Sample records for 3-methyl-2-benzothiazolinone hydrazone hydrochloride

  1. Spectrophotometric determination of isoxsuprine hydrochloride using 3-methyl-2-benzothiazolinone hydrazone hydrochloride in spiked human urine and pharmaceuticals

    Microsoft Academic Search

    Kalsang Tharpa; Kanakapura Basavaiah; Hosakere Doddarevanna Revanasiddappa; Kanakapura Basavaiah Vinay

    2010-01-01

    Two selective and sensitive spectrophotometric methods are proposed for the determination of isoxsuprine hydrochloride (ISX) in spiked human urine and in pharmaceuticals. The methods are based on the oxidative-coupling reaction between 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) and ISX in the presence of Ce(SO4)2. The novelty of the proposed reaction is the formation of two different colored chromogens at two different pHs.

  2. Copper(II)-catalysed oxidative coupling reaction of 3-hydroxyacetanilide with 3-methyl-2-benzothiazolinone hydrazone for the spectrophotometric determination of traces of copper(II)

    Microsoft Academic Search

    M. S. Hemantha Kumar; P. Nagaraja; H. S. Yathirajan

    2003-01-01

    A spectrophotometric method is developed for the determination of traces of copper(II), based on the catalytic oxidative coupling reaction of 3-hydroxyacetanilide with 3-methyl-2-benzothiazolinone hydrazone in the presence of ammonia and hydrochloric acid. Beer's law is obeyed in the copper(II) concentration range of 0.008-0.16 wg mLу, and the molar absorptivity at 530 nm is 2.5쎹 L molу cmу. The Sandell's sensitivity

  3. Assay of cisapride in pharmaceutical formulations by visible spectrophotometry

    Microsoft Academic Search

    Chilukuri S. P. Sastry; Yaramati Srinivas; Pulugurtha V. Subba Rao

    1997-01-01

    Three spectrophotometric methods (A-C) for the assay of cisapride (CPD) in pure and dosage forms are described. Method A is based on the oxidative coupling reaction of CPD with 3-methyl-2-benzothiazolinone hydrazone hydrochloride (MBTH) in the presence of ferric chloride to form a coloured species (?max; 565 nm.) Method B is based on the oxidation of CPD with Fe (III) and

  4. Development and validation of sensitive kinetic spectrophotometric method for the determination of moxifloxacin antibiotic in pure and commercial tablets.

    PubMed

    Ashour, Safwan; Bayram, Roula

    2015-04-01

    New, accurate, sensitive and reliable kinetic spectrophotometric method for the assay of moxifloxacin hydrochloride (MOXF) in pure form and pharmaceutical formulations has been developed. The method involves the oxidative coupling reaction of MOXF with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored product with lambda max at 623 and 660 nm. The reaction is followed spectrophotometrically by measuring the increase in absorbance at 623 nm as a function of time. The initial rate and fixed time methods were adopted for constructing the calibration curves. The linearity range was found to be 1.89-40.0 ?g mL(-1) for initial rate and fixed time methods. The limit of detection for initial rate and fixed time methods is 0.644 and 0.043 ?g mL(-1), respectively. Molar absorptivity for the method was found to be 0.89×10(4) L mol(-1) cm(-1). Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients. The results are compared with the official method. PMID:25596545

  5. Development and validation of sensitive kinetic spectrophotometric method for the determination of moxifloxacin antibiotic in pure and commercial tablets

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bayram, Roula

    2015-04-01

    New, accurate, sensitive and reliable kinetic spectrophotometric method for the assay of moxifloxacin hydrochloride (MOXF) in pure form and pharmaceutical formulations has been developed. The method involves the oxidative coupling reaction of MOXF with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored product with lambda max at 623 and 660 nm. The reaction is followed spectrophotometrically by measuring the increase in absorbance at 623 nm as a function of time. The initial rate and fixed time methods were adopted for constructing the calibration curves. The linearity range was found to be 1.89-40.0 ?g mL-1 for initial rate and fixed time methods. The limit of detection for initial rate and fixed time methods is 0.644 and 0.043 ?g mL-1, respectively. Molar absorptivity for the method was found to be 0.89 × 104 L mol-1 cm-1. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients. The results are compared with the official method.

  6. A novel use of oxidative coupling reactions for determination of some statins (cholesterol-lowering drugs) in pharmaceutical formulations

    NASA Astrophysics Data System (ADS)

    Ashour, Safwan; Bahbouh, Mahmoud; Khateeb, Mouhammed

    2011-03-01

    New, accurate and reliable spectrophotometric methods for the assay of three statin drugs, atorvastatin calcium (AVS), fluvastatin sodium (FVS) and pravastatin sodium (PVS) in pure form and pharmaceutical formulations have been described. All methods involve the oxidative coupling reaction of AVS, FVS and PVS with 3-methyl-2-benzothiazolinone hydrazone hydrochloride monohydrate (MBTH) in the presence of Ce(IV) in an acidic medium to form colored products with ?max at 566, 615 and 664 nm, respectively. Beer's law was obeyed in the ranges of 2.0-20.0, 4.9-35.4 and 7.0-30.0 ?g mL -1 for AVS-MBTH, FVS-MBTH and PVS-MBTH, respectively. Molar absorptivities for the above three methods were found to be 3.24 × 10 4, 1.05 × 10 4 and 0.68 × 10 4 L mol -1 cm -1, respectively. Statistical treatment of the experimental results indicates that the methods are precise and accurate. The proposed methods have been applied to the determination of the components in commercial forms with no interference from the excipients. A comparative study between the suggested procedures and the official methods for these compounds in the commercial forms showed no significant difference between the two methods.

  7. A review exploring biological activities of hydrazones

    PubMed Central

    Verma, Garima; Marella, Akranth; Shaquiquzzaman, Mohammad; Akhtar, Mymoona; Ali, Mohammad Rahmat; Alam, Mohammad Mumtaz

    2014-01-01

    The development of novel compounds, hydrazones has shown that they possess a wide variety of biological activities viz. antimicrobial, anticonvulsant, antidepressant, anti-inflammatory, analgesic, antiplatelet, antimalarial, anticancer, antifungal, antitubercular, antiviral, cardio protective etc., Hydrazones/azomethines/imines possess-NHN = CH- and constitute an important class of compounds for new drug development. A number of researchers have synthesized and evaluated the biological activities of hydrazones. This review aims at highlighting the diverse biological activities of hydrazones. PMID:24741273

  8. Reduction of formaldehyde concentrations in the air and cadaveric tissues by ammonium carbonate.

    PubMed

    Kawamata, Seiichi; Kodera, Haruto

    2004-09-01

    The reduction of formaldehyde by ammonium carbonate was examined in cadavers and in vitro. Formaldehyde concentrations in the air (10 cm above human cadavers) and in various cadaveric tissues were measured with or without perfusion of ammonium carbonate solution into formaldehyde-fixed cadavers. Air samples were monitored using Kitagawa gas detector tubes. For measurement of formaldehyde in tissues, muscles and organs were cut into small pieces and tissue fluids were separated out by centrifugation. These specimen fluids were diluted, supplemented with 3-methyl-2-benzothiazolinone hydrazone hydrochloride and quantified by spectrophotometry. In five cadavers without ammonium carbonate treatment, the formaldehyde concentrations in the air above the thorax and in various tissue fluids were 1.2-3.0 p.p.m. and 0.15-0.53%, respectively. Arterial reperfusion of saturated ammonium carbonate solution (1.0, 1.5 or 2.0 L) into five formaldehyde-fixed cadavers successfully reduced the formaldehyde levels, both in the air (0.5-1.0 p.p.m.) and in various tissue fluids (0.012-0.36%). In vitro experiments demonstrated that formaldehyde concentrations decreased, first rapidly and then gradually, with the addition of ammonium carbonate solution into fluids containing formaldehyde. It was confirmed that formaldehyde reacted with the ammonium carbonate and was thereby changed into harmless hexamethylenetetramine. The application of ammonium carbonate solution via intravascular perfusion and, if necessary, by infusion into the thoracic and peritoneal cavities, injection into muscles and spraying on denuded tissues can be anticipated to reduce formaldehyde to satisfactorily low levels in cadaveric tissues and, consequently, in the air, which may provide safe and odorless dissecting rooms. PMID:15453616

  9. Duloxetine hydrochloride

    Microsoft Academic Search

    Peter Kirkpatrick; Anathea B. Waitekus

    2004-01-01

    In August 2004, duloxetine hydrochloride (Cymbalta; Eli Lilly), a selective serotonin- and noradrenaline-reuptake inhibitor, was approved by the US FDA for the treatment of major depressive disorder. It has since become the first such antidepressant to be approved by the FDA for an indication outside of psychiatry, when its approval for use in the treatment of diabetic peripheral neuropathic pain

  10. Ketamine Hydrochloride and Xylazine Hydrochloride

    Microsoft Academic Search

    Jerrold L. Belant

    A combination of 100 mg ketamine hydrochloride (KH) and 20 mg xylazine hydro- chloride (XH) was used to immobilize fishers (Martes pennanti). Four adult males were in- tramuscularly injected a total of five times at dosages between 22.4 to 29.0 mg\\/kg KH and 4.1 to 6.6 mg\\/kg XH. Mean (±SE) induction time and arousal time were 3.3 ± 0.5 mm

  11. Lucanthone hydrochloride

    PubMed Central

    Blair, D. M.

    1958-01-01

    This review of the published work on the treatment of bilharziasis with lucanthone hydrochloride draws attention to the inconclusive nature of many of the trials carried out so far: either the dosage was inadequate or the patients were not followed up for a sufficient length of time. The author stresses the importance of obtaining a high concentration of lucanthone in the body fluids. He suggests that better results might be obtained if the total dose were given in two days or even as a single, massive dose. This method might also reduce the side effects, which do not appear, as a rule, until the second or third day. PMID:13573122

  12. Autoxidation of hydrazones. Some new insights.

    PubMed

    Harej, Maja; Dolenc, Darko

    2007-09-14

    Autoxidation of hydrazones is a generally occurring reaction, leading mostly to the formation of alpha-azohydroperoxides. All structural kinds of hydrazones, having at least one hydrogen atom on nitrogen, are prone to autoxidation; however, there are marked differences in the rate of the reaction. Hydrazones of aliphatic ketones are 1-2 orders of magnitude more reactive than analogous derivatives of aromatic ketones. Even less reactive are the hydrazones of chalcones, which function also as efficient inhibitors of autoxidation of other hydrazones. These differences can be attributed to the reduction of the rate of the addition of oxygen to a hydrazonyl radical, which is a reversible reaction. In the case of conjugated ketones, it becomes endothermic, making this elementary step slow down and the chain termination reactions become important. Substituents influence the stability of hydrazonyl radicals and, consequently, the bond dissociation energies of the N-H bonds. In acetophenone phenylhydrazones, the substituents placed on the ring of hydrazine moiety exhibit a higher effect (Hammett rho = -2.8) than those on the ketone moiety (rho = -0.82), which denotes higher importance of the structure with spin density concentrated on nitrogen in delocalized hydrazonyl radical. Electronic effects of the substituents also affect the transition state for the abstraction of hydrogen atom by electrophilic peroxy radicals; NBO analysis display a negative charge transfer of about 0.4 eu from hydrazone to a peroxy radical in the transition state. PMID:17696476

  13. Studies on hydrazone derivatives as antifungal agents.

    PubMed

    Ozdemir, Ahmet; Turan-Zitouni, Gulhan; Kaplancikli, Zafer Asim; Demirci, Fatih; Iscan, Gokalp

    2008-08-01

    The increasing clinical importance of drug-resistant fungal pathogens has urged additional need to fungal research and new antifungal compound development. For this purpose, some N-(1-benzyl-2-phenylethylidene)-N'-[4-(aryl)thiazol-2-yl]hydrazone (1a-e) and N-(1-phenylbutylidene)-N'-[4-(aryl)thiazol-2-yl]hydrazone (2a-e) derivatives were synthesised and evaluated for antifungal activity. Their antifungal activities against standard and clinical strands of Candida albicans, Candida glabrata, Candida utilis, Candida tropicalis, Candida krusei, Candida zeylanoides, and Candida parapsilosis were investigated. A significant level of activity was observed. PMID:18665994

  14. Hole mobilities in hydrazone-polycarbonate dispersions

    Microsoft Academic Search

    J. X. Mack; L. B. Schein; A. Peled

    1989-01-01

    Extensive characterization of the hole mobilities mu in dispersions of p-diethylamino- benzaldehyde-diphenyl hydrazone (DEH) in polycarbonate has been carried out. We report the effect of varying the electric field E, temperature T, and spacing between DEH molecules rho on mu. These data are analyzed by a procedure that allows proper separation of the functional dependencies of the mobility on E,

  15. Membrane solubilization technique for spectrophotometric determination of trace formaldehyde in rainwater.

    PubMed

    Murai, Keita; Okano, Mayumi; Kuramitz, Hideki; Hata, Noriko; Kawakami, Takanori; Taguchi, Shigeru

    2008-01-01

    A simple and sensitive spectrophotometry for formaldehyde in water by membrane solubilization technique was proposed. Formaldehyde was converted into a blue cationic dye with 3-methyl-2-benzothiazolinone hydrazone, and the dye was retained on a membrane filter as an ion-associate with tetraphenylborate anion. The filter retaining the blue dye was dissolved in 2-methoxyethanol containing sulfuric acid, and the absorbance of the solution was measured at 670 nm against the reagent blank. The formaldehyde from 0.007 to 0.2 mg L(-1) was determined with an RSD of less than 5%, and the detection limit was 0.002 mg L(-1). The proposed method was very simple and rapid. Twenty minutes was sufficient for the entire analytical procedure. When the method was applied to rainwater, the analytical results were in good agreement with those obtained by GC/MS. PMID:18997375

  16. Simple spectrophotometric methods for estimation of aceclofenac from bulk and formulations

    PubMed Central

    Bose, A; Dash, PP; Sahoo, MK

    2010-01-01

    Two simple, precise and accurate visible spectrophotometric methods were developed for the estimation of Aceclofenac in bulk drug and in pharmaceutical formulations. The proposed methods were indirect and based on determination of aceclofenac after its reaction with either (p-dimethylaminocinnamaldehyde or 3-Methyl-2-benzothiazolinone hydrazine hydrochloride and measuring the chromogen at the ?max by 658 and 592, respectively. Beers law obeyed in the concentration range of 1-200 ?g/ml for method A and 1-100 ?g/ml for method B. The accuracy of the methods was determined by recovery studies. The methods showed good reproducibility and recovery with relative standard deviation (in %) less than 2. The methods were found to be simple, economical, accurate and reproducible and can be used for routine analysis of Aceclofenac in bulk drug and in pharmaceutical formulations. PMID:23781418

  17. Simple spectrophotometric methods for estimation of aceclofenac from bulk and formulations.

    PubMed

    Bose, A; Dash, Pp; Sahoo, Mk

    2010-10-01

    Two simple, precise and accurate visible spectrophotometric methods were developed for the estimation of Aceclofenac in bulk drug and in pharmaceutical formulations. The proposed methods were indirect and based on determination of aceclofenac after its reaction with either (p-dimethylaminocinnamaldehyde or 3-Methyl-2-benzothiazolinone hydrazine hydrochloride and measuring the chromogen at the ?max by 658 and 592, respectively. Beers law obeyed in the concentration range of 1-200 ?g/ml for method A and 1-100 ?g/ml for method B. The accuracy of the methods was determined by recovery studies. The methods showed good reproducibility and recovery with relative standard deviation (in %) less than 2. The methods were found to be simple, economical, accurate and reproducible and can be used for routine analysis of Aceclofenac in bulk drug and in pharmaceutical formulations. PMID:23781418

  18. Reaction of hydrazones and azines with metal salts

    Microsoft Academic Search

    A. S. Gudkova; O. A. Reutov

    1962-01-01

    1.A study was made of the reaction of aliphatic ketone and aldehyde hydrazones with cupric acetate, chloride, and bromide in aqueous and methanolic media.2.All the hydrazones studied react with cupric chloride, bromide, and acetate with formation of complexes of general composition (RR'C=N)2 nCuX, in which X=Cl, Br, or I and n=2 or 3. The structure of the complex depends both

  19. Computational investigation of first hyperpolarizability in substituted hydrazones

    NASA Astrophysics Data System (ADS)

    Lu, Shih-I.

    2013-08-01

    Density functional theory has been used to calculate the ?·?(-2?;?,?,0) on a series of solution-phase hydrazones. Using the experimental and MP2(Full) calculated data as references, the qualitative trend of the Hartree-Fock, M06-HF and range-separated hybrids have been examined. Our results propose methods with long-range corrections, and without short-range exact exchange, are capable of qualitatively predicting the nonlinear optical responses of the hydrazones when reliable geometries have been provided. The same conclusion can also be applied to solution-phase push-pull phenylpolyenes.

  20. Drug release from hydrazone-containing peptide amphiphiles

    SciTech Connect

    Matson, John B.; Stupp, Samuel I. (NWU)

    2012-03-15

    Hydrolytically-labile hydrazones in peptide amphiphiles were studied as degradable tethers for release of the drug nabumetone from nanofiber gels. On-resin addition of the novel compound tri-Boc-hydrazido adipic acid to a lysine E-amine allowed for precise placement of a hydrazide in a peptide sequence.

  1. Case of anaphylaxis due to tetracycline hydrochloride.

    PubMed

    Ogita, Azusa; Takada, Kaori; Kawana, Seiji

    2011-06-01

    A 17-year-old Japanese woman showed anaphylaxis after taking tetracycline hydrochloride, pyridoxal phosphate, flavin adenine dinucleotide sodium and ascorbic acid. Prick tests were performed for these suspicious drugs and anaphylaxis due to tetracycline hydrochloride was diagnosed. PMID:21352288

  2. Fenfluramine hydrochloride, (+-)-N-ethyl-m-(trifluoromethyl)amphetamine hydrochloride

    E-print Network

    Grunewald, Gary L; Creese, Mary W; Extine, Michael W

    1981-01-01

    ) . SHELX. Program for crya structure determination. Univ. of Cambridge, England. STEWART, R . F . , DAVIDSON, E . R . & SIMPSON, W. T. J. Chem.Phys. 4 2 , 3 1 7 5 - 3 1 8 7 . Acta Cryst. (1981). B37, 1790-1793 Fenfluramine Hydrochloride, (±)-A^-Ethyl-/w-(trifluoromethyl)amphetamine... reflections after anisotropic refinement of all non-H atoms. The solid-state conformations of the fenfluramine and amphetamine cations are the same. Introduction. Single crystals of racemic fenfluramine hydrochloride were obtained by recrystallization from...

  3. Antioxidant activity of hydrazones with sterically hindered phenol fragments

    NASA Astrophysics Data System (ADS)

    Nikolaevskii, A. N.; Kniga, O. P.; Khizhan, E. I.; Tikhonova, G. A.; Vinogradov, V. V.; Khizhan, A. I.

    2012-12-01

    Kinetic parameters of the antiradical activity of derivatives of hydrazones of 4-hydroxy-3,5-di- tert-butyl-benzaldehyde are determined photocolorimetrically in their reactions with a stable diphenylpicrylhydrazyl radical, and by chemiluminescence from the capture of peroxide radicals upon the initiated oxidation of ethylbenzene. It is found that during inhibited oxidation, the reactive centers (N-H and O-H) in hetaryl- and acylhydrazone molecules operate in parallel. Regularities of the compounds' inhibiting effect are studied in heterogeneous systems upon the initiated oxidation of ethylbenzene in emulsion, and in a water-lipid model of the oxidation of phosphatidylcholine dispersion. It is established that hydrazone derivatives are antioxidants of combined action in heterophase processes of the oxidation of unsaturated substrates, displaying properties of hydroperoxide deactivators in addition to their antiradical activity.

  4. IMMOBILIZATION OF SWIFT FOXES WITH KETAMINE HYDROCHLORIDE-XYLAZINE HYDROCHLORIDE

    Microsoft Academic Search

    Rebecca L. Telesco; Marsha A. Sovada

    2002-01-01

    There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochlo- ride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an

  5. Fluorescence Quenchers for Hydrazone and Oxime Orthogonal Bioconjugation

    PubMed Central

    Crisalli, Pete; Hernández, Armando R.; Kool, Eric T.

    2012-01-01

    We describe the synthesis and properties of new fluorescence quenchers containing aldehyde, hydrazine and aminooxy groups, allowing convenient bioconjugation as oximes or hydrazones. Conjugation to oligonucleotides proceeded in high yield with aniline as catalyst. Kinetics studies of conjugation show that, under optimal conditions, a hydrazine or aminooxy quencher can react with aldehyde-modified DNA to form a stable hydrazone or oxime adduct in as little as five minutes. The resulting quencher-containing DNAs were assessed for their ability to quench the emission of fluorescein in labeled complements and compared to the commercially available dabcyl and Black Hole Quencher 2 (BHQ2), which were conjugated as phosphoramidites. Results show that the new quenchers possess slightly different absorbance properties compared to dabcyl and are as efficient as the commercial quenchers in quenching fluorescein emission. Hydrazone-based quenchers were further successfully incorporated into molecular beacons and shown to give high signal:background in single nucleotide polymorphism detection in vitro . Finally, aminooxy and hydrazine quenchers were applied to quenching of an aldehyde-containing fluorophore associated with living cells, demonstrating cellular quenching within one hour. PMID:22913527

  6. Reactions of hydrazones and azines with metal salts Communication 5. Reactions of hydrazones and azines with mercuric halides

    Microsoft Academic Search

    A. S. Gudkova; M. Yao Aleinikova; O. A. Reutov

    1966-01-01

    Hydrazones and azines of acetaldehyde, acetone, butanone, cyclohexanone, cyclopentanone, camphor, 2,3-bornanedione, and acetophenone react with mercuric chloride and bromide with formation of complexes between the reactants of general composition (R2C=N-NH2)·nHgX2; (R2C=N-N=CR2)·nHgX2, in which X=C1 or Br and n=1 or 2.

  7. Transition metal complexes of an isatinic quinolyl hydrazone

    PubMed Central

    2011-01-01

    Background The importance of the isatinic quinolyl hydrazones arises from incorporating the quinoline ring with the indole ring in the same compound. Quinoline ring has therapeutic and biological activities. On the other hand, isatin (1H-indole-2,3-dione) and its derivatives exhibit a wide range of biological activities. Also, the indole ring occurs in Jasmine flowers and Orange blossoms. Recently, the physiological and biological activities of quinolyl hydrazones arise from their tendency to form metal chelates with transition metal ions. In this context, we have reported to isolate, characterize and study the biological activity of some transition metal complexes of an isatinic quinolyl hydrazone; 3-[2-(4-methyl quinolin-2-yl)hydrazono] indolin-2-one. Results Mono- and binuclear as well as dimeric chelates were obtained from the reaction of a new isatinic quinolyl hydrazone with Fe(III), Co(II), Ni(II), Cu(II), VO(II) and Pd(II) ions. The ligand showed a variety of modes of bonding viz. (NNO)2-, (NO)- and (NO) per each metal ion supporting its ambidentate and flexidentate characters. The mode of bonding and basicity of the ligand depend mainly on the type of the metal cation and its counter anion. All the obtained Pd(II)- complexes have the preferable square planar geometry (D4h- symmetry) and depend mainly on the mole ratio (M:L). Conclusion The effect of the type of the metal ion for the same anion (Cl-) is obvious from either structural diversity of the isolated complexes (Oh, Td and D4h) or the various modes of bonding. The isatinic hydrazone uses its lactim form in all complexes (Cl-) except complex 5 (SO42-) in which it uses its lactam form. The obtained Pd(II)- complexes (dimeric, mono- and binuclear) are affected by the mole ratio (M:L) and have the square planar (D4h) geometry. Also, the antimicrobial activity is highly influenced by the nature of the metal ion and the order for S. aureus bacteria is as follows: Nickel(II) > Vanadyl(II) > Cobalt(II) > Copper(II) ? Palladium(II) >> Iron(III). PMID:21708023

  8. Synthesis and in vitro and in vivo antimycobacterial activity of isonicotinoyl hydrazones

    Microsoft Academic Search

    Dharmarajan Sriram; Perumal Yogeeswari; Kasinathan Madhu

    2005-01-01

    The purpose of this study was to prepare various isoniazid derivatives by introducing the isoniazid pharmacophore into several molecules and screening for antimycobacterial activity. Ortho-hydroxy acetophenone reacts with isoniazid to form acid hydrazones. The C-Mannich bases of the above acid hydrazones were prepared by reacting them with formaldehyde and various secondary amines. The synthesized compounds were screened against M. tuberculosis

  9. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 false Naloxone hydrochloride injection. 522.1462 Section 522.1462...522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an aqueous sterile solution...

  10. 21 CFR 522.2002 - Propiopromazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...false Propiopromazine hydrochloride injection. 522.2002 Section 522.2002...2002 Propiopromazine hydrochloride injection. (a) Chemical name. 1-Propanone...Specifications. Propiopromazine hydrochloride injection contains 5 or 10 milligrams of the...

  11. 21 CFR 522.1462 - Naloxone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 false Naloxone hydrochloride injection. 522.1462 Section 522.1462...522.1462 Naloxone hydrochloride injection. (a) Specifications. Naloxone hydrochloride injection is an aqueous sterile solution...

  12. Ligand substitution reactions of a phenolic quinolyl hydrazone; oxidovanadium (IV) complexes

    PubMed Central

    2011-01-01

    Background Quinoline ring has therapeutic and biological activities. Quinolyl hydrazones constitute a class of excellent chelating agents. Recently, the physiological and biological activities of quinolyl hydrazones arise from their tendency to form metal chelates with transition metal ions. In this context, we have aimed to study the competency effect of a phenolic quinolyl hydrazone (H2L; primary ligand) with some auxiliary ligands (Tmen, Phen or Oxine; secondary ligands) towards oxidovanadium (IV) ions. Results Mono- and binuclear oxidovanadium (IV) - complexes were obtained from the reaction of a phenolic quinolyl hydrazone with oxidovanadium (IV)- ion in absence and presence of N,N,N',N'- tetramethylethylenediamine (Tmen), 1,10-phenanthroline (Phen) or 8-hydroxyquinoline (Oxine). The phenolic quinolyl hydrazone ligand behaves as monobasic bidentate (NO- donor with O- bridging). All the obtained complexes have the preferable octahedral geometry except the oxinato complex (2) which has a square pyramid geometry with no axial interaction; the only homoleptic complex in this study. Conclusion The ligand exchange (substitution/replacement) reactions reflect the strong competency power of the auxiliary aromatic ligands (Phen/Oxine) compared to the phenolic quinolyl hydrazone (H2L) towards oxidovanadium (IV) ion; (complexes 2 and 3). By contrast, in case of the more flexible aliphatic competitor (Tmen), an adduct was obtained (4). The obtained complexes reflect the strength of the ligand field towards the oxidovanadium (IV)- ion; Oxine or Phen >> phenolic hydrazone (H2L) > Tmen. PMID:21846387

  13. Synthesis of some new diaryl and triaryl hydrazone derivatives as possible estrogen receptor modulators.

    PubMed

    Pandey, Jaya; Pal, Rekha; Dwivedi, Anila; Hajela, Kanchan

    2002-01-01

    1,2-Bis(4-substituted phenyl)-2-methyl ethanone (2,4-dinitrophenyl)hydrazones and 1-naphthyl-1-(4-substituted phenyl)-methanone (2,4-dinitrophenyl)hydrazones have been synthesized and evaluated for their anti-implantation, uterotrophic, antiuterotrophic, anticancer and antimicrobial activities. Diphenolic hydrazone (compound 6) showed maximum uterotrophic inhibition of 70%, whereas compound 20 exhibited cytotoxicity in the range of 50-70% against MCF-7 and ZR-75-1 human malignant breast cell lines. PMID:11838273

  14. Synthesis of Macrocyclic Bis-Hydrazone and Their Use in Metal Cations Extraction

    PubMed Central

    Kandil, Farouk; Chebani, Mohamad Khaled; Al Zoubi, Wail

    2012-01-01

    Two new macrocyclic hydrazone Schiff bases were synthesized by reaction of succindihydrazide and adipdihydrazide with acetylacetone. Hydrazones have been characterized by elemental analyses and IR, mass, 1H?NMR, and 13C?NMR spectral data. Hydrazones have been studied by liquid-liquid extraction towards the s-metal ions (Li+, Na+, and K+) and d-metal ions (Cu2+ and Cr3+) from aqueous phase to organic phase. The effect of chloroform and dichloromethane as organic solvents over the metal chlorides extraction was investigated at 25 ± 0.1°C by using flame atomic absorption. We found differences between the two solvents in extraction selectivity. PMID:24052837

  15. Use of yohimbine hydrochloride to reverse immobilization of polar bears by ketamine hydrochloride and xylazine hydrochloride.

    PubMed

    Ramsay, M A; Stirling, I; Knutsen, L O; Broughton, E

    1985-10-01

    Yohimbine hydrochloride (YH) effectively reversed the immobilizing effects of ketamine hydrochloride (KH) combined with xylazine hydrochloride (XH) in 48 wild polar bears (Ursus maritimus) handled in the summer. Single intravenous doses of YH ranging between 0.029 and 0.198 mg/kg resulted in a median time of 10 min (range: 1-123 min) to post-injection recovery from KH-XH immobilization. Convulsions and muscle twitching were observed in some bears after YH was administered and one death occurred. Median respiratory rate and heartbeat rate increased from 5 br/min to 12 br/min and 51 BPM to 79 BPM, respectively, soon after yohimbine was administered. The median time to recovery after KH-XH administration, including processing and handling time, was 113 min for bears administered yohimbine and 202 min for bears not administered YH. After YH-induced recovery, polar bears showed signs of reduced awareness and many remained recumbent for undetermined periods although they could coordinate movements, stand, and walk or run if disturbed. YH proved to be a useful antagonist to immobilization induced by KH-XH in a field situation. PMID:4078975

  16. Antibacterial activity of chalcones, hydrazones and oxadiazoles against methicillin-resistant Staphylococcus aureus.

    PubMed

    Moreira Osório, Thaís; Delle Monache, Franco; Domeneghini Chiaradia, Louise; Mascarello, Alessandra; Regina Stumpf, Taisa; Roberto Zanetti, Carlos; Bardini Silveira, Douglas; Regina Monte Barardi, Célia; de Fatima Albino Smânia, Elza; Viancelli, Aline; Ariel Totaro Garcia, Lucas; Augusto Yunes, Rosendo; José Nunes, Ricardo; Smânia, Artur

    2012-01-01

    The increase in antibiotic resistance due to multiple factors has encouraged the search for new compounds which are active against multidrug-resistant pathogens. In this context, chalcones, dihydrochalcones, hydrazones and oxadiazoles were tested against Staphylococcus aureus ATCC 25923 and methicillin-resistant S. aureus (MRSA) isolates, which were obtained from clinical laboratories and were characterized as MRSA using traditional and molecular methods. Among 65 tested compounds, two chalcones, one dihydrochalcone and two hydrazones were active against MRSA. Based on the minimal inhibitory concentration and cytotoxicity, hydrazones provided a better selectivity index than chalcones. Active hydrazones are promising antibiotic-like substances and they should be the subject of further microbiological studies. PMID:22169259

  17. The antibacterial activity of some sulfonamides and sulfonyl hydrazones, and 2D-QSAR study of a series of sulfonyl hydrazones

    NASA Astrophysics Data System (ADS)

    Aslan, H. Güzin; Özcan, Servet; Karacan, Nurcan

    2012-12-01

    Benzenesulfonicacid-1-methylhydrazide (1) and its four aromatic sulfonyl hydrazone derivatives (1a-1d), N-(3-amino-2-hydroxypropyl)benzene sulfonamide (2) and N-(2-hydroxyethyl)benzenesulfonamide (3) were synthesized and their structures were determined by IR, 1H NMR, 13C NMR, and LCMS techniques. Antibacterial activities of new synthesized compounds were evaluated against various bacteria strains by microdilution and disk diffusion methods. The experimental results show that presence of OH group on sulfonamides reduces the antimicrobial activity, and antimicrobial activities of the sulfonyl hydrazones (1a-1d) are smaller than that of the parent sulfonamide (1), except Candida albicans. In addition, 2D-QSAR analysis was performed on 28 aromatic sulfonyl hydrazones as antimicrobial agents against Escherichia coli and Staphylococcus aureus. In the QSAR models, the most important descriptor is total point-charge component of the molecular dipole for E. coli, and partial negative surface area (PNSA-1) for S. aureus.

  18. Preparation of magnetite/poly(styrene-divinylbenzene) nanoparticles for selective enrichment-determination of fenitrothion in environmental and biological samples.

    PubMed

    Eskandari, Habibollah; Naderi-Darehshori, Ali

    2012-09-19

    In the present study, a cross-linked nano-sized spherical magnetic poly(styrene-divinylbenzene) is synthesized and used as an adsorbent for enrichment-determination of fenitrothion. A miniemulsion polymerization procedure was used to prepare the adsorbent. The magnetic adsorbent was characterized by FT-IR, SEM and TEM. The prepared magnetic adsorbent nanoparticles were mixed with magnetite nanoparticles for faster and more efficient magnetic precipitation. The reduced fenitrothion was coupled with 3-methyl-2-benzothiazolinone hydrazone and then the blue colored complex was extracted. The blue derivative of fenitrothion was eluted by a 1 mL aliquot of 1-propanol prior to spectrophotometry at 571 nm. Beer's law was obeyed in the range of 2-230 ng mL(-1) of fenitrothion with relative standard deviation and recovery in the ranges of 0.9-5.1% and 97.2-100.0%, respectively. Selectivity of the method was evaluated, and the method was successfully applied to the determination of fenitrothion in various water, soil, urine and human plasma samples. PMID:22882834

  19. Immobilization of porcupines with tiletamine hydrochloride and zolazepam hydrochloride (Telazol).

    PubMed

    Hale, M B; Griesemer, S J; Fuller, T K

    1994-07-01

    Immobilization of North American porcupines (Erethizon dorsatum) with tiletamine hydrochloride (HCl) and zolazepam HCl (Telazol) was evaluated in central Massachusetts (USA) during 1991 and 1992. Doses between 9 and 11 mg/kg resulted in a mean (+/- SD) induction time of 3.2 +/- 1.3 min and a mean (+/- SD) immobilization time of 44.2 +/- 19.5 min. Induction time did not differ by dose, sex, capture method, or porcupine weight. Immobilization time differed by dose and porcupine weight but not by sex or capture method. Tiletamine HCl and zolazepam HCl seems to be an effective combination of drugs for immobilizing porcupines as long as sufficient time is allowed for recovery. PMID:7933289

  20. Bradyarrhythmias secondary to topical levobunolol hydrochloride solution

    PubMed Central

    Lin, Lianjun; Wang, Yuchuan; Chen, Yan; Liu, Meilin

    2014-01-01

    An 88-year-old man was admitted with fatigue, dizziness, and heart palpitations. Both the electrocardiogram and Holter confirmed the existence of sinus bradycardia and sinus arrest. One hour prior to the onset of symptoms, he received levobunolol hydrochloride solution topically. The levobunolol hydrochloride solution was discontinued and the bradycardia resolved. He was diagnosed as having intermittent sinus bradycardia and sinus arrest, induced by topical ?-blocker therapy. Levobunolol hydrochloride solution is an effective therapy for ocular hypertension, probably by reducing aqueous fluid production. However, it can induce cardiac side effects such as bradyarrhythmia and should be used with caution in elderly patients or patients with cardiac disease. PMID:25342892

  1. Bradyarrhythmias secondary to topical levobunolol hydrochloride solution.

    PubMed

    Lin, Lianjun; Wang, Yuchuan; Chen, Yan; Liu, Meilin

    2014-01-01

    An 88-year-old man was admitted with fatigue, dizziness, and heart palpitations. Both the electrocardiogram and Holter confirmed the existence of sinus bradycardia and sinus arrest. One hour prior to the onset of symptoms, he received levobunolol hydrochloride solution topically. The levobunolol hydrochloride solution was discontinued and the bradycardia resolved. He was diagnosed as having intermittent sinus bradycardia and sinus arrest, induced by topical ?-blocker therapy. Levobunolol hydrochloride solution is an effective therapy for ocular hypertension, probably by reducing aqueous fluid production. However, it can induce cardiac side effects such as bradyarrhythmia and should be used with caution in elderly patients or patients with cardiac disease. PMID:25342892

  2. Immobilization of swift foxes with ketamine hydrochloride-xylazine hydrochloride.

    PubMed

    Telesco, Rebecca L; Sovada, Marsha A

    2002-10-01

    There is an increasing need to develop field immobilization techniques that allow researchers to handle safely swift foxes (Vulpes velox) with minimal risk of stress or injury. We immobilized captive swift foxes to determine the safety and effectiveness of ketamine hydrochloride and xylazine hydrochloride at different dosages. We attempted to determine appropriate dosages to immobilize swift foxes for an adequate field-handling period based on three anesthesia intervals (induction period, immobilization period, and recovery period) and physiologic responses (rectal temperature, respiration rate, and heart rate). Between October 1998-July 1999, we conducted four trials, evaluating three different dosage ratios of ketamine and xylazine (2.27:1.2, 5.68:1.2, and 11.4:1.2 mg/kg ketamine:mg/kg xylazine, respectively), followed by a fourth trial with a higher dosage at the median ratio (11.4 mg/kg ketamine: 2.4 mg/kg xylazine). We found little difference in induction and recovery periods among trials 1-3, but immobilization time increased with increasing dosage (P < 0.08). Both the immobilization period and recovery period increased in trial 4 compared with trials 1-3 (P < or = 0.03). There was a high variation in responses of individual foxes across trials, making it difficult to identify an appropriate dosage for field handling. Heart rate and respiration rates were depressed but all physiologic measures remained within normal parameters established for domestic canids. We recommend a dosage ratio of 10 mg/kg ketamine to 1 mg/kg xylazine to immobilize swift foxes for field handling. PMID:12528444

  3. Treatment of premature ejaculation with paroxetine hydrochloride

    Microsoft Academic Search

    CG McMahon; K Touma

    1999-01-01

    Aims of this study: To evaluate the efficacy of chronic and ‘on demand’ administration of paroxetine hydrochloride in the drug treatment of premature ejaculation (PE).Materials and methods: Ninety-four normally potent men, aged 18–61 y (mean 39 y) with premature ejaculation were treated between January 1996 and March 1997, with oral paroxetine hydrochloride, a selective serotonin re-uptake inhibitor (SSRI). All men

  4. FUNCTIONALIZED BETA-C-GLYCOSIDIC KETONE HYDRAZONES. NOVEL DERIVATIVES FOR IMMOBILIZATION AND END-LABELING OF CARBOHYDRATES.

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Hydrazones are excellent derivatives for the analysis of aldehydes and ketones and are often readily prepared in quantitative yield. Unlike simple aldehydes and ketones, sugars do not usually form simple hydrazones. They react with three equivalents of aryl- or acylhydrazines at both the C1 and C2...

  5. Quinazolin-4-yl-sulfanylacetyl-hydrazone derivatives; Synthesis, molecular structure and electronic properties

    NASA Astrophysics Data System (ADS)

    Hagar, Mohamed; Soliman, Saied M.; Ibid, Farahate; El Ashry, El Sayed H.

    2013-10-01

    Four new acetylhydrazone derivatives of quinazoline have been synthesized and characterized. The molecular structures and relative stabilities of four possible isomers for each acetylhydrazone are calculated using DFT/B3LYP/6-31G(d,p) method. The calculations results predicted higher stability of the E-isomers compared to the Z-isomers in the gas phase. The syn-E isomer is the predominant form in gaseous phase for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti-E is the most stable isomer. The latter is stabilized by two strong intramolecular H-bonds instead of one in the others. The electronic and spectroscopic properties of the most stable isomers were also calculated using the same level of theory. The calculated atomic polar tensor (APT) charges indicated an increase of the positive charge density at the H-sites involved in the H-bonding interactions. The HOMO and LUMO energies are negative indicating that the compounds under investigation are stable. The electronic transition from the ground state to the excited state belongs to ?-?* transition. The calculated vibrational spectra showed strong red shifts and increase in the vibrational intensity of the Nsbnd H and Osbnd H stretching modes due to the intramolecular H-bonding interactions. In DMSO solution, the NMR spectra of the studied hydrazones revealed that such polar solvents stabilize the syn isomers for all the studied hydrazones except for the hydrazone derived from salicylaldehyde where the anti isomer is the major.

  6. Synthesis and antibacterial activity against ralstonia solanacearum for novel hydrazone derivatives containing a pyridine moiety

    PubMed Central

    2012-01-01

    Background Ralstonia solanacearum, one of the most important bacterial diseases on plants, is a devastating, soil-borne plant pathogen with a global distribution and an unusually wide host range. In order to discover new bioactive molecules and pesticides acting on tobacco bacterial wilt, we sought to combine the active structure of hydrazone and pyridine together to design and synthesize a series of novel hydrazone derivatives containing a pyridine moiety. Results A series of hydrazone derivatives containing a pyridine moiety were synthesized. Their structures were characterized by 1 H-NMR, 13 C-NMR, IR, and elemental analysis. The preliminary biological activity tests showed that compound 3e and 3g exhibited more than 80% activity against Ralstonia solanacearum at 500 mg/L, especially compound 3g displayed relatively good activity to reach 57.0% at 200 mg/L. Conclusion A practical synthetic route to hydrazone derivatives containing a pyridine moiety by the reaction of intermediates 2 with different aldehydes in ethanol at room temperature using 2-chloronicotinic acid and 2-amino-5-chloro-3-methylbenzoic acid as start materials is presented. This study suggests that the hydrazone derivatives containing a substituted pyridine ring could inhibit the growth of Ralstonia solanacearum. PMID:22483270

  7. The tautomerization between keto- to phenol-hydrazone induced by anions in the solution

    NASA Astrophysics Data System (ADS)

    Shang, Xuefang; Yuan, Jianmei; Wang, Yingling; Zhang, Jinlian; Xu, Xiufang

    2012-02-01

    Two simple anion receptors, 2-[(2-hydroxy-5-nitrophenyl)methylene]hydrazone (1) and 2-[(3,5-dibromo-2-hydroxyphenyl)methylene]hydrazone (2) with -OH binding sites, were synthesized and characterized. The anion binding ability of receptors 1 and 2 with halide anions (F-, Cl-, Br- and I-), AcO- and HPO4- was investigated using visual (naked-eye), UV-vis titration experiments in dry DMSO together with DFT theoretical calculation. The addition of F-, AcO- and HPO4- to the host solution resulted in a red shift of the charge-transfer absorbance band accompanied by a color change from yellow to orange in the naked-eye experiments. Receptor 1 containing a nitro group at the para position and receptor 2 containing two bromine groups at the ortho and para positions both showed strong binding ability for HPO4- ion in the form of phenol-hydrazone. Moreover, receptor 1, induced by anion species in the solution, converted to the form of phenol-hydrazone from keto-hydrazone.

  8. Spectral characterization and crystal structure of some 2,6-diarylthian-4-one hydrazone derivatives

    NASA Astrophysics Data System (ADS)

    Sankar, C.; Umamatheswari, S.; Pandiarajan, K.

    2014-11-01

    A series of cis and trans 2,6-diarylthian-4-one hydrazone derivatives (11-16) have been synthesized and characterized by 1H, 13C and two dimensional NMR spectroscopy. For the 2r,6t-diphenylthian-4-one N-isonicotinoylhydrazone (14) X-ray diffraction have also been recorded. The coupling constants suggested that the cis-hydrazones (11-13), which have the phenyl groups in cis orientation, largely exist in chair conformations with equatorial orientation of the phenyl groups 11C. Analysis of the vicinal coupling constants of trans-hydrazones (14-16) suggests that boat forms 14B must make significant contributions to it and the relative population is 58%. Moreover, in solution chair conformations 14C and 14C?, may contribute to 14. The NOESY and X-ray diffraction of 14 gives definite evidence for the contribution of 14C.

  9. Biliary iron excretion in rats following pyridoxal isonicotinoyl hydrazone.

    PubMed

    Cikrt, M; Ponka, P; Necas, E; Neuwirt, J

    1980-06-01

    Biliary excretion of iron after administration of pyridoxal isonicotinoyl hydrazone (PIH), a recently identified effective iron-chelating agent, was investigated in rats. PIH administered both intraperitoneally and orally was shown to increase significantly 59Fe excretion into bile of rats which had previously been injected with 59Fe-transferrin to label hepatic parenchymal cells. 59Fe-PIH appears in bile as early as 15 min after chelator administration and the peak of 59Fe-radioactivity in bile is seen 1--5 h following intraperitoneal PIH injection. PIH, administered intraperitoneally, 125--250 mg/kg, increased 24 h biliary radioiron excretion about 35 times and in addition increased urinary and faecal iron excretion. When PIH was given immediately before 59Fe-transferrin, 24 h cumulative biliary 59Fe excretion was even higher. PIH was also demonstrated to increase biliary excretion of radioiron released from 59Fe-haemoglobin catabolysed in reticuloendothelial cells. The effect of PIH was confirmed by estimation of biliary iron concentration using the method of atomic absorption spectrophotometry. Repeated PIH administration to rats decreased 59Fe radioactivity in liver and kidney and increased urinary and faecal iron excretion. PMID:7437326

  10. Synthesis and biological evaluation of hydrazone derivatives as antifungal agents.

    PubMed

    Casanova, Bruna B; Muniz, Mauro N; de Oliveira, Thayse; de Oliveira, Luís Flavio; Machado, Michel M; Fuentefria, Alexandre M; Gosmann, Grace; Gnoatto, Simone C B

    2015-01-01

    Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae) and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs) of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a) and tert-butyl-(2Z)-2-(3,4,5-trihydroxybenzylidine)hydrazine carboxylate (7b) showed the most promising MIC values in the range of 16-32 ?g/mL and 8-16 ?g/mL, respectively. The compounds' action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents. PMID:26007181

  11. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food...1242e Levamisole hydrochloride effervescent tablets. (a) Specifications. Each tablet contains 907 milligrams of levamisole...

  12. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

  13. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

  14. 21 CFR 520.863 - Ethylisobutrazine hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 false Ethylisobutrazine hydrochloride tablets. 520.863 Section 520.863 Food and...520.863 Ethylisobutrazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 50...

  15. 21 CFR 520.2582 - Triflupromazine hydrochloride tablets.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 false Triflupromazine hydrochloride tablets. 520.2582 Section 520.2582 Food and...520.2582 Triflupromazine hydrochloride tablets. (a) Specifications. Each tablet contains either 10 milligrams or 25...

  16. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 2011-04-01 false Naltrexone hydrochloride injection. 522.1465 Section 522.1465 Food and Drugs ...NEW ANIMAL DRUGS § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of...

  17. 21 CFR 522.1465 - Naltrexone hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 2010-04-01 false Naltrexone hydrochloride injection. 522.1465 Section 522.1465 Food and Drugs ...NEW ANIMAL DRUGS § 522.1465 Naltrexone hydrochloride injection. (a) Specifications. Each milliliter of...

  18. 21 CFR 522.863 - Ethylisobutrazine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 2011-04-01 false Ethylisobutrazine hydrochloride injection. 522.863 Section 522.863 Food and Drugs FOOD...ANIMAL DRUGS § 522.863 Ethylisobutrazine hydrochloride injection. (a) Specifications. The drug is a sterile...

  19. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 2011-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD...NEW ANIMAL DRUGS § 522.536 Detomidine hydrochloride injection. (a) Specification. Each milliliter of sterile...

  20. 21 CFR 522.2615 - Tripelennamine hydrochloride injection.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 2011-04-01 false Tripelennamine hydrochloride injection. 522.2615 Section 522.2615 Food and Drugs ...ANIMAL DRUGS § 522.2615 Tripelennamine hydrochloride injection. (a) Specifications. Each milliliter of...

  1. 21 CFR 522.536 - Detomidine hydrochloride injection.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 2010-04-01 false Detomidine hydrochloride injection. 522.536 Section 522.536 Food and Drugs FOOD...NEW ANIMAL DRUGS § 522.536 Detomidine hydrochloride injection. (a) Specification. Each milliliter of sterile...

  2. Epinastine hydrochloride for atopic disease.

    PubMed

    Fraunfelder, Frederick W

    2004-08-01

    Atopic conditions include allergic rhinitis, atopic eczema, allergic conjunctivitis and asthma. Doctors and patients can choose from a variety of antiallergy medications, testifying that no one medication will suffice to treat all symptoms and that each has a different side-effect profile. Antiallergy medications target histamine receptors, as histamine release contributes to the unpleasant symptoms of itching, tearing, runny nose and skin urticaria. The ideal antihistamine would control the symptoms of atopic disease but cause very few side effects. Traditionally, unwanted effects include drowsiness and somnolence due to CNS depression, and digestive tract problems such as loss of appetite, nausea, vomiting and constipation or diarrhea. Some antihistamines also have anticholinergic effects that are mediated by muscarinic receptors. These atropine-like actions, which can affect the cardiovascular system, are sufficiently prominent in some drugs to be manifest during clinical usage. Epinastine hydrochloride minimally penetrates the blood/brain barrier and has almost no effect on the muscarinic receptors. This drug is marketed as having very few CNS-depressant side effects, few drug interactions and gastrointestinal side effects, and a low risk of cardiotoxicity. PMID:15510239

  3. Tridentate hydrazone metal complexes derived from cephalexin and 2-hydrazinopyridine: synthesis, characterization and antibacterial activity.

    PubMed

    Anacona, J R; Rincones, Maria

    2015-04-15

    Metal(II) coordination compounds of a tridentate hydrazone ligand (HL) derived from the condensation of cephalexin antibiotic with 2-hydrazinopyridine were synthesized. The hydrazone ligand and mononuclear [ML(OAc)(H2O)] (M(II)=Mn, Co, Ni, Cu, Zn, Ag) complexes were characterized by several techniques, including elemental and thermal analysis, molar conductance and magnetic susceptibility measurements, electronic, FT-IR, EPR and (1)H NMR spectral studies. The cephalexin 2-pyridinylhydrazone ligand HL behaves as a monoanionic tridentate NNO chelating agent. The biological applications of complexes have been studied on three bacteria strains (Escherichia coli, Acinetobacter baumannii and Enterococcus faecalis) by agar diffusion disc method. PMID:25677531

  4. Immobilization of Coypus (Myocastor coypus) with Ketamine Hydrochloride and Xylazine Hydrochloride

    Microsoft Academic Search

    R. F. Bo; F. Palomares; J. F. Beltr; S. Moreno; Caeser Kleberg

    A combination of 100 mg\\/ml of ketamine hydrochloride (Ket) and 20 mg\\/ml of xylazine hydrochloride (Xyl) was used to im- mobilize coypus (Myocastor coypus). Eight ma- ture coypus (four males and four females) were injected intramuscularly with doses ranging from 2.33 to 6.25 mg\\/kg of KET and 0.25 to 0.86 mg\\/kg of Xyl. The mean (±SE) time for in- duction,

  5. Synthesis and larvicidal and adult topical activity of some hydrazide-hydrazone derivatives against Aedes aegypti

    Technology Transfer Automated Retrieval System (TEKTRAN)

    A series of novel hydrazide-hydrazone derivatives were synthesized and evaluated for their larvicidal and adult topical activity against Aedes aegypti. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1H-NMR, 13C-NMR and mass spectroscopy. Com...

  6. An emissive and pH switchable hydrazone-based hydrogel.

    PubMed

    Qian, Hai; Aprahamian, Ivan

    2015-06-30

    A serendipitous discovery has led to a new hydrazone-based low molecular weight fluorescent super-hydrogelator. The gelation and emission properties can be switched "ON" and "OFF" using pH, enabling the sensing of biogenic amines emanating from spoiled cod. PMID:25989245

  7. Iron chelation-afforded cardioprotection against chronic anthracycline cardiotoxicity: A study of salicylaldehyde isonicotinoyl hydrazone (SIH)

    Microsoft Academic Search

    Martin Št?rba; Olga Popelová; TomᚠŠim?nek; Yvona Mazurová; Anna Potá?ová; Michaela Adamcová; Ivana Gun?ová; Helena Kaiserová; Vladimír Pali?ka; P?emysl Po?ka; Vladimír Geršl

    2007-01-01

    Pyridoxal-derived aroylhydrazone iron chelators have been previously shown as effective cardioprotectants against chronic anthracycline cardiotoxicity. In this study we focused on a novel salicylaldehyde analogue (salicylaldehyde isonicotinoyl hydrazone, SIH), which has been recently demonstrated to possess marked and dose-dependent protective effects against oxidative injury of cardiomyocytes. Therefore, in the present study the cardioprotective potential of SIH against daunorubicin (DAU) cardiotoxicity

  8. 40 CFR 180.1280 - Poly(hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a tolerance.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a...hexamethylenebiguanide) hydrochloride (PHMB); exemption from the requirement of a...hexamethylenebiguanide) hydrochloride (PHMB)(CAS Reg. No....

  9. Comparison of Hydrazone Heterobifunctional Crosslinking Agents for Reversible Conjugation of Thiol-Containing Chemistry

    PubMed Central

    Christie, R. James; Anderson, Diana J.; Grainger, David W.

    2010-01-01

    Reversible covalent conjugation chemistries that allow site- and condition-specific coupling and uncoupling reactions are attractive components in nanotechnologies, bioconjugation methods, imaging and drug delivery systems. Here, we compare three heterobifunctional crosslinkers, containing both thiol- and amine- reactive chemistry, to form pH-labile hydrazones with hydrazide derivatives of the known and often published water-soluble polymer, poly[N-(2-hydroxypropyl methacrylamide)] (pHPMA), while subsequently coupling thiol-containing molecules to the crosslinker via maleimide addition. Two novel crosslinkers were prepared from the popular heterobifunctional crosslinking agent, succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (SMCC), modified to contain either terminal aldehyde groups (i.e., 1-(N-3-propanal)-4-(N-maleimidomethyl) cyclohexane carboxamide, PMCA) or methylketone groups (i.e., 1-(N-3-butanone)-4-(N-maleimidomethyl) cyclohexane carboxamide, BMCA). A third crosslinking agent was the commercially available N-4-acetylphenyl maleimide (APM). PMCA and BMCA exhibited excellent reactivity towards hydrazide-derivatized pHPMA with essentially complete hydrazone conjugation to polymer reactive sites, while APM coupled only ~ 60% of available reactive sites on the polymer despite a 3-fold molar excess relative to polymer hydrazide groups. All polymer hydrazone conjugates bearing these bifunctional agents were then further reacted with thiol-modified tetramethylrhodamine dye, confirming crosslinker maleimide reactivity after initial hydrazone polymer conjugation. Incubation of dye-labeled polymer conjugates in phosphate buffered saline at 37°C showed that hydrazone coupling resulting from APM exhibited the greatest difference in stability between pH 7.4 and 5.0, with hydrolysis and dye release increased at pH 5.0 over a 24hr incubation period. Polymer conjugates bearing hydrazones formed from crosslinker BMCA exhibited intermediate stability with hydrolysis much greater at pH 5.0 at early time points, but hydrolysis at pH 7.4 was significant after 5 hrs. Hydrazones formed with the PMCA crosslinker showed no difference in release rates at pH 7.4 and 5.0. PMID:20695431

  10. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...is intended for oral administration to dogs as a tranquilizer. It is used as an...handling difficult, excited, and unruly dogs, and in controlling excessive kennel...hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the...

  11. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ...is intended for oral administration to dogs as a tranquilizer. It is used as an...handling difficult, excited, and unruly dogs, and in controlling excessive kennel...hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the...

  12. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...is intended for oral administration to dogs as a tranquilizer. It is used as an...handling difficult, excited, and unruly dogs, and in controlling excessive kennel...hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the...

  13. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ...is intended for oral administration to dogs as a tranquilizer. It is used as an...handling difficult, excited, and unruly dogs, and in controlling excessive kennel...hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the...

  14. 21 CFR 520.2002 - Propiopromazine hydrochloride.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ...is intended for oral administration to dogs as a tranquilizer. It is used as an...handling difficult, excited, and unruly dogs, and in controlling excessive kennel...hydrochloride. Overdosage may produce significant depression. (3) For use only by or on the...

  15. Quality assessment of morphine hydrochloride solutions.

    PubMed

    P?otkowiak, Zyta; Popielarz-Brzezi?ska, Maria; Luczak, Jacek; Kluziak, Maciej

    2004-01-01

    The therapeutic substances in solution prepared in pharmaceutical laboratories (prescribed drugs) must preserve their activity. Therefore, they must be stable throughout the period of storage in home conditions. The maintenance of stability is particularly difficult for morphine hydrochloride solutions administered orally to cancer patients at the last stage of the disease being at home. This study, aiming at the assessment of stability of morphine hydrochloride solutions, was performed on samples of 0.5% water solutions of the drug alone, 0.25% and 0.5% solutions of the drug in water with chloroform as well as injection solutions (Morphinum hydrochloricum, 20 mg, Polfa Warsaw). All the samples were kept at 20 degrees C for six months. Throughout this time observations were made to detect changes in their appearence and pH values. Their qualitative composition was determined by TLC and the content of morphine was checked by UV spectrophotometry in an environment of 0.1 mol/l of hydrochloric acid at 285 nm. Results of the kinetic study permitted drawing conclusions as to the mechanism of the decomposition of morphine hydrochloride in the solutions studied - according to a simple first order reaction and determination of the rate constants (k, s(-1)) of the process. Results of the chromatographic and spectrophotometric study did not show differences in the stability of water and chloroform/water solutions of morphine hydrochloride studied after 4 weeks and 6 months. After that time the decrease of morphine content was 10 and 25%, respectively. PMID:15493291

  16. The use of a versatile o-vanilloyl hydrazone ligand to prepare SMM-like Dy3 molecular cluster pair.

    PubMed

    Xue, Shufang; Zhao, Lang; Guo, Yun-Nan; Zhang, Peng; Tang, Jinkui

    2012-09-14

    A novel lanthanide molecular cluster pair (MCP), displaying single molecule magnet behaviour, was assembled using the novel o-vanilloyl hydrazone ligand, versatile in terms of denticity, tautomerism and the rotatable C-C bond. PMID:22842673

  17. 40 CFR 721.6196 - Hydrochloride salt of a fatty polyalkkylene polyamine (generic).

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... 2013-07-01 false Hydrochloride salt of a fatty polyalkkylene polyamine (generic...Substances § 721.6196 Hydrochloride salt of a fatty polyalkkylene polyamine (generic...identified generically as Hydrochloride salt of a fatty polyalkkylene...

  18. 75 FR 81617 - Determination That TRANDATE (Labetalol Hydrochloride) Tablets, 300 Milligrams and 400 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-12-28

    ...That TRANDATE (Labetalol Hydrochloride) Tablets, 300 Milligrams and 400 Milligrams...that TRANDATE (labetalol hydrochloride) tablets, 300 milligrams (mg) and 400 mg, were...TRANDATE (labetalol hydrochloride) tablets, 300 mg and 400 mg, are the...

  19. 75 FR 64310 - Determination That BUSPAR (Buspirone Hydrochloride) Tablets, 10 Milligrams, 15 Milligrams, and 30...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-10-19

    ...That BUSPAR (Buspirone Hydrochloride) Tablets, 10 Milligrams, 15 Milligrams, and...that BUSPAR (buspirone hydrochloride) Tablets, 10 milligrams (mg), 15 mg, and 30...drug. BUSPAR (buspirone hydrochloride) Tablets, 10 mg, 15 mg, and 30 mg, are...

  20. 77 FR 7583 - Determination That WILPO (phentermine hydrochloride) Tablets, 8 Milligrams, Was Not Withdrawn...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ...That WILPO (phentermine hydrochloride) Tablets, 8 Milligrams, Was Not Withdrawn From...that WILPO (phentermine hydrochloride) Tablets, 8 Milligrams (mg), was not withdrawn...ANDAs) for phentermine hydrochloride tablets, 8 mg, if all other legal and...

  1. Nalfurafine hydrochloride to treat pruritus: a review

    PubMed Central

    Inui, Shigeki

    2015-01-01

    Uremic pruritus has a great negative influence on quality of life in hemodialysis (HD) patients and, importantly, negatively affects mortality risk. Recently, nalfurafine hydrochloride, an opioid ?-selective agonist, has been officially approved for resistant pruritus in HD patients on the basis of a well-evidenced clinical trial in Japan. From clinical observation, it has been suggested that the upper neuron system plays a role in its pathogenesis. According to previous experimental results, using mice injected with opioids, dynorphin suppresses itch through binding ?-opioid receptors, suggesting that ?-opioid opioid receptor agonists act as potential therapeutic reagents for pruritus in HD patients. In Japan, a large-scale placebo-controlled study was performed to examine the efficacy and safety of oral nalfurafine hydrochloride for intractable pruritus in 337 HD patients. Two daily doses of 2.5 or 5 ?g nalfurafine or placebo were orally administered for 2 weeks, and clinical responses were analyzed. The results showed that the mean decrease in the visual analog scale for pruritus from baseline was 22 mm in the 5 ?g nalfurafine hydrochloride group (n=114) and 23 mm in the 2.5 ?g group (n=112). These reductions were statistically significant compared with 13 mm, which is the mean decrease of visual analog scale in the placebo group (n=111), demonstrating that nalfurafine is an effective and safe drug for uremic pruritus in HD patients. Moreover, another open-label trial (n=145) examining the long-term effect of 5 ?g oral nalfurafine revealed the maintenance of the antipruritic effect of nalfurafine for 52 weeks. In addition, on the basis of recent data showing ?-opioid receptor expression in the epidermis of atopic dermatitis and psoriasis, nalfurafine hydrochloride also can be potentially used for these two skin diseases. PMID:26005355

  2. Treatment of premature ejaculation with sertraline hydrochloride

    Microsoft Academic Search

    CG McMahon

    1998-01-01

    Purpose: To evaluate the efficacy of sertraline hydrochloride in the drug treatment of premature ejaculation (P.E.).Materials and Method: Forty-six normally potent men, aged 22 to 63 years (mean 42 years) with premature ejaculation were treated with oral sertraline in a dose ranging study. All men were either married or in a stable relationship. The mean ejaculatory interval was 1 minute

  3. LC-UV/MS methods for the analysis of prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone (BSIH) and its active chelator salicylaldehyde isonicotinoyl hydrazone (SIH).

