Cyclazocine and norepinephrine uptake, metabolism, and turnover in the rat brain.

abstract：:Four solvates of erythromycin have been crystallographically characterized. The solvates of THF and dioxane are very similar but differ in notable ways. The isopropanol solvate exhibits uncommon modes of hydrogen bonding, which have previously been seen only in the erythomycin B hydrate. The methanol solvate is striki...

journal_title：Journal of pharmaceutical sciences

authors： Henry R,Zhang GG

更新日期：2007-05-01 00:00:00

abstract：:A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

journal_title：Journal of pharmaceutical sciences

authors： Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

更新日期：2015-10-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:Nipecotic acid (1), one of the most potent in vitro inhibitors of neuronal and glial gamma-amino butyric acid (GABA) uptake, is inactive as an anticonvulsant when administered systemically. To obtain in vivo active prodrugs of (1), we synthesized four new nipecotic acid esters (3-6), which were obtained by chemical co...

journal_title：Journal of pharmaceutical sciences

authors： Bonina FP,Arenare L,Palagiano F,Saija A,Nava F,Trombetta D,de Caprariis P

更新日期：1999-05-01 00:00:00

abstract：:Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

更新日期：2010-07-01 00:00:00

abstract：:The aim of the present study was to investigate the mechanism of aqueous degradation of Salinosporamide A (NPI-0052; 1), a potent proteasome inhibitor that is currently in Phase I clinical trials for the treatment of cancer and is characterized by a unique beta-lactone-gamma-lactam bicyclic ring structure. The degrada...

journal_title：Journal of pharmaceutical sciences

authors： Denora N,Potts BC,Stella VJ

更新日期：2007-08-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00

abstract：:This study describes the adaptation of conventional titrimetric and spectrophotometric techniques to a microscale for the determination of drug ionization constants (pKa) and partition coefficients (log P). The apparatus for determining pKa and compound purity (or equivalent weight) consists of a three-port conical gl...

journal_title：Journal of pharmaceutical sciences

authors： Morgan ME,Lui K,Anderson BD

更新日期：1998-02-01 00:00:00

abstract：:A procedure is described for the analysis of urushiol content of pharmaceutical preparations containing extracts of poison ivy (Toxicodendron radicans) and poison oak (T. diversilobum) in vegetable oils. The procedure involves extraction of the urushiols from the oily solutions using 90% methanol in water followed by ...

journal_title：Journal of pharmaceutical sciences

authors： Elsohly MA,Turner CE

更新日期：1980-05-01 00:00:00

abstract：:Simple assays for extraction and determination of the concentrations of the antibiotics oxytetracycline, oxolinic acid, and flumequine in a drug dosage form for farmed fish are described. HPLC with UV detection was used in the analyses. The recovery of all three drugs was approximately 100%, and the precision varied f...

journal_title：Journal of pharmaceutical sciences

authors： Rogstad A,Weng B

更新日期：1993-05-01 00:00:00

abstract：:Drug-induced phototoxic skin responses involves photoirritation, photoallergy, and photogenotoxicity. In the present study, we attempted to develop effective analytical tools to predict the photogenotoxic potential of pharmaceutical substances on the basis of their photobiological and DNA-binding properties. Photoclea...

journal_title：Journal of pharmaceutical sciences

authors： Onoue S,Seto Y,Oishi A,Yamada S

更新日期：2009-10-01 00:00:00

abstract：:The mechanism of organic solvent evaporation during microencapsulation and its role during microsphere hardening has been investigated. Evaporation and encapsulation studies were carried out in a jacketed beaker, filled with aqueous hardening solution, which was maintained at constant temperature and constant stirring...

journal_title：Journal of pharmaceutical sciences

authors： Wang J,Schwendeman SP

更新日期：1999-10-01 00:00:00

abstract：:Ketoconazole and posaconazole are both Biopharmaceutics Classification System class 2 drugs (highly permeable, poorly soluble), are structurally similar, and are administered at the same doses. Nevertheless, the duodenal concentration profile and the magnitude of the positive food effect observed for these 2 drugs are...

journal_title：Journal of pharmaceutical sciences

authors： Cristofoletti R,Patel N,Dressman JB

更新日期：2016-09-01 00:00:00

abstract：:A method for the measurement of a potential diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids is described. The procedure involves the addition of a related internal standard to the specimens followed by extraction of the acids into...

journal_title：Journal of pharmaceutical sciences

authors： Weidner LL,Zacchei AG

更新日期：1984-02-01 00:00:00

abstract：:The solubility of phenacetin was determined at five temperatures in solvent mixtures of aprotic-amphiprotic mixtures of dioxane and water. Enthalpy-entropy compensation analysis is used to study the effect of changing polarity of the medium on the solute. The apparent heats of solution and free energies of solution ar...

journal_title：Journal of pharmaceutical sciences

authors： Bustamante C,Bustamante P

更新日期：1996-10-01 00:00:00

abstract：:We describe the key issues and possibilities for continuous final dosage formation, otherwise known as downstream processing or drug product manufacturing. A distinction is made between heterogeneous processing and homogeneous processing, the latter of which is expected to add more value to continuous manufacturing. W...

