Synthesis and antibacterial evaluation of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles.

abstract：:The disposition kinetics of nicotine and cotinine enantiomers was determined in rabbits. The clearance of (R)-nicotine was similar to that of (S)-nicotine, but clearance of (R)-cotinine was twice that of (S)-cotinine. Fractional conversions of both enantiomers of nicotine to cotinine were approximately 50%. These resu...

journal_title：Journal of pharmaceutical sciences

authors： Jacob P 3rd,Benowitz NL,Copeland JR,Risner ME,Cone EJ

更新日期：1988-05-01 00:00:00

abstract：:Aggregation of therapeutic monoclonal antibodies has a potential risk of immunogenicity, requiring minimization of aggregate formation. We have developed a fitting formula for antibody aggregation at 40°C based on physicochemical parameters, including colloidal and conformational stabilities. An IgG1 monoclonal antibo...

journal_title：Journal of pharmaceutical sciences

authors： Oyama H,Koga H,Tadokoro T,Maenaka K,Shiota A,Yokoyama M,Noda M,Torisu T,Uchiyama S

更新日期：2020-01-01 00:00:00

abstract：:The chemical shifts of the methyl groups of 2,4-dimethylbenzo[g]quinoline are defined with respect to concentration, showing that the methyl resonances are reversed from their expected positions in concentrations normally used in NMR spectroscopy. The phenomenon is explained in terms of the probably "fixation" of bond...

journal_title：Journal of pharmaceutical sciences

authors： Born JL,Harsin CE

更新日期：1977-08-01 00:00:00

abstract：:Porcine gelatins have been widely used as stabilizers of macromolecular based pharmaceuticals but the mechanism by which they stabilize has not been precisely established. Their variability and immunogenicity, however, make them less than ideal excipients. In this work, we take advantage of the availability of recombi...

journal_title：Journal of pharmaceutical sciences

authors： Thyagarajapuram N,Olsen D,Middaugh CR

更新日期：2007-12-01 00:00:00

abstract：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

journal_title：Journal of pharmaceutical sciences

authors： Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

更新日期：2009-01-01 00:00:00

abstract：:A specific, sensitive, rapid, and reproducible analytical GLC method for lidocaine in human plasma, including pharmacokinetic parameters, is described. Aminopyrine is the internal standard. The method was used to study pharmacokinetics in four healthy volunteers following the administration of a lidocaine bolus at a d...

journal_title：Journal of pharmaceutical sciences

authors： Caille G,Lelorier J,Latour Y,Besner JG

更新日期：1977-10-01 00:00:00

abstract：:A GLC method is described for the determination of iminodibenzyl and desipramine impurities in imipramine hydrochloride and its formulated products. These impurities were extracted from an alkaline solution with a mixture of 30% methylene chloride in hexane for chromatography on a 3% OV-17 GLC column. Iminodibenzyl wa...

journal_title：Journal of pharmaceutical sciences

authors： Thompson DW

更新日期：1982-05-01 00:00:00

abstract：:A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

journal_title：Journal of pharmaceutical sciences

authors： Ellis KO,Schwan TJ,Wessels FL,Miles NJ

更新日期：1980-10-01 00:00:00

abstract：:In this study, curcumin and/or docosahexaenoic acid (DHA) were encapsulated in Thai silk fibroin/gelatin (SF/G) sponges, prepared at different blending ratios, aimed to be applied as a controlled release system for localized cancer therapy. The SF/G sponges were fabricated by freeze-drying and glutaraldehyde cross-lin...

journal_title：Journal of pharmaceutical sciences

authors： Lerdchai K,Kitsongsermthon J,Ratanavaraporn J,Kanokpanont S,Damrongsakkul S

更新日期：2016-01-01 00:00:00

abstract：:Free radical polymerization converts aqueous solutions of methacrylated inulin into cross-linked hydrogels. The purpose of this work was to study the hydrogel formation and to characterize the fully cured hydrogels. The gelation process of aqueous solutions of methacrylated inulin was monitored as a function of time b...