    PubMed

    Bureš, Jan; Jansová, Hana; Stariat, Ján; Filipský, Tomáš; Mlad?nka, P?emysl; Šim?nek, Tomáš; Ku?era, Radim; Klimeš, Ji?í; Wang, Qin; Franz, Katherine J; Kova?íková, Petra

    2015-02-01

    Salicylaldehyde isonicotinoyl hydrazone (SIH) is an intracellular iron chelator with well documented potential to protect against oxidative injury both in vitro and in vivo. However, it suffers from short biological half-life caused by fast hydrolysis of the hydrazone bond. Recently, a concept of boronate prochelators has been introduced as a strategy that might overcome these limitations. This study presents two complementary analytical methods for detecting the prochelator-boronyl salicylaldehyde isonicotinoyl hydrazone-BSIH along with its active metal-binding chelator SIH in different solution matrices and concentration ranges. An LC-UV method for determination of BSIH and SIH in buffer and cell culture medium was validated over concentrations of 7-115 and 4-115 ?M, respectively, and applied to BSIH activation experiments in vitro. An LC-MS assay was validated for quantification of BSIH and SIH in plasma over the concentration range of 0.06-23 and 0.24-23 ?M, respectively, and applied to stability studies in plasma in vitro as well as analysis of plasma taken after i.v. administration of BSIH to rats. A Zorbax-RP bonus column and mobile phases containing either phosphate buffer with EDTA or ammonium formate and methanol/acetonitrile mixture provided suitable conditions for the LC-UV and LC-MS analysis, respectively. Samples were diluted or precipitated with methanol prior to analysis. These separative analytical techniques establish the first validated protocols to investigate BSIH activation by hydrogen peroxide in multiple matrices, directly compare the stabilities of the prochelator and its chelator in plasma, and provide the first basic pharmacokinetic data of this prochelator. Experiments reveal that BSIH is stable in all media tested and is partially converted to SIH by H2O2. The observed integrity of BSIH in plasma samples from the in vivo study suggests that the concept of prochelation might be a promising strategy for further development of aroylhydrazone cytoprotective agents. PMID:25527982

  4. Particle size distribution of cocaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Kuhlman, Michael R.; Gooding, Rachel E.; Kogan, Vladimir G.; Bridges, Curtis

    1997-02-01

    A principal method for the detection of concealed shipments of cocaine hydrochloride relies upon the intake of an air sample taken near a surface onto an analytical instrument, and the detection of the narcotic present in the air or surface materials collected. The low vapor pressure of cocaine at normal temperatures indicates that particulate material present on the surfaces of target packages affords a higher probability of collection of detectable mass than does a vapor sample. An accurate representation of the particles in question is required, both for theoretical sampler design and for the performance of meaningful tests of instrument capabilities. Existing test methods for target particle preparation call for use of sand particles ranging in size from 20 to 100 micrometers in diameter, coated with a solution of cocaine hydrochloride. In this study, three seized samples and pharmaceutical cocaine hydrochloride were analyzed using an Aerosizer to measure the size distribution of the air-dispersed particles. The results obtained during these tests indicate that the actual size range of the particles is significantly smaller than the test particles cited. Results obtained in instrument evaluations using the larger target particles may therefore be misleading.

  5. Anion induced azo-hydrazone tautomerism for the selective colorimetric sensing of fluoride ion

    NASA Astrophysics Data System (ADS)

    Satheshkumar, A.; El-Mossalamy, E. H.; Manivannan, R.; Parthiban, C.; Al-Harbi, L. M.; Kosa, S.; Elango, Kuppanagounder P.

    2014-07-01

    The design, synthesis, characterization and their anion sensing properties of two receptors capable of exhibiting azo-hydrazone tautomerism are reported. The anion sensing properties have been investigated using electronic, fluorescence and nuclear magnetic spectral studies in addition to electrochemical and visual detection experiments. Both the receptors selectively bind fluoride ion with >100 nm red-shift in the electronic spectrum and the color changes from yellow to red. The results of the spectral studies revealed that the sensing mechanism involves fluoride ion induced change of chromophore from Cdbnd N (hydrazone form) to Ndbnd N (azo form) in these receptors leading to the visible color change. Density Functional Theory calculations were conducted to rationalize the optical response of the receptors.

  6. Synthesis and biological activity evaluation of hydrazone derivatives based on a Tröger's base skeleton.

    PubMed

    Kaplánek, Robert; Havlík, Martin; Dolenský, Bohumil; Rak, Jakub; Džubák, Petr; Kone?ný, Petr; Hajdúch, Marián; Králová, Jarmila; Král, Vladimír

    2015-04-01

    We report the design and synthesis of novel anticancer agents based on bis-hydrazones separated by a rigid Tröger's base skeleton. This novel approach combines a biologically active moiety (hydrazone) with this scaffold (Tröger's base) to construct DNA intercalators. Evaluation of the anticancer activity of these agents using seven cancer cell lines and two healthy cell lines found that several derivatives had potent anticancer activity and excellent selectivity indexes toward cancer cells. The antimicrobial activities were tested on a set of thirteen bacterial stains, but the prepared compounds were not active. Complexation studies using biologically important metal ions demonstrated that these compounds are able to bind Cu(2+), Fe(3+), Co(2+), Ni(2+) and Zn(2+). DNA intercalation studies showed that the compounds themselves do not interact with DNA, but their metallocomplexes do interact, most likely via intercalation into DNA. PMID:25737088

  7. Caffeine-hydrazones as anticancer agents with pronounced selectivity toward T-lymphoblastic leukaemia cells.

    PubMed

    Kaplánek, Robert; Jakubek, Milan; Rak, Jakub; Kejík, Zden?k; Havlík, Martin; Dolenský, Bohumil; Frydrych, Ivo; Hajdúch, Marián; Kolá?, Milan; Bogdanová, Kate?ina; Králová, Jarmila; Džubák, Petr; Král, Vladimír

    2015-06-01

    We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and great selectivity index toward T-lymphoblastic leukaemia cells. In general, hydrazones bearing 2-N-heteroaryl moiety are more active and selective than those with 2-hydroxyaryl moiety. Tested compounds exhibit dose-dependent inhibition of both RNA and DNA synthesis, with some exceptions. Antimicrobial activities were tested on set of twelve bacterial and yeast strains, however prepared compounds were not active, suggesting for a molecular target specific for eukaryotic cells. PMID:25912310

  8. PEGylated polyamidoamine dendrimers with bis-aryl hydrazone linkages for enhanced gene delivery.

    PubMed

    Yuan, Quan; Yeudall, W Andrew; Yang, Hu

    2010-08-01

    Surface modification of polyamidoamine (PAMAM) dendrimers with polyethylene glycol (PEG) often results in the decrease in their buffering capacity, which is essential for gene transfer. In this work, bis-aryl hydrazone bond, which possesses protonatable pyridine and amines, was explored as a new linkage for PEGylation of PAMAM dendrimers. PEGylated polyamidoamine (PAMAM) dendrimer G4.0 conjugates with bis-aryl hydrazone (BAH) linkages were synthesized following a two-step procedure: activation of PAMAM dendrimer G4.0 and monofunctional methoxypolyethylene glycol amine (MW=5000 Da) with succinimidyl 4-hydrazinonicotinate acetone hydrazone (SANH) and succinimidyl 4-formylbenzoate (SFB), respectively, and coupling of SFB-activated PEG to SANH-activated G4.0 to generate PEGylated G4.0 with bis-aryl hydrazone linkages (G4.0-BAH-PEG). It was found that the incorporation of BAH linkages into the vector significantly enhanced the buffering capacity of the vector even with a high degree of PEGylation (42 PEG chains per dendrimer). G4.0-BAH-PEG conjugates could complex with DNA plasmid tightly at low weight ratios and display dramatically improved cytocompatibility. According to gene transfection studies in 293T and HN12 cells, this new vector has been shown to be capable of both transfecting more cells and inducing higher gene expression than the parent dendrimer. This work demonstrates that the use of the BAH linkage in coupling of PEG to the dendrimer helps maintain or increase the buffering capacity of the functionalized dendrimer and results in enhanced transfection. PMID:20593893

  9. The iron chelator pyridoxal isonicotinoyl hydrazone inhibits mitochondrial lipid peroxidation induced by Fe(II)–citrate

    Microsoft Academic Search

    Natacha C. F Santos; Roger F Castilho; André R Meinicke; Marcelo Hermes-Lima

    2001-01-01

    Pyridoxal isonicotinoyl hydrazone (PIH) is able to prevent iron-mediated hydroxyl radical formation by means of iron chelation and inhibition of redox cycling of the metal. In this study, we investigated the effect of PIH on Fe(II)–citrate-mediated lipid peroxidation and damage to isolated rat liver mitochondria. Lipid peroxidation was quantified by the production of thiobarbituric acid-reactive substances (TBARS) and by antimycin

  10. Design, synthesis, computational calculation and biological evaluation of some novel 2-thiazolyl hydrazones

    NASA Astrophysics Data System (ADS)

    Anbazhagan, R.; Sankaran, K. R.

    2015-01-01

    In the present study a novel series of 1-(1-(4-isobutylphenyl)ethylidene)-2-(4-phenylthiazol-2-yl)hydrazine 2a and its derivatives 2b-2f have been synthesized by the cyclization of 1-(1-(4-isobutylphenyl)ethylidene)thiosemicarbazide with 2-bromoacetophenone/ 4-substituted 2-bromoacetophenones. The structures of the synthesized thiazolyl hydrazones 2a-2f were characterized by FT-IR, 1H, 13C NMR, 2D NMR and mass spectral techniques. The molecular geometries were also investigated theoretically using B3LYP functional with 6-311G(d,p) basis set. To explain the molecular properties energy gap (Eg), electronegativity (?), hardness (g), electrophilicity (?) and softness (S) were computed, natural bonding orbital (NBO) analysis and molecular electrostatic potential (MEP) were also performed at the same level of theory. All the synthesized thiazolyl hydrazones 2a-2f were screened for their in vitro antimicrobial activity against selected bacterial and fungal strains. The results showed that the heterocyclic thiazolyl hydrazone derivatives exhibit a promising selective inhibitory activity against various bacterial and fungal strains.

  11. Effect of Ractopamine Hydrochloride and Zilpaterol Hydrochloride on tenderness of longissimus steaks of Bos Taurus steers

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Objectives: Three experiments were conducted to determine 1) the interaction of ractopamine hydrochloride (RH) inclusion rate (0 or 300 mg·hd-1·d-1 for last 30 to 34 d before harvest) and dietary protein level (13.5 or 17.5% CP) on LM slice shear force (SSF) at 14 d postmortem (Exp. 1); 2) the inter...

  12. 78 FR 34108 - Determination That SUBOXONE (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Sublingual...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-06-06

    ...and Naloxone Hydrochloride) Sublingual Tablets, 2 Milligrams/0.5 Milligrams and...HCl) and naloxone HCl) sublingual tablets, 2 milligrams (mg)/0.5 mg and 8...buprenorphine HCl and naloxone HCl sublingual tablets, 2 mg/0.5 mg and 8 mg/2 mg,...

  13. Swelling Behavior of Hyaluronic Acid/Polyallylamine Hydrochloride Multilayer Films

    E-print Network

    Barrett, Christopher

    Swelling Behavior of Hyaluronic Acid/Polyallylamine Hydrochloride Multilayer Films Susan E. Burke The reversible swelling behavior of multilayer films containing hyaluronic acid and polyallylamine hydrochloride filtration.19-22 Hyaluronic acid (HA) is a linear polysaccharide composed of repeating disaccharide units

  14. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)].

    PubMed

    Fujii, Y; Ishii, Y; Suzuki, T; Murayama, S

    1979-10-01

    Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone. PMID:232053

  15. Enantiotropically related polymorphs of gaboxadol hydrochloride.

    PubMed

    Lopez de Diego, Heidi; Koradia, Vishal; Bond, Andrew D

    2013-11-01

    Gaboxadol hydrochloride, also known as THIP hydrochloride (systematic name: 3-hydroxy-4,5,6,7-tetrahydro-1,2-oxazolo[5,4-c]pyridin-6-ium chloride), C6H9N2O2(+)·Cl(-), exists as two enantiotropically related polymorphs. Transformation between the polymorphs occurs in a single-crystal-to-single-crystal manner at 221?K, and the enthalpy of transformation from the high-temperature form to the low-temperature form is -0.7?kJ?mol(-1). Single-crystal structures have been determined at 298 and 220?K. At 298?K, the structure is triclinic (space group P overline 1), with two formula units in the crystallographic asymmetric unit. At 220?K, the structure is monoclinic (space group I2/a), with one formula unit in the asymmetric unit. The structures contain identical hydrogen-bonded layers and the transformation between the polymorphs corresponds to a shift of adjacent layers relative to each other. The transformation is shown to be reversible by differential scanning calorimetry and variable-temperature powder X-ray diffraction. PMID:24192165

  16. A Highly Efficient Catalyst for Oxime Ligation and Hydrazone-Oxime Exchange Suitable for Bioconjugation

    PubMed Central

    Rashidian, Mohammad; Mahmoodi, Mohammad M.; Shah, Rachit; Dozier, Jonathan K.; Wagner, Carston R.; Distefano, Mark D.

    2014-01-01

    Imine-based reactions are useful for a wide range of bioconjugation applications. Although aniline is known to catalyze the oxime ligation reaction under physiological conditions, it suffers from slow reaction kinetics, specifically when a ketone is being used or when hydrazone-oxime exchange is performed. Here, we report on the discovery of a new catalyst that is up to 15 times more efficient than aniline. That catalyst, m-phenylenediamine (mPDA), was initially used to analyze the kinetics of oxime ligation on aldehyde- and ketone-containing small molecules. While mPDA is only modestly more effective than aniline when used in equal concentrations (~ 2-fold), its much greater aqueous solubility relative to aniline allows it to be used at higher concentrations, resulting in significantly more efficient catalysis. In the context of protein labeling, it was first used to site-specifically label an aldehyde-functionalized protein through oxime ligation, and its kinetics were compared to reaction with aniline. Next, a protein was labeled with an aldehyde-containing substrate in crude cell lysate, captured with hydrazide-functionalized beads and then the kinetics of immobilized protein release via hydrazone-oxime exchange were analyzed. Our results show that mPDA can release and label 15 times more protein than aniline can in 3 h. Then, using the new catalyst, ciliary neurotrophic factor, a protein with therapeutic potential, was successfully labeled with a fluorophore in only 5 min. Finally, a protein containing the unnatural amino acid, p-acetyl phenylalanine, a ketone-containing residue, was prepared and PEGylated efficiently via oxime ligation using mPDA. This new catalyst should have a significant impact on the field of bioconjugation, where oxime ligation and hydrazone-oxime exchange are commonly employed. PMID:23425124

  17. A highly efficient catalyst for oxime ligation and hydrazone-oxime exchange suitable for bioconjugation.

    PubMed

    Rashidian, Mohammad; Mahmoodi, Mohammad M; Shah, Rachit; Dozier, Jonathan K; Wagner, Carston R; Distefano, Mark D

    2013-03-20

    Imine-based reactions are useful for a wide range of bioconjugation applications. Although aniline is known to catalyze the oxime ligation reaction under physiological conditions, it suffers from slow reaction kinetics, specifically when a ketone is being used or when hydrazone-oxime exchange is performed. Here, we report on the discovery of a new catalyst that is up to 15 times more efficient than aniline. That catalyst, m-phenylenediamine (mPDA), was initially used to analyze the kinetics of oxime ligation on aldehyde- and ketone-containing small molecules. While mPDA is only modestly more effective than aniline when used in equal concentrations (~2-fold), its much greater aqueous solubility relative to aniline allows it to be used at higher concentrations, resulting in significantly more efficient catalysis. In the context of protein labeling, it was first used to site-specifically label an aldehyde-functionalized protein through oxime ligation, and its kinetics were compared to reaction with aniline. Next, a protein was labeled with an aldehyde-containing substrate in crude cell lysate, captured with hydrazide-functionalized beads and then the kinetics of immobilized protein release via hydrazone-oxime exchange were analyzed. Our results show that mPDA can release and label 15 times more protein than aniline can in 3 h. Then, using the new catalyst, ciliary neurotrophic factor, a protein with therapeutic potential, was successfully labeled with a fluorophore in only 5 min. Finally, a protein containing the unnatural amino acid, p-acetyl phenylalanine, a ketone-containing residue, was prepared and PEGylated efficiently via oxime ligation using mPDA. This new catalyst should have a significant impact on the field of bioconjugation, where oxime ligation and hydrazone-oxime exchange are commonly employed. PMID:23425124

  18. Immobilization of coypus (Myocastor coypus) with ketamine hydrochloride and xylazine hydrochloride.

    PubMed

    Bo, R F; Palomares, F; Beltrán, J F; de Villafañe, G; Moreno, S

    1994-10-01

    A combination of 100 mg/ml of ketamine hydrochloride (Ket) and 20 mg/ml of xylazine hydrochloride (Xyl) was used to immobilize coypus (Myocastor coypus). Eight mature coypus (four males and four females) were injected intramuscularly with doses ranging from 2.33 to 6.25 mg/kg of KET and 0.25 to 0.86 mg/kg of Xyl. The mean (+/- SE) time for induction, arousal, and recovery were 7.3 +/- 2 min, 23.5 +/- 0.3 min and 46 +/- 2.5 min, respectively. The mean +/- SE doses injected were 4.07 +/- 0.52 mg/kg Ket (range, 2.33 to 6.25 mg/kg) and 0.5 +/- 0.08 mg/kg Xyl (range, 0.25 to 0.86 mg/kg). No adverse responses were observed in any of the animals treated. PMID:7760499

  19. Immobilization of fishers (Martes pennanti) with ketamine hydrochloride and xylazine hydrochloride.

    PubMed

    Belant, J L

    1991-04-01

    A combination of 100 mg ketamine hydrochloride (KH) and 20 mg xylazine hydrochloride (XH) was used to immobilize fishers (Martes pennanti). Four adult males were intramuscularly injected a total of five times at dosages between 22.4 to 29.0 mg/kg KH and 4.1 to 6.6 mg/kg XH. Mean (+/- SE) induction time and arousal time were 3.3 +/- 0.5 min and 76.8 +/- 12.1 min, respectively. Respiration, heart rate, and body temperature in response to sedation appeared normal. A 5:1 mixture of KH-XH appears to be a safe immobilizing agent for fishers. PMID:2067055

  20. Cocrystals of bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride

    Microsoft Academic Search

    Z. Dega-Szafran; E. Dulewicz; G. Dutkiewicz; Z. Kosturkiewicz

    2006-01-01

    Bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride, [bis(1-carboxymethyl-4-hydroxy-1-methylpiperidinium) hydrochloride, (HO–MPB)2HCl], has been prepared from stoichiometric amounts of ?-4-hydroxy-1-methylpiperidine betaine hydrochloride with the OH group in an equatorial position and ?-4-hydroxy-1-methylpiperidine betaine inner salt with the OH group in an axial one. Cocrystals of (HO–MPB)2HCl belong to monoclinic system with C2\\/c space group. Piperidinium ring has a chair conformation with the CH2COO group in the

  1. [Colorimetric determination of sulfite in "kanpyo" (dried gourd shavings) and "konnyakuseiko" (devil's-tongue fine powder) using sulfite oxidase and catalase].

    PubMed

    Aoki, Kazuko; Ueno, Seiichi; Ishizaki, Mutsuo

    2002-06-01

    A simple and convenient method for colorimetric determination of sulfite in foods based on its conversion to formaldehyde with sulfite oxidase and catalase was developed. Sulfite in a sample was extracted with water and then diluted with methanol. One mL of sample solution containing about 5-10 micrograms of sulfite was taken into a test tube with a ground-glass stopper, and 3 mL of 0.04 mol/L borate buffer (pH 8.7), 1 mL of 0.4% 3-methyl-2-benzothiazolinone hydrazone (MBTH) solution, 2,000 units of catalase solution and 1.0 units of sulfite oxidase were added. The mixture was incubated for 35 minutes at 37 degrees C. Then 0.15 mL of 1 mol/L hydrochloric acid and 5 mL of 0.2% iron(III) nitrate solution were added. The reaction mixture was transferred to a measuring flask after standing for 5 minutes at room temperature, and diluted to 20 mL with methanol. The absorbance of this solution was measured using a spectrophotometer at the wavelength of 635 nm. The calibration curve prepared with sodium sulfite showed linearity between 0 to 16 micrograms/mL as sulfur dioxide. The recoveries of sulfite in "Kanpyo" (dried gourd shavings) and "Konnyaku-seiko" (devil's-tongue fine powder) by the proposed method were 97-104%, and the coefficients of variation were below 6%. The sulfite values in these foods determined by the proposed method were reasonably consistent with those obtained by the bubbling distillation-alkaline titration method. PMID:12238155

  2. Iron(III)-Mediated Radical Nitration of Bisarylsulfonyl Hydrazones: Synthesis of Bisarylnitromethyl Sulfones.

    PubMed

    Sar, Dinabandhu; Bag, Raghunath; Bhattacharjee, Debajyoti; Deka, Ramesh Chandra; Punniyamurthy, Tharmalingam

    2015-07-01

    Iron(III)-mediated radical nitration of bisarylsulfonyl hydrazones is described. In this protocol, the nontoxic and inexpensive Fe(NO3)3·9H2O plays a dual role as catalyst as well as nitro source. The mild conditions, broad substrate scope, and the functional group compatibility are the significant features. The reaction pathway has been demonstrated using DFT calculations, and the products can be subsequently converted into oximes using SnCl2·2H2O in high yields. PMID:26036359

  3. Synthesis of 2,4,6-trichlorophenyl hydrazones and their inhibitory potential against glycation of protein.

    PubMed

    Khan, Khalid Mohammed; Shah, Zarbad; Ahmad, Viqar Uddin; Khan, Momin; Taha, Muhammad; Rahim, Fazal; Jahan, Humera; Perveen, Shahnaz; Choudhary, M Iqbal

    2011-11-01

    2,4,6-Trichlorophenyl hydrazones 1-35 were synthesized and their in vitro antiglycation potential was evaluated. Compounds 14 (IC50 = 27.2 ± 0.00 ?M), and 18 (IC50 = 55.7 ± 0.00 ?M) showed an excellent activity against glycation of protein, better than the standard (rutin, IC50 = 70 ± 0.50 ?M). This study thus identified a novel series of antiglycation agents. A structure-activity relationship has been studied, and all the compounds were characterized by spectroscopic techniques. PMID:22313297

  4. Spectroscopy study of ephedrine hydrochloride and papaverine hydrochloride in terahertz range

    NASA Astrophysics Data System (ADS)

    Deng, Fusheng; Shen, Jingling; Wang, Guangqin; Liang, Meiyan

    2008-12-01

    The terahertz(THz) fingerprint spectra of Ephedrine Hydrochloride and Papaverine Hydrochloride have been measured using THz time-domain Spectroscopy (THz-TDS) system in the region of 0.2~2.6 THz. To explain the spectra, both gas-phase simulation methods and solid-state simulation methods were performed in the efforts to extract pictures of the molecular interior vibrational modes. By comparing the results of various gas-phase simulation methods, It was found that using the semi-empirical theory is more applicable than the density functional theory (DFT) for some chemical compounds. In the solid-state calculations, solid-state density functional theory (DFT) was employed to obtain the vibration frequencies and Difference-Dipole Method (DDM) was used to calculate the corresponding infrared (IR) intensity. In the process of calculating the IR intensity of Papaverine Hydrochloride in terahertz range, we found that the results by Hirshfeld partitioning method agree better with the experiments than the ones derived from Mulliken atomic charges. Moreover, the accuracy of simulation results depends on the basis sets and grid size being chosen.

  5. Stability of Revex, nalmefene hydrochloride injection.

    PubMed

    Brittain, H G; Lafferty, L; Bousserski, P; Diegnan, G; Lessor, R; Small, C; Pejaver, S

    1996-01-01

    The stability of Revex, nalmefene hydrochloride injection, has been studied at several temperatures for periods up to 36 months. The data were obtained using a HPLC method for the potency determination, and for the level of the sole degradation product (2,2'-bisnalmefene). These methods were found to be characterized by excellent precision, linearity, and accuracy over the analyte concentration ranges established. The stability data were found to be interpretable using first-order kinetics, and essentially comparable rate constants were calculated for both the potency loss and the formation of 2,2'-bisnalmefene. Applying the Arrhenius equation to these data, a rate constant of 0.00441 month-1 was deduced for the reactions taking place at 25 degrees C. This low value is consistent with the excellent stability exhibited by the product, and amply justifies its shelf life. PMID:8846056

  6. Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial

    Microsoft Academic Search

    B. Montes; M. Catalan; A. Roces; J. P. Jeanniot; J. M. Honorato

    1993-01-01

    The absolute bioavailability of fenspiride has been studied in twelve healthy volunteers. It was administered IV and orally in single doses of 80 mg fenspiride hydrochloride according to a randomised crossover pattern.

  7. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the order of a...

  8. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the order of a...

  9. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the order of a...

  10. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E. coli and urinary tract infections due to Staphylococcus spp. and E. coli. (3) Limitations. Federal law restricts this drug to use by or on the order of a licensed...

  11. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ...to tetracycline hydrochloride, such as bacterial gastroenteritis due to E . coli and urinary tract infections due to Staphylococcus spp. and E. coli . (3) Limitations . Federal law restricts this drug to use by or on the order of a...

  12. Stability of morphine hydrochloride in a portable pump reservoir

    Microsoft Academic Search

    P. J. Roos; J. H. Glerum; J. W. Meilink

    1992-01-01

    The stability of morphine hydrochloride in an admixture with sodium chloride 0.9% injection in a portable pump reservoir was investigated. Duplicate samples containing morphine hydrochloride 0.5, 1.5 and 2.5 mg\\/ml were stored in original 100 ml plastic drug reservoirs at 32 °C for 60 days. An amount of 3 ml was removed immediately after preparation and at fixed intervals in

  13. Synthesis of Naphthalenes through Three-Component Coupling of Alkynes, Fischer Carbene Complexes, and Benzaldehyde Hydrazones via Isoindole Intermediates

    PubMed Central

    Duan, Shaofeng; Sinha-Mahapatra, Dilip K.; Herndon, James W.

    2008-01-01

    The synthesis of naphthalene derivatives through three-component coupling of 2-alkynylbenzaldehyde hydrazones with carbene complexes and electron-deficient alkynes has been examined. The reaction involves formation of an isoindole derivative, followed by intramolecular Diels–Alder reaction, followed by nitrene extrusion. The reaction was highly regioselective using unsymmetrical alkynes. PMID:18351767

  14. SOLID-STATE SYNTHESIS OF HETEROCYCLIC HYDRAZONES USING MICROWAVES UNDER CATALYST-FREE CONDITIONS: JOURNAL ARTICLE (1605)

    EPA Science Inventory

    NRMRL-CIN-1605 Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. Solid-State Synthesis of Heterocyclic Hydrazones using Microwaves under Catalyst-free Conditions. Green Chemistry (White, J.D. (Ed.), Cambridge, United Kingdom: Royal Society of Chemistry) (4):35-38 (2002). ...

  15. 2078 J. Am. Chem. SOC.1985, 107, 2078-2082 On the Origin of the Stereoselectivity of Hydrazone

    E-print Network

    Collum, David B.

    2078 J. Am. Chem. SOC.1985, 107, 2078-2082 On the Origin of the Stereoselectivity of Hydrazone. Chem. 1973, 38, 1000. (c) Howe, R.; McQuillin, F. J. J. Chem. SOC.1958, 1194. (d) Kuwajima, I.; Nakamura, E. J. Am. Chem. SOC.1975, 97, 3257. (e) Djerassi, C.; Osiecki, J.; Eisenbraun, E. J. J. Am. Chem

  16. Novel colorimetric sensors for cyanide based on azo-hydrazone tautomeric skeletons

    NASA Astrophysics Data System (ADS)

    Adegoke, Olajire A.; Adesuji, Temitope E.; Thomas, Olusegun E.

    2014-07-01

    The monoazo dyes, 4-carboxyl-2, 6-dinitrophenylazohydroxynaphthalenes dyes (AZ-01, AZ-03 and AZ-04), were evaluated as a highly selective colorimetric chemosensor for cyanide ion. The recognition of cyanide ion gave an obvious colour change from light yellow to brownish red and upon dilution with acetone produced a purple to lilac colour. Optimum conditions for the reaction between the azo dyes and cyanide ion were established at 30 °C for 5 min, and different variables affecting the reaction were carefully studied and optimised. Under the optimum conditions, linear relationships between the CN- concentrations and light absorption were established. Using these azo-hydrazone molecular switch entities, excellent selectivity towards the detection of CN- in aqueous solution over miscellaneous competitive anions was observed. Such selectivity mainly results from the possibility of nucleophilic attack on the azo-hydrazone chemosensors by cyanide anions in aqueous system, which is not afforded by other competing anions. The cyanide chemosensor method described here should have potential application as a new family probes for detecting cyanide in aqueous solution.

  17. Vibrational spectroscopic studies and computational study of quinoline-2-carbaldehyde benzoyl hydrazone

    NASA Astrophysics Data System (ADS)

    Sheeja, S. R.; Mangalam, Neema Ani; Prathapachandra Kurup, M. R.; Sheena Mary, Y.; Raju, K.; Varghese, Hema Tresa; Panicker, C. Yohannan

    2010-06-01

    FT-IR spectrum of quinoline-2-carbaldehyde benzoyl hydrazone (HQb··H 2O) was recorded and analyzed. The synthesis and crystal structure data are also described. The vibrational wavenumbers were examined theoretically using the Gaussian03 package of programs using HF/6-31G(d) and B3LYP/6-31G(d) levels of theory. The data obtained from vibrational wavenumber calculations are used to assign vibrational bands obtained in infrared spectroscopy of the studied molecule. The first hyperpolarizability, infrared intensities and Raman activities are reported. The calculated first hyperpolarizability is comparable with the reported values of similar derivatives and is an attractive object for future studies of non-linear optics. The geometrical parameters of the title compound obtained from XRD studies are in agreement with the calculated values. The changes in the C sbnd N bond lengths suggest an extended ?-electron delocalization over quinoline and hydrazone moieties which is responsible for the non-linearity of the molecule.

  18. Vanadium Complexes with Hydrazone or Thiosemicarbazone Ligands as Potential Anti-Mycobacterium tuberculosis Agents.

    PubMed

    de Souza, Paula C; Maia, Pedro I S; de Barros, Heloisa B; Leite, Clarice Q F; Deflon, Victor M; Pavan, Fernando R

    2015-01-01

    Tuberculosis (TB) is an infectious disease caused mainly by Mycobacterium tuberculosis (MTB) and still an important public health problem worldwide. Some factors like the emergence of multidrug resistant (MDR) and extensively drug-resistant (XDR) strains make urgent the research of new active compounds. Searching for new inorganic compounds against TB, three new dioxovanadium(V) complexes were obtained upon reaction of [VO(acac)2] with hydrazone and thiosemicarbazone ligands derived from di-2-pyridyl ketone. Spectroscopic studies and X-ray crystallography revealed asymmetrically oxo bridged binuclear complexes of the type [{VO(L(1,2))}2(?-O)2], involving the hydrazone ligands, while a mononuclear square pyramidal complex of the type [VO2(L(3))] was formed with the thiosemicarbazone ligand. The compounds were tested against M. tuberculosis and three of them, with MICs values between 2.00 and 3.76 ?M were considered promising for TB treatment. Such MIC values are comparable or better than those found for some drugs currently used in TB treatment. PMID:24433444

  19. Synthesis, characterization and modeling structures of isatin-3-Girard T (IGT) and P (IGP) hydrazone complexes.

    PubMed

    Salah, Sabah; El-Wahab, Zeinab H Abd; Farag, Rabei S; Mostafa, Mohsen M

    2014-04-24

    The reactions of isatin Girard's T hydrazone, N,N,N-trimethyl-2-oxo-2[(2z)-2-(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazino]ethan ammonium chloride (IGT) and isatin Girard's P hydrazone, 1-{2-oxo-2-[(2z)(2-oxo-1,2-dihydro-3H-indole-3-ylidene)hydrazine]ethyl} pyridinium chloride (IGP), with Fe(3+), Al(3+), Sb(3+) and Sn(2+) salts afford different types of complexes. The isolated solid complexes were characterized by elemental analyses, molar conductance, spectral (IR, UV-Vis, (1)H NMR, mass), magnetic moment and thermal measurements. The results suggest that all the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectral data suggest that the ligands coordinate in a tridentate manner via the two carbonyl of both isatin and Girard's and the azomethine (C=N) groups. The amounts of solvents inside and outside the coordination sphere were determined using thermal data (TGA) and weight loss method. The octahedral geometry of the complexes is confirmed using DFT method from DMOL(3) calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi. PMID:24509535

  20. 77 FR 7581 - Determination That KAPVAY (Clonidine Hydrochloride) Extended-Release Tablets, 0.2 Milligram, Was...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ...Clonidine Hydrochloride) Extended- Release Tablets, 0.2 Milligram, Was Not Withdrawn...clonidine hydrochloride) Extended-Release Tablets, 0.2 milligram (mg), was not withdrawn...clonidine hydrochloride extended- release tablets, 0.2 mg, if all other...

  1. Potassium N-Iodo p-Toluenesulfonamide (TsNIK, Iodamine-T): A New Reagent for the Oxidation of Hydrazones to Diazo Compounds

    PubMed Central

    Nicolle, Simon M; Moody, Christopher J

    2014-01-01

    A new reagent for the oxidation of hydrazones to diazo compounds is described. N-Iodo p-toluenesulfonamide (TsNIK, iodamine-T) allows the preparation of ?-diazoesters, ?-diazoamides, ?-diazoketones and ?-diazophosphonates in good yield and in high purity after a simple extractive work-up. ?-Diazoesters were also obtained in high yield from the corresponding ketones through a one-pot process of hydrazone formation/oxidation. PMID:24615944

  2. Characterisation of the conjugate of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin with lactosaminated human albumin by 13C NMR spectroscopy

    Microsoft Academic Search

    Carla Boga; Luigi Fiume; Michele Baglioni; Carlo Bertucci; Claudio Farina; Felix Kratz; Marcella Manerba; Marina Naldi; Giuseppina Di Stefano

    2009-01-01

    In order to improve the efficacy of doxorubicin (DOXO) in the treatment of hepatocellular carcinomas, the drug was conjugated with lactosaminated human albumin (L-HSA), a hepatotropic drug carrier. Conjugation was performed using the (6-maleimidocaproyl)hydrazone derivative of the drug (DOXO-EMCH). The maleimide group of DOXO-EMCH reacts with the aminoacidic residues of the carrier forming stable bonds, whereas the hydrazone bond is

  3. The potential of iron chelators of the pyridoxal isonicotinoyl hydrazone class as effective antiproliferative agents.

    PubMed

    Richardson, D R; Tran, E H; Ponka, P

    1995-12-01

    Numerous studies have suggested that iron (Fe) chelators such as desferrioxamine (DFO) may be useful antitumor agents (Blatt and Stitely, Cancer Res 47:1749, 1987; Becton and Bryles, Cancer Res 48:7189, 1988). Recent work with several analogues of the lipophilic Fe chelator, pyridoxal isonicotinoyl hydrazone (PIH), indicate that some of these ligands are considerably more efficient than DFO both in terms of their Fe chelation efficacy and at preventing 3H-thymidine incorporation by neuroblastoma (NB) cells (Richardson and Ponka, J Lab Clin Med 124:660, 1994). Considering this fact, the present study was designed to test the antiproliferative effect of a wide range of PIH analogues to identify the most active compounds. A total of 36 ligands have been examined that were synthesized by condensation of three types of aromatic aldehydes (pyridoxal, salicylaldehyde, and 2-hydroxy-1-naphthyladehyde) with a range of acid hydrazides. The effects of these chelators were assessed using the human NB cell line, SK-N-MC. Although PIH was far more effective than DFO at preventing Fe uptake from transferrin, it was less effective than DFO at preventing cellular proliferation (DFO ID50 = 22 mumol/L; PIH ID50 = 75 mumol/L). In contrast, 14 PIH analogues were far more efficient than DFO at preventing proliferation (ID50 = 1 to 7 mumol/L) and may have potential as antitumor agents. The most effective compounds were those hydrazones derived from 2-hydroxy-1-naphthylaldehyde. Most of the PIH analogues were considerably more effective than DFO at both preventing 59Fe uptake from 59Fe-transferrin and in mobilizing 59Fe from prelabeled NB cells. In addition, a linear relationship between Fe chelation efficacy and antiproliferative activity was found only for hydrazones derived from salicylaldehyde. Apart from gallium (Ga) nitrate having an antiproliferative effect by itself, this metal potentiated the antiproliferative effect of PIH but not that of DFO. Spectrophotometric studies showed that PIH could chelate Ga, and it can be suggested that, like the PIH-Fe complex that donates Fe to reticulocytes (Ponka et al, Biochim Biophys Acta 718:151, 1982), the PIH-Ga complex may efficiently bestow Ga to NB cells. The results suggest that analogues of PIH deserve further vigorous investigation because they may be useful therapeutic agents for the treatment of cancer. PMID:7492790

  4. 77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-09-04

    ...FDA-2012-P-0458] Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram...FDA) has determined that ALOXI (palonosetron hydrochloride (HCl)) Capsules...new drug applications (ANDAs) for palonosetron HCl capsules, 0.5 mg...

  5. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ...2011-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and...DRUGS § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications . The sirup...

  6. 21 CFR 520.1263a - Lincomycin hydrochloride monohydrate tablets and sirup.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ...2010-04-01 false Lincomycin hydrochloride monohydrate tablets and sirup. 520.1263a Section 520.1263a Food and...DRUGS § 520.1263a Lincomycin hydrochloride monohydrate tablets and sirup. (a) Specifications . The sirup...

  7. 78 FR 16685 - Impax Laboratories, Inc.; Withdrawal of Approval of Bupropion Hydrochloride Extended-Release...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-03-18

    ...Bupropion Hydrochloride Extended-Release Tablets, 300 Milligrams AGENCY: Food and Drug...Hydrochloride (HCl) Extended-Release Tablets, 300 Milligrams (mg) (Bupropion HCl Extended-Release Tablets 300 mg), under Abbreviated New...

  8. 75 FR 14444 - Determination That DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2010-03-25

    ...DIDREX (Benzphetamine Hydrochloride) Tablets, 25 Milligrams, Were Not Withdrawn From...benzphetamine hydrochloride (HCl)) Tablets, 25 milligrams (mg), were not withdrawn...ANDAs) for benzphetamine HCl 25 mg tablets, if all other legal and regulatory...

  9. 78 FR 40484 - Determination That METADATE ER (Methylphenidate Hydrochloride) Extended-Release Tablet, 10...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-07-05

    ...Methylphenidate Hydrochloride) Extended-Release Tablet, 10 Milligrams, Was Not Withdrawn From...hydrochloride (HCl)) extended-release tablet, 10 milligrams (mg), was not withdrawn...methylphenidate HCl extended-release tablet, 10 mg, if all other legal and...

  10. Erlotinib Hydrochloride in Treating Patients With Bladder Cancer Undergoing Surgery | Division of Cancer Prevention

    Cancer.gov

    This randomized phase II trial studies how well erlotinib hydrochloride works in treating patients with bladder cancer undergoing surgery. Erlotinib hydrochloride may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth.

  11. Characterization of polymorphism of gepirone hydrochloride.

    PubMed

    Behme, R J; Brooke, D; Farney, R F; Kensler, T T

    1985-10-01

    Gepirone hydrochloride, an investigational anxiolytic drug, was found to have at least three polymorphic forms which melted at 180 degrees C (I), 212 degrees C (II), and 200 degrees C (III). Thermal analytical studies showed that forms I and II were an enantiotropic pair, as were forms I and III. Form III was monotropic with form II and there was no temperature at which III was the most stable polymorph. Solubility data from powder dissolution studies were used to estimate a transition temperature of 74 degrees C for the enantiotropic pair of I and II. The difference in enthalpy was 4.5 kcal/mol at 74 degrees C and 2.54 kcal/mol at 25 degrees C. Form I was the most physically stable below 74 degrees C, whereas form II was the most stable above 74 degrees C. Essentially pure samples of I and II could be obtained easily, but pure III could be developed only transiently on the differential scanning calorimeter heating block. Video taping of hot-stage microscopic observations for review was helpful for detecting seed crystals of II or III in samples of I. The information developed is presented in a hypothetical free energy-temperature diagram. PMID:4078700

  12. Extensive in vitro activity of guanidine hydrochloride polymer analogs against antibiotics-resistant clinically isolated strains

    Microsoft Academic Search

    Zhongxin Zhou; Dafu Wei; Yong Guan; Anna Zheng; Jian-Jiang Zhong

    2011-01-01

    Polyhexamethylene guanidine hydrochloride (PHMG) possesses great potential in the development of covalently bound permanent sterile-surface materials for hospital infection control. This study aimed at evaluating the extensive activity of PHMG and its three novel analogs, including polybutamethylene guanidine hydrochloride, polyoctamethylene guanidine hydrochloride (POMG) and poly(m-xylylene guanidine hydrochloride), against 370 clinical strains, especially 96 isolates of which were antibiotics-resistant. Their in

  13. Verification of the dispersive charge transport in a hydrazone:polycarbonate molecularly doped polymer

    NASA Astrophysics Data System (ADS)

    Tyutnev, Andrey P.; Saenko, Vladimir S.; Pozhidaev, Evgenii D.; Kolesnikov, Vladislav A.

    2009-03-01

    We report results of specially planned experiments intended to verify the dispersive character of the charge carrier transport in polycarbonate molecularly doped with hydrazone at 30 wt% loading, using for this purpose samples specifically featuring a well-defined plateau on a linear-linear plot. For this purpose we propose a new variant of the time-of-flight technique which allows easy changing of the generation zone width from about 0.5 µm (surface excitation) through intermediate values to full sample thickness (bulk excitation). To achieve this, we use electron pulses of 3-50 keV energy rather than traditional light pulses provided by lasers. Experimental results corroborated by numerical calculations uniquely prove that carrier transport in this molecularly doped polymer is dispersive, with the dispersion parameter equal to 0.75. Nevertheless, the mobility field dependence follows the famous Poole-Frenkel law.

  14. Isomerization mechanism in hydrazone-based rotary switches: lateral shift, rotation, or tautomerization?

    PubMed

    Landge, Shainaz M; Tkatchouk, Ekatarina; Benítez, Diego; Lanfranchi, Don Antoine; Elhabiri, Mourad; Goddard, William A; Aprahamian, Ivan

    2011-06-29

    Two intramolecularly hydrogen-bonded arylhydrazone (aryl = phenyl or naphthyl) molecular switches have been synthesized, and their full and reversible switching between the E and Z configurations have been demonstrated. These chemically controlled configurational rotary switches exist primarily as the E isomer at equilibrium and can be switched to the protonated Z configuration (Z-H(+)) by the addition of trifluoroacetic acid. The protonation of the pyridine moiety in the switch induces a rotation around the hydrazone C=N double bond, leading to isomerization. Treating Z-H(+) with base (K(2)CO(3)) yields a mixture of E and "metastable" Z isomers. The latter thermally equilibrates to reinstate the initial isomer ratio. The rate of the Z ? E isomerization process showed small changes as a function of solvent polarity, indicating that the isomerization might be going through the inversion mechanism (nonpolar transition state). However, the plot of the logarithm of the rate constant k vs the Dimroth parameter (E(T)) gave a linear fit, demonstrating the involvement of a polar transition state (rotation mechanism). These two seemingly contradicting kinetic data were not enough to determine whether the isomerization mechanism goes through the rotation or inversion pathways. The highly negative entropy values obtained for both the forward (E ? Z-H(+)) and backward (Z ? E) processes strongly suggest that the isomerization involves a polarized transition state that is highly organized (possibly involving a high degree of solvent organization), and hence it proceeds via a rotation mechanism as opposed to inversion. Computations of the Z ? E isomerization using density functional theory (DFT) at the M06/cc-pVTZ level and natural bond orbital (NBO) wave function analyses have shown that the favorable isomerization mechanism in these hydrogen-bonded systems is hydrazone-azo tautomerization followed by rotation around a C-N single bond, as opposed to the more common rotation mechanism around the C=N double bond. PMID:21585197

  15. Measurement of pseudoephedrine hydrochloride dissolution using chloride-ion electrode.

    PubMed

    Chen, S T; Thompson, R C; Poust, R I

    1981-11-01

    Experiments were performed to determine the suitability of using a chloride-ion electrode for the measurement of pseudoephedrine hydrochloride dissolution from commercially available compressed tablets. Dissolution experiments were carried out in 500 ml of distilled water using the USP paddle method at 100 rpm. Both chloride ion and pseudoephedrine (UV spectrophotometry) were measured at six different sampling times. Percent dissolved versus time values were linearized on a log-normal probability basis. The slopes of individual lines obtained from the chloride and pseudoephedrine measurements were compared using a Student t test and did not differ significantly (t = 0.415, df = 5, p greater than 0.05). In addition to providing an efficient, inexpensive, and simple method for measuring pseudoephedrine hydrochloride dissolution rates, the chloride-ion electrode could be used in the measurement of dissolution rates for a wide variety of drugs available as hydrochloride salts. PMID:7299681

  16. Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride

    NASA Astrophysics Data System (ADS)

    Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei

    2013-04-01

    Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a ? 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.

  17. Stability of ondansetron hydrochloride and 12 medications in plastic syringes.

    PubMed

    Stewart, J T; Warren, F W; King, D T; Venkateshwaran, T G; Fox, J L

    1998-12-15

    The stability and compatibility of ondansetron hydrochloride with neostigmine methylsulfate, naloxone hydrochloride, midazolam hydrochloride, fentanyl citrate, alfentanil hydrochloride, atropine sulfate, morphine sulfate, meperidine hydrochloride, propofol, droperidol, metoclopramide monohydrochloride, and glycopyrrolate were studied. Ondansetron 1.33 or 1.0 mg/mL was combined with 0.9% sodium chloride injection and each of the 12 drugs in duplicate in plastic syringes (or glass for propofol). The syringes were stored at 21.8-23.4 or 4 degrees C in the dark, except for those containing propofol, which were stored at ambient temperature. Samples were removed at 0, 4, 8, and 24 hours for analysis by high-performance liquid chromatography and pH measurement; the propofol-containing samples were removed at 0, 1, 2, and 4 hours. Syringes were visually assessed for color and clarity, and particulate content was measured with a particle counter at the end of the study period. All solutions containing ondansetron retained more than 90% of their initial ondansetron concentration. Solutions containing each of the other drugs except droperidol retained more than 90% of their initial concentration of these drugs. The solutions containing droperidol retained more than 90% of their initial droperidol concentration for up to eight hours at ambient temperature but precipitated quickly at 4 degrees C. In combinations of ondansetron 1.33 or 1.0 mg/mL and 10 of 12 drugs, all drugs were stable for 24 hours in plastic syringes at 23 and 4 degrees C; ondansetron hydrochloride 1.0 mg/mL and propofol 1.0 and 5.0 mg/mL in admixtures were stable for 4 hours, and droperidol on its own and combined with ondansetron 1.0 mg/mL was stable for no more than 8 hours at ambient temperature. PMID:9872702

  18. Phenylazoindole dyes 3: Determination of azo-hydrazone tautomers of new phenylazoindole dyes in solution and solid state

    NASA Astrophysics Data System (ADS)

    Babür, Banu; Sefero?lu, Nurgül; Aktan, Ebru; Hökelek, Tuncer; ?ahin, Ertan; Sefero?lu, Zeynel

    2015-02-01

    A new two series of phenylazo indole dyes was synthesized and the structures of the dyes were confirmed by UV-vis, FT-IR, HRMS and 1H/13C NMR spectroscopic techniques. Five of these dyes (I, I?, II?, III and III?) were also characterized in solid state by using single crystal X-ray diffraction studies besides other spectroscopic techniques. The geometries of the azo and hydrazone tautomeric forms of the dyes were optimized by using Density Functional Theory (DFT). In addition, the effects of the donor and acceptor groups on the azo and hydrazone forms of the dyes were evaluated experimentally and theoretically. The results indicate that the phenylazoindole dyes derived from 2-phenyl indole as coupling component exist as azo form in solution, gas phase and solid state.

  19. Synthesis, characterization and anticancer evaluation of novel tri-arm star shaped 1,3,5-triazine hydrazones

    NASA Astrophysics Data System (ADS)

    Machakanur, Shrinath S.; Patil, Basavaraj R.; Badiger, Dayananda S.; Bakale, Raghavendra P.; Gudasi, Kalagouda B.; Annie Bligh, S. W.

    2012-03-01

    A series of novel trisubstituted triazine hydrazones [N3C3(sbnd OC6H4-p-CHdbnd Nsbnd NHsbnd C(O)sbnd C6H4-p-X)3] (X = H, Br, Cl, F, OH, OCH3, CH3, NO2, NH2) were prepared by a three-fold condensation reaction of 2,4,6-tris(4-formylphenoxy)-1,3,5-triazine with p-substituted benzoic acid hydrazides [NH2sbnd NHsbnd C(O)sbnd C6H4-p-X] with excellent yields. The structures were confirmed by elemental analysis, FT-IR, 1H, 13C, 2D-HSQC NMR and mass spectrometry (MALDI-TOF). These derivatives bearing hydrolysable hydrazone linkages were evaluated for their invitro antiproliferative activity against the human liver carcinoma cell line (HepG2) and human cervix carcinoma cell line (HeLa).

  20. Synthesis, characterization, biological activity and equilibrium studies of metal(II) ion complexes with tridentate hydrazone ligand derived from hydralazine

    NASA Astrophysics Data System (ADS)

    El-Sherif, Ahmed A.; Shoukry, Mohamed M.; Abd-Elgawad, Mohamed M. A.

    2012-12-01

    In the present study, a new hydrazone ligand (2-((2-phthalazin-1-yl)hydrazono)methyl)phenol) prepared by condensation of hydralazine (1-Hydralazinophthalazine) with salicylaldehyde (SAH). The synthesized SAH-hydrazone and its metal complexes have been characterized by elemental analyses, IR, 1H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). The analytical data of the complexes show the formation of 1:1 [M:L] ratio, where M represents Ni(II), Co(II) and Cu(II) ions, while L represents the deprotonated hydrazone ligand. IR spectra show that SAH is coordinated to the metal ions in a tridentate manner through phthalazine-N, azomethine-N and phenolic-oxygen groups. The ligand and their metal chelates have been screened for their antimicrobial activities using the disc diffusion method against the selected bacteria and fungi. Proton-ligand association constants of (SAH) and the stepwise stability constants of its metal complexes are determined potentiometrically in 0.1 M NaNO3 at different temperatures and the corresponding thermodynamic parameters were derived and discussed. The order of -?G° and -?H° were found to obey Mn2+ < Co2+ < Ni2+ < Cu2+, in accordance with the Irving-Williams order. The complexes were stabilized by enthalpy changes and the results suggest that the complexation is an enthalpy-driven process. The concentration distribution diagrams of the complexes are evaluated.

  1. Synthesis, crystal structures and spectroscopic properties of triazine-based hydrazone derivatives; a comparative experimental-theoretical study.

    PubMed

    Arshad, Muhammad Nadeem; Bibi, Aisha; Mahmood, Tariq; Asiri, Abdullah M; Ayub, Khurshid

    2015-01-01

    We report here a comparative theoretical and experimental study of four triazine-based hydrazone derivatives. The hydrazones are synthesized by a three step process from commercially available benzil and thiosemicarbazide. The structures of all compounds were determined by using the UV-Vis., FT-IR, NMR (1H and 13C) spectroscopic techniques and finally confirmed unequivocally by single crystal X-ray diffraction analysis. Experimental geometric parameters and spectroscopic properties of the triazine based hydrazones are compared with those obtained from density functional theory (DFT) studies. The model developed here comprises of geometry optimization at B3LYP/6-31G (d, p) level of DFT. Optimized geometric parameters of all four compounds showed excellent correlations with the results obtained from X-ray diffraction studies. The vibrational spectra show nice correlations with the experimental IR spectra. Moreover, the simulated absorption spectra also agree well with experimental results (within 10-20 nm). The molecular electrostatic potential (MEP) mapped over the entire stabilized geometries of the compounds indicated their chemical reactivates. Furthermore, frontier molecular orbital (electronic properties) and first hyperpolarizability (nonlinear optical response) were also computed at the B3LYP/6-31G (d, p) level of theory. PMID:25854752

  2. Preparation of catalytically active, covalent ?-polylysine-enzyme conjugates via UV/vis-quantifiable bis-aryl hydrazone bond formation.

    PubMed

    Grotzky, Andrea; Manaka, Yuichi; Kojima, Taisuke; Walde, Peter

    2011-01-10

    Covalent UV/vis-quantifiable bis-aryl hydrazone bond formation was investigated for the preparation of conjugates between ?-poly-d-lysine (PDL) and either ?-chymotrypsin (?-CT) or horseradish peroxidase (HRP). PDL and the enzymes were first modified via free amino groups with the linking reagents succinimidyl 6-hydrazinonicotinate acetone hydrazone (S-HyNic, at pH 7.6) and succinimidyl 4-formylbenzoate (S-4FB, at pH 7.2), respectively. The modified PDL and enzymes were then conjugated at pH 4.7, whereby polymer chains carrying several enzymes were obtained. Kinetics of the bis-aryl hydrazone bond formation was investigated spectrophotometrically at 354 nm. Retention of the enzymatic activity after conjugate formation was confirmed by using the substrates N-succinimidyl-l-Ala-l-Ala-l-Pro-l-Phe-p-nitroanilide (for ?-CT) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS, for HRP). Thus, not only a mild and efficient preparation and convenient quantification of a conjugate between the polycationic ?-polylysine and enzymes could be shown, but also the complete preservation of the enzymatic activity. PMID:21171644

  3. Syntheses of (S)-(+)-trihexyphenidyl hydrochloride and (S)-(+)-procyclidine hydrochloride, two anticholinergics, using (S)-(-)-3-cyclohexyl-3-hydroxy-3-phenylpropanoic acid as chiral synthon.

    PubMed

    Schjelderup, L; Harbitz, O; Groth, P; Aasen, A J

    1987-05-01

    The absolute configuration of the more active (-)-enantiomer of the anticholinergic trihexyphenidyl hydrochloride has been established as (R) by syntheses of (S)-(+)-procyclidine hydrochloride, whose absolute configuration has been established previously, and (S)-(+)-trihexyphenidyl hydrochloride from the same chiral building block, viz. (S)-(-)-cyclohexyl-3-hydroxy-3-phenylpropanoic acid. Both enantiomers of this chiral synthon were prepared by optical resolution of the corresponding racemate, employing (R)- and (S)-1-phenylethylamine, respectively, as resolving agents. PMID:3673449

  4. Increased Mortality in Groups of Cattle Administered the ?-Adrenergic Agonists Ractopamine Hydrochloride and Zilpaterol Hydrochloride

    PubMed Central

    Loneragan, Guy H.; Thomson, Daniel U.; Scott, H. Morgan

    2014-01-01

    The United States Food and Drug Administration (FDA) approved two ?-adrenergic agonists (?AA) for in-feed administration to cattle fed in confinement for human consumption. Anecdotal reports have generated concern that administration of ?AA might be associated with an increased incidence of cattle deaths. Our objectives, therefore, were to a) quantify the association between ?AA administration and mortality in feedlot cattle, and b) explore those variables that may confound or modify this association. Three datasets were acquired for analysis: one included information from randomized and controlled clinical trials of the ?AA ractopamine hydrochloride, while the other two were observational data on zilpaterol hydrochloride administration to large numbers of cattle housed, fed, and cared for using routine commercial production practices in the U.S. Various population and time at-risk models were developed to explore potential ?AA relationships with mortality, as well as the extent of confounding and effect modification. Measures of effect were relatively consistent across datasets and models in that the cumulative risk and incidence rate of death was 75 to 90% greater in animals administered the ?AA compared to contemporaneous controls. During the exposure period, 40 to 50% of deaths among groups administered the ?AA were attributed to administration of the drug. None of the available covariates meaningfully confounded the relationship between ?AA and increased mortality. Only month of slaughter, presumably a proxy for climate, consistently modified the effect in that the biological association was generally greatest during the warmer months of the year. While death is a rare event in feedlot cattle, the data reported herein provide compelling evidence that mortality is nevertheless increased in response to administration of FDA-approved ?AA and represents a heretofore unquantified adverse drug event. PMID:24621596

  5. Cradle-to-gate life cycle inventory of vancomycin hydrochloride.

    PubMed

    Ponder, Celia; Overcash, Michael

    2010-02-15

    A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections. PMID:19942254

  6. A molecular imprinted membrane for molecular discrimination of tetracycline hydrochloride

    Microsoft Academic Search

    F. Trotta; C. Baggiani; M. P. Luda; E. Drioli; T. Massari

    2005-01-01

    Membranes of poly(acrylonitrile-co-acrylic acid) made by phase inversion technique in the presence of tetracycline hydrochloride showed molecular recognition behavior towards the template molecule. The interactions of the carboxylic groups of the polymer chain played an important role in the discrimination process. Prolonged washing with distilled water regenerated the membrane without any loss of binding capacity. Chloramphenicol, of similar polarity and

  7. Olopatadine Hydrochloride Inhibits Capsaicin-Induced Flare Response in Humans

    Microsoft Academic Search

    Masahisa Shindo; Yuichi Yoshida; Osamu Yamamoto

    2011-01-01

    Capsaicin, a vanilloid, has the potential for releasing substance P (SP) from sensory nerves. Topical application of capsaicin induces a flare response in the skin. However, it has not been clarified whether the release of SP is involved in the process of flare response or not. A potent antihistamine drug, olopatadine hydrochloride, is known to have inhibitory action against the

  8. Morphine and oxycodone hydrochloride in the management of cancer pain

    Microsoft Academic Search

    Eija Kalso; Anneli Vainio

    1990-01-01

    In a double-blind crossover study, morphine and oxycodone hydrochloride were administered to 20 patients who were experiencing severe cancer pain. The peroral doses were determined on the basis of patient-controlled intravenous titration. The assumed oral bioavailability ratios were 44% (group 1, first 10 patients) and 33% (group 2, last 10 patients) for morphine and 66% (group 1) and 50% (group

  9. Bioequivalence and pharmacokinetic profile of promethazine hydrochloride suppositories in humans.

    PubMed

    Stavchansky, S; Wallace, J E; Geary, R; Hecht, G; Robb, C A; Wu, P

    1987-06-01

    A bioequivalence study of promethazine hydrochloride (10-[2-(dimethylamino)propyl]-phenothiazine monohydrochloride) was conducted in 20 male human subjects with the purpose of comparing, under blind condition, the human serum levels of promethazine in three different formulations. The formulations tested were a 50-mg promethazine hydrochloride polyethylene glycol suppository, a 50-mg promethazine hydrochloride cocoa butter-white wax suppository, and a 50-mg oral dose of promethazine hydrochloride syrup. Each subject received single doses of each of the three formulations on each of three different days on a crossover basis. From the measured serum levels, estimates of the bioavailability parameters (area under the serum concentration versus time curve, time-to-peak serum concentration, and peak serum concentration) were obtained by least-squares digital computer fitting. Also, a one-compartment pharmacokinetic open model with two consecutive first-order input steps is proposed. Statistical analysis of the results was performed by using a linear multiple regression approach for the analysis of variance. No significant differences between the syrup and the polyethylene glycol suppositories were obtained (p greater than 0.05) for the above three bioavailability parameters. However, the polyethylene glycol suppositories provided statistically higher peak serum concentration, shorter time-to-peak serum concentration, and larger area under the serum concentration versus time curve than the cocoa butter-white wax suppositories. PMID:3625487

  10. Preparation and in vitro evaluation of suppositories of halofantrine hydrochloride

    Microsoft Academic Search

    F. A. Oladimeji; S. I. Omoruyi; C. O. Onyeji

    Halofantrine (HF) hydrochloride is commercially available only as oral dosage forms. Limitations of oral dosing of the drug coupled with non-availability of the safe parenteral preparations prompted the need to develop and evaluate suppository HF formulations, which may serve as a practical alternative. The effects of type of suppository base and incorporation of non ionic surfactants on in vitro release

  11. Biting deterrence and insecticidal activity of hydrazide–hydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles against Aedes aegypti

    Technology Transfer Automated Retrieval System (TEKTRAN)

    BACKGROUND: Hydrazones are important compounds for drug design and they have also good insecticidal activity. In this study, A series of hydrazide–hydrazones (1-10) and 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles (11-20) were investigated for their biting deterrent and insecticidal act...

