Glass formation in barbiturates and solid dispersion systems of barbiturates with citric acid.

Abstract:

:Glasses were prepared from a number of barbiturates. The viscosities and glass transition temperatures of the glasses were dependent on the structure of the groups present on the C-5 and N-1 atoms. Solid dispersions were prepared from three selected barbiturates formulated with citric acid. The glass transition temperatures of these systems indicated that a 1:1 molar ratio complex was formed between the two components and that intermolecular bonding was stronger in the complex than in the individual components.

journal_name

J Pharm Sci

authors

Summers MP

doi

10.1002/jps.2600671126

subject

Has Abstract

pub_date

1978-11-01 00:00:00

pages

1606-10

issue

11

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)42331-7

journal_volume

67

pub_type

杂志文章
  • Drug Distribution to Human Tissues: Prediction and Examination of the Basic Assumption in In Vivo Pharmacokinetics-Pharmacodynamics (PK/PD) Research.

    abstract::The tissue:plasma partition coefficients (Kp ) are good indicators of the extent of tissue distribution. Therefore, advanced tissue composition-based models were used to predict the Kp values of drugs under in vivo conditions on the basis of in vitro and physiological input data. These models, however, focus on animal...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24427

    authors: Poulin P

    更新日期:2015-06-01 00:00:00

  • Antitumor agents. XXXIV: Mechanism of action of bruceoside A and brusatol on nucleic acid metabolism of P-388 lymphocytic leukemia cells.

    abstract::The quassinoids bruceantin, brucein D, brucein E, bruceoside A, and brusatol significantly inhibited P-388 lymphocytic leukemic cell RNA and protein synthesis in tissue culture. However, DNA synthesis inhibition seemed to correlate more directly with the anti-neoplastic activity of these compounds in the in vivo P-338...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600680726

    authors: Hall IH,Lee KH,Eigebaly SA,Imakura Y,Sumida Y,Wu RY

    更新日期:1979-07-01 00:00:00

  • A new natural angelica polysaccharide based colon-specific drug delivery system.

    abstract::Colon-specific drug delivery systems are clinically necessary to treat colon diseases locally while minimizing systemic side effects. In this study, we extracted angelica polysaccharide from fresh roots of Angelica sinensis Diels and analyzed the monosaccharide components. With succinate as a cross-linker and angelica...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21790

    authors: Zhou S,Zhang B,Liu X,Teng Z,Huan M,Yang T,Yang Z,Jia M,Mei Q

    更新日期:2009-12-01 00:00:00

  • Synthesis and characterization of pH tolerant and mucoadhesive (thiol-polyethylene glycol) chitosan graft polymer for drug delivery.

    abstract::The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23832

    authors: Hauptstein S,Bonengel S,Griessinger J,Bernkop-Schnürch A

    更新日期:2014-02-01 00:00:00

  • Determination of bacmecillinam, an amdinocillin prodrug, in human and canine whole blood by reversed-phase liquid chromatography.

    abstract::Bacmecillinam is an amdinocillin prodrug designed to be easily hydrolyzed in biological materials, so special procedures were developed for the collection of blood specimens. Whole blood was collected in tubes containing bacampicillin as an adsorption inhibitor and kept at -70 degrees; the extracting solvent, hexane-m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600711018

    authors: Westerlund D,Pettersson B,Carlqvist J

    更新日期:1982-10-01 00:00:00

  • Effect of polyethylene glycol 4000 on dissolution properties of sulfathiazole polymorphs.

    abstract::The dissolution rates of the two polymorphic forms of sulfathiazole containing polyethylene glycol 4000 were significantly different in water. The effect of agitation on the dissolution rates also was studied. At higher stirring speeds, the dissolution rates of the stable form were affected more than the metastable fo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600650233

    authors: Niazi S

    更新日期:1976-02-01 00:00:00

  • Comprehensive high-performance liquid chromatographic methodology for the determination of thiothixene in bulk drug, finished product, and dissolution testing samples.

    abstract::An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600760310

    authors: Severin G

    更新日期:1987-03-01 00:00:00

  • In vitro percutaneous absorption and in vivo protoporphyrin IX accumulation in skin and tumors after topical 5-aminolevulinic acid application with enhancement using an erbium:YAG laser.

