Improved techniques for the photometric determination of partition coefficients, with particular reference to the chloroform-ammonia solvent system.

abstract：:Sugars and polyols have been used routinely with lyophilized proteins and peptides as bulking agents, cryoprotectants, and lyoprotectants. However, reducing sugars may present a problem as excipients since they are potentially reactive with proteins. In this stability study of recombinant human relaxin (Rix) with vari...

journal_title：Journal of pharmaceutical sciences

authors： Li S,Patapoff TW,Overcashier D,Hsu C,Nguyen TH,Borchardt RT

更新日期：1996-08-01 00:00:00

abstract：:A sensitive, specific and reproducible high-performance liquid chromatographic procedure, using the normal phase and radial compression system, is described for the simultaneous determination of corticosterone, hydrocortisone, and dexamethasone in plasma, with prednisolone as the internal standard. Samples were extrac...

journal_title：Journal of pharmaceutical sciences

authors： Alvinerie M,Toutain PL

更新日期：1982-07-01 00:00:00

abstract：:Fifteen pyrimidine-related compounds were evaluated for their ability to inhibit enzymatic degradation of 5-fluoro-2'-deoxyuridine (FUdR). Acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil] showed the highest inhibitory effect on the phosphorolytic degradation of FUdR in various tissue homogenates derived fro...

journal_title：Journal of pharmaceutical sciences

authors： Kawaguchi T,Saito M,Saneyoshi M

更新日期：1988-11-01 00:00:00

abstract：:A radioimmunoassay procedure was developed for the antihistamine terfenadine (alpha[4-(1,2-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol). The keto analog of terfenadine was converted to its O-carboxymethyloxime derivative, which was conjugated to bovine thyroglobulin by a mixed anhydride techniq...

journal_title：Journal of pharmaceutical sciences

authors： Cook CE,Williams DL,Myers M,Tallent CR,Leeson GA,Okerholm RA,Wright GJ

更新日期：1980-12-01 00:00:00

abstract：:New butyrate derivatives were synthesized to investigate the residence time of potent butyric acid in vivo. These derivatives were triglycerides in which one, two, or three butyric acid molecules were bound to glycerol or to mono- and dipalmitic esters of glycerol. Pharmacokinetic studies showed that a constant plasma...

journal_title：Journal of pharmaceutical sciences

authors： Planchon P,Pouillart P,Ronco G,Villa P,Pieri F

更新日期：1993-10-01 00:00:00

abstract：:A gas chromatographic-mass spectrometric method was developed for the stereoselective quantification of threo-methylphenidate (MPD) and its metabolite, ritalinic acid (RA), in plasma or urine. The plasma concentrations of (+)-MPD after oral administration of two 10-mg conventional tablets containing racemic MPD.HCl or...

journal_title：Journal of pharmaceutical sciences

authors： Aoyama T,Kotaki H,Honda Y,Nakagawa F

更新日期：1990-06-01 00:00:00

abstract：:The knowledge of physicochemical properties of organic compounds becomes increasingly important in pharmaceutical sciences, chemical engineering, and other fields. In this study, we developed UPPER (Unified Physicochemical Property Estimation Relationships), a comprehensive model for the estimation of 20 physicochemic...

journal_title：Journal of pharmaceutical sciences

authors： Lian B,Yalkowsky SH

更新日期：2014-09-01 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：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...

journal_title：Journal of pharmaceutical sciences

authors： Mohanakrishnan P,Chignell CF,Cox RH

更新日期：1985-01-01 00:00:00

abstract：:Successful development of stable solid protein formulations usually requires the addition of one or several excipients to achieve optimal stability. In these products, there is a potential risk of an inhomogeneous distribution of the various ingredients, specifically the ratio of protein and stabilizer may vary. Such ...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen KTT,Frijlink HW,Hinrichs WLJ

更新日期：2020-01-01 00:00:00

abstract：:Each of three harmala alkaloids, harmine, harmaline, and harmalol, decreased heart rate and increased pulse pressure, peak aortic flow, and myocardial contractile force in intact normotensive anesthetized dogs. Harmine reduced systemic arterial blood pressure and total peripheral vascular resistance; harmaline-evoked ...

journal_title：Journal of pharmaceutical sciences

authors： Aarons DH,Rossi GV,Orzechowski RF

更新日期：1977-09-01 00:00:00

abstract：:The effect of pretreating callus membranes with dimethyl sulfoxide, dimethylacetamide, dimethylformamide, formamide, dioxane, or methyl orthoformate on sarin permeability was studied at three temperatures to determine the activation energy for transport. In addition, the effect of membrane pretreatment on permeability...

journal_title：Journal of pharmaceutical sciences

authors： Matheson LE,Wurster DE,Ostrenga JA

更新日期：1979-11-01 00:00:00

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

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

更新日期：1989-01-01 00:00:00

abstract：:Virtually all biological variables, including those affected by drugs, are subject to adaptive self regulation. In the description of the pharmacodynamics (PD) of drugs, it may be necessary to consider the endogenous control system (ECS) as an integral part of the PD. A PDECS model based on system analysis principles ...