  12. Radiation induced conductivity of polycarbonate doped with different concentrations of aromatic hydrazone DEH

    NASA Astrophysics Data System (ADS)

    Vladimir, Saenko; Novikov, Lev; Tyutnev, Andrey

    Radiation induced conductivity (RIC) of polymers widely used on present-day spacecraft plays is an important factor affecting their charging by the hot plasma of the Earth’s magnetosphere. As a result, researchers pay special attention to laboratory investigations of RIC in polymers excited by 10 -100 keV electrons prevailing in the hot magnetospheric plasma, including auroral radiation. Due to fluctuating fluxes of plasma electrons and especially of auroral electrons, it is very important to know how RIC depends on time. In our report we present RIC results observed in polycarbonate (PC) molecularly doped with aromatic hydrazone DEH (10 to 30 mas. percent) under continuous irradiation with 50 keV electrons. It has been found that RIC behavior in this material differs markedly from what we observed earlier in most of the polymers. After beginning of the stepwise irradiation, the RIC of PC+DEH rises fast to the quasistationary level but unlike common polymers, does not fall by an order of magnitude, instead it starts to increase further thus causing the accumulating space charge to decrease. This fact combined with the confirmed high radiation and temperature tolerance allows us to recommend this material for application on the spacecraft outer surface and specifically, as a thermal blanket.

  13. Qsar study of some substituted 4-quinolinyl and 9-acridinyl hydrazones as antimalarial agents.

    PubMed

    Sahu, Nitendra K; Sharma, Mukesh; Mourya, Vishnukanth; Kohli, D V

    2012-01-01

    The quantitative structure-activity relationship (QSAR) analysis of some synthesized substituted 4-quinolinyl and 9-acridinyl hydrazone derivatives were performed to find out the structural requirements of their antimalarial activities. Various 2D descriptors were calculated and used in the present analysis. The 2D-QSAR studies were performed using three statistical methods: the multiple linear regressions, giving square of correlation coefficient (r(2)) = 0.8456, cross validated squared correlation coefficient (q(2)) = 0.7814 and predictable ability (pred_r(2)) = 0.7443; the partial least squares regression, with r(2) = 0.8402, q(2) = 0.7879 and pred_r(2) = 0.7680; and principle component regression, giving r(2) = 0.8392, q(2) = 0.7979 and pred_r(2) = 0.6440. Best equation was selected on the basis of high r(2), q(2) and pred_r(2). The QSAR model indicated that the T_N_O_3, IdAverage, chiV6chain, Most-vePotential and T_C_N_6 played an important role in determining antimalarial activities. The results of the present study may be useful on the designing of more potent analogues as antimalarial agents. PMID:23285677

  14. Z-Group ketone chain transfer agents for RAFT polymer nanoparticle modification via hydrazone conjugation

    PubMed Central

    Bandyopadhyay, Saibal; Xia, Xin; Maiseiyeu, Andrei; Mihai, Georgeta; Rajagopalan, Sanjay

    2012-01-01

    A ketal-containing trithiocarbonyl compound has been synthesized and characterized as a chain transfer agent (CTA) in Reversible Addition Fragmentation Transfer (RAFT) polymerization. The ketal functionality does not interfere with RAFT polymerization of acrylate monomers, which proceeds as previously reported to yield macro-CTA polymers and block co-polymers. Post-polymerization ketal cleavage revealed ketone functionality at the polar terminus of an amphiphilic block co-polymer. Hydrazone-formation was facile in both organic solution as well as in aqueous buffer where polymer nanoparticle assemblies were formed, indicating a conjugation/end-functionalization yield of 40–50%. Conjugation was verified with fluorescein, biotin and Gd-DOTA derivatives, and though the trithiocarbonate linkage is hydrolytically labile, we observed stable conjugation for several days at pH 7.4. and 37°C. As expected, streptavidin binding to biotinylated polymer micelles was observed, and size-change based relaxivity increases were observed when Gd-DOTA hydrazide was conjugated to polymer micelles. Cell-uptake of fluorescently labeled polymer micelles was also readily tracked by FACS and fluorescence microscopy. These polymer derivatives demonstrate a range of potential theranostic/biotechnological applications for this conveniently accessible keto-CTA, which include ligand-based nanoparticle targeting and fluorescent/MR nanoparticle contrast agents. PMID:23148126

  15. Experimental and theoretical studies on methanesulfonic acid 1-methylhydrazide: Antimicrobial activities of its sulfonyl hydrazone derivatives

    NASA Astrophysics Data System (ADS)

    Özbek, Neslihan; Alyar, Saliha; Karacan, Nurcan

    2009-12-01

    Methanesulfonic acid 1-methylhydrazide ( msmh) and its sulfonyl hydrazone derivatives, salicylaldehyde- N-methylmethanesulfonylhydrazone ( salmsmh) and 2-hydroxy-1-naphthaldehyde- N-methylmethanesulfonylhydrazone ( nafmsmh) were synthesized and characterized by using FT-IR, 1H NMR, 13C NMR, LC-MS and elemental analysis. Conformation analysis of msmh based on DFT/B3LYP/6-311G(d) method was performed. 1H and 13C shielding tensors of msmh for the most stable conformer were calculated with GIAO/DFT/B3LYP/6-311++G(2d, 2p) methods in vacuo and various solvents such as DMSO, THF, acetonitrile, methanol and aqueous solution. The harmonic vibrational wavenumbers for the most stable conformer were calculated using at B3LYP/6-311G(d) level. Antimicrobial activity of the compounds was also screened against Gram-positive bacteria ( Staphylococcus aureus ATCC 25923, Bacillus cereus RSKK 863) and Gram-negative bacteria ( Escherichia coli ATCC 11230, Salmonella enterititis ATCC 40376, Pseudomonos aeruginosa ATCC 28753) by both disc diffusion and micro dilution methods.

  16. Syntheses, spectroscopic characterization and thermal behavior on novel binuclear transition metal complexes of hydrazones derived from 4,6-diacetylresorcinol and oxalyldihydrazine

    Microsoft Academic Search

    Adel A. A. Emara; Badr A. El-Sayed; El-Sayed A. E. Ahmed

    2008-01-01

    4,6-Diacetylresorcinol (DAR) serves as precursor for the formation of different hydrazone ligands, which are di-, tetra- or hexa-basic with two symmetrical sets of O2N tridentate, O2N2 tetradentate or O4N2 hexadentate chelating sites. The condensation of 4,6-diacetylresorcinol (DAR) with oxalyldihydrazine (ODH), in the molar ratio 1:1 and 1:2, yields the corresponding hydrazone, H6La and H4Lb, ligands, respectively. The structures of these

  17. Synthesis, Magnetic, and Spectral Studies of Some Mono? and Binuclear Dioxomolybdenum(VI) Complexes with Chelating Hydrazones Derived from Acid Hydrazides and Furfural or Thiophene?2?aldehyde

    Microsoft Academic Search

    R. C. Maurya; R. Verma; T. Singh

    2003-01-01

    This paper deals with the synthesis, magnetic and spectral studies of some mono? and binuclear dioxomolybdenum(VI) complexes with chelating hydrazones derived from salicylic acid\\/benzoic acid\\/isonicotinic acid hydrazide with thiophene?2?aldehyde or furfural. The acid hydrazones synthesized are N?(furfuralidene)?N??salicyloylhydrazine [FSAH, (I)], N?(2?thiophenidene)?N??salicyloylhydrazine [TSAH, (II)], N?(furfuralidene)?N??isonicotinoylydrazine [FINH, (III)], N?(2?thiophenidene)?N??isonicotinoylhydrazine [TINH, (IV)], N?(furfuralidene)?N??benzoylhydrazine [FBZH, (V)] and N?(2?thiophenidene)?N??benzoylhydrazine [TBZH, (VI)]. The metal complexes (1)–(6) were

  18. Extractive spectrophotometric determination of TRODAT-1 hydrochloride in lyophilized kit.

    PubMed

    Li, X M; Chen, Z P; Wang, S P; Tang, J; Liu, C Y; Zou, M F

    2008-09-01

    A simple, sensitive, and accurate spectrophotometric method has been developed for the assay of TRODAT-1 hydrochloride in lyophilized kit. The method is based on the formation of ion-pair association complex of TRODAT-1 with bromothymol blue (BTB) in disodium hydrogen phosphate/citric acid buffer of pH 4.0. The colored product was extracted with chloroform, and measured spectrophotometrically at 414 nm. Beer's law was obeyed in the range of 5-25 microg/ml with molar absorptivity of 2.75 x 10(4) l/mol/cm. Optimization of experimental conditions was described for the method. The proposed method has been successfully applied for the analysis of TRODAT-1 hydrochloride in lyophilized kit. No interference with pharmaceutical excipients was observed. PMID:18819514

  19. Nasal Mucoadhesive in situ Gel of Ondansetron Hydrochloride

    PubMed Central

    Bhalerao, A. V.; Lonkar, S. L.; Deshkar, S. S.; Shirolkar, S. V.; Deshpande, A. D.

    2009-01-01

    Ondansetron is a serotonin receptor antagonist used in the management of nausea and vomiting that is associated with cancer chemotherapy. There is a need for intranasal delivery due to poor bioavailability of drug because of first pass effect. The objective of this study was to develop an intranasal delivery system of ondansetron hydrochloride using thermo-sensitive polymer PF127 and mucoadhesive polymer hydroxypropylcellulose. Due to increase in bioadhesive polymer concentration, there was increase in bioadhesion strength, at the same time there was decrease in the spredability. An in vitro diffusion study revealed that viscosity of the vehicle has an influence on drug. The release of ondansetron hydrochloride from the gel matrix showed diffusion- controlled.

  20. Colesevelam hydrochloride for the treatment of type 2 diabetes mellitus

    Microsoft Academic Search

    Travis E. Sonnett; Terri L. Levien; Joshua J. Neumiller; Brian J. Gates; Stephen M. Setter

    2009-01-01

    Background: Colesevelam hydrochloride is a bile acid sequestrant approved in January 2008 by the US Food and Drug Administration (FDA) for the treatment of adult patients with type 2 diabetes mellitus (DM) in combination with a sulfonylurea, metformin, and\\/or insulin therapy.Objective: The purpose of this article was to review the pharmacology, pharmacokinetics, efficacy, adverse effects and tolerability, drug-drug interactions, contraindications\\/precautions,

  1. Coadministration of colesevelam hydrochloride with atorvastatin lowers LDL cholesterol additively

    Microsoft Academic Search

    Donald Hunninghake; William Insull Jr; Phillip Toth; David Davidson; Joanne M. Donovan; Steven K. Burke

    2001-01-01

    Colesevelam hydrochloride is a novel, potent, non-absorbed lipid-lowering agent previously shown to reduce low density lipoprotein (LDL) cholesterol. To examine the efficacy and safety of coadministration of colesevelam and atorvastatin, administration of these agents alone or in combination was examined in a double-blind study of 94 hypercholesterolemic men and women (baseline LDL cholesterol ?160 mg\\/dl). After 4 weeks on the

  2. Solubility of paroxetine hydrochloride hemi-hydrate in (water + acetone)

    Microsoft Academic Search

    Guobin Ren; Jingkang Wang; Guizhi Li

    2005-01-01

    Using a laser monitoring observation technique, the solubilities of paroxetine hydrochloride hemi-hydrate in (water+acetone) were determined by the synthetic method from (294.45 to 323.20)K, respectively. Results of these measurements were correlated by the three variants of the combined nearly ideal binary solvent\\/Redlich–Kister (CNIBS\\/R–K) model. For the seven group data studied, three variants of the (CNIBS\\/R–K) equation were found to provide

  3. Structure and vibrational spectra of pyridine betaine hydrochloride

    Microsoft Academic Search

    Miros?aw Szafran; Jacek Koput; Jan Baran; Tadeusz G?owiak

    1997-01-01

    The crystal structure of pyridine betaine hydrochloride (PBET·HCl) was determined by X-ray diffraction to be monoclinic, space group P21c with a = 8.533(2) A?, b = 9.548(2) A?, c = 10.781(2) A?, ? = 107.228(3)° and Z = 4. Betaine is protonated and the carboxyl group forms a hydrogen bond with the chloride ion: O·Cl? distance is 2.928(3) Å.The interaction

  4. Calculation of the vibrational spectra of betaine hydrochloride

    Microsoft Academic Search

    Miroslaw Szafran; Jacek Koput

    1997-01-01

    The molecular geometries of betaine hydrochloride, BET·HCl, and free protonated betaine, BET·H+, were calculated with the 6–31G(d,p) basis set at the SCF, MP2 and DFT levels of theory. At the SCF level, the minimum energy corresponds to the ionic pair, B+Htctdot;A?, however, the equilibrium Otctdot;Cl distance is 0.14 Å shorter than the X-ray value. Inclusion of the correlation effects, both

  5. Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin

    Microsoft Academic Search

    Mohammad Al-Khalili; Victor M. Meidan; Boeena B. Michniak

    2003-01-01

    The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and\\u000a terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating\\u000a the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05\\u000a to 0.1 mA\\/cm2 resulted in doubling of the

  6. Enhanced Topical Delivery of Terbinafine Hydrochloride with Chitosan Hydrogels

    Microsoft Academic Search

    ?pek Özcan; Özlem Abac?; Alev Haliki Uztan; Buket Aksu; Hayal Boyac?o?lu; Tamer Güneri; Özgen Özer

    2009-01-01

    Chitosan-based carriers have important potential applications for the administration of drugs. In the present study, topical\\u000a gel formulations of terbinafine hydrochloride (T-HCl) were prepared using different types of chitosan at different molecular\\u000a weight, and the antifungal inhibitory activity was evaluated to suggest an effective formulation for the treatment of fungal\\u000a infections. The characteristics of gel formulations were determined with viscosity

  7. Potentiometric Flow Injection Analysis of Drotaverine Hydrochloride in Pharmaceutical Preparations

    Microsoft Academic Search

    Hosny Ibrahim; Yousry M. Issa

    2005-01-01

    Five poly (vinyl chloride) (PVC) membrane electrodes for the determination of drotaverine hydrochloride (DvCl) were constructed and fully characterized in terms of composition, life span, response time, usable pH range, working concentration range, and temperature. The membranes of these electrodes consist of drotaverinium?silicotungstate (Dv?ST), silicomolybdate (Dv?SM), phosphotungstate (Dv?PT), phosphomolybdate (Dv?PM), or tetraphenylborate (Dv?TPB) ion associations dispersed in PVC matrix with

  8. Evaluation of safety of lipomer doxycycline hydrochloride (lipomer DH).

    PubMed

    Dhumal, Rohit; Soni, Mahesh; Devarajan, Padma; Samad, Abdul; Gaikwad, Rajiv; Vanage, Geeta

    2011-02-01

    The nanoparticulate formulation of lipomer doxycycline hydrochloride (lipomer DH) has been synthesized for the treatment of Brucellosis to increase efficacy of the drug. The present study was undertaken to determine the intravenous safety of blank lipomer and Lipomer DH in terms of maximum tolerated dose in rats. It was observed that blank lipomer and lipomer DH were safe when administered intravenously at doses 2000 mg/kg Bw and 18 mg/kg bw respectively. PMID:21485844

  9. Control of recurrent supraventricular tachycardia with amiodarone hydrochloride.

    PubMed Central

    Swan, J. H.; Chisholm, A. W.

    1976-01-01

    Amiodarone hydrochloride, a new antiarrhythmic agent, controlled a recurrent supraventricular arrhythmia, refractory to conventional medical treatment, in a 57-year-old patient with an anomalous conduction system and idiopathic cardiomyopathy. For the 11 months that the patient has been taking the drug her arrhythmia has not recurred. This drug has produced no important side effects in this patient. Images FIG. 1 FIG. 2 PMID:943223

  10. The molecular conformation of clonidine hydrochloride, an ?-adrenergic agonist

    Microsoft Academic Search

    Vivian Cody; George T. DeTitta

    1979-01-01

    The molecular conformation of the antihypertensive drug clonidine hydrochloride [2-(2,6-dichlorophenylimino)-2-imidazole HCl] has been shown by crystallographic studies to have a nearly perpendicular arrangement of the phenyl and imidazole rings as described by the torsion angles C2-C1-N1-C2'= 76 ° and C1-N1-C2'-N'1 = 0 °. This conformation is not either of those suggested as the minimum energy form by CNDO\\/2 calculations for

  11. Synthesis, spectral and antimicrobial studies of rare earth metal complexes with Schiff-base hydrazone containing quinoline moiety

    Microsoft Academic Search

    Khlood S. Abou-Melha; Hanan Faruk

    2008-01-01

    The synthesis and characterization of lanthanide(III) complexes with the Schiff-base hydrazone, o-hydroxyacetophenone-7-chloro-4-quinoline, (HL) are reported. The complexes were characterized by different physicochemical methods: mass spectrometry, H NMR, C NMR, and IR, UV-visible, molar conductance and magnetic studies. They have the stoichiometry [Ln(L)2(NO3)]·nH2O where Ln = La(III), Pr(III), Nd(II), Sm(III), Eu(III) and n = 1–3. The spectra of the complexes were

  12. Spectrophotometric estimation of betahistine hydrochloride in tablet formulations

    PubMed Central

    Kumar, Amit; Nanda, Sanju; Chomwal, Rajiv

    2010-01-01

    Aim: The study aims to develop simple, sensitive, rapid, accurate and precise spectrophotometric method for estimation of Betahistine hydrochloride in tablet dosage forms. Materials and Methods: For method I and II, in a series of 10 ml volumetric flask, aliquots of standard drug solution (100 ?g/ml) in double distilled water were transferred and diluted with same so as to give several dilutions in concentration range of 15-90 ?g/ml and 10-80 ?g/ml respectively of betahistine hydrochloride. To 5 ml of each dilution taken in a separating funnel, (5 ml of methyl orange for method I and 5 ml of bromo phenol blue for method II) reagent and 5 ml of chloroform was added. Reaction mixture was shaken gently for 5 min and allowed to stand so as to separate aqueous and chloroform layer. Absorbance maxima measured at 421.6 nm and 412 nm for method I and II respectively. Results: The recovery studies were found close to 100 % that indicates accuracy and precision of the proposed methods. The statistical analysis was carried out and results of which were found satisfactory. Standard deviation values were found low that indicated reproducibility of the proposed methods. Conclusion: Based on results the developed methods could be used for routine estimation of betahistine hydrochloride from tablet formulations. PMID:21814445

  13. Syntheses, crystal structure, Hirshfeld surfaces, fluorescence properties, and DFT analysis of benzoic acid hydrazone Schiff bases

    NASA Astrophysics Data System (ADS)

    Alam, Mohammad Sayed; Lee, Dong-Ung

    2015-06-01

    Two hydrazone Schiff base analogues, namely, (E)-N?-(4-hydroxy-3-methoxybenzylidene)benzohydrazide (3a) and (E)-N?-(4-methoxybenzylidene)benzohydrazide (3b), were synthesized using a mild, efficient method and characterized by 1H NMR, mass spectrometry, elemental analysis, and single-crystal X-ray diffraction. X-ray analysis of a single crystal of 3a revealed a tetragonal, space group I4(1)/a structure, with an E-configuration around the azomethine (sbnd C8dbnd N2sbnd) double bond. In this structure, the sbnd NHsbnd and sbnd OH groups act as proton donors and the >Cdbnd O and sbnd Ndbnd groups as proton acceptors, and these facilitate hydrogen bond formation in the crystal state. Plausible intermolecular interactions were studied using 3D Hirshfeld surfaces and related 2D fingerprint plots. The optimized geometry, vibrational frequencies, Mulliken charge distribution, molecular electrostatic potential (MEP) maps, frontier molecular orbitals (FMOs), and associated energies of the ground state and the first single excited state were calculated using density functional theory (DFT) and time-dependant DFT calculations using the B3LYP/6-311G method. Vibrational frequencies calculated in the gaseous phase compared with experimental values measured in the solid state and showed good agreement with each other. The chemical reactivities of 3a and 3b were predicted by mapping MEP surface over optimized geometries and comparing these with MEP map generated over crystal structures. Mulliken charge distribution analysis and MEP map of 3a and 3b revealed that N(1), O(1), O(2) and O(3) atoms could act as electron donors and coordinate with metals and that these represented the most suitable sites for electrophilic attack. In fluorescence spectra, the absorption and emission spectra of 3a and 3b were similar in different polar solvents with few exceptions. In addition, both compounds exhibited dual emission spectra in acetone due to keto-enol tautomerism induced by photoexcitation.

  14. Iron chelation with salicylaldehyde isonicotinoyl hydrazone protects against catecholamine autoxidation and cardiotoxicity.

    PubMed

    Hašková, Pavlína; Kova?íková, Petra; Koubková, Lucie; Vávrová, Anna; Macková, Eliška; Sim?nek, Tomáš

    2011-02-15

    Elevated catecholamine levels are known to induce damage of the cardiac tissue. This catecholamine cardiotoxicity may stem from their ability to undergo oxidative conversion to aminochromes and concomitant production of reactive oxygen species (ROS), which damage cardiomyocytes via the iron-catalyzed Fenton-type reaction. This suggests the possibility of cardioprotection by iron chelation. Our in vitro experiments have demonstrated a spontaneous decrease in the concentration of the catecholamines epinephrine and isoprenaline during their 24-h preincubation in buffered solution as well as their gradual conversion to oxidation products. These changes were significantly augmented by addition of iron ions and reduced by the iron-chelating agent salicylaldehyde isonicotinoyl hydrazone (SIH). Oxidized catecholamines were shown to form complexes with iron that had significant redox activity, which could be suppressed by SIH. Experiments using the H9c2 cardiomyoblast cell line revealed higher cytotoxicity of oxidized catecholamines than of the parent compounds, apparently through the induction of caspase-independent cell death, whereas co-incubation of cells with SIH was able to significantly preserve cell viability. A significant increase in intracellular ROS formation was observed after the incubation of cells with catecholamine oxidation products; this could be significantly reduced by SIH. In contrast, parent catecholamines did not increase, but rather decreased, cellular ROS production. Hence, our results demonstrate an important role for redox-active iron in catecholamine autoxidation and subsequent toxicity. The iron chelator SIH has shown considerable potential to protect cardiac cells by both inhibition of deleterious catecholamine oxidation to reactive intermediates and prevention of ROS-mediated cardiotoxicity. PMID:21147217

  15. Csp(3)-csp(3) bond cleavage in the palladium-catalyzed aminohydroxylation of allylic hydrazones using atmospheric oxygen as the sole oxidant.

    PubMed

    Chen, Yu-Chen; Zhu, Ming-Kui; Loh, Teck-Peng

    2015-06-01

    A C-C bond cleavage was observed in the palladium-catalyzed aminohydroxylation of allylic hydrazones, using atmospheric oxygen as the sole oxidant. This reaction could also proceed in a one-pot manner, starting from keto-alkene compounds and phenylhydrazine. PMID:25973749

  16. CATALYST-FREE REACTIONS UNDER SOLVENT-FEE CONDITIONS: MICROWAVE-ASSISTED SYNTHESIS OF HETEROCYCLIC HYDRAZONES BELOW THE MELTING POINT OF NEAT REACTANTS: JOURNAL ARTICLE

    EPA Science Inventory

    NRMRL-CIN-1437 Jeselnik, M., Varma*, R.S., Polanc, S., and Kocevar, M. Catalyst-free Reactions under Solvent-fee Conditions: Microwave-assisted Synthesis of Heterocyclic Hydrazones below the Melting Point of Neat Reactants. Published in: Chemical Communications 18:1716-1717 (200...

  17. Potential amoebicidal activity of hydrazone derivatives: synthesis, characterization, electrochemical behavior, theoretical study and evaluation of the biological activity.

    PubMed

    Toledano-Magaña, Yanis; García-Ramos, Juan Carlos; Navarro-Olivarria, Marisol; Flores-Alamo, Marcos; Manzanera-Estrada, Mayra; Ortiz-Frade, Luis; Galindo-Murillo, Rodrigo; Ruiz-Azuara, Lena; Meléndrez-Luevano, Ruth Ma; Cabrera-Vivas, Blanca M

    2015-01-01

    Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity was tested in vitro against the HM1:IMSS strain of Entamoeba histolytica. The results showed the influence of the nitrobenzene group and the hydrazone linkage on the amoebicidal activity. meta-Nitro substituted compound 2 presents a promising amoebicidal activity with an IC50 = 0.84 ?M, which represents a 7-fold increase in cell growth inhibition potency with respect to metronidazole (IC50 = 6.3 ?M). Compounds 1, 3, and 4 show decreased amoebicidal activity, with IC50 values of 7, 75 and 23 µM, respectively, as a function of the nitro group position on the aromatic ring. The observed differences in the biological activity could be explained not only by the redox potential of the molecules, but also by their capacity to participate in the formation of intra- and intermolecular hydrogen bonds. Redox potentials as well as the amoebicidal activity can be described with parameters obtained from the DFT analysis. PMID:26035095

  18. Highly efficient donor-acceptor hydrazone dyes-inorganic Si/TiO2 hybrid solar cells.

    PubMed

    Al-Sehemi, Abdullah G; Irfan, Ahmad; Al-Melfi, Mohrah Abdullah M

    2015-06-15

    We have synthesized the two donor-bridge-acceptor organic dyes (hydrazone dye 1 (HD1) and hydrazone dye 2 (HD2)) with the aim to enhance intra-molecular charge transfer then characterized by FTIR and NMR. The ground state geometries have been optimized at three different levels of theories, i.e., B3LYP/6-31G(?), B3LYP/6-31G(??) and Hartee-Fock HF/6-31G(??). The absorption spectra and oscillator strengths in different solvents have been computed and compared with the experimental data. The vibrational spectral assignments have been performed on the recorded FTIR spectra based on the theoretical predicted wavenumbers at three different levels of theories. The effect of different solvents (CHCl3, CH3CN and C2H5OH) has been studied on the absorption wavelengths. Furthermore, we have computed the ionization potentials, electron affinities and reorganization energies of studied compounds and shed light on the charge transport properties. The hetero-junction solar cell devices were fabricated by organic-inorganic hetero-junction (Si/TiO2/dye) then the efficiency has been measured by applying the incident power 30, 50 and 70mW/cm(2). The maximum efficiency 3.12% has been observed for HD1. PMID:25766477

  19. Highly efficient donor-acceptor hydrazone dyes-inorganic Si/TiO2 hybrid solar cells

    NASA Astrophysics Data System (ADS)

    Al-Sehemi, Abdullah G.; Irfan, Ahmad; Al-Melfi, Mohrah Abdullah M.

    2015-06-01

    We have synthesized the two donor-bridge-acceptor organic dyes (hydrazone dye 1 (HD1) and hydrazone dye 2 (HD2)) with the aim to enhance intra-molecular charge transfer then characterized by FTIR and NMR. The ground state geometries have been optimized at three different levels of theories, i.e., B3LYP/6-31G?, B3LYP/6-31G?? and Hartee-Fock HF/6-31G??. The absorption spectra and oscillator strengths in different solvents have been computed and compared with the experimental data. The vibrational spectral assignments have been performed on the recorded FTIR spectra based on the theoretical predicted wavenumbers at three different levels of theories. The effect of different solvents (CHCl3, CH3CN and C2H5OH) has been studied on the absorption wavelengths. Furthermore, we have computed the ionization potentials, electron affinities and reorganization energies of studied compounds and shed light on the charge transport properties. The hetero-junction solar cell devices were fabricated by organic-inorganic hetero-junction (Si/TiO2/dye) then the efficiency has been measured by applying the incident power 30, 50 and 70 mW/cm2. The maximum efficiency 3.12% has been observed for HD1.

  20. Synthesis, Biological Evaluation and 2D-QSAR Study of Halophenyl Bis-Hydrazones as Antimicrobial and Antitubercular Agents

    PubMed Central

    Abdel-Aziz, Hatem A.; Eldehna, Wagdy M.; Fares, Mohamed; Al-Rashood, Sara T. A.; Al-Rashood, Khalid A.; Abdel-Aziz, Marwa M.; Soliman, Dalia H.

    2015-01-01

    In continuation of our endeavor towards the development of potent and effective antimicrobial agents, three series of halophenyl bis-hydrazones (14a–n, 16a–d, 17a and 17b) were synthesized and evaluated for their potential antibacterial, antifungal and antimycobacterial activities. These efforts led to the identification of five molecules 14c, 14g, 16b, 17a and 17b (MIC range from 0.12 to 7.81 ?g/mL) with broad antimicrobial activity against Mycobacterium tuberculosis; Aspergillus fumigates; Gram positive bacteria, Staphylococcus aureus, Streptococcus pneumonia, and Bacillis subtilis; and Gram negative bacteria, Salmonella typhimurium, Klebsiella pneumonia, and Escherichia coli. Three of the most active compounds, 16b, 17a and 17b, were also devoid of apparent cytotoxicity to lung cancer cell line A549. Amphotericin B and ciprofloxacin were used as references for antifungal and antibacterial screening, while isoniazid and pyrazinamide were used as references for antimycobacterial activity. Furthermore, three Quantitative Structure Activity Relationship (QSAR) models were built to explore the structural requirements controlling the different activities of the prepared bis-hydrazones. PMID:25903147

  1. Pharmacological Evaluation and Preparation of Nonsteroidal Anti-Inflammatory Drugs Containing an N-Acyl Hydrazone Subunit

    PubMed Central

    de Melo, Thais Regina Ferreira; Chelucci, Rafael Consolin; Pires, Maria Elisa Lopes; Dutra, Luiz Antonio; Barbieri, Karina Pereira; Bosquesi, Priscila Longhin; Trossini, Gustavo Henrique Goulart; Chung, Man Chin; dos Santos, Jean Leandro

    2014-01-01

    A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs. PMID:24714090

  2. Comparative studies, synthesis, spectroscopic and characterization of N-methylisatin-3-Girard's T and P hydrazone complexes

    NASA Astrophysics Data System (ADS)

    Azhari, Shaker J.; Salah, Sabah; Farag, Rabei S.; Mostafa, Mohsen M.

    2015-02-01

    Different types of complexes derived from the reactions of N-methylisatin Girard's T hydrazone, N,N,N-trimethyl-2-[(2z)-2-(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxo-ethan ammonium chloride (MIGT) and N-methylisatin Girard's P hydrazone, 1-{2-(2z)-2-[(1-methyl-2-oxo-1,2-dihydro-3H-indole-3-ylidene) hydrazino]-2-oxoethyl}pyridinium chloride (MIGP) with Fe3+, Al3+, Sb3+ and Sn2+ salts were synthesized. The isolated complexes were characterized by elemental analyses, molar conductivities, spectral (IR, UV-Vis., 1H NMR, mass), magnetic moments and thermal measurements. The values of conductance suggest that the complexes are conducting in polar solvents (EtOH, H2O and DMF). The IR spectra suggest that the ligands coordinate in a bidentate and/or tridentate manner via the carbonyl groups of both N-methylisatin and Girard's T and/or P and the (Cdbnd N) group. The solvents inside and outside the coordination sphere were determined by weight loss and TGA methods. The octahedral geometry of the complexes is confirmed using spectral, magnetic and DFT method from DMOL3 calculations. The ligands and their metal complexes were tested against different strains of bacteria and fungi.

  3. Synthesis and antimicrobial evaluation of some novel thiazole, pyridone, pyrazole, chromene, hydrazone derivatives bearing a biologically active sulfonamide moiety.

    PubMed

    Darwish, Elham S; Fattah, Azza M Abdel; Attaby, Fawzy A; Al-Shayea, Oqba N

    2014-01-01

    This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13a-e. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and ketene N,S-acetal derivatives respectively. Finally, reaction of 3 with carbon disulfide and 1,3-dibromopropane afforded the N-[4-(aminosulfonyl) phenyl]-2-cyano-2-(1,3-dithian-2-ylidene)acetamide product 22. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis. The compounds were evaluated for both their in vitro antibacterial and antifungal activities and showed promising results. PMID:24445259

  4. Synthesis and Antimicrobial Evaluation of Some Novel Thiazole, Pyridone, Pyrazole, Chromene, Hydrazone Derivatives Bearing a Biologically Active Sulfonamide Moiety

    PubMed Central

    Darwish, Elham S.; Abdel Fattah, Azza M.; Attaby, Fawzy A.; Al-Shayea, Oqba N.

    2014-01-01

    This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13a–e. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and ketene N,S-acetal derivatives respectively. Finally, reaction of 3 with carbon disulfide and 1,3-dibromopropane afforded the N-[4-(aminosulfonyl) phenyl]-2-cyano-2-(1,3-dithian-2-ylidene)acetamide product 22. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis. The compounds were evaluated for both their in vitro antibacterial and antifungal activities and showed promising results. PMID:24445259

  5. 77 FR 7582 - Determination That JENLOGA (Clonidine Hydrochloride) Extended-Release Tablets, 0.1 Milligram and...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-02-13

    ...Clonidine Hydrochloride) Extended- Release Tablets, 0.1 Milligram and 0.2 Milligram...clonidine hydrochloride) Extended-Release Tablets, 0.1 milligram (mg) and 0.2 mg...clonidine hydrochloride extended-release tablets, 0.1 mg and 0.2 mg, if all...

  6. 77 FR 20987 - Oral Dosage Form New Animal Drugs; Change of Sponsor; Lincomycin Hydrochloride Soluble Powder...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2012-04-09

    The Food and Drug Administration (FDA) is amending the animal drug regulations to reflect a change of sponsor for three abbreviated new animal drug applications (ANADAs) for lincomycin hydrochloride; penicillin G potassium, USP; and tetracycline hydrochloride soluble powders administered in drinking water from Teva Animal Health, Inc., to Quo Vademus,...

  7. Enantioseparation of palonosetron hydrochloride by micellar electrokinetic chromatography with sodium cholate as chiral selector

    Microsoft Academic Search

    Kan Tian; Hongli Chen; Jianghong Tang; Xingguo Chen; Zhide Hu

    2006-01-01

    The enantioseparation of four stereoisomers of palonosetron hydrochloride by micellar electrokinetic chromatography using sodium cholate as chiral surfactant was described. Sodium cholate was shown to be effective in separating palonosetron hydrochloride stereoisomers. For method optimization, several parameters such as sodium cholate concentration, buffer pH and concentration, the types and concentration of organic modifiers and applied voltage, on the enantioseparation were

  8. Controlled release of lidocaine hydrochloride from the surfactant-doped hybrid xerogels

    Microsoft Academic Search

    Zhijian Wu; Hyeonwoo Joo; Tai Gyu Lee; Kangtaek Lee

    2005-01-01

    We investigate the controlled release of lidocaine hydrochloride from the doped silica-based xerogels. In the xerogel preparation, tetraethoxysilane (TEOS), methyltriethoxysilane (MTES), and propyltriethoxysilane (PTES) are used as precursors, and a nonionic surfactant Igepal CO 720 is used as a dopant. The experimental results suggest that the release of lidocaine hydrochloride can be easily controlled by partially substituting TEOS with the

  9. Formulation of a new polymeric film of Propranolol hydrochloride using Psyllium as a natural polymer

    Microsoft Academic Search

    Objective: Propranolol hydrochloride is a widely used beta blocker agent which is administered 3 times daily due to its short half life. The aim of this study was to design and evaluate polymeric film of propranolol hydrochloride using psyllium seed's mucilage as a natural occurring substance in order to deliver the active agent in a controlled manner. Methods: In this

  10. 78 FR 38053 - Determination That OPANA ER (Oxymorphone Hydrochloride) Drug Products Covered by New Drug...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-06-25

    ...hydrochloride (HCl)) Extended-Release Tablet products approved under new drug application...for oxymorphone HCl extended-release tablets if all other legal and regulatory requirements...oxymorphone hydrochloride) Extended-Release Tablets approved under NDA 21-610 were...

  11. Effect of Carteolol Hydrochloride on Ocular Blood Flow Dynamics in Normal Human Eyes

    Microsoft Academic Search

    Kenji Mizuki; Yoshio Yamazaki

    2000-01-01

    Purpose: The effect of topical 2% carteolol hydrochloride on the ocular blood flow dynamics in normal human eyes was studied.Materials and Methods: Ten healthy volunteers were studied using color Doppler imaging and scanning laser Doppler flowmetry. In the first experiments, one eye received 30 ?l of 2% carteolol hydrochloride twice daily for 7 days and the fellow eye a placebo

  12. Adverse drug reaction to metoclopramide hydrochloride in a macaw with proventricular dilatation syndrome.

    PubMed

    Massey, J G

    1993-08-15

    A 4-year-old female blue and gold macaw (Ara ararauna) with a history of chronic vomiting was treated with metoclopramide hydrochloride. After the second treatment, ataxia, torticollis, and opisthotonos became evident. These signs resolved with the administration of diphenhydramine hydrochloride. Despite supportive care, the bird died several days later. Histologic lesions were suggestive of proventricular dilatation syndrome. PMID:8407511

  13. Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy

    Microsoft Academic Search

    J. B. Epstein; P. Stevenson-Moore

    1986-01-01

    Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for

  14. High-performance liquid chromatography method for the simultaneous determination of thiamine hydrochloride, pyridoxine hydrochloride and cyanocobalamin in pharmaceutical formulations using coulometric electrochemical and ultraviolet detection

    Microsoft Academic Search

    Marcin Leszek Marsza??; Anna Lebiedzi?ska; Wojciech Czarnowski; Piotr Szefer

    2005-01-01

    The method for the simultaneous determination of thiamine hydrochloride, pyridoxine hydrochloride and cyanocobalamin by high-performance liquid chromatography (HPLC) with coulometric electrochemical and UV detections is presented. The retention time of vitamins was repeatedly determined by isocratic elution using 0.05M phosphate buffer–10% methanol and 0.018M trimethylamine (1mlmin?1, pH 3.55) as mobile phase with the Supelco LC 18 column 5?m (25cm×4.6mm). The

  15. Cocrystals of bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride

    NASA Astrophysics Data System (ADS)

    Dega-Szafran, Z.; Dulewicz, E.; Dutkiewicz, G.; Kosturkiewicz, Z.

    2006-08-01

    Bis(4-hydroxy-1-methylpiperidine betaine) hydrochloride, [bis(1-carboxymethyl-4-hydroxy-1-methylpiperidinium) hydrochloride, (HO-MPB) 2HCl], has been prepared from stoichiometric amounts of ?-4-hydroxy-1-methylpiperidine betaine hydrochloride with the OH group in an equatorial position and ?-4-hydroxy-1-methylpiperidine betaine inner salt with the OH group in an axial one. Cocrystals of (HO-MPB) 2HCl belong to monoclinic system with C2/ c space group. Piperidinium ring has a chair conformation with the CH 2COO group in the equatorial position and the CH 3 group in the axial one, while the OH group occupies the equatorial or axial position in the disordered structure. There are three types of substituted piperidinium molecules A, B and C in the asymmetric unit. These isomers are distributed randomly yielding partially occupied sites of the hydroxyl groups. The disorder of molecules has been confirmed by the X-ray diffraction experiments at low temperature. The piperidinium molecules form two independent homoconjugated cations, A-B and C-C, with short asymmetrical (2.457(2) Å) and symmetrical (2.440(2) Å) OHO hydrogen bonds, respectively. The hydroxyl groups interact with the Cl - anions by the O-H⋯Cl hydrogen bonds. The A- B cation is linked with C- C by the O-H⋯O-H hydrogen bond, while C- C cations are joined together by the O-H⋯O=C hydrogen bonds, forming infinite zigzag chains. The FTIR spectrum shows an intense ?OH band in the 3300-3100 cm -1 region and a broad and intense ?(OHO) absorption in the 1500-400 cm -1 region, which confirm the presence of the O-H⋯Cl and O·H·O hydrogen bonds. The 1H and 13C NMR spectra, in the aqueous solution, prove the inequivalence of the piperidinium ring caused by two conformations of the OH group at the ring.

  16. Fetal Exposure to Sertraline Hydrochloride Impairs Pancreatic ?-Cell Development.

    PubMed

    De Long, Nicole E; Gutgesell, Marie K; Petrik, James J; Holloway, Alison C

    2015-06-01

    Ten percent to 15% of women take selective serotonin reuptake inhibitor (SSRI) antidepressants during pregnancy. Offspring exposed to SSRIs are more likely to have low birth weight; this is associated with an increased risk of development of diabetes in adulthood in part due to altered pancreatic development. The effects of perinatal exposure to SSRIs on pancreatic development are unknown. Therefore, the objective of this study was to determine the effect of fetal exposure to sertraline hydrochloride on pregnancy outcomes and pancreatic development. Wistar rats were given vehicle (n = 5) or sertraline hydrochloride (10 mg/kg/d; n = 8) via daily subcutaneous injection from the confirmation of mating until parturition. Results from this animal model demonstrated that offspring born to sertraline-exposed dams have no changes in birth weight but had a reduction in pancreatic ?-cell area. The altered pancreatic islet development was a result of altered gene expression regulating islet development and survival. Therefore, fetal exposure to sertraline reduces ?-cell capacity at birth, raising concerns regarding the long-term metabolic sequelae of such exposures. PMID:25763636

  17. Characterization of Hydrochloride and Tannate Salts of Diphenhydramine

    PubMed Central

    Nandgude, T. D.; Bhise, K. S.; Gupta, V. B.

    2008-01-01

    Proper characterization is an important aspect of any dosage form design. The objective of this work was to characterize tannate salt and hydrochloride salt of diphenhydramine. As a part of characterization studies, Differential scanning calorimetry was used to investigate thermal effects and nature of salts, supported by X-ray powder diffraction. Scanning electron microphotographs was used to surface topography of salts of diphenhydramine. Fourier-transform infrared spectroscopy, solubility study and flowability studies were carried out as part of characterization. Differential scanning calorimetry and X-ray powder diffraction studies indicated amorphous nature of the tannate while hydrochloride salt has crystalline properties. Scanning electron microphotographs indicated the differences in surface topography between both the salts. Solubility studies at different pH showed pH dependant solubility of both the salts and less solubility of tannate. Stability of bulk drug at accelerated conditions of 40°/75% RH was determined for both salts. Good stability of both salts was observed. PMID:20046775

  18. Oral administration of diazepam and promazine hydrochloride to immobilize pronghorn.

    PubMed

    Pusateri, F M; Hibler, C P; Pojar, T M

    1982-01-01

    Oral tranquilizers were mixed with a grain bait and fed to pronghorn (Antilocapra americana) in an attempt to immobilize and thus facilitate their capture. Diazepam, administered at 6 mg/kg body weight immobilized a tame pronghorn fawn within 30 min. Tranquilization was still apparent after 8 h. A minimum dose of 23 mg/kg body weight was necessary to immobilize a wild adult pronghorn. Immobilization occurred after 60 min and tranquilization was apparent 24 h post ingestion. Excitement severely impeded the effect of the drug and although easily captured, the animal struggled wildly when handled. Wild pronghorn fawns showed moderate tranquilization when administered diazepam at 23 mg/kg body weight but were unapproachable. Doses of diazepam between 13 and 23 mg/kg body weight were used to capture tame yearling and adult pronghorn held in a 132 ha enclosure. A dose of 23 mg/kg body weight was excessive in that the animals did not recover for 48 to 54 h post ingestion and had difficulty maintaining a sternal bedding position. Diazepam at 13 mg/kg body weight failed to tranquilize the animals sufficiently for easy capture. Promazine hydrochloride at doses of 2 to 17 mg/kg body weight, given orally to wild pronghorn fawns and an adult, did not produce visible signs of tranquilization. Animals refused to eat bait containing doses of promazine hydrochloride greater than 17 mg/kg body weight. PMID:7097876

  19. Synthesis and characterization of a new mebendazole salt: mebendazole hydrochloride.

    PubMed

    Brusau, E V; Camí, G E; Narda, G E; Cuffini, S; Ayala, A P; Ellena, J

    2008-01-01

    Mebendazole hydrochloride [(5-benzoyl-1H-benzimidazole-2-yl)-carbamic acid methyl ester hydrochloride, MBZ.HCl], a new stable salt of mebendazole (MBZ), has been synthesized and characterized. It can easily be obtained from recrystallization of forms A, B, or C of MBZ in diverse solvents with the addition of hydrochloric acid solution. Crystallographic data reveals that the particular conformation adopted by the carbamic group contributes to the stability of the network. The crystal packing is stabilized by the presence of three N-H...Cl intermolecular interactions that form chains along the b axis. The XRD analyses of the three crystalline habits found in the crystallization process (square-based pyramids, pseudohexagonal plates, and prismatic) show equivalent diffraction patterns. The vibrational behavior is consistent with crystal structure. The most important functional groups show shifts to lower or higher frequencies in relation to the MBZ polymorphs. The thermal study on MBZ.HCl indicates that the compound is stable up to 160 degrees C approximately. Decomposition occurs in four steps. In the first step the HCl group is eliminated, and after that the remaining MBZ polymorph A decomposes in three steps, as happens with polymorphs B and C. ( PMID:17854049

  20. Investigation on the toxic interaction of chrysoidine hydrochloride-CTMAB combined contamination with calf thymus DNA.

    PubMed

    Chi, Zhenxing; Liu, Rutao; Pan, Xingren; Teng, Yue; Qin, Hao; Zhu, Jianhua; Hao, Xiaopeng

    2010-01-01

    The toxic interaction of the azo dye-chrysoidine hydrochloride combined with cetyltrimethyl ammonium bromide (CTMAB) in living tissue was studied in vitro. The absorption spectrum, resonance light scattering (RLS), circular dichroism (CD) and transmission electron microscopy (TEM) results showed that the toxicity of chrysoidine hydrochloride itself to calf thymus DNA (ct-DNA) is weak, while the chrysoidine hydrochloride-CTMAB combined pollution showed obvious toxic interaction with ct-DNA. The chrysoidine hydrochloride-CTMAB combined contamination can interact with ct-DNA to form an ion-associated complex through electrostatic and hydrophobic forces. The conformation of DNA was changed in the interaction process to show toxic. The experimental results showed that the combination of chrysoidine hydrochloride-CTMAB has higher toxicity to ct-DNA than either chrysoidine hydrochloride or CTMAB individually, and the combined pollution showed a strong toxic co-effect at a dose of 3.0x10(-4) mol L(-1) chrysoidine hydrochloride and 1.6x10(-5) mol L(-1) CTMAB. PMID:19897408

  1. Gemcitabine Hydrochloride-Loaded Functionalised Carbon Nanotubes as Potential Carriers for Tumour Targeting

    PubMed Central

    Das, Shilpee; Desai, Jagruti L.; Thakkar, Hetal P.

    2013-01-01

    The objective of the present work was to formulate gemcitabine hydrochloride loaded functionalised carbon nanotubes to achieve tumour targeted drug release and thereby reducing gemcitabine hydrochloride toxicity. Multiwalled carbon nanotubes were functionalised using 1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000. Optimised ratio 1:2 of carbon nanotubes:1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000 was taken for loading of gemcitabine hydrochloride. The formulation was evaluated for different parameters. The results showed that maximum drug loading efficiency achieved was 41.59% with an average particle size of 188.7 nm and zeta potential of ?10?1 mV. Scanning electron microscopy and transmission electron microscopy images confirmed the tubular structure of the formulation. The carbon nanotubes were able to release gemcitabine hydrochloride faster in acidic pH than at neutral pH indicating its potential for tumour targeting. Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern. Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride. Stability studies indicated that lyophilised samples of the formulation were more stable for 3 months under refrigerated condition than at room temperature. Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride. PMID:24591746

  2. Structure-activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL).

    PubMed

    Mayer, Nicole; Schweiger, Martina; Melcher, Michaela-Christina; Fledelius, Christian; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf

    2015-06-15

    Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure-activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50=10?M in an assay with COS7-cell lysate overexpressing murine ATGL. PMID:25778769

  3. Structure–activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL)

    PubMed Central

    Mayer, Nicole; Schweiger, Martina; Melcher, Michaela-Christina; Fledelius, Christian; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf

    2015-01-01

    Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure–activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50 = 10 ?M in an assay with COS7-cell lysate overexpressing murine ATGL. PMID:25778769

  4. Control and analysis of hydrazine, hydrazides and hydrazones--genotoxic impurities in active pharmaceutical ingredients (APIs) and drug products.

    PubMed

    Elder, D P; Snodin, D; Teasdale, A

    2011-04-01

    This is the latest of a series of reviews focused on the analysis of genotoxic impurities. This review summarises the analytical approaches reported in the literature relating to hydrazine, hydrazines, hydrazides and hydrazones. It is intended to provide guidance for analysts needing to develop procedures to control such impurities, particularly where this is due to concerns relating to their potential genotoxicity. Of particular note is the wide variety of techniques employed, both chromatographic and spectroscopic, with most involving derivatisation. Such a wide variety of options allow the analyst a real choice in terms of selecting the most appropriate technique specific to their requirements. Several generic methodologies, covering the three main analytical approaches; i.e. HPLC (high performance liquid chromatography), GC (gas chromatography) and IC (ion chromatography), are also described. PMID:21145684

  5. Anticancer phytochemical analogs 37: synthesis, characterization, molecular docking and cytotoxicity of novel plumbagin hydrazones against breast cancer cells.

    PubMed

    Dandawate, Prasad; Ahmad, Aamir; Deshpande, Jyoti; Swamy, K Venkateswara; Khan, Ejazuddin M; Khetmalas, Madhukar; Padhye, Subhash; Sarkar, Fazlul

    2014-07-01

    We have synthesized, structurally characterized and examined cytotoxicity of novel plumbagin hydrazones against estrogen and progesterone receptor positive (ER+/PR+) MCF-7 and triple negative MDA-MB-231 breast cancer cell lines in order to evaluate the potential of these novel phytochemical analogs. Compounds were docked into the protein cavity of p50-subunit of NF-?B protein revealing better fit and better binding energies than the parent plumbagin compound. This was also reflected in their superior cytotoxicities which were found to be mediated by inhibition of NF-?B expression. These compounds can provide a starting point for the development of novel drug molecules against triple negative breast cancers. PMID:24835626

  6. Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of Indian fox (Vulpes bengalensis) in field situations.

    PubMed

    Belsare, Aniruddha V; Vanak, Abi Tamim

    2013-09-01

    Reports on doses of anesthetic agents for safe and effective immobilization of most wild species occurring in India are very limited. Further, the anesthetic agents available in India for field immobilizations are limited to xylazine hydrochloride and ketamine hydrochloride. A safe and effective dosage of xylazine-ketamine for Indian fox (Vulpes bengalensis) is reported, based on 37 wild Indian fox immobilizations between April 2006 and May 2007. Foxes captured for a radiotelemetry and health monitoring study were immobilized with a mixture of xylazine (2.27 +/- 0.44 mg/kg) and ketamine (13.39 +/- 2.26 mg/kg). Induction and recovery was smooth and uneventful in all foxes. The duration of anesthesia was sufficient for the fitting of radiotransmitters, morphometric measurements, and blood sampling. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization. The results suggest that field immobilization of Indian foxes with 2 mg/kg xylazine and 13 mg/kg ketamine is effective and safe. PMID:24063107

  7. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples

    NASA Astrophysics Data System (ADS)

    Abdel-Ghani, N. T.; Rizk, M. S.; Mostafa, M.

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 ?g mL-1, using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ?0.995 (n = 6) with a relative standard deviation (RSD) ?1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  8. Molecular association of betaine and betaine hydrochloride in aqueous solutions--a study by Raman spectroscopy.

    PubMed

    Amorim da Costa, A; Leite, J E

    2001-02-16

    Raman vibrational spectroscopy, at 298 K, has been used to study the hydration of betaine hydrochloride and betaine in the concentration range 0.5-2 M. The observed changes in the internal vibrations of the solutes, namely, in the C=O, COO- and C-H stretchings, and in the components of the O-H stretching band are consonant with anionic water-betaine and betaine hydrochloride dimeric species involving simultaneously hydrogen-bonding between two solute and water molecules. In both cases, betaine hydrochloride and 'zwitterionic' betaine behave like structure-makers promoting a larger association in the 'bulk' liquid water. PMID:11342265

  9. Spectroscopic and X-ray Crystallographic Evidence for Electrostatic Effects in 4-Substituted Cyclohexanone-Derived Hydrazones, Imines, and Corresponding Salts

    PubMed Central

    Dibble, David J.; Ziller, Joseph W.; Woerpel, K. A.

    2011-01-01

    The axial conformer of several 4-substituted cyclohexanone hydrazone salts was found to predominate in solution. Changes in the charge of the molecule and the polarity of the solvent led to changes in the conformational preference of each molecule that was consistent with electrostatic stabilization of the axial conformer. 1H NMR spectroscopic analysis was utilized to determine the structure of cyclohexanone-derived substrates by comparison to conformationally restricted trans-decalone derivatives and computational models. X-ray crystallography demonstrated that the axial configuration of a pendant benzyloxy group is the preferred conformation of an iminium ion in the solid state. The structure of a neutral hydrazone was also determined to favor the axial configuration for a pendant benzyloxy group in the solid state. PMID:21806053

  10. Structural and vibrational study of 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone - A potential metal-protein attenuating compound (MPAC) for the treatment of Alzheimer's disease

    NASA Astrophysics Data System (ADS)

    de Freitas, Leonardo Viana; da Silva, Cecilia C. P.; Ellena, Javier; Costa, Luiz Antônio Sodré; Rey, Nicolás A.

    2013-12-01

    A comprehensive structural and vibrational study of the potential metal-protein attenuating compound 8-hydroxyquinoline-2-carboxaldehyde isonicotinoyl hydrazone is reported. X-ray diffraction data, as well as FT-IR and Raman frequencies, were compared with the respective theoretical values obtained from DFT calculations. Theory agrees well with experiment. In this context, an attempt of total assignment concerning the FT-IR and Raman spectra of the title compound was performed, shedding new light on previous partial assignments published elsewhere.

  11. N-Heterocyclic Carbene-Catalyzed Oxidative Annulations of ?,?-Unsaturated Aldehydes with Hydrazones: Selective Synthesis of Optically Active 4,5-Dihydropyridazin-3-ones and Pyridazin-3-ones.

    PubMed

    Mao, Jian-Hui; Wang, Zi-Tian; Wang, Zhan-Yong; Cheng, Ying

    2015-06-19

    A novel and efficient method for the highly enantioselective synthesis of chiral 4,5-dihydropyridazin-3-one derivatives has been developed based on the chiral N-heterocyclic carbene-catalyzed oxidative annulation between ?,?-unsaturated aldehydes and hydrazones. Meanwhile, the selective synthesis of either 4,5-dihydropyridazin-3-ones or pyridazin-3-one derivatives from the same reactants has been achieved by simply varying catalytic and reaction conditions. PMID:26019007

  12. Mono and BiNuclear Metal Complexes of Schiff-Base Hydrazone (ONN) Derived from o-Hydroxyacetophenone and 2Amino4Hydrazino6Methyl Pyrimidine

    Microsoft Academic Search

    Saied M. E. Khalil; H. S. Seleem; B. A. El-Shetary; M. Shebl

    2002-01-01

    A tridentate ONN donor Schiff-base hydrazone ligand, H2L, was synthesized by the condensation of 2-amino-4-hydrazino-6-methyl pyrimidine with o-hydroxyacetophenone. The structure of the ligand was elucidated by IR and H NMR spectra which indicated the presence of three different coordinating groups, the oxygen atom of the phenolic OH group, the nitrogen atom of the azomethine, C=N, group and one of the

  13. Synthesis, characterization, and DNA-binding properties of the Ln(III) complexes with 6-hydroxy chromone-3-carbaldehyde-(2?-hydroxy) benzoyl hydrazone

    Microsoft Academic Search

    Bao-dui Wang; Zheng-Yin Yang; Tian-rong Li

    2006-01-01

    A new ligand, 6-hydroxy chromone-3-carbaldehyde-(2?-hydroxy) benzoyl hydrazone (L), was prepared by condensation of 6-hydroxy-3-carbaldehyde chromone (CDC) with 2-hydroxy benzoyl hydrazine. Its four rare earth complexes have been synthesized and characterized on the basis of elemental analyses, molar conductivities, mass spectra, 1H NMR, thermogravimetry\\/differential thermal analysis (TG–DTA), UV–vis spectra, fluorescence spectra, and IR spectra. The general formula of the complexes is

  14. Cytotoxic iron chelators: characterization of the structure, solution chemistry and redox activity of ligands and iron complexes of the di-2-pyridyl ketone isonicotinoyl hydrazone ( H PKIH) analogues

    Microsoft Academic Search

    Paul V. Bernhardt; Lorraine M. Caldwell; Timothy B. Chaston; Piao Chin; Des R. Richardson

    2003-01-01

    Di-2-pyridyl ketone isonicotinoyl hydrazone (HPKIH) and a range of its analogues comprise a series of monobasic acids that are capable of binding iron (Fe) as tridentate (N,N,O) ligands. Recently, we have shown that these chelators are highly cytotoxic, but show selective activity against cancer cells. Particularly interesting was the fact that cytotoxicity of the HPKIH analogues is maintained even after

  15. A novel method for coupling doxorubicin to lactosaminated human albumin by an acid sensitive hydrazone bond: synthesis, characterization and preliminary biological properties of the conjugate

    Microsoft Academic Search

    Giuseppina Di Stefano; Marcella Lanza; Felix Kratz; Luca Merina; Luigi Fiume

    2004-01-01

    The expression of the asialoglycoprotein receptor on the cells of the large majority of the well differentiated hepatocellular carcinomas can be exploited to improve the chemotherapy of these tumours by coupling anticancer agents to macromolecules taken up by the receptor. In line with this approach, in previous experiments we coupled doxorubicin (DOXO) to lactosaminated human albumin (L-HSA) using the (6-maleimidocaproyl)hydrazone

  16. Cytotoxic analogs of the iron(III) chelator pyridoxal isonicotinoyl hydrazone: effects of complexation with copper(II), gallium(III), and iron (III) on their antiproliferative activities.

    PubMed Central

    Richardson, D R

    1997-01-01

    This study examined if complexation with metals increased the antiproliferative activities of chelators of the pyridoxal isonicotinoyl hydrazone (PIH) class. Addition of iron(III) to some PIH analogs markedly depressed their activities, whereas it had little effect on others. The gallium(III) complex of PIH, but not its copper(II) complex, was more efficient than the apochelator at inhibiting [3H]thymidine incorporation. PMID:9303419

  17. [The degradation mechanism of penequine hydrochloride in aqueous solutions].

    PubMed

    Cheng, Z J; Yang, Z P

    1993-01-01

    Penequine hydrochloride (I) is a new potent anticholinergic drug, the degradation mechanism of I in aqueous solutions is reported in this paper. I is an ethereal compound, stable in neutral and alkaline solutions, but it decomposes in strong acidic solutions. Its main degradation products have been separated and identified by means of TLC, MS, GC/MS and GC/FTIR. With reference to the general degradation rule of ethereal compound and the structure of the degradation products, we deduced that the ether linkage of I splits in acidic solutions by the catalysis of hydrogen ion, producing 3-quinuclidinol (DP1) and 1-phenyl-1-cyclopentyl glycol. The latter turns into 1-phenyl-1-cyclopentyl acetaldehyde through dehydration and rearrangement. In addition, small amounts of other degradation compounds, e. g. benzaldehyde, acetophenone, phenylcyciopentyl ketone, etc. have also been found, but the mechanism remains to be further studied. PMID:8285076

  18. Crystal structure of bis(pyridine betaine) hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Xiao-Ming, Chen; Mak, Thomas C. W.

    1990-04-01

    Bis(pyridine betaine) hydrochloride monohydrate, 2C 5H 5NCH 2COO·HCl·H 2O, crystallizes in space group Pnna (No. 52), with a=15.623(3), b=19.707(3), c=5.069(1) Å, and Z=4. The structure has been refined to RF=0.067 for 1207 observed (| F0|>6?| F0|) Mo K? data. The carboxylate groups of a pair of pyridine betaine molecules are bridged by a proton to form a centrosymmetric dimer featuring a very strong hydrogen bond of length 2.436(6) Å. The crystal structure comprises a packing of such [(C 5H 5NCH 2COO) 2H] + moieties and hydrogen-bonded (Cl -{dH 2O} ?) zigzag chains running parallel to the c axis.

  19. Crystal structure of BIS(Betaine) hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Chen, Xiao-Ming; Mak, Thomas C. W.

    1990-11-01

    Bis(betaine) hydrochloride monohydrate, 2Me 3NCH 2COO·HCI·H 2O, crystallizes in space group Pnma (No. 62), with a=11.904(1), b=22.454(5), c=5.624(1) Å, and Z=4. The structure has been refined to RinF=0.046 for 863 observed (| Fo||>6?| Fo|) Mo K? data. the carboxylate groups of a pair of betaine molecules are bridged by a proton to form a centrosymmetric dimer featuring a very strong hydrogen bond of length 2.454(4) Å. The crystal structure comprises a packing of such [(Me 3NCH 2COO) 2H] + moieties and hydrogen-bonded (Cl -·H 2O) ? zigzag chains running parallel to the c axis.