    abstract::5-aminolevulinic acid (ALA) is used as a precursor of protoporphyrin IX (PpIX) for photodynamic therapy (PDT) of superficial skin cancers and subcutaneous metastases of internal malignancies. The permeability of ALA across intact skin is always low, making it difficult to achieve the desired therapeutic benefits. Henc...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20577

    authors: Shen SC,Lee WR,Fang YP,Hu CH,Fang JY

    更新日期:2006-04-01 00:00:00

  • Spectrophotometric method for quantitation of peroxides in sorbitan monooleate and monostearate.

    abstract::A rapid and sensitive spectrophotometric method has been developed to quantitate the peroxides present in sorbitan monooleate and monostearate. The method relies on the peroxide conversion of iodide to iodine. The method has also been found to work for polysorbate 60. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600731150

    authors: Magill A,Becker AR

    更新日期:1984-11-01 00:00:00

  • Effect of benzalkonium chloride/EDTA on the ocular bioavailability of ketorolac tromethamine following ocular instillation to normal and de-epithelialized corneas of rabbits.

    abstract::This study was designed to examine the effect of benzalkonium chloride/ethylenediaminetetraacetic acid (BAK/EDTA) on the ocular bioavailability (Focular) of ketorolac tromethamine after ocular instillation to normal and de-epithelialized corneas of rabbits both in vitro and in vivo. The in vitro Focular of the formula...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js9504189

    authors: Madhu C,Rix PJ,Shackleton MJ,Nguyen TG,Tang-Liu DD

    更新日期:1996-04-01 00:00:00

  • Graphical approach for determining whether absorption and elimination rate constants are equal in the one-compartment open model with first-order processes.

    abstract::An equation was developed which enables blood level data to be utilized for determining whether or not the first-order absorption and elimination rate constants are equal in the one-compartment open model. This equation was tested using simulated data with excellent results. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740521

    authors: Macheras PE

    更新日期:1985-05-01 00:00:00

  • Polyarginine Nanocapsules as a Potential Oral Peptide Delivery Carrier.

    abstract::We have previously reported the development of novel nanocapsules made of polyarginine (PArg) specifically designed for the delivery of small anticancer drugs into cells. Our goal, in this work, has been to investigate the potential of these nanocarriers for oral delivery of peptide anticancer drugs. To reach this obj...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.09.029

    authors: Lollo G,Gonzalez-Paredes A,Garcia-Fuentes M,Calvo P,Torres D,Alonso MJ

    更新日期:2017-02-01 00:00:00

  • The fate of free radicals in a cellulose based hydrogel: detection by electron paramagnetic resonance spectroscopy.

    abstract::Cellulose derivatives are commonly used as gelling agents in topical and ophthalmic drug formulations. During the course of manufacturing, cellulose derivatives are believed to generate free radicals. These free radicals may degrade the gelling agent, leading to lower viscosity. Free radicals also may react with the a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21632

    authors: Basumallick L,Ji JA,Naber N,Wang YJ

    更新日期:2009-07-01 00:00:00

  • Sensitive high-pressure liquid chromatographic determination of disopyramide and mono-N-dealkyldisopyramide.

    abstract::A high-pressure liquid chromatographic procedure for the accurate determination of disopyramide and its chief metabolite in plasma is presented. The method is suitable for monitoring patients receiving disopyramide therapy. A reversed-phase cyanopropylsilane column is utilized with a mobile phase of 50% acetonitrile a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600681033

    authors: Nygard G,Shelver WH,Khalil SK

    更新日期:1979-10-01 00:00:00

  • Degradation kinetics of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770) and structure-stability relationship among its analogues in aqueous solution.

    abstract::The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780115

    authors: Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

    更新日期:1989-01-01 00:00:00

  • Improved delivery through biological membranes XD: Percutaneous absorption and metabolism of methylsulfinylmethyl 2-acetoxybenzoate and related aspirin prodrugs.

    abstract::Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700710

    authors: Loftsson T,Bodor N

    更新日期:1981-07-01 00:00:00

  • Characterization of Factors Affecting Nanoparticle Tracking Analysis Results With Synthetic and Protein Nanoparticles.

    abstract::In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.02.005

    authors: Krueger AB,Carnell P,Carpenter JF

    更新日期:2016-04-01 00:00:00

  • A novel calmodulin antagonist O-(4-ethoxyl-butyl)-berbamine overcomes multidrug resistance in drug-resistant MCF-7/ADR breast carcinoma cells.

    abstract::Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22082

    authors: Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

    更新日期:2010-07-01 00:00:00

  • Enhanced transdermal delivery of sex hormones in swine with a novel topical aerosol.