journal_title：Journal of pharmaceutical sciences

authors： Vervoort L,Vinckier I,Moldenaers P,Van den Mooter G,Augustijns P,Kinget R

更新日期：1999-02-01 00:00:00

abstract：:Solubilization of nonpolar drugs constitutes one of the most important tasks in parenteral formulations design. This study investigates and assesses the solubility enhancement of Fluasterone by various techniques including cosolvency, micellization, and complexation. Of the solubilizing agents used, the modified beta-...

journal_title：Journal of pharmaceutical sciences

authors： Zhao L,Li P,Yalkowsky SH

更新日期：1999-10-01 00:00:00

abstract：:The intense blue color formed in the official assay of menadione injection by treatment of the sample with 2,4-dinitrophenylhydrazine and ammonia is shown by data from visible light spectra and mass spectra and by comparison of the pKa value with that of the corresponding reaction product of acetone to be due to proto...

journal_title：Journal of pharmaceutical sciences

authors： Burns LB,Stedman RJ,Tuckerman MM

更新日期：1978-02-01 00:00:00

abstract：:In 2005, the World Health Organization (WHO) proposed that provided an active pharmaceutical ingredient could meet certain criteria, bioequivalence could be evaluated with a set of laboratory tests, obviating the need for expensive and time-consuming pharmacokinetic studies in humans. The aim of this work was to deter...

journal_title：Journal of pharmaceutical sciences

authors： Strauch S,Jantratid E,Stahl M,Rägo L,Dressman JB

更新日期：2011-03-01 00:00:00

abstract：:A novel process based on solvent extraction was developed to produce drug-loaded polyanhydride microspheres for controlled-release applications. The technique consists of adding a chloroform solution of polyanhydride and drug into a stirred silicone oil phase containing suspended droplets of surfactant. No chemical re...

journal_title：Journal of pharmaceutical sciences

authors： Bindschaedler C,Leong K,Mathiowitz E,Langer R

更新日期：1988-08-01 00:00:00

abstract：:Model independent pharmacokinetic analysis of intravenous (iv) amphotericin B cochleates (CAMB), a new lipid-based drug delivery system, in mice (0.625 mg/kg) shows a two-phase disposition profile in blood [area under the curve of concentration versus time from time zero to infinity (AUC(0-infinity)) = 1.01 microg. h/...

journal_title：Journal of pharmaceutical sciences

authors： Segarra I,Movshin DA,Zarif L

更新日期：2002-08-01 00:00:00

abstract：:A high-performance liquid chromatographic method for the simultaneous determination of propranolol and 4-hydroxypropranolol in plasma is presented. The method involves plasma extraction at basic pH with ethyl column, and fluorescence detection. The within-run a reversed-phase column coefficient of variation were 3.0-7...

journal_title：Journal of pharmaceutical sciences

authors： Rosseel MT,Bogaert MG

更新日期：1981-06-01 00:00:00

abstract：:A consistent account of the assumptions of the well-stirred perfusion limited model leads to the equation for the organ tissue that does not coincide with that often presented in books and papers. The difference in pharmacokinetic profiles calculated by the valid and the commonly used equations could be quite signific...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2010-01-01 00:00:00

abstract：:The transition temperature, T(t), of polymorphs is estimated from both their heats of solution and solubilities (or intrinsic dissolution rates) determined at any one temperature (e.g., ambient). At a given temperature, T, the enthalpy difference, DeltaH, between polymorphs, I and II, is equal to the difference betwee...