  20. Peganine hydrochloride dihydrate an orally active antileishmanial agent.

    PubMed

    Khaliq, Tanvir; Misra, Pragya; Gupta, Swati; Reddy, K Papi; Kant, Ruchir; Maulik, P R; Dube, Anuradha; Narender, T

    2009-05-01

    Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on drug discovery and development on antileishmanial agents from plants, we carried out bioassay guided fractionation on Peganum harmala seeds which resulted in the isolation of 1 as an antileishmanial agent. 2D-NMR spectral data and single crystal X-ray crystallography data indicated 1 as peganine hydrochloride in dihydrated form. The compound 1 exhibited in-vitro activity against both extracellular promastigotes as well as intracellular amastigotes residing within murine macrophages in Leishmania donovani. Furthermore, 1 also exhibited in-vivo activity, 79.6 (+/-8.07)% against established VL in hamsters at a dose of 100mg/kgb.wt. PMID:19339182

  1. Glucosamine hydrochloride for the treatment of osteoarthritis symptoms

    PubMed Central

    Fox, Beth Anne; Stephens, Mary M

    2007-01-01

    Osteoarthritis is the most common arthritis in the world. It affects millions of people with age being the greatest risk factor for developing the disease. The burden of disease will worsen with the aging of the world’s population. The disease causes pain and functional disability. The direct costs of osteoarthritis include hospital and physician visits, medications, and assistive services. The indirect costs include work absences and lost wages. Many studies have sought to find a therapy to relieve pain and reduce disability. Glucosamine hydrochloride (HCl) is one of these therapies. There are limited studies of glucosamine HCl in humans. Although some subjects do report statistically significant improvement in pain and function from products combining glucosamine HCl and other agents, glucosamine HCl by itself appears to offer little benefit to those suffering from osteoarthritis. PMID:18225460

  2. Simultaneous Estimation of Nebivolol Hydrochloride and Valsartan using RP HPLC.

    PubMed

    Kokil, S U; Bhatia, M S

    2009-03-01

    In this study, a rapid, precise, accurate, specific and sensitive ion-paired reverse phase liquid chromatographic method has been developed for the simultaneous estimation of nebivolol hydrochloride and valsartan in their capsule formulation. The chromatographic method was standardized using a HIQ sil C(18) column (250x4.6 mm i.d., 5 mum particle size) with UV detection at 289 nm and flow rate of 1 ml/min. The mobile phase consisting of methanol:water (80:20 v/v) with addition of 0.1 percent 1-hexanesulfonic acid monohydrate sodium salt as an ion-pairing reagent was selected. The method was validated and produced accurate and precise results for estimation of the two drugs. PMID:20336202

  3. Simultaneous Estimation of Nebivolol Hydrochloride and Valsartan using RP HPLC

    PubMed Central

    Kokil, S. U.; Bhatia, M. S.

    2009-01-01

    In this study, a rapid, precise, accurate, specific and sensitive ion-paired reverse phase liquid chromatographic method has been developed for the simultaneous estimation of nebivolol hydrochloride and valsartan in their capsule formulation. The chromatographic method was standardized using a HIQ sil C18 column (250×4.6 mm i.d., 5 ?m particle size) with UV detection at 289 nm and flow rate of 1 ml/min. The mobile phase consisting of methanol:water (80:20 v/v) with addition of 0.1 percent 1-hexanesulfonic acid monohydrate sodium salt as an ion-pairing reagent was selected. The method was validated and produced accurate and precise results for estimation of the two drugs. PMID:20336202

  4. Studies on the interaction of palmatine hydrochloride with bovine hemoglobin.

    PubMed

    Liu, Baosheng; Yan, Xiaona; Cao, Shina; Chong, Baohong; Lü, Yunkai

    2014-05-01

    The interaction between bovine hemoglobin (BHb) and palmatine hydrochloride (PMT) was investigated at different temperatures using multispectroscopy, as well as the effect of common metal ions (Ca(2+) , Mg(2+) , Zn(2+) , Cu(2+) , Fe(2+) , Fe(3+) , Co(2+) , Ni(2+) ) on the BHb-PMT system. Results showed that the quenching mechanism of PMT on BHb was a static process. The electrostatic force played an important role in the conjugation reaction between BHb and PMT. The order of magnitude of the binding constants (Ka ) was 10(4) , and the number of binding sites (n) in the binary system was?~?1. The binding distance (r) was?~?2.44?nm and the primary binding for PMT was located at ?-37 tryptophan in the hydrophobic cavity of BHb. In addition, the Hill's coefficients were?~?1. Synchronous and circular dichroism spectra revealed that the microenvironment and the conformation of BHb were changed during the binding reaction. PMID:23696111

  5. Identification and characterization of potential impurities in raloxifene hydrochloride.

    PubMed

    Reddy, Reguri Buchi; Goud, Thirumani Venkateshwar; Nagamani, Nagabushanam; Kumar, Nutakki Pavan; Alagudurai, Anandan; Murugan, Raman; Parthasarathy, Kannabiran; Karthikeyan, Vinayagam; Balaji, Perumal

    2012-09-01

    During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.1%. LCMS was performed to identify the mass number of these impurities, and a systematic study was carried out to characterize them. These impurities were synthesized and characterized by spectral data, subjected to co-injection in HPLC, and were found to be matching with the impurities present in the sample. Based on their spectral data (IR, NMR, and Mass), these impurities were characterized as Raloxifene-N-Oxide [Impurity: 1]; EP impurity A [Impurity: 2]; EP impurity B [Impurity: 3]; Raloxifene Dimer [Impurity: 4]; HABT (6-Acetoxy-2-[4-hydroxyphenyl]-1-benzothiophene or 6-Hydroxy-2-[4-acetoxyphenyl]-1-benzothiophene) [Impurity: 5]; PEBE (Methyl[4-[2-(piperidin-1-yl)ethoxy

  6. Coated hydralazine hydrochloride beads for sustained release after oral administration.

    PubMed

    Mughal, M Akhlaq; Saripella, Kalyan K; Kouba, Chahinaz; Iqbal, Zafar; Neau, Steven H

    2013-09-01

    Hydralazine hydrochloride is an antihypertensive used alone or in combination with isosorbide nitrate for the treatment of congestive heart failure. Since control of blood pressure should be continuous, sustained release delivery of this drug is considered therapeutically beneficial. Core beads for oral administration of this drug were prepared by extrusion-spheronization. Using experimental design to define the coat that was applied, the core beads were coated using a fluid bed coater to different coat thickness with combinations of two commercially available products dissolved in a hydroalcoholic solvent. The coat is a film with a combination of ethylcellulose and hydroxypropylcellulose that can provide desirable release profiles. Visually spherical and rugged bead products were obtained. Two products were identified that exhibited essentially a zero order release profile following a 2-h lag time with release of greater than 70% of the drug over the next 10?h in simulated intestinal fluid. PMID:23057650

  7. Potentiometric batch and flow injection analysis of betaine hydrochloride.

    PubMed

    Badawy, Sayed S; Youssef, Ahmed F A; Mutair, Ali A

    2007-01-01

    Novel PVC membrane electrodes for the determination of betaine ion based on the formation of betaine-tetraphenylborate (Be-TPB) and betaine-phosphotungstate (Be-PT) ion-exchangers as electroactive materials are described. The sensors show a fast, stable, near Nernstian response for 6.92 x 10(-6) to 7.94 x 10(-3) M and 1.0 x 10(-4) to 1.0 x 10(-2) M betaine hydrochloride (Be.Cl) in case of Be-TPB electrode applying batch and flow injection analysis (FIA), respectively, and 2.95 x 10(-5) to 2.26 x 10(-3) M and 3.16 x 10(-5) to 1.0 x 10(-2) M in case of Be-PT electrode for batch and FIA electrodes, respectively, at 25 degrees C over the pH range of 3.5-10 with a cationic slope of 60.2 and 59.1 mV decade(-1) and a fast potential response of < or =15 s. The lower detection limits are 7.94 x 10(-6) and 3.18 x 10(-5) M Be.Cl for Be-TPB and Be-PT electrodes, respectively. Selectivity coefficient data for some common inorganic cations, sugars, amino acids and the components other than betaine, of the mixed drug investigated show negligible interference. The electrodes have been applied to the direct potentiometric determination of betaine hydrochloride in water and in a pharmaceutical preparation under batch and FIA conditions. Potentiometric titrations of Be.Cl with NaTPB and PTA as titrants were monitored with the developed betaine electrodes as an end point indicator electrode. The determination of Be.Cl shows an average recovery of 100.8% with mean relative standard deviation of 0.61%. The effect of temperature on the electrodes was also studied. PMID:17822229

  8. Sinomenine hydrochloride protects against polymicrobial sepsis via autophagy.

    PubMed

    Jiang, Yu; Gao, Min; Wang, Wenmei; Lang, Yuejiao; Tong, Zhongyi; Wang, Kangkai; Zhang, Huali; Chen, Guangwen; Liu, Meidong; Yao, Yongming; Xiao, Xianzhong

    2015-01-01

    Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs). The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN) is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl) is widely used to treat rheumatoid arthritis (RA). However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP) in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA) was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3) puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS)-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM). 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities. PMID:25625512

  9. Guanidine hydrochloride stabilization of a partially unfolded intermediate during the reversible denaturation of protein disulfide isomerase.

    PubMed Central

    Morjana, N A; McKeone, B J; Gilbert, H F

    1993-01-01

    The reversible denaturation of protein disulfide isomerase proceeds through intermediates that are stabilized by interaction with guanidine hydrochloride. At pH 7.5, the equilibrium denaturation by urea is completely reversible and the transition can be reasonably well-described by a two-state model involving only native and denatured forms. In comparison, the equilibrium denaturation by guanidine hydrochloride occurs in two distinct steps. In the presence of a low constant amount of guanidine hydrochloride (0.5-1.4 M), urea denaturation also becomes biphasic, suggesting the accumulation of an intermediate species that is stabilized by specific interaction with guanidine hydrochloride but not by high concentrations of other salts or other denaturants. PMID:8460117

  10. 78 FR 17933 - Determination That BENADRYL (diphenhydramine hydrochloride) Injection and Two Other Drug Products...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-03-25

    ...DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2013-N-0320...hydrochloride) Injection and Two Other Drug Products Were Not Withdrawn From Sale for...Safety or Effectiveness AGENCY: Food and Drug Administration, HHS. ACTION:...

  11. 78 FR 66263 - New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride; Monensin

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-11-05

    ...FDA-2013-N-0002] New Animal Drugs; Afoxolaner; Carprofen; Ceftiofur Hydrochloride...CE 1 2. Satellite Blvd., (afoxolaner), the treatment and Bldg. 500, Chewable...to read as follows: Sec. 520.43 Afoxolaner. (a) Specifications. Each...

  12. Doxapram Hydrochloride Aggravates Adrenaline-Induced Arrhythmias Accompanied by Bidirectional Ventricular Tachycardia

    PubMed Central

    Oikawa, Shota; Nomura, Hiroko; Nishio, Miki; Nagata, Rina; Hata, Tadayoshi

    2014-01-01

    Objectives. Doxapram hydrochloride is a respiratory stimulant that has an inhibitory effect on myocardial IK1 potassium channels and is thought to increase membrane instability and excitability in myocardial cells. We examined the arrhythmogenic effects of doxapram hydrochloride in a rat model of halothane adrenaline-induced arrhythmia. Methods. Thirteen female Wistar rats (12–14 weeks old) were used in the study. Animals were anesthetized with inhalation of halothane to permit observation of the effects of doxapram hydrochloride on halothane adrenaline-induced arrhythmia. Time-dependent changes in ECG repolarization characteristics (QT, QTc, JTp, JT, and Tp-e intervals) were studied. Results. Doxapram hydrochloride itself did not induce arrhythmia but did induce bidirectional ventricular tachycardia after addition of adrenaline. Conclusion. Drug-induced impairment of intracellular Ca2+ regulation caused BVT in the absence of genetic abnormalities in proteins in the sarcoplasmic reticulum. PMID:24527224

  13. Syntheses, spectroscopic characterization and thermal behavior on novel binuclear transition metal complexes of hydrazones derived from 4,6-diacetylresorcinol and oxalyldihydrazine.

    PubMed

    Emara, Adel A A; El-Sayed, Badr A; Ahmed, El-Sayed A E

    2008-03-01

    4,6-Diacetylresorcinol (DAR) serves as precursor for the formation of different hydrazone ligands, which are di-, tetra- or hexa-basic with two symmetrical sets of O(2)N tridentate, O(2)N(2) tetradentate or O(4)N(2) hexadentate chelating sites. The condensation of 4,6-diacetylresorcinol (DAR) with oxalyldihydrazine (ODH), in the molar ratio 1:1 and 1:2, yields the corresponding hydrazone, H(6)L(a) and H(4)L(b), ligands, respectively. The structures of these ligands were elucidated by elemental analyses and IR, mass, (1)H NMR and UV-vis spectra. Reactions of the hydrazone ligands with cobalt(II), nickel(II), copper(II), zinc(II), cadmium(II), iron(III) and chromium(III) ions in 1:2 molar ratio afforded the corresponding transition metal complexes. A variety of binuclear transition metal complexes were obtained in its di-, tetra- or hexa-deprotonated forms. The structures of the newly prepared complexes were identified by elemental analyses and IR, UV-vis, mass, (1)H NMR and ESR spectra, as well as, magnetic susceptibility measurements and thermal gravimetric analysis (TGA). The bonding sites are the azomethine and CO oxygen atoms in either keto or enol forms and amino nitrogen atoms, and phenolic oxygen atoms. The metal complexes exhibit different geometrical structures such as tetrahedral and octahedral arrangements. PMID:17627871

  14. Direct investigation of hydrochloride elimination from 1,2-dichlorethane by laser induced radical chain reactions

    Microsoft Academic Search

    M. Schneider

    1981-01-01

    The radical chain reaction elimination of hydrochloride from 1,2-dichlorethane was investigated in a flow reactor at a temperature from 520 to 720 K and a pressure from 60 to 600 Torr. The chain reaction was induced by KrF laser photolysis of the dichlorethane. The temperature dependence of the UV absorption spectra of dichlorethane and the products vinyl chloride and hydrochloride

  15. Molecular association of betaine and betaine hydrochloride in aqueous solutions – a study by Raman spectroscopy

    Microsoft Academic Search

    António Amorim da Costa; Joana E. S. Leite

    2001-01-01

    Raman vibrational spectroscopy, at 298 K, has been used to study the hydration of betaine hydrochloride and betaine in the concentration range 0.5–2 M. The observed changes in the internal vibrations of the solutes, namely, in the C?O, COO? and C–H stretchings, and in the components of the O–H stretching band are consonant with anionic water–betaine and betaine hydrochloride dimeric

  16. Benzydamine hydrochloride in prevention and management of pain in oral mucositis associated with radiation therapy

    SciTech Connect

    Epstein, J.B.; Stevenson-Moore, P.

    1986-08-01

    Benzydamine hydrochloride rinse reduced pain associated with radiation mucositis when it was used during the course of radiation therapy. Fewer patients using benzydamine rinse required systemic analgesics. All patients using benzydamine tolerated the rinse well and continued with regular rinsing throughout the course of radiation therapy. Benzydamine hydrochloride is currently undergoing clinical trials in the United States for application for approval from the Food and Drug Administration.

  17. HPLC study on the stability of bendamustine hydrochloride immobilized onto polyphosphoesters

    Microsoft Academic Search

    Ivanka Pencheva; Anita Bogomilova; Neli Koseva; Danka Obreshkova; Kolio Troev

    2008-01-01

    Novel water soluble polymer complexes of bendamustine hydrochloride, a bifunctional alkylating agent with antimetabolic and cytotoxic activity, were developed using biodegradable polymer carriers—poly(oxyethylene H-phosphonate), poly(methyloxyethylene phosphate) and poly(hydroxyoxyethylene phosphate). Bendamustine hydrochloride was immobilized onto polyphosphoesters via covalent, ionic and hydrogen bonding. The structure of the complexes formed was elucidated by 1H, 13C, 31P NMR and FT-IR spectroscopy. The chemical stability

  18. Sustained transdermal release of diltiazem hydrochloride through electron beam irradiated different PVA hydrogel membranes

    NASA Astrophysics Data System (ADS)

    Bhunia, Tridib; Goswami, Luna; Chattopadhyay, Dipankar; Bandyopadhyay, Abhijit

    2011-08-01

    Extremely fast release of diltiazem hydrochloride (water soluble, anti anginal drug used to treat chest pain) together with its faster erosion has been the primary problem in conventional oral therapy. It has been addressed in this paper by encapsulating the drug in electron beam irradiated various poly (vinyl alcohol) hydrogel membranes and delivering it through transdermal route. Results show excellent control over the release of diltiazem hydrochloride through these membranes subject to their physico-mechanicals.

  19. Voltammetric behaviour of drotaverine hydrochloride in surfactant media and its enhancement determination in Tween20

    Microsoft Academic Search

    Rajeev Jain; Vikas; Jahangir Ahmad Rather

    2011-01-01

    Simple, sensitive and rapid adsorptive voltammetric behaviour of drotaverine hydrochloride onto the HMDE has been explored and validated in surfactant media by using cyclic, differential pulse and square-wave voltammetry. Addition of Tween-20 to the drotaverine hydrochloride containing electrolyte enhances the reduction current signal. The voltammograms of the drug with Tween-20 in phosphate buffers of pH 2.5–11.0 exhibit a single well

  20. Optimization of the Composition and Wet Granulation Technology of Drotaverine Hydrochloride Tablets

    Microsoft Academic Search

    A. S. Gavrilov; E. V. Gusel'nikova; A. Yu. Petrov

    2005-01-01

    The process of drotaverine hydrochloride decomposition is modeled using data on the drug solution stability and the variation of RGB color coordinates of drotaverine hydrochloride tablets. The introduction of an acid into the drug composition ensures obtaining high-quality tablets of yellow-green color. The pressing of granules with dimensions below 0.6 mm and a relative humidity above 1.8% provides for a

  1. Spectrophotometric simultaneous determination of Rabeprazole Sodium and Itopride Hydrochloride in capsule dosage form

    NASA Astrophysics Data System (ADS)

    Sabnis, Shweta S.; Dhavale, Nilesh D.; Jadhav, Vijay. Y.; Gandhi, Santosh V.

    2008-03-01

    A new simple, economical, rapid, precise and accurate method for simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form has been developed. The method is based on ratio spectra derivative spectrophotometry. The amplitudes in the first derivative of the corresponding ratio spectra at 231 nm (minima) and 260 nm were selected to determine rabeprazole sodium and itopride hydrochloride, respectively. The method was validated with respect to linearity, precision and accuracy.

  2. Spectrophotometric simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form.

    PubMed

    Sabnis, Shweta S; Dhavale, Nilesh D; Jadhav, Vijay Y; Gandhi, Santosh V

    2008-03-01

    A new simple, economical, rapid, precise and accurate method for simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form has been developed. The method is based on ratio spectra derivative spectrophotometry. The amplitudes in the first derivative of the corresponding ratio spectra at 231nm (minima) and 260nm were selected to determine rabeprazole sodium and itopride hydrochloride, respectively. The method was validated with respect to linearity, precision and accuracy. PMID:17604217

  3. A study of the reaction between antimony (III) chloride and organic amine hydrochlorides

    E-print Network

    Linder, Donald Ernst

    1964-01-01

    A STUDY OF THE REACTION BET'WEEN ANTIMONY PII) CHLORIDE AND ORGANIC AMINE HYDROCHLORIDES A Thesis by Donald Ernst Linder Submitted to the Graduate College of the Texas ASM University in partial fulfillment of the requirements for the degree... of MASTER OF SCIENCE January, 1964 Major Subject: Chemistry A STUDY OF THE REACTION BETWEEN ANTIMONY (III) CHLORIDE AND ORGANIC AMINE HYDROCHLORIDES A Thesis by Donald Ernst Linder Approved as to style and content by: r rf (- &t r (Head...

  4. RP-HPLC Estimation of Imipramine Hydrochloride and Diazepam in Tablets.

    PubMed

    Srikantha, D; Raju, R R

    2015-01-01

    A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v) on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 ?g/ml for imipramine hydrochloride (r(2)=0.999) and in the range 5-30 ?g/ml for diazepam (r(2)=0.9994), respectively. The limits of detection and quantitation were 0.03 and 0.1 ?g/ml for imipramine hydrochloride and 0.02 and 0.07 ?g/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam) studies, intraday and interday precision (<2%) and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets. PMID:26180281

  5. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation

    PubMed Central

    Eassa, Bayoumy I; El-Shazly, Mohamed A

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder. It affects 20%–30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought. PMID:23103596

  6. Stability-indicating HPLC Method for Simultaneous Determination of Montelukast and Fexofenadine Hydrochloride.

    PubMed

    Pankhaniya, Mona; Patel, Parula; Shah, J S

    2013-05-01

    A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher(®) 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v), pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 ?g/ml and 24-120 ?g/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations. PMID:24082344

  7. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation.

    PubMed

    Eassa, Bayoumy I; El-Shazly, Mohamed A

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder. It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated. The aim of this study is to evaluate the efficacy, safety, tolerability, undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE. A total of 300 patients who presented with lifelong (primary) PE were included in this study. The study was performed for 28 weeks, in which placebo (starch tablet) was given for 4 weeks, and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks. Patients were divided into three equal groups, each consisting of 100 patients. The first group (A) was given tramadol hydrochloride capsule 25 mg. The second group (B) was given tramadol hydrochloride capsule 50 mg. The third group (C) was given tramadol hydrochloride capsule 100 mg. All of the 300 participants included completed the study voluntarily. The age of the patients varied from 25 to 50 years. After the treatment period, the recorded data were collected for each group and analysed. The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001). We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective, safe and tolerable, with minimal undesirable effects, and approval for this indication should be sought. PMID:23103596

  8. Nano-liposomal dry powder inhaler of Amiloride Hydrochloride.

    PubMed

    Chougule, Mahavir Bhupal; Padhi, Bijay Kumar; Misra, Ambikanandan

    2006-01-01

    The purpose of this study was to encapsulate Amiloride Hydrochloride into nano-liposomes, incorporate it into dry powder inhaler, and to provide prolonged effective concentration in airways to enhance mucociliary clearance and prevent secondary infection in cystic fibrosis. Liposomes were prepared by thin film hydration technique and then dispersion was passed through high pressure homogenizer to achieve size of nanometer range. Nano-liposomes were separated by centrifugation and were characterized. They were dispersed in phosphate buffer saline pH 7.4 containing carriers (lactose/sucrose/mannitol), and glycine as anti-adherent. The resultant dispersion was spray dried. The spray dried powders were characterized and in vitro drug release studies were performed using phosphate buffer saline pH 7.4. In vitro and in vivo drug pulmonary deposition was carried out using Andersen Cascade Impactor and by estimating drug in bronchial alveolar lavage and lung homogenate after intratracheal instillation in rats respectively. Nano-liposomes were found to have mean volume diameter of 198 +/- 15 nm, and 57% +/- 1.9% of drug entrapment. Mannitol based formulation was found to have low density, good flowability, particle size of 6.7 +/- 0.6 microm determined by Malvern MasterSizer, maximum fine particle fraction of 67.6 +/- 0.6%, mean mass aerodynamic diameter 2.3 +/- 0.1 microm, and geometric standard deviation 2.4 +/- 0.1. Developed formulations were found to have prolonged drug release following Higuchi's Controlled Release model and in vivo studies showed maximal retention time of drug of 12 hrs within the lungs and slow clearance from the lungs. This study provides a practical approach for direct lung delivery of Amiloride Hydrochloride encapsulated in liposomes for controlled and prolonged retention at the site of action from dry powder inhaler. It can provide a promising alternative to the presently available nebulizers in terms of prolonged pharmacological effect, reducing systemic side effects such as potassium retention due to rapid clearance of the drug from lungs in patients suffering from cystic fibrosis. PMID:17048511

  9. Development and validation of a HPLC method for the determination of buprenorphine hydrochloride, naloxone hydrochloride and noroxymorphone in a tablet formulation.

    PubMed

    Mostafavi, Ali; Abedi, Ghazaleh; Jamshidi, Ahmad; Afzali, Daryoush; Talebi, Mohammad

    2009-02-15

    A simple isocratic reversed-phase high-performance liquid chromatographic method (RP-HPLC) was developed for the simultaneous determination of buprenorphine hydrochloride, naloxone hydrochloride dihydrate and its major impurity, noroxymorphone, in pharmaceutical tablets. The chromatographic separation was achieved with 10 mmol L(-1) potassium phosphate buffer adjusted to pH 6.0 with orthophosphoric acid and acetonitrile (17:83, v/v) as mobile phase, a C-18 column, Perfectsil Target ODS3 (150 mm x 4.6mm i.d., 5 microm) kept at 35 degrees C and UV detection at 210 nm. The compounds were eluted isocratically at a flow rate of 1.0 mL min(-1). The average retention times for naloxone, noroxymorphone and buprenorphine were 2.4, 3.8 and 8.1 min, respectively. The method was validated according to the ICH guidelines. The validation characteristics included accuracy, precision, linearity, range, specificity, limit of quantitation and robustness. The calibration curves were linear (r>0.996) over the concentration range 0.22-220 microg mL(-1) for buprenorphine hydrochloride and 0.1-100 microg mL(-1) for naloxone hydrochloride dihydrate and noroxymorphone. The recoveries for all three compounds were above 96%. No spectral or chromatographic interferences from the tablet excipients were found. This method is rapid and simple, does not require any sample preparation and is suitable for routine quality control analyses. PMID:19084658

  10. New acyclic 1,2,4-triazole-based Schiff base hydrazone: Synthesis, characterization, spectrophotometric and computational studies

    NASA Astrophysics Data System (ADS)

    Khanmohammadi, Hamid; Erfantalab, Malihe; Azimi, Golamhassan

    2013-03-01

    A new 1,2,4-triazole-based Schiff base hydrazone with N, O, S donor set of atoms, H4L, has been prepared by condensation reaction of N,N'-bis(3-formyl-5-methylsalicylidene)ethane-1,2-diamine, H2L, with 4-amino-3-(4-pyridyl)-5-mercapto-1,2,4-triazole. The structure of H4L was characterized by using FT-IR, UV-Vis and 1H NMR spectroscopic methods as well as elemental analysis data. The formation constants of copper(II), cadmium(II), mercury(II) and silver(I) complexes of H4L in DMSO were calculated using a hard model chemometrics method applying the spectrophotometric data. The protonation constants of H4L were also measured in DMSO-water (1:10) mixture. Furthermore, 1H chemical shifts of H4L were studied by the gauge independent atomic orbital (GIAO) and continuous set of gauge transformations (CSGTs) methods at the level of density functional theory using B3LYP/6-311++G* basis sets in gas phase. The computed chemical shifts are in reasonably good agreement with the experimental data.

  11. Coordination diversity of new mononuclear ONS hydrazone with transition metals: Synthesis, characterization, molecular modeling and antimicrobial studies

    NASA Astrophysics Data System (ADS)

    Adly, Omima M. I.; Taha, A.

    2013-04-01

    The mononuclear hydrazone ligand, H2L, a condensation product of 4-amino-6-methyl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one with 2-hydroxy-1-naphthaldehyde and its metal chelates of Cu(II), Ni(II), Co(II), Zn(II), Cd(II), VO(IV) and UO2(VI) ions were synthesized and characterized using elemental analyses, spectral, magnetic and molar conductance studies as well as thermal gravimetric analysis (TGA). The physico-chemical studies support that the ligand acts as mono- or dibasic tridentate ONS donor toward metal ions forming a mononuclear square planar, tetrahedral, square pyramidal and octahedral geometrical arrangements except UO2(VI) complex in which the metal ion is octa-coordinated. The ligand field parameters, Dq, B and ? values, in the case of the cobalt and nickel complexes are calculated. The kinetics of the thermal decomposition for some metal complexes studied and their thermodynamic parameters were reported. Structural parameters of the ligand and its metal chelates have been calculated and correlated with the experimental data. The ligand and its metal chelates were screened for their antimicrobial activity against Staphylococcus aureus and Bacillus subtilis as Gram-positive bacteria, Escherichia coli and Salmonella typhimurium as Gram-negative bacteria and Candida albicans as fungus strain.

  12. Ferric-salicylaldehyde isonicotinoyl hydrazone, a synthetic iron chelate, alleviates defective iron utilization by reticulocytes of the Belgrade rat.

    PubMed

    Garrick, L M; Gniecko, K; Hoke, J E; al-Nakeeb, A; Ponka, P; Garrick, M D

    1991-03-01

    The Belgrade rat has a hypochromic, microcytic anemia inherited as an autosomal recessive mutation. Although transferrin binds normally to reticulocytes and internalizes normally, iron accumulation into cells and heme is much slower than normal. We have investigated the role of the transferrin cycle in this mutant by bypassing transferrin iron delivery with the iron chelate ferric salicylaldehyde isonicotinoyl hydrazone (Fe-SIH). Fe-SIH increases iron uptake into heme by Belgrade reticulocytes, restoring it almost to normal levels. This increase indicates that Fe-SIH delivers iron to a step in iron utilization that is after the Belgrade defect. Depleting reticulocytes of transferrin did not alter these observations. Failure to achieve above normal rates of iron incorporation could indicate damage due to chronic intracellular iron deficiency. Also, iron delivery by Fe-SIH restored globin synthesis to near-normal levels in Belgrade reticulocytes. The rates of glycine incorporation into porphyrin and heme in Belgrade reticulocytes incubated with Fe2-transferrin or Fe-SIH paralleled the rates of iron incorporation into heme. These data are consistent with the concept that iron availability limits protoporphyrin formation in rat reticulocytes. The protoporphyrin used for heme synthesis is provided by de novo synthesis and not by a pool of pre-existing protoporphyrin. The Belgrade defect occurs in the movement of iron from transferrin to a step prior to the ferrous state and insertion into heme. This defect diminishes the synthesis of heme and, consequently, that of protoporphyrin and globin. PMID:2022700

  13. Hydrothermal synthesis, structures, luminescence and magnetic properties of Zn(II) and Cu(II) complexes with new hydrazone ligand

    NASA Astrophysics Data System (ADS)

    Zheng, Chang-zheng; Wang, Liang; Liu, Juan

    2012-06-01

    Two new complexes [Zn(HL)2(py)2] (1) and [Cu(HL)]2 (2) have been synthesised from a bidentate Schiff base ligand HL (benzylidene acetophenone benzoyl hydrazone). The crystal structures of complex 1 and complex 2 were determined by single-crystal X-ray diffraction. The data indicate that: the complex 1 crystallizes in the monoclinic space group P2(1)/n, with a (nm) = 1.35816(8), b (nm) = 2.39486(13), c (nm) = 1.41368(8), ? (°) = 90, ? (°) = 96.0840(10), ? (°) = 90, Z = 4. The complex 2 crystallizes in the triclinic space group P-1, with a (nm) = 1.02483(8), b (nm) = 1.35797(11), c (nm) = 1.38271(11), ? (°) = 71.5020(10), ? (°) = 78.5850(10), ? (°) = 74.3110(10), Z = 1. Moreover, the unsaturated coordination site of metal ion is occupied by secondary ligand of pyridine. The mononuclear units in 1 and 2 are packed through weak Csbnd H⋯? and ?-? interactions respectively. The results of analytical, IR and TG analysis studies are presented in this paper. Both the ligand and complex 1 show fluorescence in DMF solutions at room temperature. The complex 2 variable-temperature (300-1.8 K) magnetic test show that there is ferromagnetic intramolecular interaction and weak antiferromagnetic intermolecular interaction.

  14. Spacer-dependent structural and physicochemical diversity in copper(II) complexes with salicyloyl hydrazones: a monomer and soluble polymers.

    PubMed

    Matoga, Dariusz; Szklarzewicz, Janusz; Grybo?, Ryszard; Kurpiewska, Katarzyna; Nitek, Wojciech

    2011-04-18

    Complexation of copper(II) with a series of heterodonor chelating Schiff bases (LL) of salicylic acid hydrazide and aliphatic or cycloaliphatic ketones affords soluble one-dimensional (1D) metallopolymers containing Schiff bases as bridging ligands. Single-crystal X-ray diffraction results reveal nanometer-sized metallopolymeric wires [Cu(?-LL)(2)](n) with off-axis linkers and a zigzag geometry. Octahedrally coordinated copper centers, exhibiting a Jahn-Teller distortion, are doubly bridged by two Schiff-base molecules in the ?(2)-?(1),?(2) coordination mode. The use of dibutylketone with long alkyl chains as a component for Schiff base formation leads to a distorted square planar monomeric copper(II) complex [Cu(LL)(2)], as evidenced by its X-ray crystal structure. The compounds are characterized by elemental analyses and IR and UV-vis spectroscopy, as well as magnetic susceptibility and cyclic voltammetry measurements. Electrochemical studies on the complexes reveal an existence of polymeric and monomeric forms in solution and the dependence of Cu(II)/Cu(I) reduction potentials on alkyl groups of salicyloyl hydrazone ligands. Polymeric complexes form conducting films on Pt electrodes upon multicycle potential sweeps. PMID:21428390

  15. Synthesis, characterization, DNA binding properties, fluorescence studies and antioxidant activity of transition metal complexes with hesperetin-2-hydroxy benzoyl hydrazone.

    PubMed

    Li, Yong; Yang, Zheng-Yin; Wang, Ming-Fang

    2010-07-01

    A novel Schiff-base ligand (H(5)L), hesperetin-2-hydroxy benzoyl hydrazone, and its copper (II), zinc (II) and nickel (II) complexes (M.H(3)L) [M(II) = Cu, Zn, Ni], have been synthesized and characterized. The ligand and Zn (II) complex exhibit green and blue fluorescence under UV light and the fluorescent properties of the ligand and Zn (II) complex in solid state and different solutions were investigated. In addition, DNA binding properties of the ligand and its metal complexes have been investigated by electronic absorption spectroscopy, fluorescence spectra, ethidium bromide displacement experiments, iodide quenching experiments, salt effect and viscosity measurements. Results suggest that all the compounds bind to DNA via an intercalation binding mode. Furthermore, the antioxidant activity of the ligand and its metal complexes was determined by superoxide and hydroxyl radical scavenging methods in vitro. The metal complexes were found to possess potent antioxidant activity and be better than the free ligand alone and some standard antioxidants like vitamin C and mannitol. PMID:20352308

  16. Discovery of Novel Orally Active Anti-Inflammatory N-Phenylpyrazolyl-N-Glycinyl-Hydrazone Derivatives That Inhibit TNF-? Production

    PubMed Central

    Lacerda, Renata B.; da Silva, Leandro L.; de Lima, Cleverton K. F.; Miguez, Eduardo; Miranda, Ana Luisa P.; Laufer, Stefan A.; Barreiro, Eliezer J.; Fraga, Carlos A. M.

    2012-01-01

    Herein, we describe the synthesis and pharmacological evaluation of novel N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that were designed as novel prototypes of p38 mitogen-activated protein kinase (MAPK) inhibitors. All of the novel synthesized compounds described in this study were evaluated for their in vitro capacity to inhibit tumor necrosis factor ? (TNF-? production in cultured macrophages) and in vitro MAPK p38? inhibition. The two most active anti-TNF-? derivatives, (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-((4-(2-morpholinoethoxy)naphthalen-1-yl)methylene)acetohydrazide (4a) and (E)-2-(3-tert-butyl-1-phenyl-1H-pyrazol-5-ylamino)-N’-(4-chlorobenzylidene)acetohydrazide (4f), were evaluated to determine their in vivo anti-hyperalgesic profiles in carrageenan-induced thermal hypernociception model in rats. Both compounds showed anti-inflammatory and antinociceptive properties comparable to SB-203580 used as a standard drug, by oral route at a dose of 100 µmol/kg. This bioprofile is correlated with the ability of NAH derivatives (4a) and (4f) suppressing TNF-? levels in vivo by 57.3 and 55.8%, respectively. PMID:23056531

  17. Synthesis and in vitro evaluation of new nitro-substituted thiazolyl hydrazone derivatives as anticandidal and anticancer agents.

    PubMed

    Alt?ntop, Mehlika Dilek; Özdemir, Ahmet; Turan-Zitouni, Gülhan; Ilg?n, Sinem; Atl?, Özlem; Demirci, Fatih; Kaplanc?kl?, Zafer As?m

    2014-01-01

    Fourteen new thiazolyl hydrazone derivatives were synthesized and evaluated for their anticandidal activity using a broth microdilution assay. Among the synthesized compounds, 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene)hydrazinyl]-4-(4-fluorophenyl)thiazole and 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene) hydrazinyl]-4-(4-methoxyphenyl)thiazole were found to be the most effective antifungal compounds against Candida utilis, with a MIC value of 250 µg/mL, when compared with fluconazole (MIC=2 µg/mL). Additionally, the synthesized compounds were evaluated for their in vitro cytotoxic effects on the MCF-7 and NIH/3T3 cell lines. As a result, 2-[2-((5-(4-chloro-2-nitrophenyl)furan-2-yl)methylene)hydrazinyl]-4-(4-chlorophenyl)thiazole was identified as the most promising anticancer compound against MCF-7 cancer cells due to its inhibitory effects (IC50=125 µg/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC50>500 µg/mL). PMID:25232704

  18. Ranitidine Hydrochloride-loaded Ethyl Cellulose and Eudragit RS 100 Buoyant Microspheres: Effect of pH Modifiers

    PubMed Central

    Kotagale, N. R.; Parkhe, A. P.; Jumde, A. B.; Khandelwal, H. M.; Umekar, M. J.

    2011-01-01

    A floating type of dosage form of ranitidine hydrochloride in the form of microspheres capable of floating on simulated gastric fluid was prepared by solvent evaporation technique. Microspheres prepared with ethyl cellulose, Eudragit® RS100 alone or in combination were evaluated for percent yield, drug entrapment, percent buoyancy and drug release and the results demonstrated satisfactory performance. Microspheres exhibited ranitidine hydrochloride release influenced by changing ranitidine hydrochloride-polymer and ranitidine hydrochloride-polymer-polymer ratio. Incorporation of a pH modifier has been the usual strategy employed to enhance the dissolution rate of weakly basic drug from floating microspheres. Further citric acid, fumaric acid, tartaric acid were employed as pH modifiers. Microspheres prepared with ethyl cellulose, Eudragit® RS100 and their combination that showed highest release were utilized to study the effect of pH modifiers on ranitidine hydrochloride release from microspheres which is mainly affected due to modulation of microenvironmental pH. In vitro release of ranitidine hydrochloride from microspheres into simulated gastric fluid at 37° showed no significant burst effect. However the amount of release increased with time and significantly enhanced by pH modifiers. 15% w/w concentration of fumaric acid provide significant drug release from ranitidine hydrochloride microspheres prepared with ranitidine hydrochloride:ethyl cellulose (1:3), ranitidine hydrochloride:Eudragit® RS100 (1:2) and ranitidine hydrochloride:ethyl cellulose:Eudragit® RS100 (1:2:1) whereas citric acid, tartaric acid showed significant cumulative release at 20% w/w. In all this study suggest that ethyl celluose, Eudragit® RS100 alone or in combination with added pH modifiers can be useful in floating microspheres which can be proved beneficial to enhance the bioavailability of ranitidine hydrochloride. PMID:23112396

  19. Structure and vibrational spectra of pyridine betaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Szafran, Miros?aw; Koput, Jacek; Baran, Jan; G?owiak, Tadeusz

    1997-12-01

    The crystal structure of pyridine betaine hydrochloride (PBET·HCl) was determined by X-ray diffraction to be monoclinic, space group {P2 1}/{c} with a = 8.533(2) Å, b = 9.548(2) Å, c = 10.781(2) Å, ? = 107.228(3)° and Z = 4. Betaine is protonated and the carboxyl group forms a hydrogen bond with the chloride ion: O·Cl - distance is 2.928(3) Å. The interaction of pyridine betaine (PBET) with HCl was examined by ab initio self-consistent field (SCF), second-order Møller-Plesset (MP2) and density functional theory (DFT) methods using the 6-31G(d,p) basis set. Two minima are located in the potential surface at the SCF level (PBET?H +·Cl - and PBET·H?Cl, with the latter being 1.2 kcal mol -1 lower in energy) and only one minimum (PBET·H?Cl) at the MP2 and DFT levels. The molecular parameters of PBET?H +·Cl -, computed by the SCF method, reproduce the corresponding experimental data. The computed vibrational frequencies of PBET?H +·Cl - resemble correctly the experimental vibrational spectrum in the solid state. The root-mean-square (r.m.s.) deviations between the experimental and calculated SCF frequencies are 65 cm -1 for all bands and 15 cm -1 without the ?Cl?H band. All measured IR bands were interpreted in terms of the calculated vibrational models.

  20. Calculation of the vibrational spectra of betaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Szafran, Miroslaw; Koput, Jacek

    1997-02-01

    The molecular geometries of betaine hydrochloride, BET·HCl, and free protonated betaine, BET·H +, were calculated with the 6-31G(d,p) basis set at the SCF, MP2 and DFT levels of theory. At the SCF level, the minimum energy corresponds to the ionic pair, B +Htctdot;A -, however, the equilibrium Otctdot;Cl distance is 0.14 Å shorter than the X-ray value. Inclusion of the correlation effects, both at the MP2 and DFT levels, predicts a minimum energy for the molecular complex, Btctdot;H-A, with the equilibrium Otctdot;Cl distance close to the experimental value. The frequencies and intensities of the vibrational bands of BET·HCl, BET·DCl and BET·H + were calculated at the SCF and DFT levels and compared with the solid IR spectra. All measured IR bands were interpreted in term of the calculated vibrational modes. The rms deviations between the experimental and calculated SCF frequencies were 21 and 29 cm -1 for BET·HCl and BET·DCl, respectively. The computed band intensities agree qualitatively with the experimental data. The coupling of the CO stretching and OH bending modes are discussed. The summation bands are probably enhanced in intensity by Fermi resonance with the fundamentals responsible for the main ?(OH) (?(OD) absorption region.

  1. Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride

    NASA Astrophysics Data System (ADS)

    Amin, A. S.; Dessouki, H. A.

    2002-10-01

    A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 ?g ml -1, respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml -1 for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method.

  2. Hydrocolloid carriers with filler inclusion for diltiazem hydrochloride release.

    PubMed

    Gal, A; Nussinovitch, A

    2007-01-01

    Hydrocolloid beads based on agarose, alginate (both 3%, w/w), or gellan (2%, w/w) were produced to study their potential as drug carriers. The beads included various fillers: talc, kaolin, calcium carbonate, potato, or corn starch (10%, w/w). After gelation, the carriers were subjected to either freeze- or vacuum-drying. The dried carriers were spheroids. The diameters of freeze- and vacuum-dried carriers ranged from 2.4 to 4.1 mm and 1.5 to 2.8 mm, respectively. The porosity values of the freeze-dried carriers were significantly higher than those of their vacuum-dried counterparts. Scanning electron microscopy (SEM) revealed that all dried carriers included internal voids that were partially occupied by the filler particles. Upon their introduction into simulated gastric fluid (3 h), followed by 6 h in intestinal fluid, all carriers were stable and underwent swelling. Release profiles of diltiazem hydrochloride from different carriers were obtained during immersion in dissolution medium. Filler inclusion (but not the type of filler) contributed to the stability of the carriers and prolonged the time of drug release (6.5-8.5 h) relative to the faster drug release from carriers that contained no filler (3.5 h). In summary, alginate, agar, and gellan beads with filler inclusion may be useful for slow drug release. PMID:17031844

  3. Enhanced topical delivery of terbinafine hydrochloride with chitosan hydrogels.

    PubMed

    Ozcan, Ipek; Abaci, Ozlem; Uztan, Alev Haliki; Aksu, Buket; Boyacio?lu, Hayal; Güneri, Tamer; Ozer, Ozgen

    2009-01-01

    Chitosan-based carriers have important potential applications for the administration of drugs. In the present study, topical gel formulations of terbinafine hydrochloride (T-HCl) were prepared using different types of chitosan at different molecular weight, and the antifungal inhibitory activity was evaluated to suggest an effective formulation for the treatment of fungal infections. The characteristics of gel formulations were determined with viscosity measurements and texture profile analysis. Stability studies were performed at different temperatures during 3 months. The ex vivo permeation properties were studied through rat skin by using Franz diffusion cells. The antifungal inhibitory activity of formulations on Candida species and filamentous fungi was also examined with agar-cup method. The microbiological assay was found suitable for determination of in vitro antifungal activity of T-HCl. A marketed product was used to compare the results. The antifungal activity of T-HCl significantly increased when it was introduced into the chitosan gels. A higher drug release and the highest zone of inhibition were obtained from gels prepared with the lowest molecular weight chitosan (Protasan UP CL 213) compared to that of other chitosan gels and marketed product. These results indicated the advantages of the suggested formulations for topical antifungal therapy against Candida species and filamentous fungi. PMID:19662536

  4. Ocular poloxamer-based ciprofloxacin hydrochloride in situ forming gels.

    PubMed

    Mansour, Mai; Mansour, Samar; Mortada, Nahed D; Abd Elhady, Seham S

    2008-07-01

    The purpose of this study was to develop poloxamer-based in situ gelling formulations of ciprofloxacin hydrochloride (HCl) aiming at prolonging corneal contact time, controlling drug release, enhancing ocular bioavailability, and increasing patient compliance. The in situ forming gels were prepared using different concentrations of poloxamer 407 (P407) and poloxamer 188 (P188). Mucoadhesives such as hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were added to the formulations to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their in vitro drug release, sol-gel transition temperature, rheological behavior, and mucoadhesion force. The in vivo antimicrobial efficacy of selected ciprofloxacin HCl in situ gelling formulations was studied on infected rabbit's eyes and compared with that of the marketed conventional eye drops. The gelation temperature of the prepared formulations ranged from 28.00 to 34.03 degrees C. Increasing the concentrations of P407, HPMC, and HEC increased the viscosity and mucoadhesion force of the preparations and decreased the in vitro drug release. Ciprofloxacin HCl in situ forming gel formulae composed of P407/P188/HPMC (18/13/1.5%, wt/wt), and P407/P188/HEC (18/13/0.5%, wt/wt) showed optimum release and mucoadhesion properties and improved ocular bioavailability as evidenced by an enhanced therapeutic response compared with the marketed conventional eye drops. PMID:18612913

  5. Adsorption behavior of epirubicin hydrochloride on carboxylated carbon nanotubes.

    PubMed

    Chen, Zhe; Pierre, Dramou; He, Hua; Tan, Shuhua; Pham-Huy, Chuong; Hong, Hao; Huang, Jilong

    2011-02-28

    The aim of this study was to understand the interaction between carboxylated carbon nanotubes (c-CNTs) and anticancer agents and evaluate the drug-loading ability of c-CNTs. We prepared carboxylated multi-walled carbon nanotubes (c-MWNTs) with nitric acid treatment, then evaluated the adsorption ability of c-MWNTs as adsorbents for loading of the anticancer drug, epirubicin hydrochloride (EPI), and investigated the adsorption behavior of EPI on c-MWNTs. Unmodified multi-walled carbon nanotubes (MWNTs) and single-walled carbon nanotubes (SWNTs) were included as comparative adsorbents. The results showed that carbon nanotubes were able to form supramolecular complexes with EPI via ?-? stacking and possessed favorable loading properties as drug carriers. The Freundilich adsorption model was successfully employed to describe the adsorption process. Because of the high surface area and hydrogen bonding, c-MWNTs' adsorption efficiency was the highest and the most stable and their drug-loading capacity was superior to that of MWNTs. With the increase of pH, the adsorption capacity of EPI on the c-MWNTs increased. Low-temperature facilitated the adsorption. More rapid EPI adsorption rate and higher drug-loading ability were observed from c-MWNTs with smaller diameter. Moreover, the adsorption kinetics of EPI on c-MWNTs could be well depicted by using the pseudo-second-order kinetic model. PMID:21145959

  6. Lipomer of doxorubicin hydrochloride for enhanced oral bioavailability.

    PubMed

    Benival, Derajram M; Devarajan, Padma V

    2012-02-28

    The present study discusses design of doxorubicin hydrochloride (Dox) loaded lipid based nanocarrier (LIPOMER) for oral delivery. High entrapment (>90 %) and high loading (38.11 ± 0.37 %w/w) of hydrophilic Dox in lipid nanocarrier of polyglyceryl-6-distearate was achieved using poly(methyl vinyl ether-co-maleic anhydride) (Gantrez AN 119) and a modified nanoprecipitation method. Dox-LIPOMER revealed nanosize (314 ± 16.80 nm) and negative zeta potential (-25.00 ± 2.41 mV). Dox-LIPOMER exhibits sustained release in vitro and was influenced by ionic strength of dissolution medium. DSC and XRD studies suggested amorphous nature of Dox in LIPOMER. TEM revealed spherical morphology of Dox-LIPOMER. Dox-LIPOMER was stable up to 12 months at 25 °C/60 % RH. A 384 % enhancement in oral bioavailability compared to Dox solution was observed following Dox-LIPOMER administration at 10 mg/kg body weight. Superoxide dismutase (SOD), catalase (CAT) and malondialdehyde (MDA) assay data of heart and kidney tissues of rats treated with Dox-LIPOMER were comparable with untreated rats. Dox-LIPOMER represents a potential safe drug delivery system for oral administration. PMID:22155412

  7. Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.

    PubMed

    Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

    2015-07-01

    Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24?h and pulsed delivery of drug for 3 days (8?h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs. PMID:25482587

  8. Stability of revex, nalmefene hydrochloride injection, in injectable solutions.

    PubMed

    Murthy, S S; Brittain, H G

    1996-11-01

    The short-term stability of Revex, nalmefene hydrochloride injection, was determined in a number of diluents commonly employed for intravenous use. An HPLC method was used to follow the potency of the diluted solutions, and was fully validated for its intended concentration range prior to its use. Dilutions of Revex were prepared separately in 0.9% sodium chloride injection, 0.45% sodium chloride injection, 5% dextrose injection, 5% dextrose and 0.45% sodium chloride injection, lactated Ringer's injection, 5% dextrose and lactated Ringer's injection and 5% sodium hydrogencarbonate injection. Each admixture was stored at 4 degrees C, room temperature (21 degrees C) and 40 degrees C, with samples being tested after storage at each temperature for 0, 24, 48 and 72 h. Defining stability as the retention of at least 95% of the initial drug concentration at the end of the storage period, it was concluded that the diluted solutions of Revex were uniformly stable for up to 72 h in all of the injectable solutions maintained at either 4, 21 or 40 degrees C. PMID:8933423

  9. Release Kinetics of Papaverine Hydrochloride from Tablets with Different Excipients

    PubMed Central

    Kasperek, Regina; Polski, Andrzej; Zimmer, ?ukasz; Poleszak, Ewa

    2014-01-01

    Abstract The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release. PMID:25853076

  10. [Determination of dopamine hydrochloride by a reverse flow injection chemiluminescence method].

    PubMed

    Wang, Shu-Hao; Du, Ling-Yun; Wei, Xin-Ting; Wang, Liang-Yu; Zhuang, Hui-Sheng

    2005-05-01

    A novel chemiluminescence system coupled with a reverse flow injection analysis for the determination of dopamine hydrochloride was presented. It is based on th e strong quench effect of dopamine hydrochloride on the chemiluminescence reaction between luminol and hexacyanoferrate(III) under alkaline condition. Various factors affecting the chemiluminescence intensity of the system were investigated. The possible mechanism of the proposed method was also studied. The decrease of chemiluminescence intensity was linear with the dopamine hydrochloride content in the range of 2.0 x 10(-9) -8.0 x 10(-7) g x mL(-1), the detection limit of the method was 1.14 x 10(-9) g x mL(-1), and the relative standard deviation was 0.99% (4.0 x 10(-7) g x mL(-1), n = 11). It was successfully used for the determination of the content of dopamine hydrochloride in dopamine hydrochloride injection. PMID:16128061

  11. Design and Development of Polyethylene Oxide Based Matrix Tablets for Verapamil Hydrochloride

    PubMed Central

    Vidyadhara, S.; Sasidhar, R. L. C.; Nagaraju, R.

    2013-01-01

    In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

  12. Fasudil hydrochloride could promote axonal growth through inhibiting the activity of ROCK

    PubMed Central

    Xiao, Wei-Dong; Yu, Ai-Xi; Liu, Dan-Li

    2014-01-01

    Objective: This study aims to investigate the neuroprotective effect of Rho kinase inhibitor fasudil hydrochloride in ischemia/reperfusion injury N2a neuron. Methods: In vitro, N2a cells induced by ischemia and ischemia-reperfusion were treated with fasudil hydrochloride, cell damage was analyzed by MTT. On the other hand, the cytoskeleton of N2a cells was scanned through immunofluorescence techniques by Confocal Laser Microscopy which stained with FITC-phalloidin for F-actin visualization. Results: The activation of ROCK-II increased significantly in the damaged local during the following phase of ischemia/reperfusion injury. Ischemia induced a striking reorganization of actin cytoskeleton with a weakening of fluorescent intensity of the peripheral filament actin bands and formation of the long and thick stress fibers, but pretreatment of Fasudil hydrochloride could reversed the changes of ultra-structure on the cellular surface. MTT assay showed that Fasudil hydrochloride could prolong the survival time of the N2a cells after mimic ischemia-reperfusion for 24 h. Conclusions: The activation of ROCK-II has an exceptional hoist after ischemia/reperfusion injury, it is likely to induce the collapse of the growth cone through MLC-P. Fasudil hydrochloride could promote axonal growth on inhibitory of ROCK activity. PMID:25337198

  13. Formulation and Evaluation of S-(-)-Amlodipine Besylate and Nebivolol Hydrochloride Tablets

    PubMed Central

    Shaikh, S.A; Shaikh, S.S; Shahi, S.R.; Shookur, M.A.; Reddy, L.K; Padalkar, A.N; Thube, Mahesh

    2010-01-01

    The objective of the present study was to develop a tablet formulation of S-(-)-amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-)- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity. The study was also carried out to design a suitable dissolution medium for S-(-) - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(-) - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(-) - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile. PMID:22247846

  14. Formulation and evaluation of s-(-)-amlodipine besylate and nebivolol hydrochloride tablets.

    PubMed

    Shaikh, S A; Shaikh, S S; Shahi, S R; Shookur, M A; Reddy, L K; Padalkar, A N; Thube, Mahesh

    2010-04-01

    The objective of the present study was to develop a tablet formulation of S-(-)-amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-)- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity.The study was also carried out to design a suitable dissolution medium for S-(-) - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(-) - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(-) - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile. PMID:22247846

  15. Hypercrosslinked poly(styrene-co-divinylbenzene) resin as a specific polymeric adsorbent for purification of berberine hydrochloride from aqueous solutions.

    PubMed

    Li, Yin; Cao, Ruofan; Wu, Xiaofei; Huang, Jianhan; Deng, Shuguang; Lu, Xiuyang

    2013-06-15

    A hypercrosslinked poly(styrene-co-divinylbenzene) resin (TEPA) was synthesized and characterized as a specific polymeric adsorbent for concentrating berberine hydrochloride from aqueous solutions. Three organic molecules of different sizes (2-naphthol, berberine hydrochloride, and Congo red) were used as target molecules to elucidate the molecular sieving effect of the TEPA adsorbent. Because the TEPA adsorbent has a pore structure consisting mainly of micropores and mesopores, the adsorption of 2-naphthol from aqueous solutions is very efficient due to the micropore filling effect. The adsorption of berberine hydrochloride mostly takes place in the mesopores as well as macropores, while the adsorption of Congo red mainly occurs in the macropores. The smaller adsorbate molecule (2-naphthol) reaches the adsorption equilibrium much faster than the larger ones (berberine hydrochloride and Congo red). An adsorption breakthrough experiment with an aqueous solution containing 2-naphthol and berberine hydrochloride demonstrated that the TEPA adsorbent could effectively remove 2-naphthol from berberine hydrochloride at 0-107 BV (bed volume, 1 BV=10 ml), and the berberine hydrochloride concentration was increased from 66.7% to 99.4%, suggesting that this polymeric adsorbent is promising for purifying berberine hydrochloride and similar alkaloids from herbal plant extracts. PMID:23582901

  16. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Guzman, David Sanchez-Migallon; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  17. 76 FR 53908 - Determination That OPANA ER (Oxymorphone Hydrochloride) Extended-Release Tablets, 7.5 Milligrams...

    Federal Register 2010, 2011, 2012, 2013, 2014

    2011-08-30

    ...Oxymorphone Hydrochloride) Extended- Release Tablets, 7.5 Milligrams and 15 Milligrams...hydrochloride (HCl)) extended-release tablets, 7.5 milligrams (mg) and 15 mg...for oxymorphone HCl extended- release tablets, 7.5 mg and 15 mg, if all other...

  18. Development and in vitro evaluation of chitosan-based transdermal drug delivery systems for the controlled delivery of propranolol hydrochloride

    Microsoft Academic Search

    D. Thacharodi; K. Panduranga Rao

    1995-01-01

    Membrane permeation-controlled transdermal drug delivery systems were prepared using the natural polymer, chitosan. An adhesive sealing technique was used to construct the devices. Propranolol hydrochloride was selected as the model drug for the present study. Chitosan membranes with different permeability to propranolol hydrochloride obtained by controlled cross-linking with glutaraldehyde were used to regulate the drug release in the devices. Chitosan

  19. Spectrophotometric microdetermination of nefopam, mebevrine and phenylpropanolamine hydrochloride in pharmaceutical formulations using alizarins

    NASA Astrophysics Data System (ADS)

    Shama, S. A.; Amin, A. S.

    2004-07-01

    Simple and rapid spectrophotometric procedures have been established for quantitation of nefopam hydrochloride (NF) mebevrine hydrochloride (MB) and phenylpropanolamine hydrochloride (PP). The procedures are based on the reaction between the examined drugs (NF, MB and PP) and alizarin (I), alizarin red S (II), alizarin yellow G (III) and quinalizarin (IV) producing ion-pair complexes which can be measured at the optimum wavelength. The optimization of the reaction conditions is investigated. Beer's law is obeyed in the concentration ranges 0.5-30.0 ?g ml -1. The molar absorptivity, Sandell sensitivity, detection and quantification limits are also calculated. The correlation coefficient was ?0.9988 ( n=6) with a relative standard deviation (R.S.D.) of ?1.3, for six determinations of 20 ?g ml -1. The methods are successfully applied to the determination of NF, MB and PP in their pharmaceutical formulations.

  20. A pilot study of acotiamide hydrochloride hydrate in patients with detrusor underactivity

    PubMed Central

    Sugimoto, Koichi; Akiyama, Takahiro; Shimizu, Nobutaka; Matsumura, Naoki; Hayashi, Taiji; Nishioka, Tsukasa; Uemura, Hirotsugu

    2015-01-01

    Aim To investigate the clinical efficacy of acotiamide hydrochloride hydrate in patients with detrusor underactivity. Methods We measured the post-void residual urinary volume in 19 patients with underactive bladders. All these patients had been under treatment with distigmine bromide and were prescribed acotiamide hydrochloride hydrate at a dose of 100 mg three times daily for 2 weeks. Results Compared with the post-void residual urinary volume value at baseline (161.4±90.0 mL) a statistically significant reduction was observed at the end of treatment (116.3±63.1 mL) (P=0.006). The drug was generally well tolerated by the majority of patients. Conclusion Maybe, acotiamide hydrochloride hydrate showed clinical efficacy in patients with underactive bladders and may, therefore, be used alternatively in patients who do not respond sufficiently to distigmine bromide.

  1. US Food and Drug Administration approval of ciprofloxacin hydrochloride for management of postexposure inhalational anthrax.

    PubMed

    Meyerhoff, Andrea; Albrecht, Renata; Meyer, Joette M; Dionne, Peter; Higgins, Karen; Murphy, Dianne

    2004-08-01

    In August 2000, the US Food and Drug Administration (FDA) approved ciprofloxacin hydrochloride (Cipro; Bayer) for management of postexposure inhalational anthrax. This was the first antimicrobial drug approved by the FDA for use in treating an infection due to a biological agent used intentionally. The terrorist attacks of 2001 involving anthrax underscore the imperative that safe and effective drugs to manage such infections be readily available in the United States. The approval of ciprofloxacin hydrochloride, which was made on the basis of a surrogate human marker of efficacy, made extensive use of data from an animal model of disease. This represents a new direction in the development of efficacy data in support of drug approval and facilitates the availability of those drugs for which there is an urgent need. This article presents the scientific data and regulatory mechanism that supported the approval of ciprofloxacin hydrochloride for management of postexposure of inhalational anthrax. PMID:15306995

  2. Photoacoustic imaging to detect rat brain activation after cocaine hydrochloride injection

    NASA Astrophysics Data System (ADS)

    Jo, Janggun; Yang, Xinmai

    2011-03-01

    Photoacoustic imaging (PAI) was employed to detect small animal brain activation after the administration of cocaine hydrochloride. Sprague Dawley rats were injected with different concentrations (2.5, 3.0, and 5.0 mg per kg body) of cocaine hydrochloride in saline solution through tail veins. The brain functional response to the injection was monitored by photoacoustic tomography (PAT) system with horizontal scanning of cerebral cortex of rat brain. Photoacoustic microscopy (PAM) was also used for coronal view images. The modified PAT system used multiple ultrasonic detectors to reduce the scanning time and maintain a good signal-to-noise ratio (SNR). The measured photoacoustic signal changes confirmed that cocaine hydrochloride injection excited high blood volume in brain. This result shows PAI can be used to monitor drug abuse-induced brain activation.

  3. Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.