    abstract::This study investigated the enhanced transdermal delivery of testosterone (Tes) and estradiol (E2) in swine in vivo with novel metered-dose topical aerosols containing the penetration enhancer padimate O (PadO) and predicted the dose deliverable in humans from the calculated drug flux across the skin. Weanling swine w...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js980026c

    authors: Morgan TM,Parr RA,Reed BL,Finnin BC

    更新日期:1998-10-01 00:00:00

  • Utilising Magnetically Isolated Lysosomes for Direct Quantification of Intralysosomal Drug Concentrations by LC-MS/MS Analysis: An Investigatory Study With Imipramine.

    abstract::Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2020.05.026

    authors: Francis L,Harrell A,Hallifax D,Galetin A

    更新日期:2020-09-01 00:00:00

  • Application of 13C CPMAS NMR for qualitative and quantitative characterization of carvedilol and its commercial formulations.

    abstract::(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and l...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23062

    authors: Zielińska-Pisklak M,Pisklak DM,Wawer I

    更新日期:2012-05-01 00:00:00

  • Anti-plasticizing effect of amorphous indomethacin induced by specific intermolecular interactions with PVA copolymer.

    abstract::The mechanism of how poly(vinyl alcohol-co-acrylic acid-co-methyl methacrylate) (PVA copolymer) stabilizes an amorphous drug was investigated. Solid dispersions of PVA copolymer, poly(vinyl pyrrolidone) (PVP), and poly(vinyl pyrrolidone-co-vinyl acetate) (PVPVA) with indomethacin (IMC) were prepared. The glass transit...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24023

    authors: Ueda H,Aikawa S,Kashima Y,Kikuchi J,Ida Y,Tanino T,Kadota K,Tozuka Y

    更新日期:2014-09-01 00:00:00

  • Stable isotope coadministration methodology for the estimation of the fraction of imipramine metabolized to desipramine.

    abstract::The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600790203

    authors: Sasaki Y,Shinohara Y,Baba S

    更新日期:1990-02-01 00:00:00

  • Degradation kinetics and isomerization of cefdinir, a new oral cephalosporin, in aqueous solution. 1.

    abstract::Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js950446r

    authors: Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda T

    更新日期:1996-09-01 00:00:00

  • Cardiovascular effects of two potential beta-hydroxylase inhibitors.

    abstract::The purpose of this study was to evaluate the cardiovascular effects of two potential beta-hydroxylase inhibitors, a dithiocarbamate and a thiourea derivative of d-amphetamine, 1 and 2, respectively. These compounds when given intravenously elicited a significant dose-dependent depressor effect in normotensive rats an...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600740621

    authors: Venugopalan CS,Jenkins HJ

    更新日期:1985-06-01 00:00:00

  • Racemic species of sodium ibuprofen: characterization and polymorphic relationships.

    abstract::Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10393

    authors: Zhang GG,Paspal SY,Suryanarayanan R,Grant DJ

    更新日期:2003-07-01 00:00:00

  • Raster image correlation spectroscopy as a novel tool for the quantitative assessment of protein diffusional behaviour in solution.

    abstract::The application of raster image correlation spectroscopy (RICS) as a tool for the characterisation of protein diffusion was assessed using a model protein, bovine serum albumin (BSA), as a function of formulation and denaturing conditions. RICS results were also validated against dynamic light scattering and fluoresce...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23105

    authors: Hamrang Z,Pluen A,Zindy E,Clarke D

    更新日期:2012-06-01 00:00:00

  • Degradation of trimethoprim.

    abstract::Trimethoprim undergoes thermally and photochemically catalyzed hydrolysis or oxidation to give rise to at least five products. The structures of these compounds were determined by physical methods and it was found that the resonance of C-5 in the 13C NMR spectrum is indicative of the substitution pattern of the result...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600780418

    authors: Bergh JJ,Breytenbach JC,Wessels PL

    更新日期:1989-04-01 00:00:00

  • Development and Evaluation of a Novel Drug Delivery: Pluronics/SDS Mixed Micelle Loaded With Myricetin In Vitro and In Vivo.

    abstract::This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.01.016

    authors: Wang G,Wang JJ,Li F,To SS

    更新日期:2016-04-01 00:00:00

  • Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.

    abstract::Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2015.12.005

    authors: Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

    更新日期:2016-02-01 00:00:00