23 in osteocytes, which then is O-glycosylated by UDP-N-acetyl-alpha-D-galactosamine: polypeptide N-acetylgalactosaminyl-transferase 3 and secreted into the circulation. FGF23 binds with high affinity to fibroblast growth factor receptor 1c in the presence of its co-receptor Klotho. It inhibits, either directly or indirectly, reabsorption of phosphate and the synthesis of 1,25-dihydroxy-vitamin-D by the renal proximal tubule and the secretion of parathyroid hormone by the parathyroid glands. Acquired or inborn errors affecting this newly discovered hormonal system can lead to abnormal phosphate homeostasis and/or tissue mineralisation. This chapter will provide an update on the current knowledge of the pathophysiology, the clinical presentation, diagnostic evaluation and therapy of the disorders of phosphate homeostasis and tissue mineralisation. PMID:19494665

  17. The evolution of the marine phosphate reservoir.

    PubMed

    Planavsky, Noah J; Rouxel, Olivier J; Bekker, Andrey; Lalonde, Stefan V; Konhauser, Kurt O; Reinhard, Christopher T; Lyons, Timothy W

    2010-10-28

    Phosphorus is a biolimiting nutrient that has an important role in regulating the burial of organic matter and the redox state of the ocean-atmosphere system. The ratio of phosphorus to iron in iron-oxide-rich sedimentary rocks can be used to track dissolved phosphate concentrations if the dissolved silica concentration of sea water is estimated. Here we present iron and phosphorus concentration ratios from distal hydrothermal sediments and iron formations through time to study the evolution of the marine phosphate reservoir. The data suggest that phosphate concentrations have been relatively constant over the Phanerozoic eon, the past 542 million years (Myr) of Earth's history. In contrast, phosphate concentrations seem to have been elevated in Precambrian oceans. Specifically, there is a peak in phosphorus-to-iron ratios in Neoproterozoic iron formations dating from ∼750 to ∼635 Myr ago, indicating unusually high dissolved phosphate concentrations in the aftermath of widespread, low-latitude 'snowball Earth' glaciations. An enhanced postglacial phosphate flux would have caused high rates of primary productivity and organic carbon burial and a transition to more oxidizing conditions in the ocean and atmosphere. The snowball Earth glaciations and Neoproterozoic oxidation are both suggested as triggers for the evolution and radiation of metazoans. We propose that these two factors are intimately linked; a glacially induced nutrient surplus could have led to an increase in atmospheric oxygen, paving the way for the rise of metazoan life. PMID:20981096

  18. Characterization of phosphate films on aluminum surfaces

    SciTech Connect

    Cheng, B.; Ramamurthy, S.; McIntyre, N.S.

    1997-08-01

    A thin layer of phosphate conversion coating was formed on pure aluminum in a commercial zinc-manganese phosphating bath. A number of surface analytical techniques were used to characterize the phosphate thin films formed after immersion times ranging from 30 s to 10 min. The coating contained mainly a crystalline structure with dispersed micrometer-scale cavities. The major constituents of the phosphate film were zinc, phosphorus, and oxygen; a small amount of manganese was also detected. Based on these results, a three-stage mechanism was proposed for the formation and the growth of phosphate conversion coatings on aluminum. Electrochemical impedance spectroscopy was used to evaluate the corrosion performance of phosphated and uncoated aluminum samples in 0.50 M Na{sub 2}SO{sub 4} and 0.10 M H{sub 2}SO{sub 4} solutions. Both types of samples exhibited a passive state in the neutral solution and general corrosion behavior in the acid solution.

  19. Disorders of Phosphate Homeostasis and Tissue Mineralisation

    PubMed Central

    Bergwitz, Clemens; Jüppner, Harald

    2013-01-01

    Phosphate is absorbed from the diet in the gut, stored as hydroxyapatite in the skeleton, and excreted with the urine. The balance between these compartments determines the circulating phosphate concentration. Fibroblast growth factor 23 (FGF23) has recently been discovered and is part of a previously unrecognised hormonal bone-kidney axis. Phosphate-regulating gene with homologies to endopeptidases on the X chromosome, and dentin matrix protein 1 regulate the expression of FGF23 in osteocytes, which then is O-glycosylated by UDP-N-acetyl-alpha-d-galactosamine: poly-peptide N-acetylgalactosaminyl-transferase 3 and secreted into the circulation. FGF23 binds with high affinity to fibroblast growth factor receptor 1c in the presence of its co-receptor Klotho. It inhibits, either directly or indirectly, reabsorption of phosphate and the synthesis of 1,25-dihydroxy-vita-min-D by the renal proximal tubule and the secretion of parathyroid hormone by the parathyroid glands. Acquired or inborn errors affecting this newly discovered hormonal system can lead to abnormal phosphate homeostasis and/or tissue mineralisation. This chapter will provide an update on the current knowledge of the pathophysiology, the clinical presentation, diagnostic evaluation and therapy of the disorders of phosphate homeostasis and tissue mineralisation. PMID:19494665

  20. 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