    PubMed

    Nanjwade, Basavaraj K; Deshmukh, Rucha V; Gaikwad, Kishori R; Parikh, Kemy A; Manvi, F V

    2012-06-01

    The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h. PMID:22015966

  4. LC determination of octreotide acetate in compound formulations of Sandostatin ® and diamorphine hydrochloride

    Microsoft Academic Search

    N Kyaterekera; J. N. A Tettey; G. G Skellern; D. G Watson; J Urie; J. R McDade; H Fielding

    1999-01-01

    The determination of octreotide acetate in compound formulations of Sandostatin® and diamorphine hydrochloride by RP–LC is described. Octreotide acetate, diamorphine hydrochloride and their respective degradants, [des-Thr-ol8]-octreotide and 6-O-acetylmorphine, were baseline resolved using a Lichrospher-60 RP-select B column with a mobile phase composition of acetonitrile\\/phosphate buffer (pH 7.4, 20 mM) (35:65 v\\/v) with UV detection at 210 nm. The method is

  5. The influence of relative humidity and temperature on stability of moexipril hydrochloride in solid phase.

    PubMed

    Stanisz, Beata

    2004-01-01

    Kinetic and thermodynamic parameters of the decomposition of moexipril hydrochloride in solid phase in the absence and presence of humidity were calculated. The evaluation of stability of moexipril hydrochloride was followed by the HPLC method. The applied method was validated (evaluation of the following parameters: selectivity, linearity, precision, limit of detection (LOD), limit of quantification (LOQ) and repeatability). The effect of humidity on the stability of MHCl in solid phase at 363 K was described by the equation: In ki = ax + b = (0.0676 +/- 0.016) . RH% - (15.53+/-0.78). Identification of degradation products of MHCl were carried out by the HPLC-MS method. PMID:15493289

  6. Flow injection with inhibited chemiluminescence method for the determination of dopamine hydrochloride.

    PubMed

    Wang, Shuhao; Du, Lingyun; Wang, Liangyu; Zhuang, Huisheng

    2004-02-01

    A simple rapid and accurate flow injection inhibitory chemiluminescence method has been developed for the determination of dopamine hydrochloride based on its inhibition of the chemiluminescence from the luminol-potassium hexacyanoferrate(III) system. The linear range of determination is 4.0 x 10(-9) - 4.0 x 10(-7) g ml(-1) for dopamine hydrochloride and the detection limit is 1.14 x 10(-9) g ml(-1). The method has been applied to determine the content of dopamine in pharmaceutical preparation with satisfactory results. PMID:15055958

  7. Disruption of zinc and copper interactions with A?(1-40) by a non-toxic, isoniazid-derived, hydrazone: a novel biometal homeostasis restoring agent in Alzheimer's disease therapy?

    PubMed

    Hauser-Davis, R A; de Freitas, L V; Cukierman, D S; Cruz, W S; Miotto, M C; Landeira-Fernandez, J; Valiente-Gabioud, A A; Fernández, C O; Rey, N A

    2015-05-13

    Disruptions of biometal-A?(1-40) interactions by an isoniazid-derived hydrazone, INHHQ, were demonstrated via in vitro NMR titrations. The compound has adequate theoretical BBB absorption properties, assessed by in silico studies. In vivo acute toxicity assays indicate that INHHQ is innocuous up to 300 mg kg(-1), showing potential as an anti-Alzheimer's drug. PMID:25860559

  8. Discovery of Selective Small-Molecule Inhibitors for the ?-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety.

    PubMed

    Catrow, J Leon; Zhang, Yongqiang; Zhang, Min; Ji, Haitao

    2015-06-11

    Acyl hydrazone is an important functional group for the discovery of bioactive small molecules. This functional group is also recognized as a pan assay interference structure. In this study, a new small-molecule inhibitor for the ?-catenin/Tcf protein-protein interaction (PPI), ZINC02092166, was identified through AlphaScreen and FP assays. This compound contains an acyl hydrazone group and exhibits higher inhibitory activities in cell-based assays than biochemical assays. Inhibitor optimization resulted in chemically stable derivatives that disrupt the ?-catenin/Tcf PPI. The binding mode of new inhibitors was characterized by site-directed mutagenesis and structure-activity relationship studies. This series of inhibitors with a new scaffold exhibits dual selectivity for ?-catenin/Tcf over ?-catenin/cadherin and ?-catenin/APC PPIs. One derivative of this series suppresses canonical Wnt signaling, downregulates the expression of Wnt target genes, and inhibits the growth of cancer cells. This compound represents a solid starting point for the development of potent and selective ?-catenin/Tcf inhibitors. PMID:25985283

  9. Investigation of the azo-hydrazone tautomeric equilibrium in an azo dye involving the naphthalene moiety by UV-vis spectroscopy and quantum chemistry

    NASA Astrophysics Data System (ADS)

    Ünal, Arslan; Eren, Bilge; Eren, Erdal

    2013-10-01

    Photophysical properties of the azo-hydrazone tautomerism of Eriochrome Blue Black B (1-(1-hydroxy-2-naphthylazo)-2-naphthol-4-sulphonic acid) in DMF, MeCN and water were investigated using UV-visible spectroscopy and quantum chemical calculations. The optimized molecular structure parameters, relative energies, mole fractions, electronic absorption spectra and HOMO-LUMO energies for possible stable tautomeric forms of EBB were theoretically calculated by using hybrid density functional theory, (B3LYP) methods with 6-31G(d) basis set level and polarizable continuum model (PCM) for solvation effect. The effects of varying pH-, dye concentration-, solvent-, temperature-, and time-dependences on the UV-vis spectra of Eriochrome Blue Black B were also investigated experimentally. The calculations showed that the dye exhibited acid-base, azo-hydrazone and aggregate equilibria in DMF solution, while the most probably preferred form in MeCN solution was azo form. Thermodynamic parameters of dimerization reaction in DMF solution proved that entropy was the driving force of this reaction.

  10. Conformational Properties of Polyglutamine Sequences in Guanidine Hydrochloride Solutions

    PubMed Central

    Khan, Md. Khurshid Alam; Bowler, Bruce E.

    2012-01-01

    Two sets of iso-1-cytochrome c variants have been prepared with N-terminal insertions of pure polyglutamine, i.e., PolyQ variants, or polyglutamine interrupted with lysine every sixth residue, i.e., Gln-rich variants. The polymer properties of these pure polyGln or Gln-rich sequences have been evaluated using equilibrium and kinetic His-heme loop formation methods for loop sizes ranging from 22 to 46 in 1.5, 3.0, and 6.0 M guanidine hydrochloride (GdnHCl). In 6.0 M GdnHCl, the scaling exponent, ?3, for the pure polyGln sequences, is ?1.7—significantly less than ?3 ? 2.15 for the Gln-rich sequences. The stability of the His-heme loops becomes progressively greater for the pure polyGln sequences relative to the Gln-rich sequences as GdnHCl concentration decreases from 6.0 to 1.5 M. Thus, the context of the sequence effects the polymer properties of Gln repeats even in denaturing concentrations of GdnHCl. Comparison of data for the Gln-rich variants with previous results for Gly-rich and Ala-rich variants shows that ?3 ? 2.2 for the Gln-rich, Gly-rich, and Ala-rich sequences in 6.0 M GdnHCl, whereas ?3 remains unchanged at 3.0 M GdnHCl concentration for the Gln-rich and Ala-rich sequences but decreases to ?1.7 for the Gly-rich sequences. Thus, the polymer properties of Gln-rich and Ala-rich sequences are less sensitive to solvent quality in denaturing solutions of GdnHCl than Gly-rich sequences. Evaluation of Flory’s characteristic ratio, Cn, for the Gln-rich and Ala-rich sequences relative to the Gly-rich sequences shows that Gln-rich sequences are stiffer than Ala-rich sequences at both 3.0 and 6.0 M GdnHCl. PMID:23199927

  11. Colon-specific drug delivery for mebeverine hydrochloride.

    PubMed

    Omar, Samia; Aldosari, Basmah; Refai, Hanan; Gohary, Omaimah Al

    2007-12-01

    Mebeverine Hydrochloride (MB-HCl), an effective spasmolytic drug, was formulated as CODES. A colon-specific drug delivery technology CODES was designed to avoid the inherent problems associated with pH- or time-dependent systems. To achieve more protection and control of drug release, MB-HCl was prepared as microspheres and compressed as core tablets of CODES (modified CODES). The core tablets contained the drug either in free form [Formula 1 (F(1))], or as microspheres with 2 different polymer:drug:lactulose ratios (1:1:0.5 [Formula 2 (F(2))] and 2:1:0.5 [Formula 3 (F(3))]. The release profiles of the coated CODES systems were compared with uncoated compressed tablets. The uncoated tablet showed a drug release of 94% after 1 h in simulated gastric condition (pH = 1.2). The release characteristics of the coated systems revealed that the enteric coating (Eudragit L(100)) prevented any drug release in simulated gastric or duodenal conditions in the first 3 h (pH 1.2-6.1), after which drug was slightly liberated in simulated intestinal fluid (pH 7.4) {Phase 1 (P1)}. After 4 h the pH was adjusted to 7 and beta-glucose-oxidase was added, which is an enzyme produced by enterobacteria present in the colon. The acid-soluble coat (Eudragit)E(100)) dissolved and the drug release suddenly increased to reach 95, 72 and 60.4% for F(1)-F(3), respectively. IR spectrum study showed a covalent bond between the drug and the polymer in the formulae F(2) and F(3) resulting in the sustained drug release from the microspheres with a significant difference (p>0.05) to F(1). The findings were confirmed by in vivo investigation using X-ray images for Guinea pigs ingested tablets containing barium sulphate (F(4)), where the tablet began to disintegrate after 10 h of tablet intake. The results of the study indicated that MB-HCl CODES colon-specific drug delivery can act as a successful trigger for drug targeting in the colon. Furthermore, a sustained release of the drug can be achieved from modified CODES containing the drug in the form of microspheres. PMID:18041637

  12. RADIOCARBON-LABELED COMPOUNDS PRODUCED BY THE NEUTRON IRRADIATION OF GUANIDINE HYDROCHLORIDE

    Microsoft Academic Search

    T. W. Lapp; R. W. Kiser

    1963-01-01

    Crystalline guanidine hydrochloride was irradiated by neutrons and ; studies were made on the Cu-labeled compounds present when the target material ; was dissolved in water. The results indicate that the cyanamide radical plays an ; important role in the production of the final chemical species incorporating the ; recoil C¹⁴ atom. The production of the cyanamide radical may occur

  13. Effects of zilpaterol hydrochloride on blood gas, electrolyte balance, and pH in feedlot cattle

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The objective of this study was to examine the effects of zilpaterol hydrochloride (ZH) on blood gas, electrolyte balance and pH in feedlot cattle. Black-hided steers and heifers (n=96) were sourced from a commercial feedlot and transported to the Texas Tech University Beef Center in New Deal, TX. C...

  14. Clinical picture of combination therapy (metronidazole sustained release film with minocycine hydrochloride) in periodontitis.

    PubMed

    Yang, Zhiliang

    2015-01-01

    This paper aimed to study the effect of metronidazole sustained-release film combined with minocycline hydrochloride on treating periodontitis. 138 patients with chronic periodontitis were collected and randomly divided into control group and observation group (each of 69 cases). Patients in control group were treated by using minocycline hydrochloride, while those in observation group were treated using metronidazole sustained-release film with minocycline hydrochloride, and each group with 4 weeks of treatment. Then we observed the periodontal mend matters, therapeutic effect, adverse reaction and relapse situation of patients in two groups. Results showed that compared with the prior treatment, the gingival index, dental plaque index, odontoseisis index and pocket depth of patients in two groups was significantly reduced. Moreover, the reduction range in observation group was significantly larger and the curative effect was superior to that in control group. Therefore, metronidazole sustained-release film combined minocycline hydrochloride can evidently improve patients' periodontal status, enhance drug therapeutic effect. It has less adverse reaction and low relapse rate, thus is worthy of clinical promotion. PMID:25631504

  15. Performance of finishing beef steers in response to anabolic implant and zilpaterol hydrochloride supplementation

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Our objectives were to evaluate the dose/payout pattern of trenbolone acetate (TBA) and estradiol-17b (E2) implants and feeding of zilpaterol hydrochloride (ZH) on performance and carcass characteristics of finishing beef steers. A randomized complete block design was used with a 3 × 2 factorial arr...

  16. A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).

    ERIC Educational Resources Information Center

    Villegas, Orlando; And Others

    This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…

  17. Stability Indicating RP-HPLC Estimation of Nebivolol Hydrochloride in Pharmaceutical Formulations.

    PubMed

    Shah, D A; Bhatt, K K; Mehta, R S; Baldania, S L; Gandhi, T R

    2008-09-01

    A simple, specific, accurate and stability indicating reversed phase liquid chromatographic method was developed for the determination of nebivolol hydrochloride in tablet dosage forms. A phenomenex Gemini C-18, 5 ?m column having 250×4.6 mm i.d., with mobile phase containing methanol: acetonitrile: 0.02 M potassium dihydrogen phosphate (60:30:10, v/v/v; pH 4.0) was used. The retention time of nebivolol hydrochloride was 2.6 min. The linearity for nebivolol hydrochloride was in the range of 0.2-10 ?g/ml. The recovery was found to be in the range of 98.68-100.86%. The detection limit and quantification limit were found to be 0.06 ?g/ml and 0.2 ?g/ml, respectively. Nebivolol stock solutions were subjected to acid, alkali and neutral hydrolysis, chemical oxidation and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. The proposed method was validated and successfully applied to the estimation of nebivolol hydrochloride in tablet formulations. PMID:21394254

  18. Stability Indicating RP-HPLC Estimation of Nebivolol Hydrochloride in Pharmaceutical Formulations

    PubMed Central

    Shah, D. A.; Bhatt, K. K.; Mehta, R. S.; Baldania, S. L.; Gandhi, T. R.

    2008-01-01

    A simple, specific, accurate and stability indicating reversed phase liquid chromatographic method was developed for the determination of nebivolol hydrochloride in tablet dosage forms. A phenomenex Gemini C-18, 5 ?m column having 250×4.6 mm i.d., with mobile phase containing methanol: acetonitrile: 0.02 M potassium dihydrogen phosphate (60:30:10, v/v/v; pH 4.0) was used. The retention time of nebivolol hydrochloride was 2.6 min. The linearity for nebivolol hydrochloride was in the range of 0.2-10 ?g/ml. The recovery was found to be in the range of 98.68-100.86%. The detection limit and quantification limit were found to be 0.06 ?g/ml and 0.2 ?g/ml, respectively. Nebivolol stock solutions were subjected to acid, alkali and neutral hydrolysis, chemical oxidation and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. The proposed method was validated and successfully applied to the estimation of nebivolol hydrochloride in tablet formulations. PMID:21394254

  19. Selective Differential Spectrophotometric Methods for Determination of Niclosamide and Drotaverine Hydrochloride

    Microsoft Academic Search

    H. G. Daabees

    2000-01-01

    Differential (?A), second derivative (?D) and third derivative (?D) differential ultraviolet spectrophotometric methods have been presented for the quantitation of niclosamide and drotaverine hydrochloride in pure forms and in their pharmaceutical formulations. For niclosamide, the method is based on measuring ?? A, ? ?D, A ?D of niclosamide in alkaline solutions against their neutral ethanolic solutions as blanks. For drotaverine

  20. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma

    Microsoft Academic Search

    Y. S. El-Saharty; F. H. Metwaly; M. Refaat; S. Z. El-Khateeb

    The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro–PTA) or ammonium reineckate (Dro–R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors,

  1. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma

    Microsoft Academic Search

    Y. S. El-Saharty; F. H. Metwaly; M. Refaat; S. Z. El-Khateeb

    2006-01-01

    The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro-PTA) or ammonium reineckate (Dro-R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors,

  2. Carbon Paste Electrode for the Potentiometric Flow Injection Analysis of Drotaverine Hydrochloride in Serum and Urine

    Microsoft Academic Search

    Yousry M. Issa; Hosny Ibrahim; Hazem M. Abu-Shawish

    2005-01-01

    A carbon paste electrode for drotaverine hydrochloride (DvCl) was prepared and fully characterized in terms of composition, life span, usable pH range, response time and temperature. The electrode was applied to the potentiometric determination of drotaverinium ions in pharmaceutical preparations and biological fluids in steady state and flow injection conditions (FIA). The electrode is based on a mixture of two

  3. Sensitive spectrophotometric determination of metoclopramide hydrochloride in dosage forms and spiked human urine using vanillin

    Microsoft Academic Search

    O. Zenita Devi; K. Basavaiah; K. B. Vinay; H. D. Revanasiddappa

    A new spectrophotometric method which is simple, sensitive, selective and rapid is described for the determination of metoclopramide hydrochloride (MCP) in bulk drug and in dosage forms using vanillin as the chromogenic agent. The method is based on the condensation reaction between primary aromatic amine group present in MCP with aromatic aldehyde, vanillin to produce an intense yellow colored product.

  4. Nano-liposomes of entrapment lidocaine hydrochloride on in vitro permeability of narcotic.

    PubMed

    Sun, Nenghong; Zhu, Yanyan; Yuan, Lei; Lang, Bao

    2015-01-01

    In order to explore two kinds of nano-liposomes in lidocaine hydrochloride nano-liposomes on in vitro permeability of drug, and conduct comparison and analysis, this paper investigates cumulative infiltration situation of lidocaine hydrochloride flexible nano-liposomes and ordinary nano-liposomes by using modified Franz diffusion pool on mice vitro skin. Cumulative osmotic quantity of lidocaine hydrochloride flexible nano-liposomes for 9h was higher than ordinary nano-liposomes. (t)max(Maximum osmotic quantity time) of lidocaine hydrochloride flexible nano-liposomes and ordinary nano-liposomes in mice skin was 5 and 60min, the former (C)max (maximum dosage time) was 1.2 times of the latter. Drug was not found in mice plasma of ordinary nano-liposomes group, traces of drugs was detected in 0.5 and 1h in flexible nano-liposomes group, but the concentration was lower than the effective concentration. Compared with the classic skin transparent promoter and ordinary liposome, flexible nano-liposomes have more advantages, but its stability is less than ordinary nano-liposomes because of the addition of surface active substance. Flexible nano-liposomes have great development potential as a carrier of transdermal drug delivery field. PMID:25631510

  5. Application of Thiocyanate Complex of Titanium (IV) to the Extractive Spectrophotometric Determination of Amitriptyline Hydrochloride

    Microsoft Academic Search

    W. Misiuk; M. Tarasiewicz

    1998-01-01

    Amitriptyline hydrochloride reacts in acidic medium with the thiocyanate complex of titanium (IV) forming a yellow ion- association compound, insoluble in water but fairly soluble in a mixture of chloroform and butyl alcohol (4:1). The formation and extraction conditions of the compound are described. The compound was characterized by UV, VIS, IR and H NMR spectrometry. The colored compound exhibits

  6. Simultaneous HPTLC Determination of Rabeprazole and Itopride Hydrochloride From Their Combined Dosage Form.

    PubMed

    Suganthi, A; John, Sofiya; Ravi, T K

    2008-01-01

    A simple, precise, sensitive, rapid and reproducible HPTLC method for the simultaneous estimation of the rabeprazole and itopride hydrochloride in tablets was developed and validated. This method involves separation of the components by TLC on precoated silica gel G60F254 plate with solvent system of n-butanol, toluene and ammonia (8.5:0.5:1 v/v/v) and detection was carried out densitometrically using a UV detector at 288 nm in absorbance mode. This system was found to give compact spots for rabeprazole (Rf value of 0.23 0.02) and for itopride hydrochloride (Rf value of 0.75+/-0.02). Linearity was found to be in the range of 40-200 ng/spot and 300-1500 ng/spot for rabeprazole and itopride hydrochloride. The limit of detection and limit of quantification for rabeprazole were 10 and 20 ng/spot and for itopride hydrochloride were 50 and 100 ng/spot, respectively. The method was found to be beneficial for the routine analysis of combined dosage form. PMID:20046748

  7. Simultaneous HPTLC Determination of Rabeprazole and Itopride Hydrochloride From Their Combined Dosage Form

    PubMed Central

    Suganthi, A.; John, Sofiya; Ravi, T. K.

    2008-01-01

    A simple, precise, sensitive, rapid and reproducible HPTLC method for the simultaneous estimation of the rabeprazole and itopride hydrochloride in tablets was developed and validated. This method involves separation of the components by TLC on precoated silica gel G60F254 plate with solvent system of n-butanol, toluene and ammonia (8.5:0.5:1 v/v/v) and detection was carried out densitometrically using a UV detector at 288 nm in absorbance mode. This system was found to give compact spots for rabeprazole (Rf value of 0.23 0.02) and for itopride hydrochloride (Rf value of 0.75±0.02). Linearity was found to be in the range of 40-200 ng/spot and 300-1500 ng/spot for rabeprazole and itopride hydrochloride. The limit of detection and limit of quantification for rabeprazole were 10 and 20 ng/spot and for itopride hydrochloride were 50 and 100 ng/spot, respectively. The method was found to be beneficial for the routine analysis of combined dosage form. PMID:20046748

  8. Clinical effects of the new phosphorus binder, bixalomer in hemodialysis patients switched from sevelamer hydrochloride.

    PubMed

    Gen, Shikou; Sasaki, Takaya; Saito, Kanako; Nobe, Kanako; Nodaira, Yuka; Ikeda, Naofumi

    2014-06-01

    It has been reported that sevelamer hydrochloride, which is often used as a polymer phosphorus (P) binder for managing serum P concentration in dialysis patients, causes gastrointestinal adverse effects such as constipation, etc. The reason for this is thought to be that sevelamer hydrochloride has high water absorption, causing it to absorb water and swell in the gastrointestinal tract. In June 2012, the new polymer P binder bixalomer was launched in Japan. Since bixalomer has low swelling due to water absorption, it can be expected to alleviate adverse effects in the gastrointestinal system. In our study, for 21 cases of maintenance hemodialysis patients undergoing treatment with sevelamer hydrochloride at our hospital, the P binder was switched from sevelamer hydrochloride to the same dosage of bixalomer, and the concentrations of serum P, corrected calcium (Ca) and whole parathyroid hormone (PTH) before and one month after the switch were compared. In addition, gastrointestinal symptoms (acid reflux, abdominal pain, indigestion, diarrhea and constipation) were evaluated before and after the switch using a questionnaire based on the Japanese version of the Gastrointestinal Symptom Rating Scale (GSRS). By switching to bixalomer, serum P concentration was significantly reduced (P=0.024), but there were no significant changes observed for serum corrected Ca and whole PTH. Furthermore, there were no significant changes observed for all five of the evaluation items of the GSRS, before and after the switch. These results suggest that although bixalomer can more potently reduce the serum P concentration than sevelamer hydrochloride, there were no significant differences in the effects of both P binders on the gastrointestinal symptoms. PMID:24975889

  9. Effect of remacemide hydrochloride on subarachnoid hemorrhage-induced vasospasm in rabbits.

    PubMed

    Zuccarello, M; Lewis, A I; Upputuri, S; Farmer, J B; Anderson, D K

    1994-12-01

    The purpose of this study was to assess the role of an excitatory amino acid (EAA) receptor antagonist (remacemide hydrochloride) in a rabbit model of subarachnoid hemorrhage (SAH)-induced cerebral vasospasm. Cerebral angiograms were performed on 22 rabbits pre-SAH and 72 h post-SAH: 6 rabbits received an injection of mock cerebrospinal fluid (1 ml/kg) into the cisterna magna (group I, the control group); 6 rabbits were subjected to SAH but received no treatment (group II); autologous blood (1 ml/kg) from the central ear artery was injected into the cisterna magna of these rabbits; 6 rabbits were subjected to SAH (1 ml/kg) and treated with intraperitoneal (IP) bolus injections of remacemide hydrochloride (15 mg/kg) every 12 h beginning 30 minutes after SAH (group III); and 4 rabbits were not subjected to SAH but received IP bolus injections of remacemide hydrochloride every 12 h (group IV). Digital subtraction angiography was used to measure the diameter of the basilar artery. At 72 h post-SAH, vasospasm was evident in all untreated rabbits. The diameter of the basilar artery was reduced significantly below pre-SAH levels by 35.3 +/- 5.8% (mean +/- standard error of the mean). Treatment with remacemide hydrochloride significantly ameliorated vasospasm (27.3 +/- 5.4%, p < 0.001). These findings suggest that in this model EAAs may cooperate in the genesis of SAH-induced cerebral vasospasm and that NMDA receptor antagonism with remacemide hydrochloride can partially prevent the SAH-induced vasospasm of a large cerebral artery. PMID:7723068

  10. Preparation and the in vitro evaluation of nanoemulsion system for the transdermal delivery of granisetron hydrochloride.

    PubMed

    Zheng, Wen-wu; Zhao, Ling; Wei, Yu-meng; Ye, Yun; Xiao, Shun-han

    2010-08-01

    The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4+/-1.5 to 82.4+/-0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1 : 1) and 10% NMP showed that the skin permeation rate was the highest (85.39+/-2.90 microg/cm(2)/h) and enhancement of drug permeability was 4.1-fold for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8+/-2.86 microg/cm(2)) with the shortest lag time (0.11+/-0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms. PMID:20686252

  11. Synthesis and antitumor mechanisms of a copper(ii) complex of anthracene-9-imidazoline hydrazone (9-AIH).

    PubMed

    Qin, Qi-Pin; Liu, Yan-Cheng; Wang, Hai-Lu; Qin, Jiao-Lan; Cheng, Feng-Jie; Tang, Shang-Feng; Liang, Hong

    2015-07-01

    A new anthracycline derivative, anthracene-9-imidazoline hydrazone (9-AIH), was synthesized and selected as an antitumor ligand to afford a copper(ii) complex of 9-AIH, cis-[Cu(II)Cl2(9-AIH)] (). Complex was structurally characterized by IR, elemental analysis, ESI-MS and single crystal X-ray diffraction analysis. By MTT assay, it was revealed that showed overall a higher in vitro cytotoxicity than 9-AIH towards a panel of human tumour cell lines, with IC50 values from 0.94-3.68 ?M, in which the BEL-7404 cell line was the most sensitive to . By spectral analyses and gel electrophoresis, the DNA binding affinity of 9-AIH and was determined. 9-AIH was suggested to bind with DNA in an intercalative mode, with a quenching constant of 1.04 × 10(4) M(-1) on the EB-DNA complex. While for , both intercalative and covalent binding modes were suggested. By flow cytometry, was found to block the cell cycle of BEL-7404 cells in a dose-dependent mode, in which it induced the G2/M phase arrest at 0.5 ?M and induced the S phase arrest at higher concentrations of 1.0 or 2.0 ?M. From the cellular morphological observations under different fluorescence probe staining, a dose-dependent manner of to induce cell apoptosis in the late stage was suggested. Comparatively, equivalent apoptotic cells, respectively, in the early and late stages were found when incubated with 2.0 ?M of 9-AIH. The mitochondrial membrane potential measured by JC-1 staining and the ROS generation in cells detected using a DCFH-DA probe suggested that the cell apoptosis induced by might undergo the ROS-related mitochondrial pathway. Accordingly, the mutant p53 expression was found to be suppressed and the caspase cascade (caspase-9/3) was consequently activated by . This action mechanism for in the BEL-7404 cells was unique and was not found in the presence of 9-AIH under the same conditions, indicating their different antitumor mechanism. Furthermore, the in vivo acute toxicity of tested on mice indicated that should be a high cytotoxic antitumor agent, with the LD50 value in the range of 32-45 mg kg(-1), which is much higher than that of 9-AIH. From the above results, the central Cu(ii) of in the coordinated mode with 9-AIH was believed to play a key role in exerting both the high cytotoxicity and the effective antitumor mechanism. PMID:25904543

  12. Synthesis of water-soluble azomethines based on the substituted benzaldehydes of vanillin series and D-(+)-glucosamine hydrochloride

    Microsoft Academic Search

    E. A. Dikusar; V. I. Potkin; N. G. Kozlov

    2009-01-01

    A preparative method for the synthesis of water-soluble azomethines by the reaction of substituted benzaldehydes of vanillin\\u000a series with D-(+)-glucosamine hydrochloride in the presence of potassium hydrogen carbonate in methanol was developed.

  13. Antioxidant and antimicrobial activity of Maillard reaction products from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems.

    PubMed

    Wu, Shuping; Hu, Jiao; Wei, Liuting; Du, Yumin; Shi, Xiaowen; Zhang, Lina

    2014-04-01

    The structure, UV absorbance, browning intensity, fluorescence changes, antioxidant activity and antimicrobial assessment of Maillard reaction products (MRPs) derived from xylan with chitosan, chitooligomer, glucosamine hydrochloride and taurine model systems were evaluated. The results revealed that all MRPs had similar infrared spectra and molecular structures. MRPs from different model systems on the UV absorbance at 294 nm after heated 90 min and browning intensity at 420 nm showed the similar law: xylan-taurine > xylan-glucosamine hydrochloride > xylan-chitooligomer > xylan-chitosan, and the order of DPPH scavenging activity of MRPs was as follows: xylan-chitosan > xylan-chitooligomer > xylan-glucosamine hydrochloride > xylan-taurine, which revealed that the properties of MRPs were closely related to molecular weight of model systems. Moreover, the highest radical scavenging activity of MRPs from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems was 65.9%, 63.7%, 46.4% and 42.5%, respectively. PMID:24262546

  14. Reagents for Astatination of Biomolecules. 5. Evaluation of hydrazone linkers in 211At- and 125I-labeled closo-decaborate(2-) conjugates of Fab? as a means of decreasing kidney retention

    PubMed Central

    Wilbur, D. Scott; Chyan, Ming-Kuan; Hamlin, Donald K.; Nguyen, Holly; Vessella, Robert L.

    2011-01-01

    Evaluation of monoclonal antibody (MAb) fragments (e.g. Fab?, Fab or engineered fragments) as cancer-targeting reagents for therapy with the ?-particle emitting radionuclide astatine-211 (211At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the 211At label, generally a meta- or para-[211At]astatobenzoyl conjugate, on MAb Fab? fragments can be dramatically improved by use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled MAb Fab? conjugates appears to result in retention of the radioactivity in kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of acid-cleavable hydrazone between the Fab? and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete polyethylene glycol (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole or methyl) to provide varying acid-sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated (125I or 131I), then conjugated with an anti-PSMA Fab? (107-1A4 Fab?). Biodistributions of the five radioiodinated Fab? conjugates were obtained in nude mice at 1, 4 and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab? through a non-cleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver and spleen that were similar to those obtained with directly radioiodinated Fab? (i.e. no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a benzoate substituent on the hydrazone was chosen for study with 211At. That reagent was conjugated with 107-1A4 Fab?, then labeled (separately) with 125I and 211At. The radiolabeled Fab? conjugates were coinjected into nude mice bearing LNCaP human tumor xenografts, and biodistribution data was obtained at 1, 4 and 24 h pi. Tumor targeting was achieved with both 125I- and 211At-labeled Fab?, but the 211At-labeled Fab? reached a higher concentration (25.56 ± 11.20 vs. 11.97 ± 1.31 %ID/g). Surprisingly, while the 125I-labeled Fab? was cleared from kidney similar to earlier studies, the 211At-labeled Fab? was not (i.e. kidney conc. for 125I vs. 211At; 4h: 13.14 ± 2.03 ID/g vs. 42.28 ± 16.38 %D/g, 24h: 4.23 ± 1.57 ID/g vs. 39.52 ± 15.87 %ID/g). Since the Fab? conjugate is identical in both cases except for the radionuclide, it seems likely that the difference in tissue clearance seen is due to an effect that 211At has on either the hydrazone cleavage or on the retention of a metabolite. Results from other studies in our laboratory suggest that the latter case is most likely. The hydrazone linkers tested do not provide the tissue clearance sought for 211At, so additional hydrazones linkers will be evaluated. However, the results support the use of hydrazone linkers when Fab? conjugated with closo-decaborate(2-) reagents are radioiodinated. PMID:21513347

  15. Reagents for astatination of biomolecules. 5. Evaluation of hydrazone linkers in (211)At- and (125)I-labeled closo-decaborate(2-) conjugates of Fab' as a means of decreasing kidney retention.

    PubMed

    Wilbur, D Scott; Chyan, Ming-Kuan; Hamlin, Donald K; Nguyen, Holly; Vessella, Robert L

    2011-06-15

    Evaluation of monoclonal antibody (mAb) fragments (e.g., Fab', Fab, or engineered fragments) as cancer-targeting reagents for therapy with the ?-particle emitting radionuclide astatine-211 ((211)At) has been hampered by low in vivo stability of the label and a propensity of these proteins localize to kidneys. Fortunately, our group has shown that the low stability of the (211)At label, generally a meta- or para-[(211)At]astatobenzoyl conjugate, on mAb Fab' fragments can be dramatically improved by the use of closo-decaborate(2-) conjugates. However, the higher stability of radiolabeled mAb Fab' conjugates appears to result in retention of radioactivity in the kidneys. This investigation was conducted to evaluate whether the retention of radioactivity in kidney might be decreased by the use of an acid-cleavable hydrazone between the Fab' and the radiolabeled closo-decaborate(2-) moiety. Five conjugation reagents containing sulfhydryl-reactive maleimide groups, a hydrazone functionality, and a closo-decaborate(2-) moiety were prepared. In four of the five conjugation reagents, a discrete poly(ethylene glycol) (PEG) linker was used, and one substituent adjacent to the hydrazone was varied (phenyl, benzoate, anisole, or methyl) to provide varying acid sensitivity. In the initial studies, the five maleimido-closo-decaborate(2-) conjugation reagents were radioiodinated ((125)I or (131)I), then conjugated with an anti-PSMA Fab' (107-1A4 Fab'). Biodistributions of the five radioiodinated Fab' conjugates were obtained in nude mice at 1, 4, and 24 h post injection (pi). In contrast to closo-decaborate(2-) conjugated to 107-1A4 Fab' through a noncleavable linker, two conjugates containing either a benzoate or a methyl substituent on the hydrazone functionality displayed clearance rates from kidney, liver, and spleen that were similar to those obtained with directly radioiodinated Fab' (i.e., no conjugate). The maleimido-closo-decaborate(2-) conjugation reagent containing a benzoate substituent on the hydrazone was chosen for study with (211)At. That reagent was conjugated with 107-1A4 Fab', then labeled (separately) with (125)I and (211)At. The radiolabeled Fab' conjugates were coinjected into nude mice bearing LNCaP human tumor xenografts, and biodistribution data were obtained at 1, 4, and 24 h pi. Tumor targeting was achieved with both (125)I- and (211)At-labeled Fab', but the (211)At-labeled Fab' reached a higher concentration (25.56 ± 11.20 vs 11.97 ± 1.31%ID/g). Surprisingly, while the (125)I-labeled Fab' was cleared from kidney similar to earlier studies, the (211)At-labeled Fab'was not (i.e., kidney conc. for (125)I vs (211)At; 4 h, 13.14 ± 2.03 ID/g vs 42.28 ± 16.38%D/g; 24 h, 4.23 ± 1.57 ID/g vs 39.52 ± 15.87%ID/g). Since the Fab' conjugate is identical in both cases except for the radionuclide, it seems likely that the difference in tissue clearance seen is due to an effect that (211)At has on either the hydrazone cleavage or on the retention of a metabolite. Results from other studies in our laboratory suggest that the latter case is most likely. The hydrazone linkers tested do not provide the tissue clearance sought for (211)At, so additional hydrazones linkers will be evaluated. However, the results support the use of hydrazone linkers when Fab' conjugated with closo-decaborate(2-) reagents are radioiodinated. PMID:21513347

  16. Pharmacokinetics of hydromorphone hydrochloride after intravenous and intramuscular administration of a single dose to American kestrels (Falco sparverius)

    USGS Publications Warehouse

    Sanchez-Migallon Guzman, David; KuKanich, Butch; Drazenovich, Tracy L.; Olsen, Glenn H.; Paul-Murphy, Joanne R.

    2014-01-01

    Conclusion and Clinical Relevance—Results indicated hydromorphone hydrochloride had high bioavailability and rapid elimination after IM administration, with a short terminal half-life, rapid plasma clearance, and large volume of distribution in American kestrels. Further studies regarding the effects of other doses, other administration routes, constantrate infusions, and slow release formulations on the pharmacokinetics of hydromorphone hydrochloride and its metabolites in American kestrels may be indicated.

  17. Relative bioavailability and bioequivalence of metforphin hydrochloride extended-released and immediate-released tablets in healthy Chinese volunteers

    Microsoft Academic Search

    Jun Li; Yong Jin; Ting-Yu Wang; Xiong-Wen Lü; Yuan-Hai Li

    2007-01-01

    Summary  The aim of the present study was to investigate the relative bioavailability and bioequivalence of a new tablet formulation\\u000a of metformin hydrochloride with reference to a standard product in healthy Chinese adult male volunteers. Two randomized,\\u000a comparative, two-way crossover studies were therefore conducted. In study 1, which was a single-dose study, 20 subjects received\\u000a 1000 mg metformin hydrochloride lest product

  18. Resonance Rayleigh scattering spectra, non-linear scattering spectra of tetracaine hydrochloride–erythrosin system and its analytical application

    Microsoft Academic Search

    Mingyou Qin; Shaopu Liu; Zhongfang Liu; Xiaoli Hu

    2009-01-01

    The interaction between erythrosine (ET) and tetracaine hydrochloride (TA) was studied by resonance Rayleigh scattering (RRS), frequency doubling scattering (FDS) and second-order scattering (SOS) combining with absorption spectrum. In a weak acidic medium of Britton–Robinson (BR) buffer solution of pH 4.5, erythrosine reacted with tetracaine hydrochloride to form 1:1 ion-association complex. As a result, the new spectra of RRS, SOS

  19. A highly selective turn-on fluorescent probe for hypochlorous acid based on hypochlorous acid-induced oxidative intramolecular cyclization of boron dipyrromethene-hydrazone.

    PubMed

    Chen, Wei-Chieh; Venkatesan, Parthiban; Wu, Shu-Pao

    2015-07-01

    A BODIPY-based fluorescent probe, HBP, was developed for the detection of hypochlorous acid based on the specific hypochlorous acid-promoted oxidative intramolecular cyclization of heterocyclic hydrazone in response to the amount of HOCl. The reaction is accompanied by a 41-fold increase in the fluorescent quantum yield (from 0.004 to 0.164). The fluorescence intensity of the reaction between HOCl and HBP is linear in the HOCl concentration range of 1-8?M with a detection limit of 2.4nM (S/N=3). Confocal fluorescence microscopy imaging using RAW264.7 cells showed that the new probe HBP could be used as an effective fluorescent probe for detecting HOCl in living cells. PMID:26043093

  20. The K-band ?max values of the ultraviolet-visible spectra of some hydrazones in ethanol by a TD-DFT/PCM approach

    NASA Astrophysics Data System (ADS)

    Lu, Shih-I.

    2010-07-01

    We presented the time-dependent density functional theory calculated ultraviolet-visible (UV-vis) spectra for derivatives of phenylhydrazones, semicarbazones and pyrrole hydrazones in ethanol. We employed the B3LYP, PBE0, CAM-B3LYP, LC- ?PBE, LC-PBE and ?B97X-D functionals. We gauged the performance of the six hybrid functionals of choice in determination of the K-band ?max values of the UV-vis spectra. The PCM-TD-PBE0/6-311+G(2d,p)//PCM-PBE0/6-311G(d,p) approach provided the smallest error with an average absolute deviation limited to 14 nm. We also investigated the impacts of including explicit solvent molecules and considering vibrational envelope with the Franck-Condon Herzberg-Teller method.

  1. The role of co-spray-drying procedure in the preformulation of intranasal propranolol hydrochloride.

    PubMed

    Ambrus, Rita; Gergely, Matild; Zvonar, Alenka; Szabó-Révész, Piroska; Sipos, Emese

    2014-01-01

    The use of dry powder formulations presents an alternative through which to achieve better deposition and residence time in the nasal cavity, increased stability and possible absorption enhancement. The most important factors involved in the preformulation are particle size and physical stability. Propranolol hydrochloride a model drug was subjected to spray-drying technology to form an intranasal dry powder. Particle size reduction of the drug was carried out by integration (spray-drying) methods, using different excipients. The micrometric properties were characterized by size and morphology. The structure was determined through the use of differential scanning calorimetry, X-ray powder diffraction and Fourier transform infrared spectroscopy investigations. It was concluded that the intranasal dry powder formulation of propranolol hydrochloride can be achieved with a suitable particle size without polymorph modification or chemical decomposition. PMID:25286216

  2. Preparation and Characterisation of Mucoadhesive Nasal Gel of Venlafaxine Hydrochloride for Treatment of Anxiety Disorders

    PubMed Central

    Basu, Shyamoshree; Maity, S.

    2012-01-01

    The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug. PMID:23716871

  3. Inhibition of in vitro proliferative responses of human lymphocytes by rimantadine hydrochloride.

    PubMed Central

    Koff, W C; Peavy, D L; Knight, V

    1979-01-01

    Rimantadine hydrochloride (alpha-methyl-1-adamantanemethylamine hydrochloride) inhibits the in vitro proliferative response of human peripheral blood lymphocytes to mitogenic and antigenic stimulation. Addition of drug (25 micrograms/ml) at the initiation of 5-day cultures suppressed the responses to phytohemagglutinin, pokeweed mitogen, and concanavalin A by 25, 65, and 90%, respectively. Similarly, responses to streptokinase-streptodornase, tetanus toxoid, and A2/Aichi influenza vaccine were significantly inhibited at concentrations as low as 10 micrograms of rimantadine per ml. Viability studies on 5-day cultures using trypan blue exclusion showed no significant difference between drug-treated and untreated controls. Furthermore, addition of drug on day 3 of 8-day cultures, at a time when the majority of cells had undergone blastogenesis, greatly suppressed the responses to these mitogens. These studies suggest that, in addition to its antiviral action, rimantadine interferes with the generation of cellular immune responses. PMID:457254

  4. Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

    PubMed

    Hathout, Rania M; Nasr, Maha

    2013-10-01

    Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride. PMID:23732802

  5. Quantitative Estimation of Itopride Hydrochloride and Rabeprazole Sodium from Capsule Formulation

    PubMed Central

    Pillai, S.; Singhvi, I.

    2008-01-01

    Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C18 column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies. PMID:21394269

  6. Quantitative estimation of itopride hydrochloride and rabeprazole sodium from capsule formulation.

    PubMed

    Pillai, S; Singhvi, I

    2008-09-01

    Two simple, accurate, economical and reproducible UV spectrophotometric methods and one HPLC method for simultaneous estimation of two component drug mixture of itopride hydrochloride and rabeprazole sodium from combined capsule dosage form have been developed. First developed method involves formation and solving of simultaneous equations using 265.2 nm and 290.8 nm as two wavelengths. Second method is based on two wavelength calculation, wavelengths selected for estimation of itopride hydrochloride was 278.0 nm and 298.8 nm and for rabeprazole sodium 253.6 nm and 275.2 nm. Developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile: phosphate buffer (35:65 v/v) pH 7.0 as mobile phase. All developed methods obey Beer's law in concentration range employed for respective methods. Results of analysis were validated statistically and by recovery studies. PMID:21394269

  7. Stability of lidocaine hydrochloride in 5% dextrose injection in plastic bags

    SciTech Connect

    Smith, F.M.; Nuessle, N.O.

    1981-11-01

    The stability of lidocaine injection mixed with 5% dextrose injection and refrigerated or stored at room temperature was studied. Lidocaine injection was added to 5% dextrose injection to provide a lidocaine hydrochloride concentration of 4 mg/ml. Samples were assayed for lidocaine and its degradation product, 2,6-dimethylaniline, after 30, 60, and 120 days of storage at room temperature (30 degrees C) and refrigerated temperature (4 degrees C). The analysis was by a stability-indicating HPLC method. Degradation product 2,6-dimethylaniline was not detected at any assay time at either temperature. No statistically significant loss of lidocaine occurred at either temperature. Lidocaine hydrochloride injection is chemically stable for up to 120 days at either 30 degrees C or 4 degrees C when mixed with 5% dextrose injection in plastic infusion bags.

  8. Dietary Administration of Colesevelam Hydrochloride Does Not Affect Fertility or Reproductive Performance in Rats

    Microsoft Academic Search

    Judith K. Marquis; Rafif Dagher; Michael R. Jones

    2004-01-01

    Colesevelam hydrochloride (HC1) (WelChol; Sankyo Pharma) is a novel, highly potent, bile acid-binding polymer used for the treatment of hypercholesterolemia. The primary aim of this study was to determine the effects of dietarily administered colesevelam HC1 on fertility and reproductive performance parameters. To assess these effects, sexually mature Sprague-Dawley rats were randomized to one of five treatment groups: feed alone,

  9. Drug Interactions with Colesevelam Hydrochloride, a Novel, Potent Lipid-Lowering Agent

    Microsoft Academic Search

    Joanne M. Donovan; Daria Stypinski; Mark R. Stiles; Timothy A. Olson; Steven K. Burke

    2000-01-01

    Colesevelam hydrochloride (colesevelam) is a novel, potent, bile acid–binding agent that has been shown to lower LDL cholesterol a mean of 19% at a dose of 3.8 g\\/d. We studied the pharmacokinetics of colesevelam coadministered with six drugs: digoxin and warfarin, agents with narrow therapeutic indices; sustained-release verapamil and metoprolol; quinidine, an antiarrhythmic with a narrow therapeutic index; and valproic

  10. Colesevelam hydrochloride: A novel agent in patients with type 2 diabetes.

    PubMed

    Sekhri, Kavita; Saha, Lekha

    2011-07-01

    Hyperglycemia and hyperlipidemia are both risk factors for the development of various complications in patients with type 2 diabetes mellitus. Colesevelam hydrochloride is a novel agent that can improve both hypercholesterolemia and hyperglycemia in such patients. It is an orally administered bile acid sequestrant with high capacity for binding bile acids. This drug can offer potential new diabetes treatment along with other drugs. PMID:23776789

  11. Electron Spin Resonance Study of ?-Irradiated Single Crystals of Semicarbazide Hydrochloride

    Microsoft Academic Search

    Keshav N. Shrivastava; Roy S. Anderson

    1968-01-01

    Electron spin resonance studies of ?-irradiated single crystals of semicarbazide hydrochloride and the deuterated form, ND2CONHND3+·Cl?, revealed the presence of the stably trapped ·N(?)H(?) ? N(?)H(?)3+ radical obtained by C&sngbnd;N bond rupture of the parent molecule. The principal g values were gaa = 2.0041 ± 0.0003, gbb = 2.0023, and gcc = 2.0044. The principal elements of the hyperfine couplings

  12. Short and symmetrical OHO hydrogen bond in bis(quinuclidine betaine) hydrochloride

    Microsoft Academic Search

    Z. Dega-Szafran; A. Katrusiak; M. Szafran

    2010-01-01

    The molecular structure of bis(quinuclidine betaine) hydrochloride, (QNB)2HCl, has been characterized by single crystal X-ray diffraction, infrared spectroscopy and by DFT calculations. The crystals are centrosymmetric, monoclinic, space group C2\\/c. Two QNB moieties are joined by a very short and centered O?H?O hydrogen bond of 2.461(2)Å. Its existence is confirmed by the broad absorption band below 1500cm?1 in the FTIR

  13. Theoretical and experimental study of vibrational spectra of two polymorphic 4-hydroxy-1-methylpiperidine betaine hydrochlorides

    NASA Astrophysics Data System (ADS)

    Szafran, M.; Koput, J.; Dega-Szafran, Z.

    2008-09-01

    The molecular geometries, harmonic frequencies and intensities of the vibrational bands of ? and ? polymorphs of 4-hydroxy-1-methylpiperidine betaine hydrochloride (?-HO-MPBH·Cl, ?-HO-MPBH·Cl) and their deuterated derivatives have been calculated with the B3LYP/6-31G(d,p) level of theory. The calculated frequencies are compared with the solid FTIR and Raman spectra. Unequivocal assignments of the experimental infrared bands are performed on the basis of the potential energy distribution (PED).

  14. Theoretical and experimental study of vibrational spectra of two polymorphic 4-hydroxy-1-methylpiperidine betaine hydrochlorides

    Microsoft Academic Search

    M. Szafran; J. Koput; Z. Dega-Szafran

    2008-01-01

    The molecular geometries, harmonic frequencies and intensities of the vibrational bands of ? and ? polymorphs of 4-hydroxy-1-methylpiperidine betaine hydrochloride (?-HO-MPBH·Cl, ?-HO-MPBH·Cl) and their deuterated derivatives have been calculated with the B3LYP\\/6-31G(d,p) level of theory. The calculated frequencies are compared with the solid FTIR and Raman spectra. Unequivocal assignments of the experimental infrared bands are performed on the basis of

  15. A study on the supramolecular structure of inclusion complex of ?-cyclodextrin with prazosin hydrochloride

    Microsoft Academic Search

    Longxiao Liu; Suyan Zhu

    2007-01-01

    The supramolecular structure of the inclusion complex of ?-cyclodextrin (?CD) with prazosin hydrochloride (PRH) has been investigated. The 1:1 stoichiometry of complexation was achieved by phase solubility study and the inclusion complex with 1:1 molar ratio was prepared by co-precipitation method. DSC analysis confirmed that the inclusion complex was formed. XRD patterns of ?CD and inclusion complex indicated that the

  16. HPLC and chemometric assisted spectrophotometric methods for simultaneous determination of diprophylline, phenobarbitone and papaverine hydrochloride

    Microsoft Academic Search

    Alaa El-Gindy

    2005-01-01

    Three methods are developed for the simultaneous determination of diprophylline (DP), phenobarbitone (PH) and papaverine hydrochloride (PP). The chromatographic method depends on a high performance liquid chromatographic (HPLC) separation on a reversed-phase C18 column with a mobile phase consisting of 0.02 M potassium dihydrogen phosphate, pH 3.5—acetonitrile (55:45 v\\/v). Quantitation was achieved with UV detection at 210 nm based on peak area. The

  17. Drug-Induced Hypersensitivity Syndrome due to Mexiletine Hydrochloride Associated with Reactivation of Human Herpesvirus 7

    Microsoft Academic Search

    Akiko Yagami; Tetsushi Yoshikawa; Yoshizo Asano; Shin Koie; Tetsuo Shiohara; Kayoko Matsunaga

    2006-01-01

    It has been suggested that reactivation of human herpesvirus 6 (HHV-6) infection may be involved in the pathogenesis of drug-induced hypersensitivity syndrome. We report a 45-year-old Japanese man who developed a generalized papuloerythematous rash, fever, hepatitis, lymphadenopathy and lymphocytosis with an increased number of atypical lymphocytes. He was diagnosed with DIHS due to mexiletine hydrochloride based on laboratory data, results

  18. IMMOBILIZATION OF WILD COLLARED ANTEATERS WITH KETAMINE AND XYLAZINE-HYDROCHLORIDE

    Microsoft Academic Search

    Christine Fournier-Chambrillon; Pascal Fournler; Jean-Christophe Vie

    1997-01-01

    d'Etude pour I'Amenagement et Ia Protection de Ia Nature en Guyane), BP 411, 97328 Cayenne cedex, Guyane fran#{231}aise ABSTRACT: Collared anteaters (Tarnandua tetradactyla) were immobilized for clinical procedures as part of a wildlife rescue during the filling of a hydroelectric dam (Petit Saut, French Guiana) from March 1994 to March 1995. Two doses of ketamine hydrochloride (KH) (group I I

  19. Liquid Chromatographic and Spectrophotometric Determination of Phenazopyridine Hydrochloride, Ampicilline Trihydrate, and Nitrofurantoine in Pharmaceutical Preparations

    Microsoft Academic Search

    ?. M. Palab?y?k; F. Onur

    2004-01-01

    The present work describes two new liquid chromatographic (LC) methods and three new spectrophotometric methods for the simultaneous determination of phenazopyridine hydrochloride (PHEN), ampicilline trihydrate (AMP), and nitrofurantoine (NIT) in their binary combinations. In the LC methods, a Nucleosil C8 column with a mobile phase composed of methanol–acetonitril–water (42:42:16, v\\/v\\/v) with ultraviolet (UV) detection at 260 nm was used for a

  20. HPLC and chemometric-assisted spectrophotometric methods for simultaneous determination of atenolol, amiloride hydrochloride and chlorthalidone

    Microsoft Academic Search

    Alaa El-Gindy; Samy Emara; Ahmed Mostafa

    2005-01-01

    Three methods are presented for the simultaneous determination of atenolol (AT), amiloride hydrochloride (AM) and chlorthalidone (CD). The high performance liquid chromatographic (HPLC) method depends on the separation of each drug on a reversed phase, RP 18 column. Elution was carried out with a mobile phase consisting of acetonitrile -5mM heptansulphonic acid sodium salt (20:80, v\\/v, pH 4.4). Quantitation was achieved

  1. Development of Gelucire 43\\/01 Beads of Metformin Hydrochloride for Floating Delivery

    Microsoft Academic Search

    Sunil K. Jain; Anuj Gupta

    2009-01-01

    The objective of this study was to prepare and characterize beads of Gelucire 43\\/01 for floating delivery of metformin hydrochloride\\u000a (MH). The beads were evaluated for particle size, surface morphology, percent drug entrapment, percent yield, differential\\u000a scanning calorimetry (DSC), in vitro floating ability, and in vitro drug release. Aging effect on storage was evaluated using hot stage microscopy (HSM), DSC,

  2. Kinetic modelling for the assay of nortriptyline hydrochloride using potassium permanganate as oxidant.

    PubMed

    Rahman, Nafisur; Khan, Sumaiya

    2015-06-01

    Kinetic methods for accurate determination of nortriptyline hydrochloride have been described. The methods are based on the oxidation of nortriptyline hydrochloride with KMnO4 in acidic and basic media. In acidic medium, the decrease in absorbance at 525.5 nm and in basic medium, the increase in absorbance at 608.5 nm were measured as a function of time. The variables affecting the reactions were carefully investigated and optimised. Kinetic models such as initial rate, rate constant, variable time and fixed time were employed to construct the calibration curves. The initial rate and fixed time methods were selected for quantification of nortriptyline hydrochloride. In acidic medium, the calibration curves showed a linear response over the concentration range 10-50 ?g mL(-1) for initial rate and 10-60 ?g mL(-1) for fixed time method (2 min). In basic medium, the calibration graphs were linear over the concentration range 10-100 ?g mL(-1) for initial rate and fixed time methods (4 min). In acidic medium, the limits of detection for initial rate and fixed time methods (2 min) were 1.02 and 3.26 ?g mL(-1), respectively. In basic medium, the limits of detection were found to be 1.67 and 1.55 ?g mL(-1) for initial rate and fixed time methods (4 min), respectively. The initial rate and fixed time methods have been successfully applied to the determination of nortriptyline hydrochloride in commercial dosage form. Statistical comparison of the results of the proposed methods with those of reference method exhibited excellent agreement and there is no significant difference between the compared methods in terms of accuracy and precision. PMID:25380790

  3. Simultaneous determination of lidocaine hydrochloride, hydrocortisone and nystatin in a pharmaceutical preparation by RP-LC

    Microsoft Academic Search

    Murali Pendela; Getu Kahsay; Isabel Baekelandt; Ann Van Schepdael; Erwin Adams

    2011-01-01

    A liquid chromatographic (LC) method was developed to analyze a formulation (mouthwash) containing lidocaine hydrochloride, hydrocortisone and nystatin. A single LC method with UV detection was developed. A Waters Symmetry C18 HPLC column (150mm× 4.6mm, 5?m) was used as stationary phase and the assay was performed with gradient elution using mobile phases containing methanol – 0.1M NaH2PO4 with a pH

  4. Buccoadhesive oxycodone hydrochloride disks: plasma pharmacokinetics in healthy volunteers and clinical study

    Microsoft Academic Search

    Brunella Parodi; Eleonora Russo; Gabriele Caviglioli; Marisa Vallarino; Flavio Fusco; Franco Henriquet

    1997-01-01

    The pharmacokinetics of oxycodone hydrochloride were investigated following a single 10 mg buccal dose administered to nine healthy volunteers. Plasma samples were collected up to 24 h after administration and analyzed by an original, sensitive and specific selected ion monitoring (SIM) gas chromatography\\/mass spectrometry (GC-MS) assay, after purification with a solid-phase extraction procedure. The limit of quantitation was 1 ng\\/ml

  5. Redispersion of dried gold nanorods in the presence of 6-amino-1-hexanethiol hydrochloride

    Microsoft Academic Search

    Kanako Honda; Hirofumi Kawazumi; Naotoshi Nakashima; Yasuro Niidome

    Aggregates of phosphatidylcholine-passivated gold nanorods were prepared by the addition of hydrochloric acid in the presence\\u000a of 6-amino-1-hexanethiol hydrochloride (AHT). The aggregates dried in vacuum formed a solid film showing a metallic gold color.\\u000a In spite of the absence of the stable surface-wrapping agents, such as balky polymer or thiol-molecules that form stable self-organized\\u000a films on a gold surface, the

  6. The behavioral pharmacology of butaclamol hydrochloride (AY23,028), a new potent neuroleptic drug

    Microsoft Academic Search

    Katherine Voith; Francis Herr

    1975-01-01

    Butaclamol hydrochloride (AY-23,028) is a member of a new chemical class for which antipsychotic activity in humans has recently been demonstrated. The compound antagonized amphetamine-induced stereotyped behavior in rats, amphetamine toxicity in aggregated mice and apomorphine-induced emesis in dogs. It depressed both discriminated avoidance and continuous lever-pressing behavior in rats and inhibited ambulation and rearing in the open field. At

  7. An analytical chemical study of pilocarpine hydrochloride and its hydrolysis products 

    E-print Network

    Ibert, Edward R

    1956-01-01

    little excess base. To measure the effect of hydrolysis on optical activity, stan- dard solutions of pi. locsrpine were reacted with incremental additions of sodium hydroxide, diluted to volume, and the optical activities compared. It was found... LIBRARY h S SI COLLEGE OF TEXAS moles of' 'base had been added for each mole of' pilocarpine hydrochloride. After two moles of sodium hydroxide hsd been add. ed, further adcLLtions produced no appreciable change in optical activity even when they were...

  8. Effects of switching from sevelamer hydrochloride to bixalomer on laboratory parameters in hemodialysis patients.

    PubMed

    Furukawa, Kazunori; Ikawa, Tomoyoshi; Yokoi, Sayuri; Yokouchi, Shuhei; Kato, Kieko; Ueno, Miki; Takahashi, Junichiro

    2014-06-01

    In Japan, the clinical use of bixalomer, a new polymer preparation like sevelamer hydrochloride, became possible from 2012. In our study, in order to investigate the clinical characteristics of this new phosphorus (P) binder, bixalomer in a clinical practice, for 18 cases of hemodialysis patients at our hospital being treated with sevelamer hydrochloride, we switched the P binder to bixalomer, and compared the laboratory parameters before and after switching. Subjects used for analysis were nine cases in which it was possible to use bixalomer continuously for 10 months. The laboratory parameters measured were the concentrations of serum P, corrected calcium (Ca), whole parathyroid hormone (PTH), albumin and alkaline phosphatase (ALP) as indicators of mineral and bone disorder, and serum high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C) and triglyceride (TG) as indicators of lipid metabolism. Regarding the results after switching to bixalomer and starting treatment using the same dosage as the dosage previously used for sevelamer hydrochloride, there were many cases that showed increasing P concentrations that required increasing the dosage of bixalomer, the dosage after switching was increased significantly (P=0.002). In the comparison of laboratory parameters before and after switching, the concentrations of serum P and albumin decreased significantly (P=0.035 and 0.033). From these results, it was considered that the decreases in serum P concentrations were due not only to the effects of bixalomer, but that suppression of food intake by patients was another reason. There were no significant changes in corrected Ca, whole PTH or ALP. In addition, after changing the P binder, serum HDL-C concentration decreased significantly (P=0.015) and LDL-C increased significantly (P<0.001), and serum TG concentration showed no significant changes. This indicated that the beneficial effects of bixalomer on lipid metabolism may be less than those of sevelamer hydrochloride. PMID:24975888

  9. High Performance Liquid Chromatographic Estimation of Drotaverine Hydrochloride and Mefenamic Acid in Human Plasma

    Microsoft Academic Search

    Prasad Prakash Dahivelkar; Sanjay Baburao Bari; Suvarna Bhoir; Ashok Mukund Bhagwat; R. C. Patel; C. B. Patel

    2009-01-01

    The present work describes a reverse phase HPLC method for the quantitation of drotaverine hydrochloride and mefenamic acid in human plasma. Organic solvent system used for liquid extraction composed of dichloromethane, and isopropyl alcohol in the ratio 80:20 (v\\/v). The compounds were separated on a Thermo BDS Hypersil C 8 (25.0 cm × 4.6 mm, 5 µm particle size) column

  10. Crystal Structure of (?)-Mefloquine Hydrochloride Reveals Consistency of Configuration with Biological Activity

    PubMed Central

    Karle, Jean M.; Karle, Isabella L.

    2002-01-01

    The absolute configuration of (?)-mefloquine has been established as 11R,12S by X-ray crystallography of the hydrochloride salt, thus allowing comparison of the configuration of mefloquine's optical isomers to those of quinine and quinidine. (?)-Mefloquine has the same stereochemistry as quinine, and (+)-mefloquine has the same stereochemistry as quinidine. Since (+)-mefloquine is more potent than (?)-mefloquine in vitro against the D6 and W2 strains of Plasmodium falciparum and quinidine is more potent than quinine, a common stereochemical component for antimalarial activity is implicated. The crystal of (?)-mefloquine hydrochloride contained four different conformations which mainly differ in a small rotation of the piperidine ring. These conformations are essentially the same as the crystalline conformations of racemic mefloquine methylsulfonate monohydrate, mefloquine hydrochloride, and mefloquine free base. The crystallographic parameters for (?)-mefloquine hydrochloride hydrate were as follows: C17H17F 6N2O+Cl? · 0.25 H2O; Mr, 419.3; symmetry of unit cell, orthorhombic; space group, P212121; parameters of unit cell, a = 12.6890 ± 0.0006 Å (1 Å = 0.1 nm), b = 18.9720 ± 0.0009 Å, c = 32.189 ± 0.017 Å; volume of unit cell, 7,749 ± 4 Å3; number of molecules per unit cell, 16; calculated density, 1.44 g cm?3; source of radiation, Cu K? (? = 1.54178 Å); ? (absorption coefficient), 2.373 mm?1; room temperature was used; final R1 (residual index), 0.0874 for 3,692 reflections with intensities greater than 2?. All of the hydroxyl and amine hydrogen atoms participate in intermolecular hydrogen bonds with chloride ions. The orientation of the amine and hydroxyl groups in (+)-mefloquine may define the optimal geometry for hydrogen bonding with cellular constituents. PMID:11959592

  11. Simultaneous determination of rabeprazole sodium and itopride hydrochloride in capsule dosage form by spectrophotometry.