journal_title：Journal of pharmaceutical sciences

authors： Veng-Pedersen P,Modi NB

更新日期：1993-03-01 00:00:00

abstract：:The penetration of benzyl alcohol (BA) through split-thickness cadaver skin was measured in nonoccluded Franz cells placed in a fume hood. BA, dissolved in a small volume of ethanol and spiked with (14)C radiolabel, was applied to skin at nine doses ranging from 0.9 to 10600 microg/cm(2). The percentage of radioactivi...

journal_title：Journal of pharmaceutical sciences

authors： Miller MA,Bhatt V,Kasting GB

更新日期：2006-02-01 00:00:00

abstract：:The dissolution of the 60-85-mesh fraction os recording, flow-through dissolution apparatus equipped with a dissolution cell; it was particularly suitable for kinetic analysis of multiparticulate systems. By using a time-scaling approach, experimental data are compared with theoretical calculations to evaluate, quanti...

journal_title：Journal of pharmaceutical sciences

authors： Pedersen PV,Brown KF

更新日期：1976-10-01 00:00:00

abstract：:The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL...

journal_title：Journal of pharmaceutical sciences

authors： Stange U,Führling C,Gieseler H

更新日期：2013-06-01 00:00:00

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

journal_title：Journal of pharmaceutical sciences

authors： Buchan B,Kay G,Matthews KH,Cairns D

更新日期：2012-10-01 00:00:00

abstract：:Application of ultrasound enhances transdermal transport of drugs (sonophoresis). The enhancement may result from enhanced diffusion due to ultrasound-induced skin alteration and/or from forced convection. To understand the relative roles played by these two mechanisms in low-frequency sonophoresis (LFS, 20 kHz), a th...

journal_title：Journal of pharmaceutical sciences

authors： Tang H,Mitragotri S,Blankschtein D,Langer R

更新日期：2001-05-01 00:00:00

abstract：:The effect of caffeine on the absorption of ergotamine from the rat small intestine was studied. The results of a series of experiments showed that caffeine significantly enhanced absorption of ergotamine from solutions of pH 5.0 when both substances were in solution and when an intact blood supply was either absent (...

journal_title：Journal of pharmaceutical sciences

authors： Anderson JR,Drehsen G,Pitman IH

更新日期：1981-06-01 00:00:00

abstract：:The hepatic distribution, biliary excretion, and mass balance of liposomal amphotericin B (L-AmB) were investigated in recirculated isolated perfused rat liver. The results were compared with those from the conventional AmB formulation, amphotericin B deoxycholate (D-AmB). L-AmB was introduced as a bolus into the perf...

journal_title：Journal of pharmaceutical sciences

authors： Hong Y,Ramzan I,McLachlan AJ

更新日期：2005-01-01 00:00:00

abstract：:Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style ...

journal_title：Journal of pharmaceutical sciences

authors： Ran W,Ma H,Li M

更新日期：2020-06-01 00:00:00

abstract：:NF-kappaB activation is clearly linked to the pathogenesis of multiple inflammatory diseases including arthritis. The prominent role of IkappaB kinase-2 (IKK-2) in regulating NF-kappaB signaling in response to proinflammatory stimuli has made IKK-2 a primary anti-inflammation therapeutic target. PHA-408, a potent and ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Kishore NN,Thompson DC

更新日期：2010-03-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:A rapid, sensitive, and accurate reversed-phase HPLC method has been developed for the analysis and quantification of pharmaceutical formulations containing tyrothricin (1), an antibiotic used in antiseptic buccal compressed tablets for local application. The assay has been carried out under isocratic conditions, usin...

journal_title：Journal of pharmaceutical sciences

authors： Caraballo I,Fernandez-Arevalo M,Holgado MA,Vela MT,Rabasco AM

更新日期：1994-08-01 00:00:00

abstract：:The delivery of drugs via the mucous membranes lining the oral cavity (i.e., sublingual and buccal), with consideration of both systemic delivery and local therapy, is reviewed in this paper. The structure and composition of the mucosae at different sites in the oral cavity, factors affecting mucosal permeability, pen...

journal_title：Journal of pharmaceutical sciences

authors： Harris D,Robinson JR

更新日期：1992-01-01 00:00:00

abstract：:The dissolution characteristics of dicumarol were markedly enhanced by preparing dispersions of drug in polyethylene glycol 4000. Solid dispersions of varying weight fractions were formed by a melt method without measurable drug degradation or evaporation. There were no significant differences in dissolution rates amo...

journal_title：Journal of pharmaceutical sciences

authors： Ravis WR,Chen CY

更新日期：1981-12-01 00:00:00

abstract：:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusua...

journal_title：Journal of pharmaceutical sciences

authors： Leong NJ,Prankerd RJ,Shackleford DM,Mcintosh MP

更新日期：2015-04-01 00:00:00