journal_title：Journal of pharmaceutical sciences

authors： Byrn S,Futran M,Thomas H,Jayjock E,Maron N,Meyer RF,Myerson AS,Thien MP,Trout BL

更新日期：2015-03-01 00:00:00

abstract：:Recently, our laboratory reported that intravenous immunoglobulin (IVIG) treatment increased antiplatelet antibody (7E3) clearance in a rat model of immune thrombocytopenic purpura (ITP). However, due to the multifaceted nature of IVIG therapy, the contribution of this increase in antiplatelet antibody clearance to th...

journal_title：Journal of pharmaceutical sciences

authors： Hansen RJ,Balthasar JP

更新日期：2003-06-01 00:00:00

abstract：:Biodegradable, dextran-based ion-exchange microspheres (IE-MS) have been used for localized delivery of anticancer drugs and chemosensitizers. Because of their hydrophilic nature, the IE-MS release their payload quickly. The purpose of this work was to develop an IE-MS system that could provide a broad range of releas...

journal_title：Journal of pharmaceutical sciences

authors： Liu Z,Wu XY,Ballinger JR,Bendayan R

更新日期：2000-06-01 00:00:00

abstract：:In recent years, computational methods have garnered much attention in protein engineering. A large number of computational methods have been developed to analyze the sequences and structures of proteins and have been used to predict the various properties. Antibodies are one of the emergent protein therapeutics, and ...

journal_title：Journal of pharmaceutical sciences

authors： Kuroda D,Tsumoto K

更新日期：2020-05-01 00:00:00

abstract：:A rapid solubility-screening assay was developed with a focus on Biopharmaceutic Classification Scheme (BCS) class II drug solubility in animal and simulated human gastrointestinal (GI) fluids. The assay enables biologically promising drug leads to be evaluated for solubility limitations earlier in the drug developmen...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Elzinga PA,Hageman MJ,Herron JN

更新日期：2008-04-01 00:00:00

abstract：:A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

journal_title：Journal of pharmaceutical sciences

authors： Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

更新日期：2012-12-01 00:00:00

abstract：:A high-pressure liquid chromatographic procedure for quantitative dexamethasone and dexamethasone sodium phosphate determinations in all types of commercially available pharmaceutical dosage forms was developed. The method also separates dexamethasone from its phosphate salt and separates dexamethasone or its salt fro...

journal_title：Journal of pharmaceutical sciences

authors： Gupta VD

更新日期：1979-07-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. This apparatus is very sensitiv...

journal_title：Journal of pharmaceutical sciences

authors： Wang Y,Armenante PM

更新日期：2012-02-01 00:00:00

abstract：:The degradation kinetics of moricizine hydrochloride (1) were examined over a pH range of 0.6 to 6.0 at an ionic strength of 0.3 and 60 degrees C. The disappearance of intact 1 was followed by a stability-indicating HPLC assay. The degradation products, which had approximate solubilities of less than 100 micrograms/mL...

journal_title：Journal of pharmaceutical sciences

authors： King SP,Sigvardson KW,Dudzinski J,Torosian G

更新日期：1992-06-01 00:00:00

abstract：:Papers and patents that deal with polymorphism (crystal systems for which a substance can exist in structures characterized by different unit cells, but where each of the forms has exactly the same elemental composition) and solvatomorphism (systems where the crystal structures of the substance are defined by differen...

journal_title：Journal of pharmaceutical sciences

authors： Brittain HG

更新日期：2009-05-01 00:00:00

abstract：:New dihydropyridine in equilibrium pyridinium salt-type redox carrier systems were developed in which the drug is linked via the ring nitrogen atom of nicotinamide. The rate of oxidation of the dihydropyridine forms, and thus the overall and brain-specific distribution of the corresponding 3-carbamoyl-1-carbamoylalkyl...

journal_title：Journal of pharmaceutical sciences

authors： Bodor N,AbdelAlim AM

更新日期：1985-03-01 00:00:00

abstract：:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with eth...

journal_title：Journal of pharmaceutical sciences

authors： Varin F,Cubeddu LX,Powell JR

更新日期：1986-12-01 00:00:00

abstract：:The release kinetics of a polymeric-controlled release device are determined by its geometry and dimensions. A method to calculate the required size and shape of diffusion-controlled dosage forms to achieve a particular release profile is presented. The diffusion parameters are determined for various drugs (theophylli...

journal_title：Journal of pharmaceutical sciences

authors： Siepmann J,Ainaoui A,Vergnaud JM,Bodmeier R

更新日期：1998-07-01 00:00:00

abstract：:The aim of this work was to evaluate the low molecular weight chitosans (LMWCs) as enhancers of transdermal administration of baicalin, an useful drug for the treatment of atopic dermatitis, viral hepatitis, and HIV infection. Permeation experiments were performed in vitro through mouse skin by using Franz cells. Impr...

journal_title：Journal of pharmaceutical sciences

authors： Zhou X,Liu D,Liu H,Yang Q,Yao K,Wang X,Wang L,Yang X

更新日期：2010-07-01 00:00:00