    PubMed

    Sabnis, Shweta S; Gandhi, Santosh V; Madgulkar, A R; Bothara, K G

    Three methods viz. Absorbance Ratio Method (I), Dual Wavelength Method (II) and First Order Derivative Spectroscopic Method (III) for simultaneous estimation of Rabeprazole sodium and Itopride hydrochloride have been developed. The drugs obey Beer's law in the concentration range 2-20 microg/ml for RAB and 5-75 microg/ml for ITO. The results of analysis of drugs have been validated statistically and by recovery studies. PMID:19957542

  12. Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.

    PubMed

    Khan, Lubna Ghazal; Razvi, Nighat; Anjum, Fakhsheena; Siddiqui, Saeed Ahmed; Ghayas, Sana

    2014-09-01

    This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC). Various excipients are available for DC method; we selected those excipients that are used commonly in tablet manufacturing. The excipients used included lactose anhydrous, di-basic calcium phosphate anhydrous, starch, talc, sodium carboxy methyl cellulose, polyvinyl pyrrolidone (PVP), silicon dioxide (Aerosil), stearic acid, magnesium stearate and microcrystalline cellulose (Avicel). These tablets were then evaluated by performing different pharmacopoeial and non-pharmacopoeial tests (i.e. diameter, hardness, thickness, weight variation, disintegration and assay). It was observed that Formulations B, D and H of Tizanidine hydrochloride gave best results within USP specified limits for the tests employed among all the formulations whereas Formulations F and G showed poor friability, disintegration and dissolution profiles rendering starch in combination of talc and sodium carboxy-methyl cellulose unsuitable for Tizanidine hydrochloride tablet formulations. With the present approach, more studies can be designed using other active ingredients and excipients to get an optimal and cost effective product. PMID:25176379

  13. Pharmacokinetics and pharmacodynamics of ritodrine hydrochloride administered orally and intramuscularly to female healthy volunteers.

    PubMed

    Marzo, Antonio; Coa, Katrin; Fontana, Elena; Tavazzi, Simona; Bo, Lorenzo Dal; Ismaili, Shefqet; Zava, Dario; Cantoni, Vittorio; Bertolini, Andrea

    2010-01-01

    Ritodrine hydrochloride ((R,S)-4-hydroxy-alpha-[1-[2-((4-hydroxyphenyl)ethyl]amino)ethyl]benzenemethanol, CAS 26652-09-5) is a direct-acting sympathomimetic agent with a predominant beta-adrenergic activity and a selective action on beta2-receptors. A clinical trial was carried out to investigate the pharmacokinetics, pharmacodynamics and safety of ritodrine hydrochloride administered at the doses of 10, 20 and 30 mg p.o. and 10 mg by i. m. route. A four-way randomised crossover design was adopted on 12 healthy female volunteers with a wash-out of at least 14 days. Concentrations of ritodrine and of the pool of ritodrine in plasma and concentrations of the pool of ritodrine in urine of volunteers were bioassayed with tandem mass spectrometry. The following pharmacokinetic parameters were calculated, using the non-compartmental model: Cmax, AUC0-t, AUC0-INF, t1/2, Vd/f, and Aet after each administration. The distribution volume of ritodrine proved to be about 3 times higher than that of the pool of ritodrine after i. m. injection, confirming the good permeability of ritodrine that massively enters tissue compartments. Statistical analyses of pharmacokinetic parameters ascertained that the p. o. absorption of ritodrine hydrochloride was linearly related with the doses administered in the 10-30 mg range. The pharmacodynamic parameters evaluated complied with the mechanism of action of this drug. PMID:20863008

  14. HPLC and chemometric methods for the simultaneous determination of cyproheptadine hydrochloride, multivitamins, and sorbic acid.

    PubMed

    el-Gindy, Alaa; el-Yazby, Fawzy; Mostafa, Ahmed; Maher, Moustafa M

    2004-06-29

    Three methods are presented for the simultaneous determination of cyproheptadine hydrochloride (CP), thiamine hydrochloride (B1), riboflavin-5-phosphate sodium dihydrate (B2), nicotinamide (B3), pyridoxine hydrochloride (B6), and sorbic acid (SO). The chromatographic method depends on a high performance liquid chromatographic (HPLC) separation on a reversed-phase, RP 18 column. Elution was carried out with 0.1% methanolic hexane sulphonic acid sodium salt (solvent A) and 0.01 M phosphate buffer containing 0.1% hexane sulphonic acid sodium salt, adjusted to an apparent pH of 2.7 (solvent B). Gradient HPLC was used with the solvent ratio changed from 20:80 to 70:30 (over 9 min), then to 80:20 (over 11 min) for solvent A:B, respectively. Quantitation was achieved with UV detection at 220 and 288 nm based on peak area. The other two chemometric methods applied were principal component regression (PCR) and partial least squares (PLS). These approaches were successfully applied to quantify each drug in the mixture using the information included in the UV absorption spectra of appropriate solutions in the range 250-290 nm with the intervals Deltalambda = 0.4 nm at 100 wavelengths. The chemometric methods do not require any separation step. The three methods were successfully applied to a pharmaceutical formulation and the results were compared with each other. PMID:15193715

  15. Pioglitazone hydrochloride: chemopreventive potential and development of site-specific drug delivery systems.

    PubMed

    Sinha, Vivek Ranjan; Sethi, Shilpa

    2015-05-01

    The aim of this study was to investigate the potential of pioglitazone hydrochloride as a promising anticancer agent and then to design and evaluate the colon-targeted delivery system. The role of pioglitazone hydrochloride as a promising anticancer agent was evaluated by in vitro cell line studies and in vivo 1,2-dimethylhydrazine-induced colon carcinogenesis in rats. In order to deliver the drug at site of action, i.e. colon, drug embedded in matrices containing a release retarding polymer (HPMC K4M) and a polysaccharide (locust bean gum) were prepared. These matrix systems were further enteric coated with Eudragit®S100 to minimize the premature drug release in the upper segments of the GIT. In vitro dissolution studies were performed in absence and presence of rat caecal contents on selected batches and samples were analyzed using a validated RP-HPLC method. Hence, the studies led to the conclusion that successful site-specific delivery systems of pioglitazone hydrochloride were developed to improve its therapeutic efficacy in the management of colorectal cancer. PMID:24547712

  16. Incidence of next-day anterograde amnesia caused by flurazepam hydrochloride and triazolam.

    PubMed

    Juhl, R P; Daugherty, V M; Kroboth, P D

    1984-01-01

    The incidence of next-day anterograde amnesia was evaluated in hospitalized patients who received flurazepam hydrochloride or triazolam. A blinded observer assessed memory and daytime drowsiness in 154 patients after the bedtime ingestion of flurazepam hydrochloride (n = 54), triazolam (n = 49), or no hypnotic drug (n = 51). The hypnotic agents were administered before midnight. At approximately 0800 the next morning, the patients were shown a picture of an object on colored construction paper and asked to remember it as well as the color of the background. Both the observer and patient assessed drowsiness using the Stanford Sleepiness Scale. The observer also made a note of the items on the patient's breakfast tray. Patients were then revisited at 1100 and asked to recall the object in the picture, the color of the background, and at least three items from their breakfast tray. Ten of the 54 patients in the flurazepam group failed to recall all three items compared with only two in the triazolam group and two in the control group. The 14 patients who experienced memory impairment were significantly more drowsy at 0800 than those who were able to recall the items. Next-day anterograde amnesia occurred more frequently in patients who received flurazepam hydrochloride than in those who received triazolam or no hypnotic drug. This effect may be related to the next-day drowsiness caused by flurazepam and its slowly eliminated active metabolite. PMID:6150782

  17. Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC.

    PubMed

    Arayne, M Saeed; Sultana, Najma; Siddiqui, Farhan Ahmed

    2006-10-01

    An isocratic reversed phase high-performance liquid chromatographic (HPLC) method with ultraviolet detection at 230 nm has been developed for the determination of buclizine hydrochloride in human serum and dosage formulation. Methylparaben was successfully used as an internal standard. Good chromatographic separation between buclizine and internal standard peaks was achieved by using a stainless steel analytical column Nucleosil, C18 (10 microm, 25 cm x 0.46 cm). The system was operated at room temperature using a mobile phase consisting of acetonitrile-water (1:1) (pH 2.6) with phosphoric acid 85% at a flow rate of 2 ml/min. The calibration curve for buclizine hydrochloride in human serum was linear over the tested concentration range of 10, 3, 1.5, 0.5, 0.15, 0.05, and 0.025 microg/ml with a correlation coefficient of 0.9999. The intra- and inter-run precision and accuracy results were 98.07 to 100.34. The proposed method was validated for selectivity, linearity, accuracy, and precision. The method was found to be suitable for the quality control of buclizine hydrochloride in bulk drug as well as in human serum. PMID:17105713

  18. Effect of modulated alternating and direct current iontophoresis on transdermal delivery of lidocaine hydrochloride.

    PubMed

    Bhatia, Gaurav; Banga, Ajay K

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determine the amount of drug in stripped skin. Receptor was sampled and analyzed over predefined time periods. The amount of lidocaine delivered across porcine skin after modulated direct current iontophoresis for 2 h was 1069.87 ± 120.03 ? g/sq · cm compared to 744.81 ± 125.41 ? g/sq · cm after modulated alternating current iontophoresis for 2 h. Modulated direct current iontophoresis also enhanced lidocaine delivery by twelvefold compared to passive delivery as 91.27 ± 18.71 ? g/sq · cm of lidocaine was delivered after passive delivery. Modulated iontophoresis enhanced the delivery of lidocaine hydrochloride across porcine skin compared to the passive delivery. Modulated alternating current iontophoresis for duration of 2 h at frequency of 1 kHz was found to be comparable to the continuous direct current iontophoresis for 1 h. PMID:24959580

  19. Controlled delivery of ropinirole hydrochloride through skin using modulated iontophoresis and microneedles.

    PubMed

    Singh, Neha D; Banga, Ajay K

    2013-05-01

    The objective of this study was to investigate the effect of modulated current application using iontophoresis- and microneedle-mediated delivery on transdermal permeation of ropinirole hydrochloride. AdminPatch® microneedles and microchannels formed by them were characterized by scanning electron microscopy, dye staining and confocal microscopy. In vitro permeation studies were carried out using Franz diffusion cells, and skin extraction was used to quantify drug in underlying skin. Effect of microneedle pore density and ions in donor formulation was studied. Active enhancement techniques, continuous iontophoresis (74.13 ± 2.20 µg/cm(2)) and microneedles (66.97 ± 10.39 µg/cm(2)), significantly increased the permeation of drug with respect to passive delivery (8.25 ± 2.41?µg/cm(2)). Modulated iontophoresis could control the amount of drug delivered at a given time point with the highest flux being 5.12 ± 1.70 µg/cm(2)/h (5-7 h) and 5.99 ± 0.81 µg/cm(2)/h (20-22 h). Combination of modulated iontophoresis and microneedles (46.50 ± 6.46 µg/cm(2)) showed significantly higher delivery of ropinirole hydrochloride compared to modulated iontophoresis alone (84.91 ± 9.21 µg/cm(2)). Modulated iontophoresis can help in maintaining precise control over ropinirole hydrochloride delivery for dose titration in Parkinson's disease therapy and deliver therapeutic amounts over a suitable patch area and time. PMID:23311703

  20. A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation

    PubMed Central

    Trivedi, Rakshit Kanubhai; Patel, Mukesh C.; Jadhav, Sushant B.

    2011-01-01

    A stability indicating reversed phase ultra performance liquid chromatography (RP-UPLC) method was developed for simultaneous determination of ambroxol hydrochloride (AMB), cetirizine hydrochloride (CTZ), methylparaben (MP) and propylparaben (PP) in liquid pharmaceutical formulation. The desired chromatographic separation was achieved on an Agilent Eclipse plus C18, 1.8 ?m (50 × 2.1 mm) column using gradient elution at 237 nm detector wavelength. The optimized mobile phase consists of a mixture of 0.01 M phosphate buffer and 0.1 % triethylamine as a solvent-A and acetonitrile as a solvent-B. The developed method separates AMB, CTZ, MP and PP in presence of twelve known impurities/degradation products and one unknown degradation product within 3.5 min. Stability indicating capability was established by forced degradation experiments and seperation of known and unknown degradation products. The lower limit of quantification was established for AMB, CTZ, MP and PP. The developed RP-UPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. This validated method is applied for simultaneous estimation of AMB, CTZ, MP and PP in commercially available syrup samples. Further, the method can be extended for estimation of AMB, CTZ, MP, PP and levo-cetirizine (LCTZ) in various commercially available dosage forms. PMID:21886901

  1. High-performance liquid chromatography method for the simultaneous determination of thiamine hydrochloride, pyridoxine hydrochloride and cyanocobalamin in pharmaceutical formulations using coulometric electrochemical and ultraviolet detection.

    PubMed

    Marsza??, Marcin Leszek; Lebiedzi?ska, Anna; Czarnowski, Wojciech; Szefer, Piotr

    2005-11-11

    The method for the simultaneous determination of thiamine hydrochloride, pyridoxine hydrochloride and cyanocobalamin by high-performance liquid chromatography (HPLC) with coulometric electrochemical and UV detections is presented. The retention time of vitamins was repeatedly determined by isocratic elution using 0.05 M phosphate buffer-10% methanol and 0.018 M trimethylamine (1 ml min(-1), pH 3.55) as mobile phase with the Supelco LC 18 column 5 microm (25 cm x 4.6 mm). The specificity of the method was demonstrated by the retention characteristics, coulometric electrochemical and UV detection. The limits of detection of thiamine, pyridoxine and cyanocobalamin were: 9.2, 2.7 and 0.08 ng/ml, respectively. The method was characterized also by wide concentration range, high sensitivity and good accuracy (99.6-102.7%). The repeatability of the method was evaluated at different level of concentration of vitamins and the relative standard deviation was below 4.5%. The method was successfully applied for the quantification of Vitamins B1, B6 and B12 in pharmaceutical preparations and dietary supplements. PMID:16257294

  2. Comparative antifungal efficacy of light-activated disinfection and octenidine hydrochloride with contemporary endodontic irrigants.

    PubMed

    Eldeniz, Ayce Unverdi; Guneser, Mehmet Burak; Akbulut, Makbule Bilge

    2015-02-01

    The aim of this study was to evaluate the antifungal effects of light-activated disinfection (LAD) in comparison with contemporary root canal irrigation solutions: sodium hypochlorite and 2% chlorhexidine gluconate and a new wound antiseptic, octenidine hydrochloride. Seventy extracted teeth having single root canals were contaminated with Candida albicans for 14 days. The samples were divided into five experimental (n?=?10) and two control (positive and negative) groups (n?=?10): (1) LAD with toluidine blue O, (2) octenidine hydrochloride (OCT), (3) 2.5% sodium hypochlorite (2.5% NaOCl), (4) 5.25% sodium hypochlorite (5.25% NaOCl) and (5) 2% chlorhexidine. Five millilitres of each test solution was applied for 3 min, and irradiation time used for LAD was 30 s. After treatment, the dentin chips were collected from inner canal walls into vials containing phosphate buffered saline, vortexed, serially diluted, seeded on Tryptic Soy Agar plates and incubated (37 °C, 48 h). The number of colony-forming units was then counted. Differences between LAD group and positive control group were statistically significant (P?hydrochloride, demonstrated better potential than LAD in elimination of Candida albicans cells and may be a promising alternative to NaOCl and chlorhexidine solutions in future. PMID:23884903

  3. Evaluation of metomidate hydrochloride as an anesthetic in leopard frogs (Rana pipiens).

    PubMed

    Doss, Grayson A; Nevarez, Javier G; Fowlkes, Natalie; da Cunha, Anderson F

    2014-03-01

    Metomidate hydrochloride is an imidazole-based, nonbarbiturate hypnotic drug primarily used as an immersion sedation and anesthetic agent in freshwater and marine finfish. To the authors' knowledge, there is no documentation in the literature of its use in amphibians. In this study, 7 male and 4 female leopard frogs (Rana pipiens) were induced with metomidate hydrochloride via immersion bath at a concentration of 30 mg/L for 60 min. The pH of the induction solution ranged from 7.63 to 7.75. Each frog was then removed from the induction solution, rinsed, and recovered in 26.6 degrees C amphibian Ringer's solution. After 210 min in the Ringer's solution, the frogs were transferred to moist paper towels for recovery. Heart rate, gular and abdominal respiration rates, righting reflex, superficial and deep pain withdrawal reflexes, corneal and palpebral reflexes, and escape response were monitored and recorded at defined intervals during both induction and recovery. The average time to loss of righting reflex and escape response was 17.36 min and 17.82 min, respectively. Metomidate produced clinical sedation in all frogs (n = 11). Surgical anesthesia was achieved in only 27% (3/11), with an anesthetic duration that ranged from 9 to 20 min. Recovery times were extremely prolonged and varied, with a range from 313 min to longer than 600 min. The findings of this study indicate that metomidate hydrochloride is unsuitable as a sole anesthetic agent in leopard frogs, and further research is needed to evaluate its suitability in other amphibians. PMID:24712162

  4. Hydrogen bonds in the crystal packings of mesalazine and mesalazine hydrochloride

    NASA Astrophysics Data System (ADS)

    Bani?-Tomiši?, Z.; Koji?-Prodi?, B.; Širola, I.

    1997-10-01

    The crystal structures of pharmaceutical product mesalazine (marketed also under different proprietary names as Salofalk, Asacol, Asacolitin, and Claversal) and its hydrochloride are reported. In the crystal mesalazine is in zwitterion form as 5-ammoniosalicylate ( 1) whereas mesalazine hydrochloride crystallizes in an ionized form as 5-ammoniosalicylium chloride ( 2). Compound 1 (C 7H 7O 3N) crystallizes in the monoclinic space group {P2 1}/{n} with a = 3.769(1) Å, b = 7.353(2) Å, c = 23.475(5) Å, ? = 94.38(2)°, V = 648.7(8) Å3, Z = 4, Dc = 1.568 g cm -3 and ?( MoK?) = 1.2 cm -1. Compound 2 (C 7H 8O 3NCl) crystallizes in the triclinic space group P 1¯ with a = 4.4839(2) Å, b = 5.7936(2) Å, c = 15.6819(5) Å, ? = 81.329(3)°, ? = 88.026(3)°, ? = 79.317(4)°, V = 395.74(3) Å3, Z = 2, Dc = 1.591 g cm -3 and ?(CuK ?) = 40.8 cm -1. The crystal structures were solved by direct methods and refined to R = 0.041 for 1 and 0.028 for 2, using 607 and 1374 observed reflections, respectively. The configuration of both molecules, with the ortho hydroxyl to a carboxyl group, favours the intramolecular hydrogen bonds. Very complex systems of intermolecular hydrogen bonds were observed in both crystal packings. They are discussed in terms of graph-set notation. The mesalazine crystal structure is characterized by two-dimensional network of hydrogen bonds in the ab plane. The crystal structure pattern of mesalazine hydrochloride is a three-dimensional network significantly supported by N +?H⋯Cl - interactions.

  5. Molecular structure, hydrogen bonding, basicity and spectroscopic properties of 3-hydroxypyridine betaine hydrochloride monohydrate

    Microsoft Academic Search

    P. Barczynski; A. Komasa; A. Katrusiak; Z. Dega-Szafran; M. Szafran

    2007-01-01

    The effect of hydrogen bonding, inter- and intramolecular electrostatic interactions on the structure of 3-hydroxy-pyridine betaine hydrochloride monohydrate (1-carboxymethyl-3-hydroxypyridinium chloride monohydrate), 3-HO-PBH·Cl·H2O, has been studied by X-ray diffraction, 1H and 13C NMR and FTIR spectroscopies, and by the B3LYP\\/6-31G(d,p) calculations. In the crystal, the Cl? anion is connected with protonated betaine via the hydrogen bond, OCOH?Cl?=2.993(2) Å and with neighboring

  6. Photostabilization of doxorubicin hydrochloride with radioprotective and photoprotective agents: Potential mechanism for enhancing chemotherapy during radiotherapy

    SciTech Connect

    Habib, M.J.; Asker, A.F.

    1989-11-01

    p-Aminobenzoic acid (PABA), urocanic acid, and sodium urate were found to significantly enhance the photostability of doxorubicin hydrochloride (adriamycin, (ADR)). d1-Methionine, thiourea, and glycine also increased the photostability of this drug, but to a lesser degree. Sodium thiosulfate on the other hand, was found to be detrimental to the photostability of ADR. The photostabilizing effect of PABA was found to increase with increase of its concentration and was influenced by the pH and the buffer species of the vehicle. The findings would have an impact on the enhancement of therapeutic efficacy of adriamycin when administered during radiation therapy.

  7. A study of the reaction between antimony (III) chloride and organic amine hydrochlorides 

    E-print Network

    Linder, Donald Ernst

    1964-01-01

    in an excess of hydrochloric acid and added this to the amine hydro- chloride. The amine hydrochloride was also in an excess of hydrochloric acid. The compounds they reported were: pyridiniumtetrachloroantimonate (III), (C H NH)SbC1...; tluinoliniumtetrachloroantimenate (III), (C H NH)SbC1 phenyltrimethylammoniumtetrachloroantimonate (III), C H N(CH ) SbC1 and m-chlorophenyltrimethylammoniumtetrachloroantimonate (III), m-Cl. C H N(CH ) SbC1 Binz and Sclmickh allowed antimony (III) chloride to res, ct with 2 3...

  8. Derivatives of benzimidazole: vasodilator activity of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride. Preliminary study.

    PubMed

    Demenge, P; Carraz, G; Luu Duc, C; Silice, C

    1979-01-01

    The effects of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride (HBBPC) have been studied in the rabbit and rat. Most of these studies were performed comparatively with reference vasodilators and papaverine. HBBPC vasodilator activity is nearly the same as that of papaverine in the isolated rabbit ear. The characteristic of the vasoactive action of HBBPC seems to reside in its duration. The mechanism of action of HBBPC seems of peripheral type, that is to say it acts on the vascular smooth muscle. PMID:582758

  9. Influence of nine surfactants on the activity of oxytetracycline hydrochloride against Lipaphis erysimi Kalt.

    PubMed

    Lal, O P; Teotia, T P

    1975-12-01

    The effect of nine surfactants on the activity of oxytetracycline hydrochloride (OCT) was investigated against Lipaphis erysimi Kalt feeding on cabbage plants. All the surfactants, except Emulgator EL and Emulgator IP, at 0.1% increased the efficacy of OTC at 0.25% and the maximum reduction of 83.93% in fertility was observed for the combination OTC+Arkopal N-110. The nymphal development was delayed by various treatments. The treated adults were lighter in weight and smaller in size compared to the control insects. No photoxicity was observed in any case. PMID:1206011

  10. Configuration and conformation of alfentanil hydrochloride. Conformational study by NMR and theoretical calculations.

    PubMed

    Jaime, Carlos; Virgili, Albert; Portillo, Susana; Caparrós, Antoni; Burusco, Kepa K

    2014-08-01

    The configurational and conformational structure of alfentanil hydrochloride (1) was studied by nuclear magnetic resonance and theoretical calculations. Compound 1 is best described by equilibrium between two stereoisomeric piperidinium rings with the N-substituent always being in equatorial position. Nuclear magnetic resonance spectra demonstrate that, depending on the solvent, 1 adopts the conformation with an axial methoxymethylene group. Computations were crucial in determining the importance of the transannular attractive interaction between the positive charge at the piperidinium N-atom and the methoxymethyl group in position 4. PMID:24889875

  11. A randomised controlled study comparing Drotaverine hydrochloride and Valethamate bromide in the augmentation of labour

    Microsoft Academic Search

    Chendrimada Madhu; Suvarna Mahavarkar; Sudhir Bhave

    2010-01-01

    Objectives  Cervical dilatation is a poorly understood process. Various drugs have been used to facilitate this process and reduce the\\u000a duration of labour and thereby reduce feto-maternal complications. The present study is an attempt to compare and evaluate\\u000a the efficacy of Drotaverine hydrochloride and Valethamate bromide in the process of cervical dilatation and labour augmentation.\\u000a \\u000a \\u000a \\u000a \\u000a Study design  A prospective randomised trial of

  12. X-ray radiation of poly-L-arginine hydrochloride and multilayered DNA-coatings

    NASA Astrophysics Data System (ADS)

    Stypczy?ska, Agnieszka; Nixon, Tony; Mason, Nigel

    2014-11-01

    The aim of this work was to determine the chemical changes induced in thin films of the dry polypeptide poly-L-arginine hydrochloride and its mixture with calf thymus deoxyribonucleic acid (DNA) during 5 h of soft X-ray exposure. The physical and chemical effects of the soft X-ray irradiation were studied using X-ray Photoelectron Spectroscopy (XPS). Analysis of O1 s, N1 s and C1 s features in XPS spectra reveals the existence of several routes of radiation-induced decomposition and shows quantitative and qualitative changes.

  13. Crystal and molecular structure of quinuclidine betaine hydrochloride studied by X-ray diffraction, DFT, FTIR, and NMR methods

    Microsoft Academic Search

    Z. Dega-Szafran; A. Katrusiak; M. Szafran

    2009-01-01

    Quinuclidine betaine hydrochloride (1-carboxymethyl-1-azabicyclo[2.2.2]octane hydrochloride, QNBH·Cl) has been synthesized and characterized by X-ray diffraction, FTIR and NMR spectroscopy, and DFT calculations. QNBH·Cl crystallizes in orthorhombic space group Pnma. In the crystal the Cl? anion is engaged in a medium–strong COOH·Cl hydrogen bond of 2.921(2)Å, in which the acidic proton is closer the carboxylate group and additionally in some C–H···Cl contacts,

  14. [Effect of low doses of emoxipine and pyridoxine hydrochloride on the status of patients with cataract and glaucoma].

    PubMed

    Ianovskaia, N P; Shtol'ko, V N; Burlakova, E B

    1993-05-01

    It has been shown that eyes instillation of pyridoxine hydrochloride low doses during 20 days affects the vision and tonographic characteristics of patients with glaucoma and earlier stage of cataract. Light eyes have been shown to be more sensitive to treatment than dark ones. From 10 to 40 min after emoxipin or pyridoxine hydrochloride low doses instillation, some pupil constriction has been registered. The data obtained suggest that low doses of this substances affect eyes cholinoreactive structures and may be useful for treatment glaucoma and early stage cataract. PMID:8043826

  15. Simultaneous determination of the counter ion and possible impurity from the synthetic route in the pharmaceutical substance prasugrel hydrochloride.

    PubMed

    Maruszak, Wioleta; Cybulski, Marcin

    2015-02-01

    A fast and selective capillary electrophoresis method was developed and validated for the simultaneous determination of the hydrochloride and acetic acid content in prasugrel hydrochloride. Because of the poor chromophore, the indirect detection was chosen. Among different compositions studied as the background electrolyte, the pyromellitic acid with diethylamine (DEA) and myristyltrimethylammonium bromide (TTAB) was chosen. During the validation the specificity, linearity, accuracy, precision, range, and stability of the sample solution were confirmed. The results indicate that the method is suitable for the determination of the counter ion and impurity from the synthetic route of the pharmaceutical drug substance in the same assay. PMID:25527979

  16. Spectroscopic and biological studies of new mononuclear metal complexes of a bidentate NN and NO hydrazone-oxime ligand derived from egonol.

    PubMed

    Babahan, Ilknur; Emirda?-Öztürk, Safiye; Poyrazo?lu-Çoban, Esin

    2015-04-15

    A novel ligand, vicinal dioxime ligand (egonol-hydrazone glyoxime) (LH2) was synthesized and characterized using (1)H NMR, (13)C NMR, MS, AAS, infrared spectroscopy, and magnetic susceptibility measurements. Mononuclear nickel (II), copper (II) and cobalt (II) complexes with a metal:ligand ratio of 1:2 for LH2 were also synthesized. Zn(II) forms complex [Zn(LH)Cl2] with a metal to ligand ratio of 1:1. IR spectrum shows that the ligand act in a bidentate manner and coordinates N4 donor groups of the ligands to Ni(II), Cu(II), Co(II) and Zn(II) ions. The detection of H-bonding (OH?O) in the [M(LH)2] metal complexes by IR spectra supported the square-planar MN4 coordination of Ni(II), Cu(II) and Co(II) complexes. The antimicrobial activities of compounds LH2 and their Ni(II), Cu(II), Co(II) and Zn(II) complexes were evaluated using the disc diffusion method against 16 bacteria and 5 yeasts. The minimal inhibitory concentrations (MICs) against all the bacteria and yeasts were also determined. Among the attempted test compounds, it is showed that all the compounds (L, LH2, [Ni(LH)2], [Cu(LH)2], [Co(LH)2(H2O)2], [Zn(LH)Cl2]) were effective against used test microorganisms. PMID:25686861

  17. Mono- and binuclear copper(II) complexes of new hydrazone ligands derived from 4,6-diacetylresorcinol: Synthesis, spectral studies and antimicrobial activity

    NASA Astrophysics Data System (ADS)

    Shebl, Magdy; El-ghamry, Mosad A.; Khalil, Saied M. E.; Kishk, Mona A. A.

    Two new hydrazone ligands, H2L1 and H2L2, were synthesized by the condensation of 4,6-diacetylresorcinol with 3-hydrazino-5,6-diphenyl-1,2,4-triazine and isatin monohydrazone, respectively. The structures of the ligands were elucidated by elemental analyses, IR, 1H NMR, electronic and mass spectra. Reactions of the ligands with several copper(II) salts, including AcO-, NO3-, SO42-, Cl- and Br- afforded mono- and binuclear metal complexes. Also, the ligands were allowed to react with Cu(II) ion in the presence of a secondary ligand (L?) [N,O-donor; 8-hydroxyquinoline, N,N-donor; 1,10-phenanthroline or O,O-donor; benzoylacetone]. Characterization and structure elucidation of the prepared complexes were achieved by elemental and thermal analyses, IR, electronic, mass and ESR spectra as well as conductivity and magnetic susceptibility measurements. The ESR spin Hamiltonian parameters of some complexes were calculated. The spectroscopic data showed that the H2L1 ligand acts as a neutral or monobasic tridentate ligand while the H2L2 ligand acts as a bis(monobasic tridentate) ligand. The coordination sites with the copper(II) ion are phenolic oxygen, azomethine nitrogen and triazinic nitrogen (H2L1 ligand) or isatinic oxygen (H2L2 ligand). The metal complexes exhibited octahedral and square planar geometrical arrangements depending on the nature of the anion. The ligands and some metal complexes showed antimicrobial activity.

  18. Reactivity Differences between [alpha, beta]-Unsaturated Carbonyls and Hydrazones Investigated by Experimental and Theoretical Electron Density and Electron Localizability Analyses

    SciTech Connect

    Grabowsky, Simon; Weber, Manuela; Jayatilaka, Dylan; Chen, Yu-Sheng; Grabowski, Matthias T.; Brehme, Rainer; Hesse, Malte; Schirmeister, Tanja; Luger, Peter (UWA); (Wurzburg); (UC); (Berlin)

    2012-10-11

    It is still a challenge to predict a compound's reactivity from its ground-state electronic nature although Bader-type topological analyses of the electron density (ED) and electron localizability indicator (ELI) give detailed and useful information on electron concentration and electron-pair localization, respectively. Both ED and ELI can be obtained from theoretical calculations as well as high-resolution X-ray diffraction experiments. Besides ED and ELI descriptors, the delocalization index is used here; it is likewise derived from theoretical calculations as well as from experimental X-ray results, but in the latter case, demonstrated here for the first time. We investigate {alpha},{beta}-unsaturated carbonyl and hydrazone compounds because resonance exhibited by these compounds in the electronic ground-state determines their reactive behavior. The degree of resonance as well as the reactivity contrast are quantified with the electronic descriptors. Moreover, competitive mesomeric substituent effects are studied using the two biologically important compounds acrolein and acrylamide. The reactivity differences predicted from the analyses are in line with the known reactivity of these compounds in organic synthesis. Hence, the capability of the ED and ELI for rationalizing and predicting different and competing substituent effects with respect to reactivity is demonstrated.

  19. Novel Potent Imidazo[1,2-a]pyridine-N-Glycinyl-Hydrazone Inhibitors of TNF-? Production: In Vitro and In Vivo Studies

    PubMed Central

    Lacerda, Renata B.; Sales, Natália M.; da Silva, Leandro L.; Tesch, Roberta; Miranda, Ana Luisa P.; Barreiro, Eliezer J.; Fernandes, Patricia D.; Fraga, Carlos A. M.

    2014-01-01

    In this work, we describe the design, synthesis and pharmacological evaluation of novel imidazo[1,2-a]pyridine-N-glycinyl-hydrazone derivatives (1a–k) intended for use as inhibitors of tumor necrosis factor alpha (TNF-?) production. The compounds were designed based on the orally active anti-inflammatory prototype LASSBio-1504 (2), which decreases the levels of the pro-inflammatory cytokine TNF-? in vitro and in vivo. The in vitro pharmacological evaluation of the imidazo[1,2-a]pyridine compounds (1) showed that substitution of the N-phenylpyrazole core present in prototype 2 by a bioisosteric imidazo[1,2-a]pyridine scaffold generated anti-TNF-? compounds that were more potent than the previously described N-phenylpyrazole derivative 2 and as potent as SB-203580, a p38 MAPK inhibitor. The most active derivative (E)-2-(2-tert-butylimidazo[1,2-a]pyridin-3-ylamino)-N’-(4-chlorobenzylidene) acetohydrazide, or LASSBio-1749 (1i) was orally active as an anti-inflammatory agent in a subcutaneous air pouch model, reducing expressively the levels in vivo of TNF-? and other pro-inflammatory cytokines at all of the tested doses. PMID:24632827

  20. Development of Duloxetine Hydrochloride Loaded Mesoporous Silica Nanoparticles: Characterizations and In Vitro Evaluation.

    PubMed

    Ganesh, Mani; Ubaidulla, Udhumansha; Hemalatha, Pushparaj; Peng, Mei Mei; Jang, Hyun Tae

    2015-08-01

    This study investigated the potential use of mesoporous silica nanoparticles (MSNs) as a carrier for duloxetine hydrochloride (DX), which is prone to acid degradation. Sol-gel and solvothermal methods were used to synthesize the MSNs, which, after calcination and drug loading, were then characterized using X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) technique, thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and diffuse reflectance ultraviolet-visible (DRS-UV-Vis) spectroscopy. Releases of DX from the MSNs were good in pH 7.4 (90%) phosphate buffer but poor in acidic pH (40%). In a comparative release study between the MSNs in phosphate buffer, TW60-3DX showed sustained release for 140 h, which was higher than the other nanoparticles. The mechanism of DX release from the MSNs was studied using Peppas kinetics model. The "n" value of all three MSNs ranged from 0.45 to 1 with a correlation coefficient (r (2)) >0.9, which indicated that the release of the drug from the system follows the anomalous transport or non-Fickian diffusion. The results supported the efficacy of mesoporous silica nanoparticles synthesized here as a promising carrier for duloxetine hydrochloride with higher drug loading and greater pH-sensitive release. PMID:25604699

  1. Synthesis of novel 10-hydroxycamptothecin derivatives utilizing topotecan hydrochloride as ortho-quinonemethide precursor.

    PubMed

    Tan, Hanyi; Wang, Guolin; Li, Jiajun; Meng, Guangrong; Liu, Zhenfeng; Dong, Mengjie; Li, Yubin; Ju, Dianwen; Zhang, Qian

    2015-01-01

    A series of 9-(alkylthiomethyl)-10-hydroxycamptothecins and pyrano-fused camptothecin derivatives were synthesized via the reaction of topotecan hydrochloride with various thiols and alkyl vinyl ethers respectively. In the reactions, topotecan hydrochloride was utilized as ortho-quinonemethide (o-QM) precursor. The configuration of 19 was determined by (1)H NMR and NOESY spectra as syn-isomers, suggesting that the cycloaddition of topotecan with alkyl vinyl ethers could undergo a hetero Diels-Alder reaction. All the synthesized compounds were screened on cancer cell lines HepG2, KB, HCT-8 and SGC7901. Some compounds were selected to assess their inhibitory activity against Topo I via Topo I mediated DNA cleavage assays. The results showed that among those tested 9-(alkylthiomethyl)-10-hydroxycamptothecins, the compounds with bulkier hydrophobic side chains at 9-position have better bioactivities. As well as all pyrano-fused camptothecins possess antiproliferative activity against the tested cancer cell lines. Docking studies suggested that there are more interactions between the novel analogues and the binding site of Topo I. PMID:25481395

  2. Lyophilized Chitosan/xanthan Polyelectrolyte Complex Based Mucoadhesive Inserts for Nasal Delivery of Promethazine Hydrochloride

    PubMed Central

    G Dehghan, Mohamed Hassan; Marzuka, Marzuka

    2014-01-01

    The objective of this investigation was the development of chitosan/xanthan polyelectrolyte complex based mucoadhesive nasal insert of promethazine hydrochloride a drug used in the treatment of motion sickness. A 32 factorial design was applied for preparing chitosan/xanthan polyelectrolyte complex and to study the effect of independent variables i.e. concentration of xanthan [X1] and concentration of chitosan [X2] on various responses i.e. viscosity of polyelectrolyte complex solution, water uptake of nasal inserts (at pH 2, 5.5, 7.4), bioadhesion potential of nasal inserts and in-vitro drug release at Q6h through nasal inserts. FTIR and DSC analysis were carried out to confirm complex formation and on loaded and unloaded nasal insert to investigate any drug excipient interaction. The nasal inserts were also characterized by powder X-ray diffractometry (PXRD) and Scanning electron microscopy (SEM) and for ex-vivo permeation studies. The results show that higher amount of xanthan in polyelectrolyte complexes with respect to higher amount of chitosan retarded in-vitro drug release. The water uptake behaviour of nasal insert was strongly influenced by pH of the medium and by polycation/ polyanion concentration. The investigation verifies the formation of polyelectrolyte complexes formation between chitosan and xanthan at pH values in the vicinity of pKa intervals of the two polymers and confirms their potential for the nasal delivery of promethazine hydrochloride. PMID:25276178

  3. Spectrophotometric estimation of eflornithine hydrochloride by using ion-pair reagents.

    PubMed

    Kumar, Amit; Singh, Vijender; Kumar, Praveen

    2015-03-01

    Four newer, cost effective and sensitive ion-pair complex methods were estimated for the determination of eflornithine hydrochloride drug in pharmaceutical formulation. In these methods eflornithine hydrochloride react with bromocresol green (buffer of pH 4), bromophenol blue (buffer pH 4.5), methyl orange (buffer of pH 5.5) and bromothymol blue (buffer of pH 5) respectively. The chloroform was used for extraction of ion-pair complexes. The measurement of complexes was done at 413, 416, 417 and 425 nm respectively. Under the described conditions the proposed methods are linear over the concentration range of 3-18, 4-16, 6-30 and 2-12 ?g/ml and the coefficient of determination were >0.999 (n=6) with a relative standard deviation of <1% (n=6). The average recovery of the target compound is >100% with a limit of quantification (LOQ) of 20, 0.869, 2 and 4.167 ?g/ml and the limit of detection (LOD) 6.6, 0.287, 0.66 and 1.375 ?g/ml. The mechanism of the derivatization reaction is proposed and advantages of the proposed method are discussed. PMID:25730793

  4. Development and Validation of RP-HPLC Method for the Estimation of Ivabradine Hydrochloride in Tablets.

    PubMed

    Seerapu, Sunitha; Srinivasan, B P

    2010-09-01

    A simple, sensitive, precise and robust reverse-phase high-performance liquid chromatographic method for analysis of ivabradine hydrochloride in pharmaceutical formulations was developed and validated as per ICH guidelines. The separation was performed on SS Wakosil C18AR, 250×4.6 mm, 5 ?m column with methanol:25 mM phosphate buffer (60:40 v/v), adjusted to pH 6.5 with orthophosphoric acid, added drop wise, as mobile phase. A well defined chromatographic peak of Ivabradine hydrochloride was exhibited with a retention time of 6.55±0.05 min and tailing factor of 1.14 at the flow rate of 0.8 ml/min and at ambient temperature, when monitored at 285 nm. The linear regression analysis data for calibration plots showed good linear relationship with R=0.9998 in the concentration range of 30-210 ?g/ml. The method was validated for precision, recovery and robustness. Intra and Inter-day precision (% relative standard deviation) were always less than 2%. The method showed the mean % recovery of 99.00 and 98.55 % for Ivabrad and Inapure tablets, respectively. The proposed method has been successfully applied to the commercial tablets without any interference of excipients. PMID:21695008

  5. Characterization of nicardipine hydrochloride-induced cell injury in human vascular endothelial cells.

    PubMed

    Ochi, Masanori; Kawai, Yoshiko; Tanaka, Yoshiyuki; Toyoda, Hiromu

    2015-02-01

    Nicardipine hydrochloride (NIC), a dihydropyridine calcium-channel blocking agent, has been widely used for the treatment of hypertension. Especially, nicardipine hydrochloride injection is used as first-line therapy for emergency treatment of abnormally high blood pressure. Although NIC has an attractive pharmacological profile, one of the dose-limiting factors of NIC is severe peripheral vascular injury after intravenous injection. The goal of this study was to better understand and thereby reduce NIC-mediated vascular injury. Here, we investigated the mechanism of NIC-induced vascular injury using human dermal microvascular endothelial cells (HMVECs). NIC decreased cell viability and increased percent of dead cells in a dose-dependent manner (10-30 ?g/mL). Although cell membrane injury was not significant over 9 hr exposure, significant changes of cell morphology and increases in vacuoles in HMVECs were observed within 30 min of NIC exposure (30 ?g/mL). Autophagosome labeling with monodansylcadaverine revealed increased autophagosomes in the NIC-treated cells, whereas caspase 3/7 activity was not increased in the NIC-treated cells (30 ?g/mL). Additionally, NIC-induced reduction of cell viability was inhibited by 3-methyladenine, an inhibitor of autophagosome formation. These findings suggest that NIC causes severe peripheral venous irritation via induction of autophagic cell death and that inhibition of autophagy could contribute to the reduction of NIC-induced vascular injury. PMID:25743564

  6. Randomized Controlled Trial of Levamisole Hydrochloride as Adjunctive Therapy in Severe Falciparum Malaria With High Parasitemia

    PubMed Central

    Maude, Richard J.; Silamut, Kamolrat; Plewes, Katherine; Charunwatthana, Prakaykaew; Ho, May; Abul Faiz, M.; Rahman, Ridwanur; Hossain, Md Amir; Hassan, Mahtab U.; Bin Yunus, Emran; Hoque, Gofranul; Islam, Faridul; Ghose, Aniruddha; Hanson, Josh; Schlatter, Joel; Lacey, Rachel; Eastaugh, Alison; Tarning, Joel; Lee, Sue J.; White, Nicholas J.; Chotivanich, Kesinee; Day, Nicholas P. J.; Dondorp, Arjen M.

    2014-01-01

    Background.?Cytoadherence and sequestration of erythrocytes containing mature stages of Plasmodium falciparum are central to the pathogenesis of severe malaria. The oral anthelminthic drug levamisole inhibits cytoadherence in vitro and reduces sequestration of late-stage parasites in uncomplicated falciparum malaria treated with quinine. Methods.?Fifty-six adult patients with severe malaria and high parasitemia admitted to a referral hospital in Bangladesh were randomized to receive a single dose of levamisole hydrochloride (150 mg) or no adjuvant to antimalarial treatment with intravenous artesunate. Results.?Circulating late-stage parasites measured as the median area under the parasite clearance curves were 2150 (interquartile range [IQR], 0–28 025) parasites/µL × hour in patients treated with levamisole and 5489 (IQR, 192–25 848) parasites/µL × hour in controls (P = .25). The “sequestration ratios” at 6 and 12 hours for all parasite stages and changes in microvascular blood flow did not differ between treatment groups (all P > .40). The median time to normalization of plasma lactate (<2 mmol/L) was 24 (IQR, 12–30) hours with levamisole vs 28 (IQR, 12–36) hours without levamisole (P = .15). Conclusions.?There was no benefit of a single-dose of levamisole hydrochloride as adjuvant to intravenous artesunate in the treatment of adults with severe falciparum malaria. Rapid parasite killing by intravenous artesunate might obscure the effects of levamisole. PMID:23943850

  7. Development of an enhanced formulation for delivering sustained release of buprenorphine hydrochloride

    PubMed Central

    Koocheki, S.; Madaeni, S.S.; Niroomandi, P.

    2011-01-01

    To control the minimum effective dose, and reduce the number and quantity of administered potent drugs are unique features of advanced drug delivery in situ forming gel formulation. The efficacy, consistency, and increasing the application of existing injection therapies can be enhanced through optimization of controlled released systems by using FDA approved biodegradable PLGA (poly-d,l-lactide-co-glycolide) polymer. The purpose of this study was to develop different in situ forming implant (ISFI) formulations of buprenorphine hydrochloride for post treatment of drug addicts, acute and chronic pains. The drug releases from different ISFIs membranes with and without Tween 80 were compared over a period of time. Kinetic equation followed the Korsmeyer–Peppas model, as the plots showed high linearity. The influence of this additive on polymer properties was investigated using differential scanning calorimetry (DSC), and the membranes structure was studied by X-ray diffractometry (XRD) and scanning electron microscope (SEM). Data revealed that Tween 80 modified the drug release pattern using diffusion mechanism and decreased the glass transition temperature (Tg) significantly. The degree of crystallinity was decreased after phase inversion which helps the dissolution of drug from membrane. The porosity of modified membranes was in accordance with release profiles. These findings suggest four different in situ forming implant formulations which can release various dose of the buprenorphine hydrochloride in a prolonged time. Also this surfactant can be an attractive additive for modifying the release rate of drugs from PLGA-based membrane drug delivery systems. PMID:23960766

  8. Testing lyoequivalency for three commercially sustained-release tablets containing diltiazem hydrochloride.

    PubMed

    Maswadeh, Hamzah A; Al-Hanbali, Othman A; Kanaan, Reem A; Shakya, Ashok K; Maraqa, Anwar

    2010-01-01

    In vitro release kinetics of three commercially available sustained release tablets (SR) diltiazem hydrochloride were studied at pH 1.1 for 2 h and for another 6 h at pH 6.8 using the USP dissolution apparatus with the paddle assemble. The kinetics of the dissolution process was studied by analyzing the dissolution data using five kinetic equations: the zero-order equation, the first-order equation, the Higuchi square root equation, the Hixson-Crowell cube root law and the Peppas equation. Analyses of the dissolution kinetic data for diltiazem hydrochloride commercial SR tablets showed that both Dilzacard and Dilzem SR tablets released drug by Non-Fickian (Anomalous transport) release with release exponent (n) equal to 0.59 and 0.54, respectively, which indicate the summation of both diffusion and dissolution controlled drug release. Bi-Tildiem SR tablets released drug by super case II (n = 1.29) which indicate zero-order release due to the dissolution of polymeric matrix and relaxation of the polymer chain. This finding was also in agreement with results obtained from application of zero-order and Hixson-Crowell equations. A dissolution profile comparative study was done to test the lyoequivelancy of the three products by using the mean dissolution time (MDT), dissimilarity factor f1 and similarity factor f2. Results showed that the three products are different and not lyoequivalent. PMID:20210085

  9. Efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia.

    PubMed

    Shenoy, K T; Veenasree; Leena, K B

    2003-06-01

    To document the clinical efficacy and tolerability of itopride hydrochloride in patients with non-ulcer dyspepsia an open-label, non-comparative study, was undertaken at the Medical College, Thiruvananthapuram, among patients with endoscopically confirmed diagnosis of non-ulcer dyspepsia or chronic gastritis. Itopride hydrochloride 50 mg (1 tablet) thrice a day for 2 weeks was administered among them. Relief of symptoms at the end of two weeks treatment, assessed as marked/complete, moderate, slight, none or worse; QT interval on ECG; adverse events; haemogram; serum chemistry for hepatic and renal functions. None had QT prolongation on ECG. At the end of 2 weeks' treatment, moderate to complete relief of symptoms was reported by 22 patients (73%), whereas 5 (17%) reproted slight improvement, and 3 (10%) reported no improvement. Clinical tolerability was excellent in 28 patients (93%) and good in 2 (7%). None of the patients had any prolongation of QT on ECG, nor did any patient show any abnormality in haemogram or serum chemistry during the treatment. PMID:14579989

  10. Stability-indicating spectrofluorimetric method for determination of itopride hydrochloride in raw material and pharmaceutical formulations.

    PubMed

    Walash, Mohamed I; Ibrahim, Fawzia; Eid, Manal I; El Abass, Samah Abo

    2013-11-01

    A simple, sensitive and rapid spectrofluorimetric method for determination of itopride hydrochloride in raw material and tablets has been developed. The proposed method is based on the measurement of the native fluorescence of the drug in water at 363 nm after excitation at 255 nm. The relative fluorescence intensity-concentration plot was rectilinear over the range of 0.1-2 ?g/mL (2.5?×?10(-7)-5.06?×?10(-6) mole/L), with good correlation (r?=?0.9999), limit of detection of 0.015 ?g/mL and a lower limit of quantification of 0.045 ?g/mL. The described method was successfully applied for the determination of itopride hydrochloride in its commercial tablets with average percentage recovery of 100.11?±?0.32 without interference from common excipients. Additionally, the proposed method can be applied for determination of itopride in combined tablets with rabeprazole or pantoprazole without prior separation. The method was extended to stability study of itopride. The drug was exposed to acidic, alkaline, oxidative and photolytic degradation according to ICH guidelines. Moreover, the method was utilized to investigate the kinetics of the alkaline, acidic and oxidative degradation of the drug. A proposal for the degradation pathways was postulated. PMID:23852162

  11. Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo.

    PubMed

    Tsubouchi, Tadashi; Saito, Takaharu; Mizutani, Fujie; Yamauchi, Toshie; Iwanaga, Yuji

    2003-08-01

    We investigated the effects of itopride hydrochloride (itopride, N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride), a gastroprokinetic agent, on the colonic motor activity in vitro and in vivo, in comparison with benzamides, cisapride hydrate (cisapride), and mosapride citrate (mosapride). Itopride stimulated both peristaltic and segmental motility induced by applying intraluminal pressure to the isolated guinea pig colon. Although cisapride and mosapride enhanced the segmental motility, they markedly reduced the peristaltic motility. In conscious dogs with implanted strain gauge force transducers, itopride stimulated contractile activity in the gastrointestinal tract from the stomach to the colon. Cisapride stimulated contractile activity in the gastric antrum, ileum, and ascending colon. Mosapride stimulated contractile activity only in the gastric antrum and ileum. In guinea pigs and rats, itopride accelerated colonic luminal transit. On the other hand, cisapride and mosapride failed to enhance colonic transit. These results demonstrate that itopride has a stimulatory action on colonic peristalsis, propelling colonic luminal contents, different from that of cisapride and mosapride. Therefore, itopride may be a useful drug for the treatment of functional bowel disorders such as functional constipation. PMID:12724347

  12. Noscapine hydrochloride disrupts the mitotic spindle in mammalian cells and induces aneuploidy as well as polyploidy in cultured human lymphocytes

    Microsoft Academic Search

    M. Schuler; P. Muehlbauer; P. Guzzie; D. A. Eastmond

    1999-01-01

    Noscapine hydrochloride is a centrally acting antitussive opium derivative widely used in cough suppressants. Recent studies have reported that noscapine is a potent inducer of polyploidy but not of aneuploidy in vitro. To obtain more comprehensive information about the cytogenetic effects of this compound, we treated cultured human lymphocytes (HPL) and Chinese hamster ovary (CHO) cells with various concentrations of

  13. Lipoprotein effects of combined ezetimibe and colesevelam hydrochloride versus ezetimibe alone in hypercholesterolemic subjects: a pilot study

    Microsoft Academic Search

    Robert H. Knopp; Christine Tsunehara; Barbara M. Retzlaff; Brian Fish; Hien Nguyen; Susan Anderson; Thuy Nguyen

    2006-01-01

    Two drug classes act in the intestine to lower cholesterol. Ezetimibe inhibits cholesterol absorption, whereas bile acid–binding resins enhance cholesterol excretion via enhanced conversion to bile acids. Combining these 2 classes may be beneficial, but cholestyramine binds ezetimibe, and the combined effect of colesevelam hydrochloride and ezetimibe was little studied. The aim of the study was to determine if adding

  14. Photophysical and photochemical properties of amitriptyline and nortriptyline hydrochloride: a 266 nm nanosecond laser flash and theoretical study

    Microsoft Academic Search

    Rafael Arce; Carmelo Garc??a; Rolando Oyola; Luis Piñero; Ileana Nieves; Nadya Cruz

    2003-01-01

    Amitriptyline (AMI) and nortriptyline (NT) hydrochlorides were studied by 266nm laser transient absorption spectroscopy and quantum theoretical calculations. Both drugs photoionize through a biphotonic mechanism producing a radical cation and the solvated electron. A triplet excited state in a twisted conformation around the exocyclic bond is proposed as the intermediate state in the photoionization process. The solvated electron reacts with

  15. Simultaneous spectrophotometric determination of metformin hydrochloride and glibenclamide in binary mixtures using combined discrete and continuous wavelet transforms.

    PubMed

    Sohrabi, Mahmoud Reza; Kamali, Naghmeh; Khakpour, Mazyar

    2011-01-01

    In this work, a combined discrete and continuous wavelet transform analysis was developed for simultaneous spectrophotometric determinations of metformin hydrochloride and glibenclamide, two antidiabetic drugs, in binary mixtures without any chemical pretreatment. Absorption spectra were subjected to the 4-level db4 discrete wavelet transform (DWT) for signal de-noising. Selected continuous wavelet transform (CWT) families (rbio3.1 with scaling factor, a = 80, and gaus2, a = 60) were applied on these de-noised signals. Finally, a zero-crossing technique was used for the construction of calibration curves for both drugs. The proposed method was validated by analyzing synthetic mixtures of the investigated drugs with various concentrations. The amount of metformin hydrochloride and glibenclamide were determined by using CWT amplitudes in zero-crossing points. The mean recovery values of metformin hydrochloride and glibenclamide were found between 98.6-102.0 and 97.9-102.4% for rbio3 and 98.3-101.2 and 97.1-101.4% for gaus2 families, respectively. The obtained results showed that the developed method is a simple, rapid and precise procedure for the simultaneous determination of metformin hydrochloride and glibenclamide in binary mixtures. PMID:21985929

  16. Palonosetron Hydrochloride Compatiblity and Stability with Three B-Lactam Anitbiotic During Simulated Y-Site Adminstration.

    PubMed

    Ben, Michel; Trusley, Craig; Kupiec, Thomas C; Trissel, Lawrence A

    2007-01-01

    Palonosetron hydrochloride is a relatively long-acting selective 5-HT3 receptor antagonist that has been approved for the prevention of chemotherapy-induced nausea and vomiting and is being ealuated for the prevention of postoperative nausea and vomiting. The objective of this study was to evaluate the physical and chemical stability of palonosetron hydrochloride 50 mcg/mL with the B-lactam antibiotics cefazolin sodium 20 mg/mL, cefotetan disodium 20 mg/mL, and the combination ampicillin sodium-sulbactam sodium 20 mg/mL and 10 mg/mL, respectively, during simulated Y-site administration. The effects of each of the antibiotics on palonosetron hydrochloride in these admixtures were tested in triplicate. Samples were stored and evaluated for up to 4 hours at room temperature. Physical stability was assessed by turbidimetric and particulate measurements and visual inspection. Chemical stability was assessed by high-performnace liquid chromatography. All of the admixtures were clear and colorless when viewed in normal fluorescent room light and when viewed with a Tyndall beam. Measured turbidity and particulate content were low initially and remained low throughout the study . The drug concentration was unchanged in all of the samples tested. Palonosetron hydrochloride is physically and chemically stable in admixtures with cefazolin sodium, cefotetan disodium and the combination ampicillin sodium-sulbactam sodium at the concentrations tested during simulated Y-site administration over 4 hours at ambient room temperature. PMID:23994813

  17. Extractive spectrophotometric methods for the determination of doxepin hydrochloride in pharmaceutical preparations using titanium (IV) and iron (III) thiocyanate complexes

    Microsoft Academic Search

    Wies?awa Misiuk

    2005-01-01

    Two simple, precise, and accurate extractive spectrophotometric methods have been developed for the determination of doxepin hydrochloride in pharmaceutical preparations. The methods are based on the formation of ion association complexes of doxepin with titanium (IV) and iron (III) thiocyanate complexes in acidic medium. The produced compounds are insoluble in water but well soluble in some organic solvents. They are

  18. Sevelamer hydrochloride dose-dependent increase in prevalence of severe acidosis in hemodialysis patients: analysis of nationwide statistical survey in Japan.

    PubMed

    Oka, Yoshinari; Miyazaki, Masashi; Matsuda, Hiroaki; Takatsu, Shigeko; Katsube, Ryouichi; Mori, Toshiko; Takehara, Kiyoto; Umeda, Yuzo; Uno, Futoshi

    2014-02-01

    Metabolic acidosis has a negative impact on prognosis of dialysis patients. The aim of this study was to determine the prevalence of severe metabolic acidosis in dialysis patients treated with sevelamer hydrochloride. In 2004, a nationwide survey (101,516 dialysis patients) was conducted by the Japanese Society for Dialysis Therapy. We analyzed 32,686 dialysis patients whose bicarbonate levels were measured in the survey. Sevelamer hydrochloride was prescribed to 9231 dialysis patients while 23,455 dialysis patients were not prescribed sevelamer hydrochloride. In the present study, we defined severe acidosis as bicarbonate <15.8 mmol/L. The mean serum bicarbonate level correlated significantly and negatively with the daily dose of sevelamer hydrochloride (R(2)?= 0.806, P < 0.0001). Logistic regression analysis indicated that the percentage of patients with severe acidosis increased significantly with increased dose of sevelamer hydrochloride (R(2) = 0.885, P < 0.00001). The estimated doses of sevelamer hydrochloride associated with severe acidosis in 10% and 15% of patients were 3.5 g/day (95% confidence interval [95%CI], 2.8-4.4) and 7.7 g/day (95%CI = 5.9-10.9), respectively. Severe acidosis was noted in 4.5% of patients who were not treated with sevelamer hydrochloride and in 16.1% of patients treated with sevelamer hydrochloride at ? 5.25 g/day (P < 0.0001). The results call for careful monitoring of serum bicarbonate level in hemodialysis patients treated with sevelamer hydrochloride. PMID:24499082

  19. Pre-treatment of Dairy and Breast Milk with Sevelamer Hydrochloride and Sevelamer Carbonate to Reduce Phosphate

    PubMed Central

    Raaijmakers, Renske; Houkes, Lambertus M.W.; Schröder, Cornelis H.; Willems, Johannes L.; Monnens, Leo A.H.

    2013-01-01

    ? Introduction: Young children and infants with chronic kidney disease are at increased risk of hyperphosphatemia because of high intake of dairy products. Hyperphosphatemia leads to metastatic calcifications and an increased risk of cardiovascular complications. Sevelamer is an effective phosphate binder, but for children it has important practical disadvantages: it clogs enteral feeding tubes and can cause gastrointestinal complaints. Pre-treatment of dairy products to reduce their phosphate content might solve those problems. ? Methods: Sevelamer hydrochloride and sevelamer carbonate were suspended in various dairy products (cow’s milk, breast milk, baby formula, and tube-feeding formula). Each product was tested with varying concentrations of sevelamer. After suspension, each sample was stored for 10 minutes, allowing the sevelamer to precipitate. The supernatant was decanted and analyzed for pH and for phosphate, calcium, magnesium, potassium, sodium, and chloride content. ? Results: We observed a significant decrease in the phosphate content of all tested products. With sevelamer hydrochloride, the phosphate reduction was 48% - 91% in the various products, and with sevelamer carbonate, it was 22% - 87%. The highest effectiveness was found in breast milk. A pH increase was found in all products. With sevelamer hydrochloride, a significant increase in chloride occurred. Notably, a significant decrease in calcium content (-75%) was observed in treated breast milk. ? Conclusions: Pretreatment of a variety of dairy products with either sevelamer hydrochloride or sevelamer carbonate effectively reduced their phosphate content and might avoid troublesome ingestion of sevelamer in children. The change in pH with sevelamer hydrochloride was remarkable, reflecting buffering mechanisms. The reduction in the calcium content of breast milk is a potential concern and should be carefully considered and monitored during clinical use of sevelamer. PMID:23636435

  20. Therapeutic class-specific signal detection of bradycardia associated with propranolol hydrochloride

    PubMed Central

    Gavali, Dhaval K.; Kulkarni, Kala S.; Kumar, Amal; Chakraborty, Bhaswat S.