journal_title：Journal of pharmaceutical sciences

authors： Gu CH,Grant DJ

更新日期：2001-09-01 00:00:00

abstract：:The absorption, protein binding, blood-to-plasma ratio, renal excretion, and pharmacokinetics of the dopamine-2 agonists (D2-agonists) 4-(2-di-n-propylaminoethyl)-7-hydroxy-2-(3H)-indolone (1), N-(2'-hydroxy-5'-[N,N-di-n-propylaminoethylphenyl])methanesulfonamide (2), and 4-(2-di-n-propylaminoethyl)-2-(3H)-indolone (3...

journal_title：Journal of pharmaceutical sciences

authors： Swagzdis JE,Wittendorf RW,DeMarinis RM,Mico BA

更新日期：1986-10-01 00:00:00

abstract：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

journal_title：Journal of pharmaceutical sciences

authors： Grant J,Blicker M,Piquette-Miller M,Allen C

更新日期：2005-07-01 00:00:00

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

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

更新日期：2016-02-01 00:00:00

abstract：:A comprehensive model is developed to describe the swelling/dissolution behaviors and drug release from hydrophilic matrices. The major thrust of this model is to employ an important physical property of the polymer, the polymer disentanglement concentration, rho p,dis, the polymer concentration below which polymer ch...

journal_title：Journal of pharmaceutical sciences

authors： Ju RT,Nixon PR,Patel MV,Tong DM

更新日期：1995-12-01 00:00:00

abstract：:The application of direct zero-order UV spectrophotometric and graphical or derivative background correction methods to selected pharmaceutical preparations shows their relative advantages in different situations. The assay of the active components in a changeable matrix is a problem with formulations having a limited...

journal_title：Journal of pharmaceutical sciences

authors： Traveset J,Such V,Gonzalo R,Gelpi E

更新日期：1980-06-01 00:00:00

abstract：:Two nonporous and three porous amorphous silicas were used as dispersion media to convert corticoid solutions into free-flowing powders. The corticoids (prednisone, prednisolone, and hydrocortisone) were dissolved in N,N-dimethylacetamide-polyethylene glycol 400 (7:3 v/v) and their 10% (w/v) solutions were mixed with ...

journal_title：Journal of pharmaceutical sciences

authors： Liao CC,Jarowski CI

更新日期：1984-03-01 00:00:00

abstract：:A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

journal_title：Journal of pharmaceutical sciences

authors： El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

更新日期：2012-11-01 00:00:00

abstract：:Industry experience suggests that g-forces sustained when vials containing protein formulations are accidentally dropped can cause aggregation and particle formation. To study this phenomenon, a shock tower was used to apply controlled g-forces to glass vials containing formulations of two monoclonal antibodies and re...

journal_title：Journal of pharmaceutical sciences

authors： Randolph TW,Schiltz E,Sederstrom D,Steinmann D,Mozziconacci O,Schöneich C,Freund E,Ricci MS,Carpenter JF,Lengsfeld CS

更新日期：2015-02-01 00:00:00

abstract：:The inclusion complexation of homologous derivatives of steroid hormones with cyclodextrins and 2-hydroxypropyl-beta-cyclodextrin (2-HP-beta-CD) was investigated with regard to underlying structure-interaction relationship. The interaction was studied by phase solubility analysis and stabilization effects of complex f...

journal_title：Journal of pharmaceutical sciences

authors： Albers E,Müller BW

更新日期：1992-08-01 00:00:00

abstract：:Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

journal_title：Journal of pharmaceutical sciences

authors： Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

更新日期：2002-04-01 00:00:00

abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...

journal_title：Journal of pharmaceutical sciences

authors： Plise EG,Tran D,Salphati L

更新日期：2010-12-01 00:00:00

abstract：:The bioavailability of clofibric acid from formulations containing calcium clofibrate along and mixed with calcium carbonate (1:1 w/w) was compared to that from a standard clofibrate formulation in a crossover study in 12 human subjects. The 95% confidence intervals of bioavailability differences were such that they ...

journal_title：Journal of pharmaceutical sciences

authors： Taylor T,Chasseaud LF

更新日期：1977-11-01 00:00:00