    2009-01-01

    Background: Propranolol hydrochloride, one of the most widely used ?-blocker in the treatment of hypertension since 1960s, shows a number of serious and non-serious adverse events. Objective: Major objectives of this study were to extract the Canadian Adverse Drug Reaction Monitoring Program (CADRMP) database for possible toxic signal detection (SD) of propranolol hydrochloride, evaluate the frequency of the bradycardia associated with it in different stratified groups for a putative signal, and generate awareness in healthcare professionals regarding usefulness of SD. Materials and Methods: Appropriate statistical methods were used for adverse drug reaction (ADR) signal detection such as, proportional reporting ratio (PRR); reporting odds ratio (ROR); the Chi-square (?2) statistic method; the 95% confidence interval (CI); the observed to expected ratio (O/E); and Du Mouchel method were used to calculate the possible signals. Significance of ?2 and other calculated statistics, e.g., PRR and ROR, was based on a composite criterion of regulatory guidelines and not on any particular statistical level of significance. Results: Calculated statistics by different methods were compared with the regulatory criteria of a statistic value ?4.0 for ?2, and ?3.0 for the rest for SD to be declared significant. The PRR statistic was found to be 2.5054; by the ROR method it was 2.5820; the ?2 statistic was 3.2598, whereas the lower and upper limits of 95% CI of PRR were found to be 0.0778 and 1.9104, respectively, by the O/E ratio was found to be 2.3978, and PRR with the help of Du Mouchel was found to be 2.3979. Thus, the bradycardia–propranolol signals calculated in this study were not significant. Conclusions: The therapeutic class specific signal of bradycardia associated with propranolol hydrochloride was not found potent enough to cause bradycardia. However, since the calculated statistics were very high albeit not significant, the possibility of bradycardia–propranolol pairing should still be analyzed from larger databases. PMID:20523866

  1. Bivalent transition metal complexes of o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone: spectroscopic, antibacterial, antifungal activity and thermogravimetric studies.

    PubMed

    Zaky, R R; Ibrahim, K M; Gabr, I M

    2011-10-15

    Schiff base complexes of Cu(II), Ni(II) and Zn(II) with the o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone (H(2)o-HAHNH) containing N and O donor sites have been synthesized. Both ligand and its metal complexes were characterized by different physicochemical methods, elemental analysis, molar conductivity ((1)H NMR, (13)C NMR, IR, UV-visible, ESR, MS spectra) and also thermal analysis (TG and DTG) techniques. The discussion of the outcome data of the prepared complexes indicates that the ligand behave as a bidentate and/or tridentate ligand. The electronic spectra of the complexes as well as their magnetic moments suggest octahedral geometries for all isolated complexes. The room temperature solid state ESR spectrum of the Cu(II) complex shows d(x2-y2) as a ground state, suggesting tetragonally distorted octahedral geometry around Cu(II) centre. The molar conductance measurements proved that the complexes are non-electrolytes. The kinetic thermodynamic parameters such as: E(#), ?H(#), ?G(#), ?S(#) are calculated from the DTG curves, for the [Ni(H(O)-HAHNH)(2)] and [Zn(H(2O)-HAHNH)(OAc)(2)]·H(2)O complexes using the Coats-Redfern equation. Also, the antimicrobial properties of all compounds were studied using a wide spectrum of bacterial and fungal strains. The [Cu(Ho-HAHNH)(OAc)(H(2)O)(2)] complex was the most active against all strains, including Aspergillus sp., Stemphylium sp. and Trichoderma sp. Fungi; E. coli and Clostridium sp. Bacteria. PMID:21782500

  2. Bivalent transition metal complexes of o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone: Spectroscopic, antibacterial, antifungal activity and thermogravimetric studies

    NASA Astrophysics Data System (ADS)

    Zaky, R. R.; Ibrahim, K. M.; Gabr, I. M.

    2011-10-01

    Schiff base complexes of Cu(II), Ni(II) and Zn(II) with the o-hydroxyacetophenone [N-(3-hydroxy-2-naphthoyl)] hydrazone (H 2o-HAHNH) containing N and O donor sites have been synthesized. Both ligand and its metal complexes were characterized by different physicochemical methods, elemental analysis, molar conductivity ( 1H NMR, 13C NMR, IR, UV-visible, ESR, MS spectra) and also thermal analysis (TG and DTG) techniques. The discussion of the outcome data of the prepared complexes indicates that the ligand behave as a bidentate and/or tridentate ligand. The electronic spectra of the complexes as well as their magnetic moments suggest octahedral geometries for all isolated complexes. The room temperature solid state ESR spectrum of the Cu(II) complex shows d x2- y2 as a ground state, suggesting tetragonally distorted octahedral geometry around Cu(II) centre. The molar conductance measurements proved that the complexes are non-electrolytes. The kinetic thermodynamic parameters such as: E#, ? H#, ? G#, ? S# are calculated from the DTG curves, for the [Ni(H O-HAHNH) 2] and [Zn(H 2 O-HAHNH)(OAc) 2]·H 2O complexes using the Coats-Redfern equation. Also, the antimicrobial properties of all compounds were studied using a wide spectrum of bacterial and fungal strains. The [Cu(H o-HAHNH)(OAc)(H 2O) 2] complex was the most active against all strains, including Aspergillus sp., Stemphylium sp. and Trichoderma sp. Fungi; E. coli and Clostridium sp. Bacteria.

  3. Mono- and binuclear copper(II) complexes of new hydrazone ligands derived from 4,6-diacetylresorcinol: Synthesis, spectral studies and antimicrobial activity.

    PubMed

    Shebl, Magdy; El-ghamry, Mosad A; Khalil, Saied M E; Kishk, Mona A A

    2014-05-21

    Two new hydrazone ligands, H2L(1) and H2L(2), were synthesized by the condensation of 4,6-diacetylresorcinol with 3-hydrazino-5,6-diphenyl-1,2,4-triazine and isatin monohydrazone, respectively. The structures of the ligands were elucidated by elemental analyses, IR, (1)H NMR, electronic and mass spectra. Reactions of the ligands with several copper(II) salts, including AcO(-), NO3(-), SO4(2-), Cl(-) and Br(-) afforded mono- and binuclear metal complexes. Also, the ligands were allowed to react with Cu(II) ion in the presence of a secondary ligand (L') [N,O-donor; 8-hydroxyquinoline, N,N-donor; 1,10-phenanthroline or O,O-donor; benzoylacetone]. Characterization and structure elucidation of the prepared complexes were achieved by elemental and thermal analyses, IR, electronic, mass and ESR spectra as well as conductivity and magnetic susceptibility measurements. The ESR spin Hamiltonian parameters of some complexes were calculated. The spectroscopic data showed that the H2L(1) ligand acts as a neutral or monobasic tridentate ligand while the H2L(2) ligand acts as a bis(monobasic tridentate) ligand. The coordination sites with the copper(II) ion are phenolic oxygen, azomethine nitrogen and triazinic nitrogen (H2L(1) ligand) or isatinic oxygen (H2L(2) ligand). The metal complexes exhibited octahedral and square planar geometrical arrangements depending on the nature of the anion. The ligands and some metal complexes showed antimicrobial activity. PMID:24607473

  4. Chitosan and cyclodextrin in intranasal microemulsion for improved brain buspirone hydrochloride pharmacokinetics in rats.

    PubMed

    Bshara, Hamza; Osman, Rihab; Mansour, Samar; El-Shamy, Abd El-Hameed A

    2014-01-01

    The aim of this study was to develop buspirone hydrochloride microemulsion formulations for intranasal administration to improve the drug bioavailability and provide high drug brain levels. For the purpose, chitosan aspartate, and hydroxypropyl-?-cyclodextrin were incorporated in the microemulsions. The prepared formulations were characterized. Biological investigations including pharmacokinetic studies, brain drug targeting efficiency determinations and histopathological examinations were performed on rats. The results showed that safe and stable mucoadhesive microemulsion suitable for nasal administration were successfully prepared. Ex vivo drug permeation revealed high drug permeation from microemulsions. Absolute bioavailability after intranasal administration of buspirone mucoadhesive microemulsion increased significantly and plasma concentration peaked at 15 min. The AUC0-360(brain) was 3 times that obtained after intravenous administration. A high brain targeting efficiency (86.6%) and a direct nose to brain transport (88%) confirmed the direct nose to brain transport of buspirone following nasal administration of the microemulsions. PMID:24274510

  5. Taro corms mucilage/HPMC based transdermal patch: an efficient device for delivery of diltiazem hydrochloride.

    PubMed

    Sarkar, Gunjan; Saha, Nayan Ranjan; Roy, Indranil; Bhattacharyya, Amartya; Bose, Madhura; Mishra, Roshnara; Rana, Dipak; Bhattacharjee, Debashis; Chattopadhyay, Dipankar

    2014-05-01

    The aim of this work is to examine the effectiveness of mucilage/hydroxypropylmethylcellulose (HPMC) based transdermal patch (matrix type) as a drug delivery device. We have successfully extracted mucilage from Colocasia esculenta (Taro) corms and prepared diltiazem hydrochloride incorporated mucilage/HPMC based transdermal patches using various wt% of mucilage by the solvent evaporation technique. Characterization of both mucilage and transdermal patches has been done by several techniques such as Molisch's test, organoleptic evaluation of mucilage, mechanical, morphological and thermal analysis of transdermal patches. Skin irritation test is studied on hairless Albino rat skin showing that transdermal patches are apparently free of potentially hazardous skin irritation. Fourier transform infrared analysis shows that there is no interaction between drug, mucilage and HPMC while scanning electron microscopy shows the surface morphology of transdermal patches. In vitro drug release time of mucilage-HPMC based transdermal patches is prolonged with increasing mucilage concentration in the formulation. PMID:24556117

  6. Synthesis, crystal structure, characterization and DFT studies of L-valine L-valinium hydrochloride

    NASA Astrophysics Data System (ADS)

    Moitra, Sweta; Kumar Seth, Saikat; Kar, Tanusree

    2010-06-01

    A new nonlinear optical material L-valine L-valinium hydrochloride (VHCl) has been synthesized and identified by CHN test, FT-IR spectroscopy and XRD analysis. Formation of new crystal has been confirmed by single crystal X-ray diffraction analysis. VHCl crystallizes in monoclinic system with cell parameters a=11.144(2) Å, b=5.179(9) Å, c=13.028(2) Å, ?=111.85(3)°. Thermal stability of the crystal was investigated using thermogravimetric and differential thermal analysis studies. The suitability of this material for NLO application was studied by optical transmission studies and second harmonic generation (SHG) efficiency measurement by powder method. SHG efficiency of VHCl is found to be comparable to KDP. The molecular geometries and electronic structure of VHCl were calculated at the DFT level using the hybrid exchange-correlation functional, BLYP, PW91, PBE and BP.

  7. Metformin hydrochloride-loaded poly(vinyl alcohol) composites as drug delivery systems.

    PubMed

    Cai, Xiaoqing; Shao, Wei; Luan, Yuxia; Pang, Jianmei; Li, Feifei; Li, Zhonghao

    2011-10-01

    A straightforward method is proposed for the preparation of drug-loaded biocompatible polymer composites based on the freeze drying technique. The solution of poly(vinyl alcohol) (PVA) and metformin hydrochloride (MH) is frozen using liquid nitrogen and the ice crystals are removed by sublimation through freeze drying, which results in the formation of MH-loaded PVA composite. By controlling the PVA concentration in the solution, both MH-loaded PVA fibers and porous products can be obtained. The synthesized MH-loaded PVA composites are characterized with scanning electron microscopy (SEM), powder X-ray diffraction (XRD), Fourier-transformed infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The drug release behavior of the as-prepared products is studied to reveal their potential use in drug delivery system. PMID:22400234

  8. High pressure study of molecular dynamics of protic ionic liquid lidocaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Swiety-Pospiech, A.; Wojnarowska, Z.; Pionteck, J.; Pawlus, S.; Grzybowski, A.; Hensel-Bielowka, S.; Grzybowska, K.; Szulc, A.; Paluch, M.

    2012-06-01

    In this paper, we investigate the effect of pressure on the molecular dynamics of protic ionic liquid lidocaine hydrochloride, a commonly used pharmaceutical, by means of dielectric spectroscopy and pressure-temperature-volume methods. We observed that near Tg the pressure dependence of conductivity relaxation times reveals a peculiar behavior, which can be treated as a manifestation of decoupling between ion migration and structural relaxation times. Moreover, we discuss the validity of thermodynamic scaling in lidocaine HCl. We also employed the temperature-volume Avramov model to determine the value of pressure coefficient of glass transition temperature, dTg/dP|P = 0.1. Finally, we investigate the role of thermal and density fluctuations in controlling of molecular dynamics of the examined compound.

  9. High pressure study of molecular dynamics of protic ionic liquid lidocaine hydrochloride.

    PubMed

    Swiety-Pospiech, A; Wojnarowska, Z; Pionteck, J; Pawlus, S; Grzybowski, A; Hensel-Bielowka, S; Grzybowska, K; Szulc, A; Paluch, M

    2012-06-14

    In this paper, we investigate the effect of pressure on the molecular dynamics of protic ionic liquid lidocaine hydrochloride, a commonly used pharmaceutical, by means of dielectric spectroscopy and pressure-temperature-volume methods. We observed that near T(g) the pressure dependence of conductivity relaxation times reveals a peculiar behavior, which can be treated as a manifestation of decoupling between ion migration and structural relaxation times. Moreover, we discuss the validity of thermodynamic scaling in lidocaine HCl. We also employed the temperature-volume Avramov model to determine the value of pressure coefficient of glass transition temperature, dT(g)/dP|(P = 0.1). Finally, we investigate the role of thermal and density fluctuations in controlling of molecular dynamics of the examined compound. PMID:22713051

  10. Metallic-like Wilson ratio in the polyaniline hydrochloride conducting polymer

    NASA Astrophysics Data System (ADS)

    Limelette, P.; Schmaltz, B.; Brault, D.; Tran Van, F.

    2015-03-01

    We report on the calorimetric and magnetic properties of the polyaniline hydrochloride in order to discuss its metallicity. Both the specific heat and the magnetic susceptibility ? have been investigated as a function of temperature from 300 K down to 2 K. The measurements of the specific heat have allowed us to determine the electronic Sommerfeld coefficient ? and the temperature dependence of the susceptibility has revealed a Pauli-like component. By combining ? and ?, the dimensionless Wilson ratio RW??/? demonstrates that the universal free electrons limit is reached above 100 K as a strong check of the metallicity of this conducting polymer. By removing the Pauli component from the measured susceptibility, the resulting contribution displays below 100 K a well-defined Curie-like component in agreement with a few percents of spins localized by disorder at low temperatures. These results are therefore consistent with an electronic itinerancy, namely, a metallic state even in the presence of disorder.

  11. Development and Validation of Simultaneous Spectrophotometric Methods for Drotaverine Hydrochloride and Aceclofenac from Tablet Dosage Form

    PubMed Central

    Shah, S. A.; Shah, D. R.; Chauhan, R. S.; Jain, J. R.

    2011-01-01

    Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt's method), wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis), which employs 298.5 nm as ?1 and 276 nm as ?2 (?max of AF) for formation of equations. Both the methods were found to be linear between the range of 8-32 ?g/ml for drotaverine and 10-40 ?g/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form. PMID:22457554

  12. Simultaneous determination of lidocaine hydrochloride, hydrocortisone and nystatin in a pharmaceutical preparation by RP-LC.

    PubMed

    Pendela, Murali; Kahsay, Getu; Baekelandt, Isabel; Van Schepdael, Ann; Adams, Erwin

    2011-11-01

    A liquid chromatographic (LC) method was developed to analyze a formulation (mouthwash) containing lidocaine hydrochloride, hydrocortisone and nystatin. A single LC method with UV detection was developed. A Waters Symmetry C18 HPLC column (150 mm × 4.6 mm, 5 ?m) was used as stationary phase and the assay was performed with gradient elution using mobile phases containing methanol - 0.1M NaH(2)PO(4) with a pH that was previously adjusted to 4.5 with dilute phosphoric acid. The sample pretreatment was performed by treating the formulation with methanol followed by filtration. After method development, the influence of the different chromatographic parameters on the separation, the interference of other active compounds and excipients, linearity, accuracy, repeatability and intermediate precision were investigated. The method was shown to be selective, linear, accurate, precise and repeatable. Finally, the content of the compounds in the formulation was determined. PMID:21794999

  13. Simultaneous removal of tetracycline hydrochloride and As(III) using poorly-crystalline manganese dioxide.

    PubMed

    Wang, Huawei; Zhang, Daoyong; Mou, Shuyong; Song, Wenjuan; Al-Misned, Fahad A; Golam Mortuza, M; Pan, Xiangliang

    2015-10-01

    Simultaneous removal of antibiotic tetracycline hydrochloride (TC) and As(III) by poorly-crystalline Mn dioxide was investigated. TC and As(III) can be effectively oxidized and removed by MnO2. High concentrations of TC and As(III) competed with each other for oxidation or adsorption sites on MnO2 and thus affected their removal efficiency. The intermediates and products of TC after reaction with poorly-crystalline manganese dioxide were identified by LC-ESI-MS (liquid chromatography-electrospray ionization-mass spectrometry), and the decomposition pathways of TC by MnO2 were proposed. This study is helpful for understanding the importance of environmental Mn dioxides in the decontamination of combined pollution by organic pollutants and metal(loid)s. PMID:25966328

  14. Reduced cytotoxicity of polyhexamethylene biguanide hydrochloride (PHMB) by egg phosphatidylcholine while maintaining antimicrobial efficacy.

    PubMed

    Müller, Gerald; Kramer, Axel; Schmitt, Jürgen; Harden, Daniela; Koburger, Torsten

    2011-04-25

    Liposomes or oil-in-water emulsions containing egg yolk phosphatidylcholine (EPC) were combined with aqueous polyhexamethylene biguanide hydrochloride (PHMB). The bactericidal activity of these preparations against Pseudomonas aeruginosa and Staphylococcus aureus as well as their cytotoxicity on cultured murine fibroblasts (L929 cells) was then assayed for either 30 min or 60 min in the presence of cell culture medium containing 10% fetal bovine serum as surrogate for wound fluid. We used two assay designs: in the first bactericidal activity and cytotoxicity were determined in separate experiments; in the second both were determined in one experiment. Combining PHMB and EPC containing o/w emulsions or liposomes protects mammalian cells without neutralizing the antiseptic effect. From all tested combinations the o/w emulsions containing 0.05% PHMB proved to be superior in this respect to the aqueous preparation. PMID:21356204

  15. Transdermal Delivery of Venlafaxine Hydrochloride: The Effects of Enhancers on Permeation Across Pig Ear Skin

    PubMed Central

    Vijaya, C.; Bingi, Manasa; Vigneshwaran, L. V.

    2011-01-01

    Venlafaxine representing a new class of antidepressants is a potent serotonin/ norepinephrine reuptake inhibitor. Transdermal delivery of venlafaxine hydrochloride (VHCl) may result in proper patient compliance by reducing the incidence of the undesirable GI problems generally associated with its plural oral dosing. The present study is an attempt to investigate the improvement of the transdermal flux of the hydrophilic VHCl by certain permeation enhancers viz. glycerin, urea, propylene glycol and mixture of propylene glycol and ethanol across pig ear skin. The cumulative drug release was the highest from the formulation F5 consisting of the mixture of propylene glycol and ethanol in sodium alginate gel with a load of 25% w/w VHCl with 96% permeation enhancement. The steady state flux observed with F5 was 0.203 mg cm-2 hr and an area of 15.27 cm2 would suffice to arrive at a required therapeutic concentration of VHCl in the blood. PMID:22707834

  16. Studies on binding interactions between clenbuterol hydrochloride and two serum albumins by multispectroscopic approaches in vitro.

    PubMed

    Wang, Qin; Zhang, Shengrui

    2014-08-01

    In this study, binding properties of clenbuterol hydrochloride (CL) with human serum albumin (HSA) and bovine serum albumin (BSA) were examined using constant protein concentrations and various CL contents under physiological conditions. The binding parameters were confirmed using fluorescence quenching spectroscopy at various temperatures. The experimental results confirmed that the quenching mechanisms of CL and HSA/BSA were both static quenching processes. The thermodynamic parameters, namely, enthalpy change (?H) and entropy change (?S), were calculated according to the van't Hoff equation, which suggested that the electrostatic interactions were the predominant intermolecular forces in stabilizing the CL-HSA complex, and hydrogen bonds and van der Waals force were the predominant intermolecular forces in stabilizing the CL-BSA complex. Furthermore, the conformational changes of HSA/BSA in the presence of CL were determined using the data obtained from three-dimensional fluorescence spectroscopy, ultraviolet-visible absorption spectroscopy and circular dichroism spectroscopy. PMID:24030872

  17. Bladder tissue permeability and transport modelling of intravesical alum, lidocaine hydrochloride, methylprednisolone hemisuccinate and mitomycin C.

    PubMed

    Moch, Céline; Salmon, Damien; Rodríguez Armesto, Laura; Colombel, Marc; Pivot, Christine; Pirot, Fabrice

    2014-04-10

    The aims of this study were to assess the tissue permeability of the bladder and to characterize the transport of four drugs displaying different physico-chemical properties and commonly used in intravesical delivery, through porcine bladder. The transport of aluminium through porcine bladder was assessed by using a vertical static diffusion cell. Lidocaine hydrochloride, methylprednisolone hemisuccinate and mitomycin C were tested by using three different experimental setups, including vertical static diffusion cell, microdialyseur and lab-patented device. Penetration results on different experimental setups were homogenous suggesting dependency on physico-chemical characteristics of drug and subsequent interaction with bladder wall structure. Oppositely, permeation varied consistently with experimental setup characteristics (i.e., permeation surface, receptor fluid volume and hydrodynamic). Mathematical modelling of drug transport through bladder wall is proposed considering scarce literature on this route of administration. Practical outcome of this study could drive compounding optimization towards improvement of safety and efficacy in patient undergoing intravesical administration. PMID:24463072

  18. Saved by the Nose: Bystander-Administered Intranasal Naloxone Hydrochloride for Opioid Overdose

    PubMed Central

    Doe-Simkins, Maya; Epstein, Andy; Moyer, Peter

    2009-01-01

    Administering naloxone hydrochloride (naloxone) during an opioid overdose reverses the overdose and can prevent death. Although typically delivered via intramuscular or intravenous injection, naloxone may be delivered via intranasal spray device. In August 2006, the Boston Public Health Commission passed a public health regulation that authorized an opioid overdose prevention program that included intranasal naloxone education and distribution of the spray to potential bystanders. Participants were taught by trained nonmedical needle exchange staff. After 15 months, the program provided training and intranasal naloxone to 385 participants who reported 74 successful overdose reversals. Problems with intranasal naloxone were uncommon. Overdose prevention education with distribution of intranasal naloxone is a feasible public health intervention to address opioid overdose. PMID:19363214

  19. Simultaneous determination of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate in pharmaceutical preparations using multivariate calibration 1

    NASA Astrophysics Data System (ADS)

    Samadi-Maybodi, Abdolraouf; Hassani Nejad-Darzi, Seyed Karim

    2010-04-01

    Resolution of binary mixtures of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate with minimum sample pre-treatment and without analyte separation has been successfully achieved by methods of partial least squares algorithm with one dependent variable, principal component regression and hybrid linear analysis. Data of analysis were obtained from UV-vis spectra of the above compounds. The method of central composite design was used in the ranges of 1-15 mg L -1 for both calibration and validation sets. The models refinement procedure and their validation were performed by cross-validation. Figures of merit such as selectivity, sensitivity, analytical sensitivity and limit of detection were determined for all three compounds. The procedure was successfully applied to simultaneous determination of the above compounds in pharmaceutical tablets.

  20. Biogenic gold nanoparticles as fotillas to fire berberine hydrochloride using folic acid as molecular road map.

    PubMed

    Pandey, Sunil; Mewada, Ashmi; Thakur, Mukeshchand; Shah, Ritu; Oza, Goldie; Sharon, Madhuri

    2013-10-01

    Use of biologically modified gold nanoparticles (GNPs) as molecular vehicle to ferry potential anti-cancer drug berberine hydrochloride (BHC) using folic acid (FA) as targeting molecule is reported in this work. A tropical fruit peel, Trapa bispinosa is used to fabricate highly monodispersed GNPs, passivated with essential functional groups which were used as linkers to attach FA and BHC via amide linkage. Flocculation Parameter (FP) of biologically synthesized GNPs was calculated under different salt concentrations which were found to be very ideal under a physiological condition. Various statistical models were used to find drug release profile out of which Higuchi was found to be the most ideal. GNP-FA-BHC complexes were found to be active against folic acid expressing HeLa cells. PMID:23910269

  1. Guanidine hydrochloride induced reversible dissociation and denaturation of duck delta2-crystallin.

    PubMed

    Lee, H J; Chang, G G

    2000-07-01

    The tetrameric delta2-crystallin from duck lens exhibits a reversible dissociation-denaturation process in solutions containing guanidine hydrochloride (GdnHCl). Sigmoidal or biphasic curves for the dissociation/denaturation processes, obtained using different methods of structural analysis, as a function of GdnHCl concentration were not coincidental with each other. delta2-crystallin in 0.91 M GdnHCl existed primarily as a monomer, which had no endogenous argininosuccinate lyase activity. After dilution of the GdnHCl-treated protein, the monomers reassociated into tetramers with concomitant recovery of enzyme activity. The sigmoidal recovery of enzyme activity demonstrates a cooperative hysteretic reactivation process. When the concentration of GdnHCl was higher than 1.2 M, various partially unfolded soluble forms of delta2-crystallin were produced from the dissociated monomers as shown by size-exclusion chromatography. The formation of a partially unfolded intermediate during the dissociation-denaturation process is proposed. PMID:10866796

  2. Development and validation of simultaneous spectrophotometric methods for drotaverine hydrochloride and aceclofenac from tablet dosage form.

    PubMed

    Shah, S A; Shah, D R; Chauhan, R S; Jain, J R

    2011-05-01

    Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt's method), wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis), which employs 298.5 nm as ?(1) and 276 nm as ?(2) (?max of AF) for formation of equations. Both the methods were found to be linear between the range of 8-32 ?g/ml for drotaverine and 10-40 ?g/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form. PMID:22457554

  3. Pulmonary effects in man of oral prizidilol hydrochloride (SK&F 92657), a new antihypertensive agent.

    PubMed Central

    Edmondstone, W M; Waller, J F; Manghani, K K; Hill, P L; Bell, A J; Denison, D M

    1983-01-01

    The effects on heart rate, blood pressure and pulmonary function of single oral doses of prizidilol hydrochloride (400 mg SK&F 92657) and propranolol (40 mg) were compared with placebo in nine healthy volunteers, in a double blind crossover study. Prizidilol had no effect on heart rate while propranolol caused a significant reduction compared with placebo. Diastolic blood pressure was lowered to the same extent by both prizidilol and propranolol. Propranolol significantly reduced the forced expiratory volume in 1 second (FEV1), forced vital capacity (FVC) and the maximal expiratory flow at 50% vital capacity (MEF 50). Prizidilol had no effect on flow-volume loop parameters. Effective pulmonary blood flow was not altered by propranolol, but it was significantly increased by prizidilol. Oral prizidilol exerts its hypotensive effect by vasodilatation without reflex tachycardia. It does not cause airways obstruction in healthy subjects. PMID:6140939

  4. Functional photoacoustic imaging to observe regional brain activation induced by cocaine hydrochloride

    NASA Astrophysics Data System (ADS)

    Jo, Janggun; Yang, Xinmai

    2011-09-01

    Photoacoustic microscopy (PAM) was used to detect small animal brain activation in response to drug abuse. Cocaine hydrochloride in saline solution was injected into the blood stream of Sprague Dawley rats through tail veins. The rat brain functional change in response to the injection of drug was then monitored by the PAM technique. Images in the coronal view of the rat brain at the locations of 1.2 and 3.4 mm posterior to bregma were obtained. The resulted photoacoustic (PA) images showed the regional changes in the blood volume. Additionally, the regional changes in blood oxygenation were also presented. The results demonstrated that PA imaging is capable of monitoring regional hemodynamic changes induced by drug abuse.

  5. Simultaneous determination of a binary mixture of pantoprazole sodium and itopride hydrochloride by four spectrophotometric methods.

    PubMed

    Ramadan, Nesrin K; El-Ragehy, Nariman A; Ragab, Mona T; El-Zeany, Badr A

    2015-02-25

    Four simple, sensitive, accurate and precise spectrophotometric methods were developed for the simultaneous determination of a binary mixture containing Pantoprazole Sodium Sesquihydrate (PAN) and Itopride Hydrochloride (ITH). Method (A) is the derivative ratio method ((1)DD), method (B) is the mean centering of ratio spectra method (MCR), method (C) is the ratio difference method (RD) and method (D) is the isoabsorptive point coupled with third derivative method ((3)D). Linear correlation was obtained in range 8-44 ?g/mL for PAN by the four proposed methods, 8-40 ?g/mL for ITH by methods A, B and C and 10-40 ?g/mL for ITH by method D. The suggested methods were validated according to ICH guidelines. The obtained results were statistically compared with those obtained by the official and a reported method for PAN and ITH, respectively, showing no significant difference with respect to accuracy and precision. PMID:25238185

  6. Evaluation of anti-GERD activity of gastro retentive drug delivery system of itopride hydrochloride.

    PubMed

    Satapathy, Trilochan; Panda, Prasana K; Goyal, Amit K; Rath, Goutam

    2010-08-01

    The present work describes the formulation and evaluation of the gastroretentive system of Itopride hydrochloride. In this research, we have formulated floating hydrogel-based microspheres employing calcium carbonate (CaCO(3)) as a gas forming agent dispersed in alginate matrix. In vitro characterizations such as drug content, particle size, and drug release were carried out. GI motility was determined by administration of charcoal meal to rats. Results demonstrated that prepared microspheres were spherical in shape with smooth surface, good loading efficiency, and excellent buoyancy. The gastro retentive dosage form of itiopride demonstrated significant antacid, anti-ulcer, and anti-GERD activity after 12 hours in comparison with the conventional dosage form. PMID:20515421

  7. Detection of Clenbuterol Hydrochloride Residuals in Pork Liver Using a Customized Surface Plasmon Resonance Bioanalyzer

    PubMed Central

    Hu, Jiandong; Chen, Ruipeng; Wang, Shun; Wang, Tingting; Zhao, Yuanyuan; Li, Jianwei; Hu, Xinran; Liang, Hao; Zhu, Juanhua; Sun, Xiaohui; Ma, Liuzheng; Jiang, Min

    2015-01-01

    A surface plasmon resonance (SPR) immunoassay with an immobilization of self-assembled molecular identification membrane for the detection of residual Clenbuterol Hydrochloride (CLB) in pork liver was systematically investigated and experimentally validated for its high performance. SPR immunoassay with a regular competitive inhibition assay cannot be directly verified to detect CLB residuals. In this study, the binding of Au film with mercaptopropionic acid was investigated using the known form of the strong S-Au covalent bonds formed by the chemical radical of the mercaptopropionic acid and the Au film. After that, the immunoglobulin IgG of swine (SwIgG-CLB) was bonded with the mercaptopropionic acid by covalent -CO-NH- amide bonding. The modified comprehensive analysis of how the membrane structure works was introduced together with the customized SPR bioanalyzer. In order to evaluate the performance of this biomembrane structure, the concentrations of CLB-contained solutions of 0 ng•mL-1, 10 ng•mL-1, 20 ng•mL-1, 33.3 ng•mL-1, and 40 ng•mL-1 were prepared by adding CLB reagents into the solutions of CLB antibody (Clenbuterol Hydrochloride Antibody, CLB-Ab), successively and then the response unit (RU) was measured individually. Using the data collected from the linear CCD array, the fitting curve was established with the R-Square value of 0.9929. Correspondingly, the recovery rate ranged from 88.48% to 103.21% was experimented and the limit of detection of CLB in 1.26 ng•mL-1 was obtained efficiently. It was concluded that the detection method associated with biomembrane properties is expected to contribute much to the determination of residual CLB in pork liver quantitatively by using the customized SPR bioanalyzer. PMID:25799327

  8. Stability indicating methods for determination of Donepezil Hydrochloride according to ICH guidelines.

    PubMed

    Abbas, Samah Sayed; Fayez, Yasmin Mohamed; Abdel Fattah, Laila El-Sayed

    2006-10-01

    Stability indicating assays for determination of Donepezil Hydrochloride in presence of its oxidative degradate were developed and validated. The first three are spectrophotometric methods depending on using zero order (D(0)), first order (D(1)) and second order (D(2)) spectra. The absorbance was measured at 315 nm for (D(0)) while the amplitude was measured at 332.1nm for (D(1)) and 340 nm for (D(2)) using deionized water as a solvent. Donepezil Hydrochloride (I) can be determined in the presence of up to 70% of its oxidative degradate (II) using (D(0)), 80% using (D(1)) and 90% using (D(2)). The linearity range was found to be 8-56 microg ml(-1) for (D(0)), (D(1)) and (D(2)). These methods were applied for the analysis of I in both powder and tablet form. Also, a spectrofluorimetric method depending on measuring the native fluorescence of I in deionized water using lambda excitation 226 nm and lambda emission 391 nm is suggested. The linearity range was found to be 0.32-3.20 microg ml(-1) using this method, I was determined in the presence of up to 90% of II. The proposed method was applied for the analysis of I in tablet form as well as in human plasma. The last method depends on using TLC separation of I from its oxidative degradate II and I was then determined spectrodensitometrically. The mobile phase was methanol : chloroform : 25% ammonia (16 : 64 : 0.1 by volume). The linearity range was found to be 2-15 microg/spot. This method was applied to the analysis of I in both powder and tablet form using acetonitrile as a solvent. PMID:17015988

  9. Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in patients with peripheral arterial disease

    PubMed Central

    Kunisawa, Takayuki; Yamagishi, Akio; Suno, Manabu; Nakade, Susumu; Honda, Naoki; Kurosawa, Atsushi; Sugawara, Ami; Tasaki, Yoshikazu; Iwasaki, Hiroshi

    2015-01-01

    Purpose We previously determined the pharmacokinetic (PK) parameters of landiolol in healthy male volunteers and gynecological patients. In this study, we determined the PK parameters of landiolol in patients with peripheral arterial disease. Methods Eight patients scheduled to undergo peripheral arterial surgery were enrolled in the study. After inducing anesthesia, landiolol hydrochloride was administered at target plasma concentrations of 500 and 1,000 ng/mL for 30 minutes each. A total of 112 data points of plasma concentration were collected from the patients and used for the population PK analysis. A population PK model was developed using a nonlinear mixed-effect modeling software program (NONMEM). Results The patients had markedly decreased heart rates at 2 minutes after initiation of landiolol hydrochloride administration; however, systolic blood pressures were lower than the baseline values at only five time points. The concentration time course of landiolol was best described by a two-compartment model with lag time. The estimates of PK parameters were as follows: total body clearance, 30.7 mL/min/kg; distribution volume of the central compartment, 65.0 mL/kg; intercompartmental clearance, 48.3 mL/min/kg; distribution volume of the peripheral compartment, 54.4 mL/kg; and lag time, 0.633 minutes. The predictive performance of this model was better than that of the previous model. Conclusion The PK parameters of landiolol were best described by a two-compartment model with lag time. Distribution volume of the central compartment and total body clearance of landiolol in patients with peripheral arterial disease were approximately 64% and 84% of those in healthy volunteers, respectively. PMID:25653534

  10. Detection of clenbuterol hydrochloride residuals in pork liver using a customized surface plasmon resonance bioanalyzer.

    PubMed

    Hu, Jiandong; Chen, Ruipeng; Wang, Shun; Wang, Tingting; Zhao, Yuanyuan; Li, Jianwei; Hu, Xinran; Liang, Hao; Zhu, Juanhua; Sun, Xiaohui; Ma, Liuzheng; Jiang, Min

    2015-01-01

    A surface plasmon resonance (SPR) immunoassay with an immobilization of self-assembled molecular identification membrane for the detection of residual Clenbuterol Hydrochloride (CLB) in pork liver was systematically investigated and experimentally validated for its high performance. SPR immunoassay with a regular competitive inhibition assay cannot be directly verified to detect CLB residuals. In this study, the binding of Au film with mercaptopropionic acid was investigated using the known form of the strong S-Au covalent bonds formed by the chemical radical of the mercaptopropionic acid and the Au film. After that, the immunoglobulin IgG of swine (SwIgG-CLB) was bonded with the mercaptopropionic acid by covalent -CO-NH- amide bonding. The modified comprehensive analysis of how the membrane structure works was introduced together with the customized SPR bioanalyzer. In order to evaluate the performance of this biomembrane structure, the concentrations of CLB-contained solutions of 0 ng · mL(-1), 10 ng · mL(-1), 20 ng · mL(-1), 33.3 ng · mL(-1), and 40 ng · mL(-1) were prepared by adding CLB reagents into the solutions of CLB antibody (Clenbuterol Hydrochloride Antibody, CLB-Ab), successively and then the response unit (RU) was measured individually. Using the data collected from the linear CCD array, the fitting curve was established with the R-Square value of 0.9929. Correspondingly, the recovery rate ranged from 88.48% to 103.21% was experimented and the limit of detection of CLB in 1.26 ng · mL(-1) was obtained efficiently. It was concluded that the detection method associated with biomembrane properties is expected to contribute much to the determination of residual CLB in pork liver quantitatively by using the customized SPR bioanalyzer. PMID:25799327

  11. Randomized controlled trial of bixalomer versus sevelamer hydrochloride in hemodialysis patients with hyperphosphatemia.

    PubMed

    Akizawa, Tadao; Origasa, Hideki; Kameoka, Chisato; Kaneko, Yuichiro; Kawasaki, Shigenori

    2014-04-01

    Hyperphosphatemia is a prognostic factor for morbidity and mortality in chronic kidney disease. Bixalomer is a nonabsorbable polymer that decreases serum phosphate levels by binding phosphate in the gastrointestinal tract. This study compared the efficacy and safety of bixalomer versus sevelamer hydrochloride for controlling hyperphosphatemia in hemodialysis patients. This was a multicenter, randomized open-label, non-inferiority study. The primary endpoint was serum phosphate on completion of treatment. Administration of bixalomer was started at 1.5?g/day and adjusted to a maximum of 7.5?g/day depending on the serum phosphate level. Sevelamer hydrochloride was started at 3.0 or 6.0?g/day and adjusted to a maximum of 9.0?g/day. Treatment was continued for 12 weeks. Fifty-five patients were randomized to each treatment group. After 12 weeks, the baseline adjusted mean serum phosphate level was 5.87?mg/dL in the bixalomer group and 5.55?mg/dL in the sevelamer group, with a difference of 0.31?mg/dL and 95% confidence interval (CI) of [-0.13 to 0.76]. The upper limit of the 95%CI for the difference of the mean serum phosphate level between the two groups was <1.0?mg/dL, which was the non-inferiority margin in this study. Thus, non-inferiority of bixalomer to sevelamer was confirmed. The incidence of adverse events was lower in the bixalomer group, and bixalomer did not promote acidosis. Bixalomer achieved a similar reduction of serum phosphate to sevelamer, while causing fewer adverse reactions. Consequently, the usefulness of bixalomer for treating hyperphosphatemia was confirmed. PMID:24720402

  12. Surfactant-mediated dissolution of metformin hydrochloride tablets: wetting effects versus ion pairs diffusivity.

    PubMed

    Desai, Divyakant; Wong, Benjamin; Huang, Yande; Ye, Qingmei; Tang, Dan; Guo, Hang; Huang, Ming; Timmins, Peter

    2014-03-01

    The aqueous solubility of metformin (pKa: 2.8 and 11.5) in the pH range of 1.2-6.8 is 300 mg/mL. Thus, the dissolution of metformin hydrochloride tablets should be pH independent. However, 850 mg metformin hydrochloride tablets dissolved more slowly in pH 1.2 and 4.5 dissolution media than in pH 6.8 medium. It is hypothesized that the additional protonation of metformin at the acidic pH results in higher solvation and a larger hydrodynamic radius, leading to slower diffusion and dissolution. This hypothesis was supported by the observation that cationic metformin and anionic sodium lauryl sulfate (SLS), 0.1% (w/v), formed an insoluble salt (1:2 molar ratio) at pH 1.2 and 4.5, but not at pH 6.8. SLS at 0.01% (w/v) in all three media enhanced metformin dissolution. The slower metformin dissolution at pH 1.2 and 4.5 media with SLS can be attributed to the formation of metformin-lauryl sulfate (Met-LS) (1:2 and 1:1) ion pairs, which are more hydrophobic than Met-LS (1:1) ion pairs at pH 6.8. Slower metformin diffusivity in pH 4.5 with 0.05% (w/v) SLS was observed by diffusion-ordered spectroscopy nuclear magnetic resonance. Improved metformin wetting by SLS outweighed the lower diffusivity of metformin-LS ion pairs because similar enhancement in dissolution was noted with 0.5% (w/v) nonionic polysorbate 80. PMID:24549733

  13. Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices.

    PubMed

    Javadzadeh, Yousef; Musaalrezaei, Leila; Nokhodchi, Ali

    2008-10-01

    It is suggested here that liquisolid technique has the potential to be optimized for the reduction of drug dissolution rate and thereby production of sustained release systems. In the present study, propranolol hydrochloride was dispersed in polysorbate 80 as the liquid vehicle. Then a binary mixture of carrier-coating materials (Eudragit RL or RS as the carrier and silica as the coating material) was added to the liquid medication under continuous mixing in a mortar. The final mixture was compressed using the manual tableting machine. The effect of drug concentration, loading factor, thermal treating and aging on release profile of propranolol hydrochloride from liquisolid compacts were investigated at two pH values (1.2 and 6.8). The release rate of propranolol HCl from liquisolid compacts was compared to the release of propranolol HCl from conventional tablets. X-ray crystallography and DSC were used to investigate the formation of any complex between drug and excipients or any crystallinity changes during the manufacturing process. Propranolol HCl tablets prepared by liquisolid technique showed greater retardation properties in comparison with conventional matrix tablets. This investigation provided evidence that polysorbate 80 (Tween 80) has important role in sustaining the release of drug from liquisolid matrices, and a reduction of T(g) of the polymer can be the reason for the release prolongation of liquisolid tablets. The results also showed that wet granulation had remarkable impact on release rate of propranolol HCl from liquisolid compacts, reducing the release rate of drug from liquisolid compacts. The results showed that aging (liquisolid tablets were kept at 25 degrees C/75% relative humidity for 6 months) had no effect on hardness and dissolution profile of drug. The kinetics studies revealed that most of the liquisolid formulations followed the zero-order release pattern. X-ray crystallography and DSC ruled out any changes in crystallinity or complex formation during the manufacturing process of liquisolid formulations. PMID:18647643

  14. End-to-end continuous flow synthesis and purification of diphenhydramine hydrochloride featuring atom economy, in-line separation, and flow of molten ammonium salts

    E-print Network

    Snead, David R.

    A continuous end-to-end synthesis and purification of diphenhydramine hydrochloride featuring atom economy and waste minimization is described. Combining a 1 : 1 molar ratio of the two starting material streams ...

  15. Memantine Hydrochloride and Whole-Brain Radiotherapy With or Without Hippocampal Avoidance in Reducing Neurocognitive Decline in Patients With Brain Metastases | Division of Cancer Prevention

    Cancer.gov

    This randomized phase III trial compares memantine hydrochloride and whole-brain radiotherapy with or without hippocampal avoidance in reducing neurocognitive decline in patients with cancer that has spread to the brain. Whole brain radiotherapy (WBRT) is the most common treatment for brain metastasis. Unfortunately, the majority of patients with brain metastases experience cognitive deterioration after WBRT. Memantine hydrochloride may enhance cognitive function by binding to and inhibiting channels of receptors located in the central nervous system.

  16. Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate.

    PubMed

    Taha, Ali; Emara, Adel A A; Mashaly, Mahmoud M; Adly, Omima M I

    2014-09-15

    Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L=dianion of the hydrazone, m=0-1, x=0-2, n=0-4 and z=0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms. PMID:24810030

  17. Spectral characterization, molecular modeling and antimicrobial studies on hydrazone metal complexes of 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)dione and S-methyl dithiocarbazate

    NASA Astrophysics Data System (ADS)

    Taha, Ali; Emara, Adel A. A.; Mashaly, Mahmoud M.; Adly, Omima M. I.

    2014-09-01

    Metal complexes of copper(II), nickel(II), cobalt(II), oxovanadium(IV), chromium(III) and cadmium(II) with a new bridged ONS dibasic tridentate hydrazone (H2L) derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione with S-methyl dithiocarbazate have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, spectral (infrared, electronic, mass, 1H NMR and ESR) studies as well as thermal gravimetric analysis (TGA). The synthesized complexes have dimeric structures with the general formula [ML(NO3)m(H2O)x]2·nH2O·zMeOH, L = dianion of the hydrazone, m = 0-1, x = 0-2, n = 0-4 and z = 0-1. The metal complexes exhibited square planar, tetrahedral and octahedral geometrical arrangements, the molar conductivity data indicates that all complexes are neutral. The Coats-Redfern equation was used to calculate the kinetic and thermodynamic parameters for the different thermal decomposition stages of some complexes. Structural parameters of the ligand and its metal complexes have been theoretically computed on the basis of semiempirical PM3 level and the results were correlated with their experimental data. Antibacterial activities of the free ligand and its metal complexes were screened against various organisms.

  18. Effects of ractopamine hydrochloride and zilpaterol hydrochloride supplementation on longissimus muscle shear force and sensory attributes of calf-fed Holstein steers.

    PubMed

    Howard, S T; Woerner, D R; Vote, D J; Scanga, J A; Chapman, P L; Bryant, T C; Acheson, R J; Tatum, J D; Belk, K E

    2014-01-01

    The effect of ractopamine hydrochloride (RH) and zilpaterol hydrochloride (ZH) on slice shear force (SSF) and sensory characteristics of beef from calf-fed Holstein steers was evaluated. All steers were implanted with a progesterone (100 mg) plus estradiol benzoate (10 mg) implant followed by a terminal trenbolone acetate (200 mg) plus estradiol (40 mg) implant. Steers were blocked by weight into pens (n = 32) randomly assigned to 1 of 4 treatments: control, RH fed at 300 mg·steer(-1)·d(-1) (RH 300) or RH fed at 400 mg·steer(-1)·d(-1)(RH 400) for the final 31 d of finishing, or ZH fed at 6.8 g/t for 21 d with a 5-d withdrawal before harvest. Fourteen carcasses were randomly selected from each pen, and two LM samples (1 per side) were excised and aged either 14 or 21 d before SSF testing. For trained panel evaluation, two steaks were collected from each of 60 low Choice strip loins (20 each from control, RH 300, and ZH treatments) and aged either 14 or 21 d. Steers fed RH and ZH produced steaks with SSF values that were 9% to 25% higher than controls. No difference in SSF was detected between the two levels of RH (P > 0.05). Compared to controls, the probability of steaks aged 14 d failing to meet SSF requirements to be certified tender (SSF < 20 kg) was increased 0.15, 0.17, and 0.26 in steers fed RH 300, RH 400, and ZH, respectively. Compared to controls, the probability of steaks aged 21 d having SSF values >20 kg was increased 0.03, 0.08, and 0.16 in steers fed RH 300, RH 400, and ZH, respectively. Steaks from Select carcasses of steers fed ZH aged 21 d postmortem had double the probability (0.39 vs. 0.17) of having SSF values >20 kg compared to steaks from steers fed either level of RH (P < 0.05). This difference tended to be identical in steaks from Select carcasses 14 d postmortem (0.50 vs. 0.33; P = 0.11); however, no difference was found in low Choice samples at 14 or 21 d postmortem. Trained panelists rated steaks aged 14 d from steers fed ZH lower for overall tenderness and flavor compared to controls (P < 0.05); however, no difference was found between controls and those fed RH 300. Steaks from steers fed ZH aged 21 d were rated lower for overall tenderness and juiciness compared to controls and those from steers fed RH 300 (P < 0.05). This study suggests RH and ZH negatively impact sensory attributes of beef from calf-fed Holstein steers. PMID:24243905

  19. Carteolol Hydrochloride Suppresses the Generation of Reactive Oxygen Species and Rescues Cell Death After Ultraviolet Irradiation of Cultured Lens Epithelial Cells

    PubMed Central

    Kaji, Yuichi; Kiuchi, Takahiro; Oshika, Tetsuro

    2010-01-01

    Introduction: Anti-oxidant activities of adrenergic ?-blockers are proposed in various organs. The aim of the present study was to investigate the effect of carteolol hydrochloride, an adrenergic ?-blocker, on the production of reactive oxygen species (ROS) and the viable cell number after ultraviolet irradiation of cultured lens epithelial cells (LECs). Materials and Methodology: Cultured LECs were exposed to 0, 10–5, 10–4, and 10–3 M carteolol hydrochloride for 30 min followed by ultraviolet B (UVB) irradiation at intensity of 100, 200, or 400 mJ/cm2. The amount of ROS in the LECs was measured using dichlorodihydrofluorescein at 30 min after exposure to UVB. In addition, the number of living LECs was counted at 15 h after exposure to UVB. Results: Exposure to 10–3 M carteolol hydrochloride significantly decreased the amount of ROS after exposure to UVB at intensities of 100, 200, and 400 mJ/cm2. In addition, 10–3 M carteolol hydrochloride significantly increased the viable cell number after exposure to UVB at 400 mJ/cm2. However, 10–4 and 10–5M carteolol hydrochloride had no significant effect on ROS or the viable cell number in LECs. Discussions: Carteolol hydrochloride protects LECs against UVB irradiation by inhibiting the intracellular production of ROS. PMID:21283534

  20. Effect of arginine hydrochloride and hydroxypropyl cellulose as stabilizers on the physical stability of high drug loading nanosuspensions of a poorly soluble compound.

    PubMed

    Ain-Ai, Anchalee; Gupta, Pardeep K

    2008-03-01

    The objective of the present study is to formulate Naproxen nanosuspensions at high drug concentrations of up to 300 mg/ml using ball milling and is to investigate the additive effect between hydroxypropyl cellulose (HPC) and arginine hydrochloride as stabilizers. The nanosuspensions were obtained at different arginine hydrochloride/polymer weight ratios. Stability of Naproxen suspensions at 100 and 300 mg/ml was determined over a period of 14 days by measuring the particle size. The control, which contained only drug and buffers without the stabilizers agglomerated immediately after preparation. The study of the effect of arginine hydrochloride as a primary stabilizer indicated that arginine hydrochloride levels of up to 0.8% (w/v) were not able to help reduce particle size below one micron, and were also not able to provide stabilization to the suspensions on storage. Therefore, HPC was also added to the system to increase suspensions stability, presumably by a steric repulsion mechanism. When the Naproxen concentration was increased to 300 mg/ml, 1% (w/v) HPC was not able to provide good stabilization and it was found that arginine hydrochloride increased the stabilization efficiency of 1% (w/v) HPC by preventing flocculation. When HPC level was increased to 4% (w/v), HPC was high enough to sufficiently stabilize the nanosuspensions for 2 weeks and thereby could maintain the mean size diameter of the suspensions without the presence of arginine hydrochloride. Furthermore, stable nanosuspensions were successfully lyophilized without the use of additional cryoprotectants. PMID:18036751

  1. Spectrophotometric methods for the determination of benazepril hydrochloride in its single and multi-component dosage forms.

    PubMed

    El-Yazbi, F A; Abdine, H H; Shaalan, R A

    1999-06-01

    Three sensitive and accurate methods are presented for the determination of benazepril in its dosage forms. The first method uses derivative spectrophotometry to resolve the interference due to formulation matrix. The second method depends on the color formed by the reaction of the drug with bromocresol green (BCG). The third one utilizes the reaction of benazepril, after alkaline hydrolysis, with 3-methylbenzothialozone (MBTH) hydrazone where the produced color is measured at 593 nm. The latter method was extended to develop a stability-indicating method for this drug. Moreover, the derivative method was applied for the determination of benazepril in its combination with hydrochlorothiazide. The proposed methods were applied for the analysis of benazepril in the pure form and in tablets. The coefficient of variation was less than 2%. PMID:10704041

  2. Spectrofluorimetric determination of 3-methylflavone-8-carboxylic acid, the main active metabolite of flavoxate hydrochloride in human urine.

    PubMed

    Zaazaa, Hala E; Mohamed, Afaf O; Hawwam, Maha A; Abdelkawy, Mohamed

    2015-01-01

    A simple, sensitive and selective spectrofluorimetric method has been developed for the determination of 3-methylflavone-8-carboxylic acid as the main active metabolite of flavoxate hydrochloride in human urine. The proposed method was based on the measurement of the native fluorescence of the metabolite in methanol at an emission wavelength 390 nm, upon excitation at 338 nm. Moreover, the urinary excretion pattern has been calculated using the proposed method. Taking the advantage that 3-methylflavone-8-carboxylic acid is also the alkaline degradate, the proposed method was applied to in vitro determination of flavoxate hydrochloride in tablets dosage form via the measurement of its corresponding degradate. The method was validated in accordance with the ICH requirements and statistically compared to the official method with no significant difference in performance. PMID:25004902

  3. Spectrofluorimetric determination of 3-methylflavone-8-carboxylic acid, the main active metabolite of flavoxate hydrochloride in human urine

    NASA Astrophysics Data System (ADS)

    Zaazaa, Hala E.; Mohamed, Afaf O.; Hawwam, Maha A.; Abdelkawy, Mohamed

    2015-01-01

    A simple, sensitive and selective spectrofluorimetric method has been developed for the determination of 3-methylflavone-8-carboxylic acid as the main active metabolite of flavoxate hydrochloride in human urine. The proposed method was based on the measurement of the native fluorescence of the metabolite in methanol at an emission wavelength 390 nm, upon excitation at 338 nm. Moreover, the urinary excretion pattern has been calculated using the proposed method. Taking the advantage that 3-methylflavone-8-carboxylic acid is also the alkaline degradate, the proposed method was applied to in vitro determination of flavoxate hydrochloride in tablets dosage form via the measurement of its corresponding degradate. The method was validated in accordance with the ICH requirements and statistically compared to the official method with no significant difference in performance.

  4. Formulation and in vitro evaluation of metformin hydrochloride loaded microspheres prepared with polysaccharide extracted from natural sources.

    PubMed

    Sharma, Hemanta Kumar; Lahkar, Sunita; Kanta Nath, Lila

    2013-06-01

    The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study. PMID:23846143

  5. Self-interaction of native and denatured lysozyme in the presence of osmolytes, l-arginine and guanidine hydrochloride

    Microsoft Academic Search

    Xiao-Yan Dong; Jian-Hua Liu; Fu-Feng Liu; Yan Sun

    2009-01-01

    Osmolyte molecules such as betaine and trehalose are protein stabilizers while l-arginine (Arg) and guanidine hydrochloride (GdnHCl) are the most widely used aggregation suppressor in protein refolding. We have herein studied the effects of the osmolyte molecules and l-arginine together with GdnHCl (0–6mol\\/L) on the intermolecular interaction of native and denatured lysozyme by self-interaction chromatography. The self-interaction is characterized in

  6. Structure of and hydrogen bonding in a 3:2 inclusion compound of N-methylmorpholine betaine hydrochloride with acetonitrile

    Microsoft Academic Search

    Z. Dega-Szafran; M. Szafran; A. Antkowiak; M. Grundwald-Wyspianska; E. Nowak; M. Gdaniec; Z. Kosturkiewicz

    2002-01-01

    N-Methylmorpholine betaine hydrochloride (MMB·HCl) forms a 3:2 inclusion compound with acetonitrile. The crystal structure of the compound has been determined at 100K from a twinned crystal to be trigonal with the space group P3; a=b=16.767(2), c=6.996(1)A?,?=120°. The host framework is constructed from the ionic pairs formed by the chlorine anion and the protonated, at the carboxylate group, betaine cation. The

  7. Two polymorphs of 4-hydroxy-1-methylpiperidine betaine hydrochloride studied by X-ray and DFT methods

    Microsoft Academic Search

    Z. Dega-Szafran; E. Dulewicz; G. Dutkiewicz; Z. Kosturkiewicz; M. Szafran

    2005-01-01

    Two polymorphic crystals (? and ?) of 4-hydroxy-1-methylpiperidine betaine hydrochloride, HO-MPBH+·Cl?, have been synthesized and their structures solved by the X-ray diffraction methods. The piperidine ring adopts the chair conformation and the hydroxy group at C(4) in the ?-polymorph is in the axial position, while in the ?-polymorph it is in the equatorial one. The CH2COOH group in both polymorphs

  8. Crystal and molecular structures of 3-amino-4-hydroxy benzenesulfonamide and its hydrochloride: Quantum-chemical study of their tautomerism

    SciTech Connect

    Kovalchukova, O. V., E-mail: okovalchukova@mail.ru; Strashnova, S. B.; Romashkina, E. P.; Strashnov, P. V.; Zaitsev, B. E. [Peoples' Friendship University of Russia (Russian Federation)] [Peoples' Friendship University of Russia (Russian Federation); Sergienko, V. S. [Russian Academy of Sciences, Kurnakov Institute of General and Inorganic Chemistry (Russian Federation)] [Russian Academy of Sciences, Kurnakov Institute of General and Inorganic Chemistry (Russian Federation)

    2013-03-15

    3-amino-4-hydroxy benzenesulfonamide and its hydrochloride have been isolated in the crystalline state. Their crystal and molecular structures are determined by X-ray diffraction. The equilibrium between neutral tautomeric forms of the 3-amino-4-hydroxy benzenesulfonamide molecule is studied within the approximation of density functional theory (B3LYP/aug-cc-pVDZ). The constants of acid-base equilibrium of 3-amino-4-hydroxy benzenesulfonamide are deter-mined using spectrophotometry.

  9. Computer simulations of extractant primary amine N1923 and N1923 hydrochloride salt at water\\/chloroform interface

    Microsoft Academic Search

    J.-X. Guo; S.-X. Sun; S.-L. Yuan; X.-K. Ran; G. Y. Xu

    2006-01-01

    A molecular dynamics (MD) simulation has been carried out to investigate the structural and dynamical properties of extractant methyloctadecyl amine (N1923), and its hydrochloride salt at water\\/chloroform interface. The simulation results show that both N1923 molecule and protonated N1923 ion can self-assembly form a monolayer at the interface like most non-ionic or cationic surfactants. It is not only observed that

  10. Chemosensitivity of Glioblastoma Cells during Treatment with the Organo–tin Compound Triethyltin(IV)lupinylsulfide Hydrochloride

    Microsoft Academic Search

    Federica Barbieri; Fabio Sparatore; Rudy Bonavia; Cristina Bruzzo; Gennaro Schettini; Angela Alama

    2002-01-01

    Malignant gliomas are the most common primary brain tumors in humans. However, poor response to conventional therapeutic approaches, including chemotherapy, leads invariably to disease recurrence and progression. The organo–tin derivative triethyltin(IV)lupinylsulfide hydrochloride (IST-FS 29) was identified and developed as potential antiproliferative agent in human cancer cell lines. However, for its peculiar chemical structure and good lipophilicity, this compound also appeared

  11. Calcium-silicate-based floating granular delivery system of ranitidine hydrochloride for effective management of peptic ulcer

    Microsoft Academic Search

    Ashish Jain; Prateek Jain; Sunil K. Jain; Ram K. Agrawal; Govind P. Agrawal

    2008-01-01

    The objective of the present investigation was to prepare and evaluate a floating granular delivery system for the treatment\\u000a of mucosal ulcer consisting of (i) calcium silicate (CS) as a porous carrier; (ii) ranitidine hydrochloride (RH), an anti-ulcer\\u000a agent; and (iii) hydroxypropyl methylcellulose K4M (HPMC) and ethylcellulose (EC) as matrix-forming polymers. The effect of\\u000a various formulation and process variables on

  12. Bupivacaine Hydrochloride Induces Muscle Fiber Necrosis and Hydroxyl Radical Formation-Dimethyl Sulphoxide Reduces Hydroxyl Radical Formation

    Microsoft Academic Search

    Nobuo Wakata; Hideki Sugimoto; Hiroaki Iguchi; Nobuatsu Nomoto; Masao Kinoshita

    2001-01-01

    We induced acute skeletal muscle necrosis in rats using bupivacaine hydrochloride and found that both 2,5- and 2,3-dihydroxybenzoic acid significantly increased in skeletal muscle. A single administration of dimethyl sulphoxide, a free radical scavenger, significantly lowered concentrations of 2,5- and 2,3-dihydroxybenzoic acid. These results suggest that dimethyl sulphoxide is an effective hydroxyl radical scavenger and may be useful in the

  13. Paroxetine hydrochloride controlled release POLYOX® matrix tablets: Screening of formulation variables using Plackett-Burman screening design

    Microsoft Academic Search

    Shun-Ji Jin; Yeon-Hee Yoo; Min-Soo Kim; Jeong-Soo Kim; Jeong-Sook Park; Sung-Joo Hwang

    2008-01-01

    The aim of the present study was to screen the effects of the formulation variables — POLYOX® molecular weight (X1), the ratio of POLYOX®\\/Avicel® PH102 (X2) and the amount of POLYOX® and Avicel® PH102 (X3), hardness (X4), HPMCP amount (X5), Eudragit® L100 amount (X6), and citric acid amount (X7) — on the paroxetine hydrochloride release from POLYOX® matrix tablet using

  14. Effects of tetracycline hydrochloride on measurements with the laser fluorescence device DIAGNOdent: in vitro and in vivo studies

    Microsoft Academic Search

    Eriko Nagaoka; Tomio Morohashi; Junichirou Kinoshita; Akiko Karakawa; Nobuhiro Sakai; Shoji Yamada; Mitsuko Inoue

    Dental materials that fluoresce affect the reading of the laser fluorescence device DIAGNOdent. Tetracycline hydrochloride\\u000a (TCH) shows fluorescence and is retained in teeth. The aim of this study was to evaluate the effects of TCH on the DIAGNOdent\\u000a reading. Filter-paper discs that contained various amounts of TCH were prepared (0.16–10 mg per disc). One-day-old newborn\\u000a rats were subcutaneously injected with TCH

  15. Reconstruction of an in vitro cornea and its use for drug permeation studies from different formulations containing pilocarpine hydrochloride

    Microsoft Academic Search

    Stefanie Tegtmeyer; Ioannis Papantoniou; Christel C. Müller-Goymann

    2001-01-01

    The aim of the present contribution was to develop a functional three-dimensional tissue construct to study ocular permeation of pilocarpine hydrochloride from different formulations. The in vitro model was compared to excised bovine cornea. Modified Franz cells were used to study the transcorneal permeability. Analysis was performed by reversed-phase high-performance liquid chromatography. Comparisons of the permeation rates through excised bovine

  16. Preliminary study of fortnightly irinotecan hydrochloride plus cisplatin therapy in patients with advanced gastric and colorectal cancer

    Microsoft Academic Search

    Atsushi Sato; Minoru Kurihara; Masaaki Matsukawa; Ken Shimada; Takeshi Yamazaki; Masatoshi Nakamachi; Takahiko Koda

    2001-01-01

    Purpose: Irinotecan hydrochloride shows a strong activity against gastric cancer and colorectal cancer, while combined therapy with irinotecan and cisplatin is useful for gastric cancer. However, myelosuppression and diarrhea are still dose-limiting factors. To reduce such toxicities to enable therapy to be performed on an outpatient basis, we tested the effect of divided administration of cisplatin. Methods: Irinotecan (60 mg\\/m2)

  17. HPLC-DAD STABILITY INDICATING DETERMINATION OF THE FIXED-DOSE COMBINATION OF NIFUROXAZIDE AND DROTAVERINE HYDROCHLORIDE IN CAPSULES

    Microsoft Academic Search

    Hadir M. Maher; Tarek S. Belal

    2012-01-01

    A simple and selective HPLC-DAD method was developed for the simultaneous determination of nifuroxazide and drotaverine hydrochloride in their combined pharmaceutical formulation. Effective chromatographic separation was achieved using Zorbax SB-C18 (4.6 × 250 mm, 5 µm) column with gradient elution of the mobile phase composed of 0.05 M phosphoric acid and methanol. The multiple wavelength detector was set at 245, 285 and 370 nm. The retention

  18. Cathodic adsorptive stripping voltammetry of drotaverine hydrochloride and its determination in tablets and human urine by differential pulse voltammetry

    Microsoft Academic Search

    S. I. M. Zayed; Y. M. Issa

    2009-01-01

    The stripping voltammetric behaviour of drotaverine hydrochloride (DvCl) was studied using a hanging mercury drop electrode (HMDE). The adsorptive stripping response has been evaluated with respect to pH, accumulation time, accumulation potential, scan rate and other variables. Differential pulse DP mode; over the potential range ?400 to ?1200 mV, is used in the presence of 0.04 M Britton–Robinson buffer pH 2. Cyclic

  19. Simultaneous Determination of Diclofenac Potassium and Drotaverine Hydrochloride in Human Plasma using Reversed-Phase High-Performance Liquid Chromatography

    Microsoft Academic Search

    Prasad P. Dahivelkar

    2012-01-01

    A simple high-performance liquid chromatographic method with ultraviolet detection is proposed for the estimation of diclofenac potassium and drotaverine hydrochloride in human plasma. Liquid - liquid extraction was carried out with a mixture of dichloro- methane- isopropyl alcohol (80:20, v\\/v). Chromatographic separ- ation of the analytes and internal standard was achieved on an analytical 250 3 4.6 mm i.d. reversed-phase

  20. An open clinical trial on the efficacy of cetirizine hydrochloride in the management of allergic pruritus in cats

    PubMed Central

    Griffin, Joya S.; Scott, Danny W.; Miller, William H.; Tranchina, Michelle M.

    2012-01-01

    Cetirizine hydrochloride was administered orally at 5 mg/cat, q24h, to 32 cats with allergic skin disease. Pruritus was reduced in 41% (13/32) of the cats. The antipruritic effect was repeatable and sustainable. There was no significant association between patient age, disease severity, or cutaneous reaction pattern and improvement during cetirizine administration. No adverse side effects were reported. PMID:22753962

  1. Preparation and adsorption behavior of berberine hydrochloride imprinted polymers by using silica gel as sacrificed support material

    NASA Astrophysics Data System (ADS)

    Li, Hui; Li, Yuzhuo; Li, Zhiping; Peng, Xiyang; Li, Yanan; Li, Gui; Tan, Xianzhou; Chen, Gongxi

    2012-03-01

    Preparation of berberine hydrochloride (B-Cl) imprinted polymers (MIPs) based on surface imprinting technique with silica gel as sacrificial support material was performed successfully by using B-Cl as template, methacrylic acid (MAA) and ethylene glycol dimethacrylate (EGDMA) as functional monomer and cross-linker, respectively. The prepared polymers were characterized by Fourier transmission infrared spectrometry (FTIR) and scanning electron microscopy (SEM). Adsorption behavior of the MIPs for the template and its structural analogues was investigated. Sites distribution on the surface of MIPs was explored by using different isotherm adsorption models and thermodynamic parameters for the adsorption of B-Cl on the MIPs determined. Sample application and reusability for the MIPs was also evaluated. Results indicated the strong adsorption and high selectivity of the MIPs for B-Cl. Saturated adsorption capacity reached 27.2 ?mol g-1 and the selectivity coefficient of the MIPs for B-Cl relative to jatrorrhizine hydrochloride (J-Cl) and palmatine palmatus hydrochloride (P-Cl) are 3.70 and 6.03, respectively. In addition, the MIPs were shown with good reusability and selectively retention ability in sample application.

  2. Determination of antihypertensive drug moexipril hydrochloride based on the enhancement effect of sodium dodecyl sulfate at carbon paste electrode.

    PubMed

    Attia, Ali K

    2010-04-15

    Herein, an electrochemical differential pulse voltammetric method was developed for the determination of moexipril hydrochloride based on the enhancement effect of sodium dodecyl sulfate. The oxidation process has been carried out in Britton-Robinson buffer. Moexipril hydrochloride exhibits a well-defined irreversible oxidation peak over the entire pH range (2-11). The peak current varied linearly over the range from 4.0 x 10(-7) to 5.2 x 10(-6) mol L(-1). The limits of detection and quantification were 6.87 x 10(-8) mol L(-1) and 2.29 x 10(-7) mol L(-1), respectively. The recovery was found in the range from 99.65% to 100.76%. The relative standard deviation was found in the range from 0.429% to 0.845%. The proposed method possesses high sensitivity, accuracy and rapid response. Finally, this method was successfully used to determine moexipril hydrochloride in tablets. PMID:20188882

  3. Formulation of bi-layer matrix tablets of tramadol hydrochloride: Comparison of rate retarding ability of the incorporated hydrophilic polymers.

    PubMed

    Arif, Hasanul; Al-Masum, Abdullah; Sharmin, Florida; Reza, Selim; Sm Islam, Sm Ashraful

    2015-05-01

    Bi-layer tablets of tramadol hydrochloride were prepared by direct compression technique. Each tablet contains an instant release layer with a sustained release layer. The instant release layer was found to release the initial dose immediately within minutes. The instant release layer was combined with sustained release matrix made of varying quantity of Methocel K4M, Methocel K15MCR and Carbomer 974P. Bi-layer tablets were evaluated for various physical tests including weight variation, thickness and diameter, hardness and percent friability. Drug release from bi-layer tablet was studied in acidic medium and buffer medium for two and six hours respectively. Sustained release of tramadol hydrochloride was observed with a controlled fashion that was characteristic to the type and extent of polymer used. % Drug release from eight-hour dissolution study was fitted with several kinetic models. Mean dissolution time (MDT) and fractional dissolution values (T25%, T50% and T80%) were also calculated as well, to compare the retarding ability of the polymers. Methocel K15MCR was found to be the most effective in rate retardation of freely water-soluble tramadol hydrochloride compared to Methocel K4M and Capbomer 974P, when incorporated at equal ratio in the formulation. PMID:26004717

  4. Determination of itopride hydrochloride in human plasma by RP-HPLC with fluorescence detection and its use in bioequivalence study.

    PubMed

    Ma, Jing; Yuan, Li-Hua; Ding, Mei-Juan; Zhang, Jun; Zhang, Qing; Xu, Qun-Wei; Zhou, Xue-Min

    2009-03-01

    A sensitive, selective and simple method using a precipitation of protein with 10% perchloric acid, followed by high-performance liquid chromatography (HPLC) with fluorescence detection was developed for the determination of itopride hydrochloride in human plasma, using levofloxacin as the internal standard (IS). Chromatographic separation was obtained within 7.0 min using a reverse phase Hypersil BDS C(18) (250 mm x 4.6 mm, 5 microm) column and an isocratic mobile phase, constituting of a mixture of 0.1 mol/l ammonium acetate-methanol (30:70, v/v) flowing at 1.1 ml/min. The excitation and emission wavelengths were set at 304 and 344 nm, respectively. The method was validated over the concentration range of 5 ng/ml to 1000.0 ng/ml. The lower limit of quantitation (LLOQ) was 5 ng/ml. The extractive recovery of itopride hydrochloride from the biological matrix was more than 80.77%. The intra-day accuracy of the drug containing serum samples was more than 82.94% with a precision of 2.81-4.37%. The inter-day accuracy was 82.91% or more, with a precision of 6.89-9.54%. The limit we have used (70-143%) is based on the local regulatory authority (SFDA). The developed method was validated and successfully applied to bioequivalence studies of itopride hydrochloride in healthy male volunteers. PMID:19101632

  5. Molecular structure, hydrogen bonding, basicity and spectroscopic properties of 3-hydroxypyridine betaine hydrochloride monohydrate

    NASA Astrophysics Data System (ADS)

    Barczy?ski, P.; Komasa, A.; Katrusiak, A.; Dega-Szafran, Z.; Szafran, M.

    2007-04-01

    The effect of hydrogen bonding, inter- and intramolecular electrostatic interactions on the structure of 3-hydroxy-pyridine betaine hydrochloride monohydrate (1-carboxymethyl-3-hydroxypyridinium chloride monohydrate), 3-HO-PBH·Cl·H 2O, has been studied by X-ray diffraction, 1H and 13C NMR and FTIR spectroscopies, and by the B3LYP/6-31G(d,p) calculations. In the crystal, the Cl - anion is connected with protonated betaine via the hydrogen bond, O dbnd C sbnd O sbnd H⋯Cl - = 2.993(2) Å and with neighboring H 2O molecules via the 3.111(1) and 3.578(1) Å bonds, while the 3-OH group interacts with water molecule by the hydrogen bond of 2.566(2) Å, forming an aggregate along the [b] direction. The water molecule additionally forms hydrogen bonds of 2.888(3) Å to the C dbnd O bond of O dbnd C sbnd OH group. On recrystallization the 1:1 complex slowly converts into the 2:1 complex, bis(3-hydroxy-pyridine betaine) hydrochloride, [bis(1-carboxymethyl-3-hydroxypyridinium) chloride], [(3-HO-PB) 2H·Cl]. The geometries of 3-HO-PBH·Cl·H 2O in the gas phase (vacuum), DMSO and water solutions have been optimized by the B3LYP/6-31G(d,p) level of theory using the COSMO model. Good linear correlations between 13C and 1H experimental chemical shifts and GIAO/ B3LYP/6-31G(d,p) calculated magnetic isotropic shielding tensors ( ?) have been obtained. The FTIR spectrum of the 1:1 complex shows a broad and intense absorption in the 3100-2500 cm -1 region due to the stretching vibration of hydrogen bonds between the Cl - anion and COOH, OH substituents and H 2O molecules, and the ?C dbnd O band at 1739 cm -1. The spectrum of the 2:1 complex shows an additional broad absorption in the 1900-800 cm -1 region due to the O sbnd H·O hydrogen bonds between COO groups.

  6. Perspectives on the application of zilpaterol hydrochloride in the United States beef industry.

    PubMed

    Delmore, R J; Hodgen, J M; Johnson, B J

    2010-08-01

    Zilpaterol hydrochloride (ZH) is a beta-adrenergic agonist approved to be fed at a rate of 8.3 mg/kg (100% DM basis) during the final 20 to 40 d of the finishing period in beef cattle followed by a minimum 3-d withdrawal period antemortem. The Federal Drug Administration (FDA) approved label claims of increased rate of BW gain, improved feed efficiency, and increased carcass leanness. Before the release of ZH for commercial use in 2007, approximately 10 independent research trials at various universities and commercial feedlots were initiated. Articles in recent issues of the Journal of Animal Science are a result of the large comprehensive body of research designed to increase the understanding of the effect of ZH on beef cattle growth, carcass traits, and beef quality. The feeding of ZH for 20 to 40 d with a 3-d withdrawal resulted in significantly increased ADG. The increases equate to an average of 9 kg heavier BW in ZH-fed steers. Hot carcass weight has been shown to increase to a larger degree compared with BW, with an average improvement of 15 kg. Dressing percent is increased by 1.5 to 2.0% with the feeding of ZH. Increases in carcass leanness were reported for cattle fed ZH mainly through a reduction in yield grades. The LM area was increased, along with yield of subprimal cuts from the round, flank, and loin. Warner-Bratzler shear force studies have shown LM steaks from ZH-treated cattle to have increased shear force values of 1.1 to 1.7 kg for 7-d-aged steaks, 0.4 to 1.3 kg for 14-d-aged steaks, and 0.27 to 1.4 kg for 21-d-aged steaks compared with controls. Recent research has suggested that the aging response is normal in ZH steaks. Consumers were able to identify tenderness differences in 14-d-aged Choice steaks from cattle fed ZH for 20 d compared with 14-d-aged steaks from control cattle; this difference was mitigated with 21 d of postmortem aging. Zilpaterol hydrochloride has been shown to increase cattle growth and efficiency as well as lean tissue deposition in the carcass, with some impact on carcass traits such as Warner-Bratzler shear force. PMID:20382871

  7. Formulation and evaluation of buccal film of Ivabradine hydrochloride for the treatment of stable angina pectoris

    PubMed Central

    Lodhi, Mohasin; Dubey, Akhilesh; Narayan, Reema; Prabhu, Prabhakara; Priya, Sneh

    2013-01-01

    Background: Ivabradine hydrochloride is an anti-anginal drug with a biological half-life of about 2 h, and repeated daily administration is needed to maintain effective plasma level. Present investigation of buccal films of Ivabradine hydrochloride is an attempt to avoid the repeated administration and release of drug in more controlled fashion, thereby, to improve the bioavailability. Materials and Methods: Buccal patches were fabricated by solvent casting technique and were evaluated for its physical properties like physical appearance, weight uniformity, thickness, swelling index, surface pH, mucoadhesive time, and folding endurance, in vitro and ex vivo release studies. Results: A combination of hydroxypropyl methyl cellulose (HPMC) K15M and K100M with carbopol 940, PEG 6000 gave promising results. Further, the drug content of all the formulations was determined and was found to be uniform. All the formulations were subjected to in vitro release study using phosphate buffer pH 6.6. Patches exhibited drug release in the range of 90.36% ± 0.854 to 98.37% ± 0.589 at the end of six hrs. The best formulations (F2 and F5) containing the composition of HPMC K15-37.50 mg, carbopol-0.42 mg, PEG6000-16.87 mg, Aspertane-0.28 mg, Tween-0.0023 mg and HPMC K100-37.50 mg, carbopol-0.42 mg, PEG6000-16.87 mg, Aspertane-0.28 mg, Tween-0.0023 mg respectively exhibited in vitro drug release of 97.61% ± 0.589 and 98.37% ± 0.114 respectively. The results of ex vivo diffusion using goat cheek pouch revealed that the drug release rate was retarded up to seven hrs. Films prepared with permeation enhancer (Tween 80) showed faster drug release. Finally, stability studies were carried out by using human saliva for the optimized formulation (F2-F5). Conclusion: The present study indicated enormous potential of mucoadhesive buccal patches containing Ivabradine for systemic delivery with an added advantage of circumventing hepatic first pass metabolism. Further work is recommended to support its efficacy claims by long term pharmacokinetic and pharmacodynamic studies in human beings. PMID:23799205

  8. Fresh meat quality and further processing characteristics of shoulders from finishing pigs fed ractopamine hydrochloride (Paylean).

    PubMed

    Tavárez, M A; Boler, D D; Carr, S N; Ritter, M J; Petry, D B; Souza, C M; Killefer, J; McKeith, F K; Dilger, A C

    2012-12-01

    Our objectives were to characterize the effects of ractopamine hydrochloride (RAC) on fresh meat and further processing characteristics of muscles (serratus ventralis and triceps brachii) from the shoulders of finishing pigs. Two hundred forty shoulders originating from 120 carcasses (60 barrows and 60 gilts) were selected from a commercial population of pigs. A 2 × 2 factorial in a completely randomized design was used, with factors of RAC inclusion in the diet (0 or 7.4 mg/kg, as-fed basis) and sex (barrow or gilt). Paired shoulders (120 rights and 120 lefts) were transported from a federally inspected slaughter facility under refrigeration to the University of Illinois Meat Science Laboratory for evaluation. Subsequently, right and left shoulders were separated and designated for 2 separate experiments. Shoulders from right side were used in Exp. 1 to determine further processing characteristics. Cellar trimmed (CT) butts from the Boston butt of the shoulders were cured and dried-cured to manufacture cottage bacon and coppa, respectively. Shoulders from left side were used in Exp. 2 to determine fresh meat characteristics. Pigs fed RAC had greater shoulder weights and increased yields of cuts from the shoulder. Feeding RAC decreased Boston butt fat content (P = 0.01) but had no effect on picnic fat content (P = 0.86). Pigs fed RAC had greater (P < 0.01) iodine values than controls (67.00 vs. 64.95, respectively). Inclusion of RAC in the diet had no effect on cottage bacon cooked yield (P = 0.33), but it decreased (P < 0.01) cottage bacon fat content without having an effect on protein content (P = 0.50). In addition, cottage bacon from RAC shoulders had greater slice total area (P = 0.01) and less seam fat (P = 0.01) than controls. Ractopamine hydrochloride had no detrimental effect on coppa processing characteristics and visual appearance. Cottage bacon and coppa from RAC pigs had sensory characteristics similar to controls. Shoulders from pigs fed RAC might be of benefit to the industry because they provide more pounds of sellable product with no detrimental effects on processing characteristics. PMID:22952374

  9. PLGA Biodegradable Nanoparticles Containing Perphenazine or Chlorpromazine Hydrochloride: Effect of Formulation and Release

    PubMed Central

    Halayqa, Mohammed; Doma?ska, Urszula

    2014-01-01

    In our study, poly(dl-lactide-co-glycolide) (PLGA) nanoparticles loaded with perphenazine (PPH) and chlorpromazine hydrochloride (CPZ-HCl) were formulated by emulsion solvent evaporation technique. The effect of various processing variables, including PLGA concentration, theoretical drug loading, poly(vinyl alcohol) (PVA) concentration and the power of sonication were assessed systematically to obtain higher encapsulation efficiency and to minimize the nanoparticles size. By the optimization formulation process, the nanoparticles were obtained in submicron size from 325.5 ± 32.4 to 374.3 ± 10.1 nm for nanoparticles loaded with PPH and CPZ-HCl, respectively. Nanoparticles observed by scanning electron microscopy (SEM) presented smooth surface and spherical shape. The encapsulation efficiency of nanoparticles loaded with PPH and CPZ-HCl were 83.9% and 71.0%, respectively. The drug loading were 51.1% and 39.4% for PPH and CPZ-HCl, respectively. Lyophilized nanoparticles with different PLGA concentration 0.8%, 1.3% and 1.6% (w/v) in formulation process were evaluated for in vitro release in phosphate buffered saline (pH = 7.4) by using dialysis bags. The release profile for both drugs have shown that the rate of PPH and CPZ-HCl release were dependent on a size and amount of drugs in the nanoparticles. PMID:25535080

  10. Effects of a new centrally acting muscle relaxant, NK433 (lanperisone hydrochloride) on spinal reflexes.

    PubMed

    Sakitama, K; Ozawa, Y; Aoto, N; Tomita, H; Ishikawa, M

    1997-10-22

    (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone++ + monohydrochloride, lanperisone hydrochloride (NK433) administered intravenously or orally depressed the mono- and polysynaptic reflex potential, dorsal root reflex potential, flexor reflex mediated by group II afferent fibers, patellar and flexor reflexes. These effects were reduced by spinal transection. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. (+)-(1R,2R)-2-methyl-3-(1-pyrrolidinyl)-1-(4-trifluoromethylphenyl)-1-pr opanol (LPS-9)-HCl, a metabolite of NK433, also inhibited the spinal reflexes. Given orally, NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spinal cord is involved in the mechanism of spinal reflex depression by NK433. LPS-9 could contribute to the potent activity of NK433 after oral administration. PMID:9430412

  11. Long-lasting muscle relaxant activity of eperisone hydrochloride after percutaneous administration in rats.

    PubMed

    Matsunaga, M; Uemura, Y; Yonemoto, Y; Kanai, K; Etoh, H; Tanaka, S; Atsuta, Y; Nishizawa, Y; Yamanishi, Y

    1997-03-01

    Potency and duration of muscle relaxant activity of eperisone hydrochloride were examined after percutaneous administration in the intercollicular decerebrated rat rigidity model and compared to those of eperisone after intravenous injection. A continuous movement was loaded on the hindlimb of the rat model to maintain stable rigidity. The tonus of the hindlimb was recorded by EMG from the triceps surae and was quantified by using the public domain NIH Image program. Eperisone ointment administered percutaneously showed significant muscle relaxant activity at 8.4 cm2 (4.2 mg of eperisone)/rat. The effect was dose-dependent and lasted over 60 min. Intravenously injected eperisone showed significant activity at 1.25 mg/kg, but the decrease of tone was lost within 30 min after injection. Plasma eperisone levels were monitored in the same model, and they were well correlated to the dosage. These results suggest that percutaneously administered eperisone is absorbed efficiently and shows potent and long-lasting muscle relaxant activity. PMID:9127816

  12. Short and symmetrical OHO hydrogen bond in bis(quinuclidine betaine) hydrochloride

    NASA Astrophysics Data System (ADS)

    Dega-Szafran, Z.; Katrusiak, A.; Szafran, M.

    2010-05-01

    The molecular structure of bis(quinuclidine betaine) hydrochloride, (QNB) 2HCl, has been characterized by single crystal X-ray diffraction, infrared spectroscopy and by DFT calculations. The crystals are centrosymmetric, monoclinic, space group C2/c. Two QNB moieties are joined by a very short and centered O⋯H⋯O hydrogen bond of 2.461(2) Å. Its existence is confirmed by the broad absorption band below 1500 cm -1 in the FTIR spectrum. In the structure of (QNB) 2HCl optimized at the B3LYP/6-31G(d,p) level of theory, the quinuclidine betaine units are non-equivalent. The protonated quinuclidine betaine interacts with the QNB inner salt by the O sbnd H⋯O hydrogen bond of 2.494 Å. In the structure of (QNB) 2H homoconjugated cation, optimized by the B3LYP/6-31G(d,p) approach, the OHO bond is shorter than in the crystal (2.415 Å). A study of the motion of the proton along the O sbnd H⋯O bridge has been carried out by the semiempirical PM3 method.

  13. High performance liquid chromatographic determination of oxeladin citrate and oxybutynin hydrochloride and their degradation products.

    PubMed

    El-Gindy, Alaa

    2005-08-01

    Two high performance liquid chromatographic (HPLC) methods are presented for the determination of oxeladin citrate (OL) and oxybutynin hydrochloride (OB) and their degradation products. The first method was based on HPLC separation of OL from its degradation product using a Nucleosil C(18) column with a mobile phase consisting of acetonitrile -0.1% phosphoric acid (60:40 v/v). The second method was based on HPLC separation of OB from its degradation product using a VP-ODS C(18) column with a mobile phase consisting of acetonitrile/0.01 M potassium dihydrogen phosphate/diethylamine (60:40:0.2). Quantitation was achieved with UV detection at 220 nm based on peak area. The two HPLC methods were applied for the determination of OL or OB, their degradation products, methylparaben and propylparaben in pharmaceutical preparations. The proposed methods were used to investigate the kinetics of acidic and alkaline degradation processes of OL and OB at different temperatures and the apparent pseudofirst-order rate constant, half-life and activation energy were calculated. The pH-rate profiles of degradation of OL and OB in Britton-Robinson buffer solutions within the pH range 2-12 were studied. PMID:16023117

  14. Development of HPTLC method for the estimation of ondansetron hydrochloride in bulk drug and sublingual tablets.

    PubMed

    Mujtaba, Ali; Kohli, Kanchan; Ali, J; Baboota, Sanjula

    2013-02-01

    A new, simple, rapid, accurate and precise high performance thin layer chromatography (HPTLC) method has been developed for the estimation of ondansetron hydrochloride in bulk and sublingual tablets. The mobile phase composition was chloroform : ethyl acetate : methanol : ammonia (9:5:4:0.1 v/v). Spectrodensitometric analysis of ondansetron was carried out at 254 nm and a symmetrical, well-resolved, well-defined peak was obtained at mean retardation factor (R(f) ) 0.52 ± 0.02. The calibration plot was linear in the range 200-1200 ng/spot and showed good linear relationship with coefficient of regression, R(2) = 0.9952 with respect to peak area. The method was validated according to the guidelines of the International Conference on Harmonization (ICH Q2(R1). The limit of detection and quantitation were 14.83 and 44.92 ng per spot, respectively. The recovery study was carried out by standard addition method and the percentage recovery was found to be 99.34 ± 1.08. Therefore it was concluded that the proposed developed HPTLC method can be applied for identification and quantitative determination of ondansetron in bulk drug and dosage forms. PMID:23413100

  15. Probing Conformational Stability and Dynamics of Erythroid and Nonerythroid Spectrin: Effects of Urea and Guanidine Hydrochloride

    PubMed Central

    Patra, Malay; Mukhopadhyay, Chaitali; Chakrabarti, Abhijit

    2015-01-01

    We have studied the conformational stability of the two homologous membrane skeletal proteins, the erythroid and non-erythroid spectrins, in their dimeric and tetrameric forms respectively during unfolding in the presence of urea and guanidine hydrochloride (GuHCl). Fluorescence and circular dichroism (CD) spectroscopy have been used to study the changes of intrinsic tryptophan fluorescence, anisotropy, far UV-CD and extrinsic fluorescence of bound 1-anilinonapthalene-8-sulfonic acid (ANS). Chemical unfolding of both proteins were reversible and could be described as a two state transition. The folded erythroid spectrin and non-erythroid spectrin were directly converted to unfolded monomer without formation of any intermediate. Fluorescence quenching, anisotropy, ANS binding and dynamic light scattering data suggest that in presence of low concentrations of the denaturants (up-to 1M) hydrogen bonding network and van der Waals interaction play a role inducing changes in quaternary as well as tertiary structures without complete dissociation of the subunits. This is the first report of two large worm like, multi-domain proteins obeying twofold rule which is commonly found in small globular proteins. The free energy of stabilization (?GuH20) for the dimeric spectrin has been 20 kcal/mol lesser than the tetrameric from. PMID:25617632

  16. Lyophilized sustained release mucoadhesive chitosan sponges for buccal buspirone hydrochloride delivery: formulation and in vitro evaluation.

    PubMed

    Kassem, Mohamed A A; ElMeshad, Aliaa N; Fares, Ahmed R

    2015-06-01

    This work aims to prepare sustained release buccal mucoadhesive lyophilized chitosan sponges of buspirone hydrochloride (BH) to improve its systemic bioavailability. Chitosan sponges were prepared using simple casting/freeze-drying technique according to 3(2) factorial design where chitosan grade was set at three levels (low, medium, and high molecular weight), and concentration of chitosan solution at three levels (0.5, 1, and 2%). Mucoadhesion force, ex vivo mucoadhesion time, percent BH released after 8 h (Q8h), and time for release of 50% BH (T50%) were chosen as dependent variables. Additional BH cup and core buccal chitosan sponge were prepared to achieve uni-directional BH release toward the buccal mucosa. Sponges were evaluated in terms of drug content, surface pH, scanning electron microscopy, swelling index, mucoadhesion strength, ex vivo mucoadhesion time, and in vitro drug release. Cup and core sponge (HCH 0.5E) were able to adhere to the buccal mucosa for 8 h. It showed Q8h of 68.89% and exhibited a uni-directional drug release profile following Higuchi diffusion model. PMID:25370025

  17. Polyhexamethylene guanidine hydrochloride shows bactericidal advantages over chlorhexidine digluconate against ESKAPE bacteria.

    PubMed

    Zhou, Zhongxin; Wei, Dafu; Lu, Yanhua

    2015-03-01

    More information regarding the bactericidal properties of polyhexamethylene guanidine hydrochloride (PHMG) against clinically important antibiotic-resistant ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species) pathogens needs to be provided for its uses in infection control. The bactericidal properties of PHMG and chlorhexidine digluconate (CHG) were compared based on their minimum inhibitory concentrations (MICs), minimum bactericidal concentrations, and time-course-killing curves against clinically important antibiotic-susceptible and antibiotic-resistant ESKAPE pathogens. Results showed that PHMG exhibited significantly higher bactericidal activities against methicillin-resistant Staphylococcus aureus, carbapenem-resistant Klebsiella pneumoniae, and ceftazidime-resistant Enterobacter spp. than CHG. A slight bactericidal advantage over CHG was obtained against vancomycin-resistant Enterococcus faecium, ciprofloxacin- and levofloxacin-resistant Acinetobacter spp., and multidrug-resistant Pseudomonas aeruginosa. In previous reports, PHMG had higher antimicrobial activity against almost all tested Gram-negative bacteria and several Gram-positive bacteria than CHG using MIC test. These studies support the further development of covalently bound PHMG in sterile-surface materials and the incorporation of PHMG in novel disinfectant formulas. PMID:24888899

  18. Feasibility of terahertz time-domain spectroscopy to detect tetracyclines hydrochloride in infant milk powder.

    PubMed

    Qin, Jianyuan; Xie, Lijuan; Ying, Yibin

    2014-12-01

    We report the use of terahertz time-domain spectroscopy (THz-TDS) to detect tetracyclines hydrochloride (TCsH) in infant milk powder for the first time. Four kinds of TCsH exhibited their unique spectral features in the region of 0.3-1.8 THz. The main spectral features of these TCsH were still detectable when mixed with infant milk powder with concentrations at 1%-50%, even in the ternary mixtures. The results from chemometrics analysis showed that qualitative and quantitative detection of TCsH in infant milk powder could be successfully achieved. The residual predictive deviation (RPD) values of all these TCsH models were all higher than 2, indicating these models were considered good and could be used in screening purposes. The RPD values of TCH, DTCH, and CTCH models were higher than 3, which were considered excellent for prediction purposes. These preliminary results indicated that THz-TDS combined with chemometrics analysis was suitable for detecting the presence of TCsH residues in a food matrix. PMID:25348376

  19. Development of Gelucire 43/01 beads of metformin hydrochloride for floating delivery.

    PubMed

    Jain, Sunil K; Gupta, Anuj

    2009-01-01

    The objective of this study was to prepare and characterize beads of Gelucire 43/01 for floating delivery of metformin hydrochloride (MH). The beads were evaluated for particle size, surface morphology, percent drug entrapment, percent yield, differential scanning calorimetry (DSC), in vitro floating ability, and in vitro drug release. Aging effect on storage was evaluated using hot stage microscopy (HSM), DSC, scanning electron microscopy, and in vitro floating ability. The formed beads were sufficiently hard and spherical in shape. Photomicrographs show that the surface was porous in nature. The average particle diameter of beads was found to be in the size range of 3.85 to 3.95 mm, and percent entrapment was 83.07% to 86.13%. The beads demonstrated favorable in vitro floating ability. The analysis of DSC thermograms revealed no physical interaction between the lipid and the drug in the prepared beads. Prepared formulations showed better controlled release behavior when compared with its conventional dosage form and comparable release profile with marketed sustained release product. HSM photomicrograph showed presence of some unmelted portion even at 43 degrees C and completely melts on 51 degrees C in aged sample. It was found that there was no significant effect on floating ability of aged beads since it remains floats up to 8 h study period. Thus, it is concluded that beads of Gelucire 43/01 could be serve as an effective carrier for highly water-soluble antihyperglycemic drugs like MH for the controlled delivery. PMID:19830579

  20. New copper(II) complexes with dopamine hydrochloride and vanillymandelic acid: Spectroscopic and thermal characterization

    NASA Astrophysics Data System (ADS)

    Mohamed, Gehad G.; Nour El-Dien, F. A.; El-Nahas, R. G.

    2011-10-01

    The dopamine derivatives participate in the regulation of wide variety of physiological functions in the human body and in medication life. Increase and/or decrease in the concentration of dopamine in human body reflect an indication for diseases such as Schizophrenia and/or Parkinson diseases. The Cu(II) chelates with coupled products of dopamine hydrochloride (DO.HCl) and vanillymandelic acid (VMA) with 4-aminoantipyrine (4-AAP) are prepared and characterized. Different physico-chemical techniques namely IR, magnetic and UV-vis spectra are used to investigate the structure of these chelates. Cu(II) forms 1:1 (Cu:DO) and 1:2 (Cu:VMA) chelates. DO behave as a uninegative tridentate ligand in binding to the Cu(II) ion while VMA behaves as a uninegative bidentate ligand. IR spectra show that the DO is coordinated to the Cu(II) ion in a tridentate manner with ONO donor sites of the phenolic- OH, -NH and carbonyl- O, while VMA is coordinated with OO donor sites of the phenolic- OH and -NH. Magnetic moment measurements reveal the presence of Cu(II) chelates in octahedral and square planar geometries with DO and VMA, respectively. The thermal decomposition of Cu(II) complexes is studied using thermogravimetric (TG) and differential thermal analysis (DTA) techniques. The activation thermodynamic parameters, such as, energy of activation, enthalpy, entropy and free energy change of the complexes are evaluated and the relative thermal stability of the complexes are discussed.

  1. Effects of penehyclidine hydrochloride on the propofol dose requirement and Bispectral Index for loss of consciousness

    PubMed Central

    Liang, Peng; Zhang, Yanju; Yu, Hai; Liu, Bin

    2014-01-01

    Penehyclidine hydrochloride (PH), a new anticholinerigic drug associated with few cardiovascular side effects, was used widely as premedication in China. There is no information on the pharmacodynamic interaction between PH and anesthetics for loss of consciousness (LOC). This study was designed to determine the effects of premedicated PH on the propofol dose requirement for LOC and Bispectral Index (BIS) during target-controlled infusion (TCI) of propofol. Forty patients were randomly allocated to 1 of 2 groups to receive PH (Group PH) or normal saline (Group NS). TCI propofol was administered 30 min after PH or normal saline was given. During study period, BIS value, mean arterial pressure (MAP), heart rate (HR) and the Observer’s Assessment of Alertness/Sedation (OAA/S) rating scale were recorded. Predicted effect-site propofol concentrations (Ce) and the total propofol dose were recorded when end-point was achieved. The time to reach end point was also noted. The time to reach LOC was shorter in Group PH than Group NS (p < 0.05). The predicted propofol Ce and consumption based on body weight of each patient were lower in Group PH than Group NS (p < 0.05). BIS values were not significantly changed before propofol infusion, and decreased gradually as propofol Ce increased and were not significantly different when LOC was reached between two groups (p > 0.05). We conclude that premedicated PH reduces the propofol Ce and dose requirement for LOC, but has no effect on BIS. PMID:25232414

  2. Antimicrobial electrospun membranes of chitosan/poly(ethylene oxide) incorporating poly(hexamethylene biguanide) hydrochloride.

    PubMed

    Dilamian, M; Montazer, M; Masoumi, J

    2013-04-15

    Here, antimicrobial nanofibrous membranes were produced by electrospinning of chitosan/poly(ethylene oxide) (PEO) solution in the presence of poly(hexamethylene biguanide) hydrochloride (PHMB). The influence of PHMB on the electrospinnability and antimicrobial properties of chitosan/PEO nanofibers were studied. Further, viscosity of the solutions as well as morphology of the nanofibrous structures were investigated. Results revealed that incorporation of PHMB in chitosan/PEO solutions led to decrease in the zero-shear rate viscosity up to 20%. Moreover, increasing PHMB from 0.5 mM to 1 mM led to formation of thinner fibers with diameters ranging from 240 nm to 60 nm, respectively. Fourier transform infrared (FT-IR) spectrums indicated the functional groups of chitosan, PEO and PHMB in nanofibrous structure. Differential scanning calorimetry (DSC) thermograms indicated interaction of PHMB with PEO and chitosan through alteration in the thermal behavior of the nanofibers. Inhibition of the bacteria growth for both Escherichia coli and Staphylococcus aureus were achieved on the PHMB loaded nanofibers. Also, a burst release of PHMB from mats has been observed in the first hour. These findings suggest that there is a great potential in fabrication of biomaterials with incorporation of PHMB using electrospinning. PMID:23544550

  3. Formulation, characterization and clinical evaluation of propranolol hydrochloride gel for transdermal treatment of superficial infantile hemangioma.

    PubMed

    Zhou, Wenhu; He, Shiying; Yang, Yijun; Jian, Dan; Chen, Xiang; Ding, Jinsong

    2015-07-01

    The objective of the present study is to formulate and characterize propranolol hydrochloride (PPL?·?HCl) gel, and to evaluate the efficacy of this formulation in transdermal treatment for superficial infantile hemangioma (IH). The transdermal PPL?·?HCl gel was prepared by a direct swelling method, which chose hydroxypropyl methylcellulose (HPMC) as the matrix and used terpenes plus alcohols as permeation enhancer. Permeation studies of PPL?·?HCl were carried out with modified Franz diffusion cells through piglet skin. Our results pointed to that among all studied permeation enhancers, farnesol plus isopropanol was the most effective combination (Q24, 6027.4?±?563.1??g/cm(2), ER, 6.8), which was significantly higher than that of control gel (p?

  4. Fluorescent reversible regulation based on the interactions of topotecan hydrochloride, neutral red and quantum dots

    NASA Astrophysics Data System (ADS)

    Wang, Linlin; Shen, Yizhong; Liu, Shaopu; Yang, Jidong; Liang, Wanjun; Li, Dan; He, Youqiu

    2015-02-01

    The interactions of topotecan hydrochloride (THC), neutral red (NR) and thioglycolic acid (TGA) capped CdTe/CdS quantum dots (QDs) built a solid base for the controlling of the fluorescent reversible regulation of the system. This study was developed by means of ultraviolet-visible (UV-vis) absorption, fluorescence (FL), resonance Rayleigh scattering (RRS) spectroscopy and transmission electron microscopy (TEM). Corresponding experimental results revealed that the fluorescence of TGA-CdTe/CdS QDs could be effectively quenched by NR, while the RRS of the QDs enhanced gradually with the each increment of NR concentration. After the addition of THC, the strong covalent conjugation between NR and THC which was in carboxylate state enabled NR to be dissociated from the surface of TGA-CdTe/CdS QDs to form more stable complex with THC, thereby enhancing the fluorescence of the TGA-CdTe/CdS QDs-NR system. What is more, through analyzing the optical properties and experimental data of the reaction between TGA-CdTe/CdS QDs and NR, the possible reaction mechanism of the whole system was discussed. This combination of multiple spectroscopic techniques could contribute to the investigation for the fluorescent reversible regulation of QDs and a method could also be established to research the interactions between camptothecin drugs and dyes.

  5. Impact of tert-butyl alcohol on crystallization kinetics of gemcitabine hydrochloride in frozen aqueous solutions.

    PubMed

    Munjal, Bhushan; Bansal, Arvind K

    2015-01-01

    The effect of tert-butyl alcohol (TBA) on isothermal crystallization kinetics of gemcitabine hydrochloride (GHCl) in frozen aqueous solutions was assessed by cold-stage microscopy. Addition of TBA (0%-5%, w/w) increased the value of Johnson-Mehl-Avrami rate constant (1.3-33.3 h(-1) ) and reduced the Avrami exponent (2.5-1.0). Thermodynamic parameters [enthalpy (?H(‡) ), entropy (?S(‡) ), and free energy (?G(‡) ) of activation], calculated using Arrhenius and Eyring-Polanyi equations, established that TBA (2%, w/w) accelerated GHCl crystallization by reducing its ?H(‡) (53.9 cf. 96.5 kJ/mol(-1) ) and ?G(‡) (68.5 cf. 74.9 kJ/mol(-1) ). Further, to explore insights into the effect of TBA on nucleation and crystal growth of GHCl, crystallization kinetics data were deconvolved using Finke-Watzky model. This revealed that addition of TBA decreased ?H(‡) of nucleation and increased ?S(‡) of crystal growth, thereby reducing ?G(‡) of nucleation and crystal growth by 11.7% and 4.2%, respectively. Finkey-Watzky model also predicted a reduction in the crystal size upon TBA addition, which was confirmed by comparing particle size of GHCl lyophilized in the presence and absence of TBA. In conclusion, TBA reduces ?G(‡) of nucleation and crystal growth in a differential manner, thereby enhancing the crystallization kinetics of GHCl and affecting its morphological features. PMID:25393155

  6. Crystal growth, spectral, optical and thermal properties of semiorganic nonlinear optical material: picolinic acid hydrochloride.

    PubMed

    Gowri, S; Uma Devi, T; Sajan, D; Surendra Dilip, C; Chandramohan, A; Lawrence, N

    2013-06-01

    The bulk single crystal of 2-picolinic acid hydrochloride (PHCL) (a semi-organic nonlinear optical material of dimensions 25×15×10 mm(3)) was successfully grown by slow solvent evaporation technique. The XRD results revealed the cell parameters and the centrosymmetric nature of the crystal structure. FT-IR spectral study identified the functional groups, nature of bonding and their bond strength. The UV-Vis-NIR studies recognized the optical transmittance window and the lower cut off wavelength of the PHCL crystal and thus it could be performed as a NLO material. (1)H NMR and (13)CNMR spectra were correlated with the XRD standard for the molecular structure reveals harmony of the materials. Thermal properties of the crystal were studied by thermo gravimetric analysis (TGA) and differential thermal analysis (DTA); the derived kinetic parameter values support the intuitive association of picolinicacid and HCl leads to the spontaneous formation of PHCL with a first order reaction. The presence of a proton and a proton acceptor groups provide the necessary stability to induce charge asymmetry in the PHCL structure. The load dependent hardness values of the crystal were measured by microhardness testing. PMID:23557771

  7. Preparation and evaluation of lidocaine hydrochloride-loaded TAT-conjugated polymeric liposomes for transdermal delivery.

    PubMed

    Wang, Yue; Su, Wenya; Li, Qin; Li, Changyi; Wang, Hanjie; Li, Yuchen; Cao, Yan; Chang, Jin; Zhang, Lianyun

    2013-01-30

    Transactivation transcriptional activator (TAT) peptides were conjugated on the octadecyl-quaternized, lysine-modified chitosan to form polymeric liposomes (TAT-PLs) with cholesterol for improving transdermal delivery of local anesthetic lidocaine hydrochloride (LID). In this study, the LID loaded TAT-conjugated polymeric liposomes (LID-TAT-PLs) have been successfully prepared. LID-TAT-PLs were characterized by determination of their particle size, polydispersity, morphology, drug encapsulation efficiency, drug release behavior in vitro, and storage-stability. The skin permeation of LID-TAT-PLs was examined using a Franz diffusion cell mounted with depilated mouse skin in vitro, and penetration of TAT-PLs was visualized by confocal laser scanning microscopy (CLSM). The results showed that LID-TAT-PLs were spherical in solution, with substantially smaller mean diameter (154.7±10.7 nm), higher encapsulation efficiency (80.05±2.64%) and better stability in contrast to conventional liposomes (CLs). From the in vitro skin permeation results, transdermal flux of LID-TAT-PLs was approximately 4.17 and 1.75 times higher than that of LID solution and LID CLs (P<0.05). CLSM studies also confirmed that TAT-PLs reached viable layers of the skin. Hence, the results indicate that LID-TAT-PLs are effective and potential alternative for the LID transdermal formulation. PMID:23089577

  8. Determination of polyhexamethylene biguanide hydrochloride using photometric colloidal titration with crystal violet as a color indicator.

    PubMed

    Masadome, Takashi; Miyanishi, Takaaki; Watanabe, Keita; Ueda, Hiroshi; Hattori, Toshiaki

    2011-01-01

    A solution of polyhexamethylene biguanide hydrochloride (PHMB-HCl) was titrated with a standard solution of potassium poly(vinyl sulfate) (PVSK) using crystal violet (CV) as an photometric indicator cation. The end point was detected by a sharp absorbance change due to an abrupt decrease in the concentration of CV. A linear relationship between the concentration of PHMB-HCl and the end-point volume of the titrant existed in the concentration range from 2 to 10 × 10(-6) eq mol L(-1). Back-titration was based on adding an excess amount of PVSK to a sample solution containing CV, which was titrated with a standard solution of poly(diallyldimethylammonium chloride) (PDADMAC). The calibration curve of the PHMB-HCl concentration to the end point volume of the titrant was also linear in the concentration range from 2 to 8 × 10(-6) eq mol L(-1). Both photometric titrations were applied to the determination of PHMB-HCl in a few contact-lens detergents. Back-titration showed a clear end point, but direct titration showed an unclear end point. The results of the back-titration of PHMB-HCl were compared with the content registered in its labels. PMID:21828919

  9. The role of dapoxetine hydrochloride on-demand for the treatment of men with premature ejaculation.

    PubMed

    De Hong, Cao; Ren, Liu Liang; Yu, Huang; Qiang, Wei

    2014-01-01

    Premature ejaculation (PE) is the most common male sexual dysfunction. Dapoxetine hydrochloride, belonging to a class of drugs known as selective serotonin reuptake inhibitors or, was the first drug originally approved for the on-demand treatment of men with PE. We aimed to compare the intravaginal ejaculatory latency time (IELT), patient-reported global impression of change (PGIC), and adverse effect (AE) incidence associated with the use of dapoxetine (30 mg and 60 mg) versus placebo, and evaluate the differences in administering 60 mg versus 30 mg as on-demand medical oral therapy for the treatment of PE via a literature review and meta-analysis. Relevant randomized controlled trials (RCTs) were identified from PubMed, EMBASE, and Cochrane Central Register of Controlled Trials (Cochrane Library) databases. Ultimately, a total of seven RCTs with 8039 patients were included. Our meta-analysis demonstrated that dapoxetine (in the 30 mg and 60 mg subgroup) resulted in significantly higher IELT, PGIC, and AE incidence relative to the placebo, with higher proportions observed for 60 mg versus 30 mg of dapoxetine administration. The most common AEs were mild and tolerable. We conclude that dapoxetine (particularly the 60 mg dosage) may be considered a safe and effective drug for patients with PE. PMID:25434754

  10. [Adsorption and release behavior of epirubicin hydrochloride on carboxylated single-walled carbon nanotubes].

    PubMed

    Lin, Rui; Li, Li-li; He, Jia; Qiu, Lan-lan; He, Hua

    2013-11-01

    In this study, the adsorption behavior of epirubicin hydrochloride (EPI) on carboxylated single-walled carbon nanotubes (c-SWNTs) obtained by mixture acid treatment was investigated. The results indicated that the dispersion of c-SWNTs in water was obviously improved. The absorption of EPI on c-SWNTs came to equilibrium after 240 min and could be explained by pseudo-second-order model. Moreover, there were heterogeneous distribution of active sites onto c-SWNTs surface and the Freundlich isotherm model was better fit to describe the absorption precess of EPI on c-SWNTs. The absorption capacity of EPI on c-SWNTs increased obviously with the increasing pH and decreasing temperature. Compared with multi-walled carbon nanotubes, carboxylated multi-walled carbon nanotubes, SWNTs, c-SWNTs possessed higher absorption capacity for EPI. The controlled, targeted and sustained release of EPI from c-SWNTs-EPI could be instructive for the development of nano-carrier. PMID:24475710

  11. Guanidine hydrochloride and urea effects upon thermal stability of Glossoscolex paulistus hemoglobin (HbGp).

    PubMed

    Carvalho, Francisco A O; Alves, Fernanda R; Carvalho, José W P; Tabak, Marcel

    2015-03-01

    Glossoscolex paulistus hemoglobin (HbGp) has a molecular mass of 3600kDa. It belongs to the hexagonal bilayer hemoglobin class, which consists of highly cooperative respiratory macromolecules found in mollusks and annelids. The present work focusses on oxy-HbGp thermal stability, in the presence of urea and guanidine hydrochloride (GuHCl), monitored by several techniques. Initially, dynamic light scattering data show that the presence of GuHCl induces the protein oligomeric dissociation, followed by a significant 11-fold increase in the hydrodynamic diameter (DH) values, due to the formation of protein aggregates in solution. In contrast, urea promotes the HbGp oligomeric dissociation, followed by unfolding process at high temperatures, without aggregation. Circular dichroism data show that unfolding critical temperature (Tc) of oxy-HbGp decreases from 57°C, at 0.0 mol/L of the denaturant, to 45°C, in the presence of 3.5 mol/L of urea, suggesting the reduction of HbGp oligomeric stability. Moreover, differential scanning calorimetry results show that at lower GuHCl concentrations, some thermal stabilization of the hemoglobin is observed, whereas at higher concentrations, the reduction of stability takes place. Besides, HbGp is more stable in the presence of urea when compared with the guanidine effect, as deduced from the differences in the concentration range of denaturants. PMID:25433131

  12. Propranolol hydrochloride-loaded liposomal gel for transdermal delivery: Characterization and in vivo evaluation.

    PubMed

    Guan, Yuanyuan; Zuo, Tiantian; Chang, Minglu; Zhang, Fang; Wei, Ting; Shao, Wei; Lin, Guimei

    2015-06-20

    This study was to develop propranolol hydrochloride (PRO)-loaded liposomal gel as a topical drug delivery system. Scanning electron microscope (SEM) revealed that the liposomes were spherical and scattered in the surface of the gel. Pseudoplastic flows of PRO liposomal gel were showed after stored at three different temperatures. Besides, PRO liposomal gel showed non-irritating to the skin of rabbit. Skin deposition studies in vivo demonstrated that PRO liposomal gel can apparently increase drug content in skin compared with PRO gel. Histopathology examination showed that PRO liposomal gel could obviously weaken the barrier function of stratum corneum (SC) by comparison with PRO gel. What is more, the plasma pharmacokinetic showed the maximum concentration in plasma was 0.41?g/mL and 1.17?g/mL after topical and oral administration respectively. However, tissue distribution study showed PRO liposomal gel obviously changed drug distribution in tissues, significantly increased drug concentration in skin with about 74 folds compared with PRO gel. In conclusion, liposomes-based gel could be a promising vehicle as a transdermal delivery system of PRO. PMID:25882014

  13. Development and characterisation of thermo reversible mucoadhesive moxifloxacin hydrochloride in situ ophthalmic gel

    PubMed Central

    Dholakia, M.; Thakkar, V.; Patel, N.; Gandhi, T.

    2012-01-01

    A sustain release thermo reversible in situ gel of Moxifloxacin Hydrochloride using mucoadhesive polymer was prepared. Mucoadhesive polymer was used to obtain an ophthalmic delivery system with improved mechanical and mucoadhesive properties that will provide prolong retention time for treatment of ocular diseases. Developed formulations were evaluated for drug-excipient compatibility study, pH, Clarity, Gelation temperature study, Mucoadhesion properties and in-vitro release studies. Drug-excipient compatibility study was performed by FTIR technique. The individual IR spectra of the pure drug and polymers as well as the combination spectra of the drug and polymer were taken, which indicate no interaction between Moxifloxacin and polymers when compared with infrared spectrum of pure drug as all functional group frequencies were present. The values of other parameters obtained were in acceptable range. In vitro release tests revealed that 98% drug was released from the in situ gel containing 0.5% and 1.00% HPMC in 12 hr. provides prolonged release. PMID:23066202

  14. Formulation and evaluation of an in situ gel-forming ophthalmic formulation of moxifloxacin hydrochloride

    PubMed Central

    Mandal, Sonjoy; Thimmasetty, Manjunath KMJ; Prabhushankar, GL; Geetha, MS

    2012-01-01

    Background/Aim: The aim of the present investigation is to prepare and evaluate in situ gel-forming ophthalmic drug delivery system of moxifloxacin hydrochloride. Materials and Methods: Sodium alginate, a novel ophthalmic gel-forming mucoadhesive polymer, which gets converted to gel in the presence of divalent-cations (calcium ion) present in the lachrymal fluid, was used as the gelling agent. Hydroxy propyl methyl cellulose (HPMC) is a mucoadhesive polymer used as viscosity enhancer. Suitable concentrations of buffering agents were used to adjust the pH to 6.5. All the formulations were sterilized in an autoclave at 121°C for 15 minutes. The formulations were evaluated for clarity, pH measurement, gelling capacity, drug content estimation, rheological study, in vitro diffusion study, antibacterial activity, isotonicity, and eye irritation study. Results: The developed formulations exhibited sustained release of drug from formulation over a period of 10 hours thus increasing residence time of the drug. The optimized formulations were tested for eye irritation on albino rabbit (male). The formulations were found to be non-irritating with no ocular damage or abnormal clinical signs to the cornea, iris or conjunctiva observed. Conclusion: These in situ gelling systems containing gums may be a valuable alternative to the conventional systems. PMID:23119236

  15. Effects of colestipol hydrochloride and neomycin sulfate on cholesterol turnover in the rat.

    PubMed

    Phillips, W A; Elfring, G L

    1977-01-01

    Three groups of male rats were fed diets containing the bile acid sequestrant colestipol hydrochloride (1%), neomycin sulfate (0.25%), or basic diet during the test. After 15 days, each rat was injected IV with 3.9 muCi cholesterol-1,2(-3)H complexed with serum lipoproteins; specific radioactivity of the total serum cholesterol was measured at several time intervals for a period of 7 weeks. Computer analysis of the data indicated that the turnover of cholesterol could best be fitted by a three-pool model. In pool 1, colestipol HC1 caused a significant increase in production rate (10.09 to 15.96 mg/day) and the excretion rate constant (0.53 to 0.79 day-1) of cholesterol without significantly altering the size of the pool or serum cholesterol concentrations. These results are compatible with an agent capable of binding bile acids in the rat but do not cause a decrease of the sterol pool because of an adequate compensatory increase in cholesterol biosynthesis. Neomycin SO4 caused a significant reduction in serum cholesterol (9%) without altering turnover parameters and apparently exerts its hypocholesterolemia by some mechanism other than bile acid sequestration. PMID:834115

  16. Synthesis and bioactivities of silver nanoparticles capped with 5-Amino-?-resorcylic acid hydrochloride dihydrate

    PubMed Central

    2014-01-01

    Background Conjugated and drug loaded silver nanoparticles are getting an increased attention for various biomedical applications. Nanoconjugates showed significant enhancement in biological activity in comparison to free drug molecules. In this perspective, we report the synthesis of bioactive silver capped with 5-Amino-?-resorcylic acid hydrochloride dihydrate (AR). The in vitro antimicrobial (antibacterial, antifungal), enzyme inhibition (xanthine oxidase, urease, carbonic anhydrase, ?-chymotrypsin, cholinesterase) and antioxidant activities of the developed nanostructures was investigated before and after conjugation to silver metal. Results The conjugation of AR to silver was confirmed through FTIR, UV¿vis and TEM techniques. The amount of AR conjugated with silver was characterized through UV¿vis spectroscopy and found to be 9% by weight. The stability of synthesized nanoconjugates against temperature, high salt concentration and pH was found to be good. Nanoconjugates, showed significant synergic enzyme inhibition effect against xanthine and urease enzymes in comparison to standard drugs, pure ligand and silver. Conclusions Our synthesized nanoconjugate was found be to efficient selective xanthine and urease inhibitors in comparison to Ag and AR. On a per weight basis, our nanoconjugates required less amount of AR (about 11 times) for inhibition of these enzymes. PMID:25201390

  17. Optimization of tetracycline hydrochloride adsorption on amino modified SBA-15 using response surface methodology.

    PubMed

    Hashemikia, Samaneh; Hemmatinejad, Nahid; Ahmadi, Ebrahim; Montazer, Majid

    2015-04-01

    Several researchers are focused on preparation of mesoporous silica as drug carriers with high loading efficiency to control or sustain the drug release. Carriers with highly loaded drug are utilized to minimize the time of drug intake. In this study, amino modified SBA-15 was synthesized through grafting with amino propyl triethoxy silane and then loaded with tetracycline hydrochloride. The drug loading was optimized by using the response surface method considering various factors including drug to silica ratio, operation time, and temperature. The drug to silica ratio indicated as the most influential factor on the drug loading yield. Further, a quadratic polynomial equation was developed to predict the loading percentage. The experimental results indicated reasonable agreement with the predicted values. The modified and drug loaded mesoporous particles were characterized by FT-IR, SEM, TEM, X-ray diffraction (XRD), elemental analysis and N2 adsorption-desorption. The release profiles of tetracycline-loaded particles were studied in different pH. Also, Higuchi equation was used to analyze the release profile of the drug and to evaluate the kinetic of drug release. The drug release rate followed the conventional Higuchi model that could be controlled by amino-functionalized SBA-15. Further, the drug delivery system based on amino modified SBA-15 exhibits novel features with an appropriate usage as an anti-bacterial drug delivery system with effective management of drug adsorption and release. PMID:25540827

  18. Chemical stability of tramadol hydrochloride injection admixed with selected pain drugs

    PubMed Central

    Di Stefano, V; Pitonzo, R; Bavetta, S; Polidori, P; Sidoti, MG

    2011-01-01

    Background: Tramadol hydrochloride (HCl) and ketorolac tromethamine are analgesic drugs, which are commonly used in combination in postoperative pain management. According to some studies, metoclopramide and magnesium sulfate (MgSO4) as adjuvant agents can improve analgesia and decrease the need for other pain drugs. Materials and Methods: The chemical stability of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl has been studied using a stability-indicating high-performance liquid chromatographic assay method. Calibration curves were produced using linear regression of the peak area against concentration of each drug, with an r2 value ? 0.96. Our aim was to investigate the stability of admixture solution of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl for 48 h (25°C) and 5 days (5°C), with MgSO4, which has never been assessed. Results: Data obtained for admixtures prepared and stored at temperatures of 25°C and 5°C, show that all drugs have reached at least 98% of the initial concentration. Conclusions: For the purpose of pre-preparing drug admixtures to use with confidence, tramadol HCl infusions may be prepared in advance and then thawed before use in clinical units. On the basis of our results, the intravenous mixture of tramadol (7.69 mg/mL), metoclopramide (0.19 mg/mL), ketorolac (1.15 mg/mL), and magnesium sulfate (77 mg/mL) may be considered for a possible commercial formulation. PMID:23071920

  19. Optimization of thermosensitive chitosan hydrogels for the sustained delivery of venlafaxine hydrochloride.

    PubMed

    Peng, Ying; Li, Jie; Li, Jing; Fei, Yin; Dong, Jiangnan; Pan, Weisan

    2013-01-30

    Chitosan/glycerophosphate disodium (GP) thermosensitive hydrogels were prepared for the sustained delivery of venlafaxine hydrochloride (VH) and optimization of this formulation was mainly studied. Release mechanism was investigated by applying various mathematical models to the in vitro release profiles. Overall, drug release from the hydrogels showed best fit in first-order model and drug release mechanism was diffusion-controlled release. Optimization of VH chitosan/GP thermosensitive hydrogels was conducted by using a three-level three-factorial Box-Behnken experimental design to evaluate the effects of considered variables, the strength of the formulation, chitosan concentration and GP amount, on the selected responses: cumulative percentage drug release in 1h, 24h and the rate constant. It presented that higher strength and GP concentration resulted in higher initial release and rate constant, which supported the hypothesis that the kinetic gelation mechanism of this system was nucleation and growth. Drug release profiles illustrated that controlled drug delivery could be obtained over 24h, which confirmed the validity of optimization. In vivo pharmacokinetic study was investigated and it demonstrated that compared with VH solution, chitosan/GP thermosensitive hydrogels had a better sustained delivery of VH. PMID:23159345

  20. Novel glucosamine hydrochloride-rectorite nanocomposites with antioxidant and anti-ultraviolet activity

    NASA Astrophysics Data System (ADS)

    Wang, Xiaoying; Liu, Bo; Li, Xiang; Sun, Runcang

    2012-12-01

    In this study, an attempt was made to prepare novel D-glucosamine hydrochloride-rectorite (DGH-REC) nanocomposites with improved antioxidant and anti-ultraviolet activity via the solution-intercalation method. The structure and morphology of DGH-REC nanocomposites were characterized by XRD, TEM, 13C CP/MAS NMR, FT-IR, XPS and SEM. The results showed that the interlayer distance of REC was enlarged after intercalation of DGH; the largest value reached 11.76 nm, and in this case exfoliation of the REC layer was observed. Moreover, most strong crystals of DGH were greatly disrupted while two other weak crystals of DGH were stronger after intercalation of DGH into REC. More importantly, it was found that DGH-REC nanocomposites showed pronounced antioxidant activity, in contrast with DGH, and the nanocomposites had anti-ultraviolet capacity, which was not observed in DGH. Furthermore, the nanocomposites did not show apparent cytotoxicity. Therefore, DGH-REC nanocomposites have great potential in health or functional food application as compared to DGH.