The use of 13C labeling to enhance the sensitivity of 13C solid-state CPMAS NMR to study polymorphism in low dose solid formulations.

abstract：:Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

journal_title：Journal of pharmaceutical sciences

authors： Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

更新日期：1984-11-01 00:00:00

abstract：:The disposition of radioactivity following oral administration of 14C-norgestimate was compared to that following administration of the drug in combination with 3H-ethinyl estradiol in humans. Seven normal, healthy female subjects were each administered one capsule orally containing 14C-norgestimate either alone (74.4...

journal_title：Journal of pharmaceutical sciences

authors： Weintraub HS,Abrams LS,Patrick JE,McGuire JL

更新日期：1978-10-01 00:00:00

abstract：:Quantification of protein binding of new chemical entities is an important early screening step during drug discovery and is of fundamental interest for the estimation of safety margins during drug development. In this publication, we describe the development of a new high-throughput assay for the determination of the...

journal_title：Journal of pharmaceutical sciences

authors： Schuhmacher J,Kohlsdorfer C,Bühner K,Brandenburger T,Kruk R

更新日期：2004-04-01 00:00:00

abstract：:The applicability of bioavailability assessment at quasi- and nonsteady state is illustrated with data from a study comparing two formulations of amitriptyline hydrochloride in humans. Relative bioavailability as a function of the observed mean plasma concentrations may be expressed in closed form, provided the affect...

journal_title：Journal of pharmaceutical sciences

authors： Bondi JV,Hucker HB,Yeh KC,Kwan KC

更新日期：1976-11-01 00:00:00

abstract：:Wounds, particularly burns, are prone to colonization of potentially life-threatening bacteria. Local delivery of antimicrobial agents in sufficient quantities and over longer period of time can reduce risk of burn infections. Mupirocin-in-liposomes-in-hydrogels were proposed as advanced delivery system for improved b...

journal_title：Journal of pharmaceutical sciences

authors： Hurler J,Berg OA,Skar M,Conradi AH,Johnsen PJ,Skalko-Basnet N

更新日期：2012-10-01 00:00:00

abstract：:Many pharmaceuticals are formulated as powders to aid drug delivery. A major problem is how to produce powders having high purity, controlled morphology, and retained bioactivity. We demonstrate the use of supercritical carbon dioxide as an antisolvent for meeting this need for two model drug systems, quercetin, a spa...

journal_title：Journal of pharmaceutical sciences

authors： Jacobson GB,Shinde R,McCullough RL,Cheng NJ,Creasman A,Beyene A,Hickerson RP,Quan C,Turner C,Kaspar RL,Contag CH,Zare RN

更新日期：2010-06-01 00:00:00

abstract：:A high-pressure liquid chromatographic method suitable for determining plasma metoclopramide levels at normal (10-20 mg) doses is described. Eight metabolites as well as metclopramide were isolated and identified in rat, dog. and human urine. The only common metabolite in these species is 2-[(4-amino-5-chloro-2-metho...

journal_title：Journal of pharmaceutical sciences

authors： Teng L,Bruce RB,Dunning LK

更新日期：1977-11-01 00:00:00

abstract：:A solution of selegiline hydrochloride reference standard, which contained no detectable impurities at the time of its preparation, was found by HPLC to contain a trace of a compound at the locus of methamphetamine when analyzed after 1 year. Heating selegiline solutions at pH 7 and 105 degrees C produced methamphetam...

journal_title：Journal of pharmaceutical sciences

authors： Chafetz L,Desai MP,Sukonik L

更新日期：1994-09-01 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：: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：:The rising popularity of microwaves for drying, material processing and quality sensing has fuelled the need for knowledge concerning dielectric properties of common pharmaceutical materials. This article represents one of the few reports on the density and moisture content dependence of the dielectric properties of p...

journal_title：Journal of pharmaceutical sciences

authors： Heng PW,Loh ZH,Liew CV,Lee CC

更新日期：2010-02-01 00:00:00

abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

journal_title：Journal of pharmaceutical sciences

authors： Rayfield WJ,Kandula S,Khan H,Tugcu N

更新日期：2017-08-01 00:00:00

abstract：:The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

journal_title：Journal of pharmaceutical sciences

authors： Meffin PJ,Williams RL,Blaschke TF,Rowland M

更新日期：1977-01-01 00:00:00

abstract：:Dissolution profiles are classified in accordance with the shape of fractional dissolution rate function. This function is constant in time for the classical first-order model and, in this case, the dissolution is described by a monoexponential function. Therefore, any deviation of the fractional dissolution rate from...

journal_title：Journal of pharmaceutical sciences

authors： Lánský P,Weiss M

更新日期：2003-08-01 00:00:00

abstract：:Human skin samples are permeable to theophylline delivered from 1.5% solutions in various alkanecarboxylic acids and their mixtures. The respective permeability coefficients of theophylline, calculated from steady-state flux, correlate negatively with the permeability coefficients of the donor carboxylic acids and pos...

journal_title：Journal of pharmaceutical sciences

authors： Kadir R,Stempler D,Liron Z,Cohen S

更新日期：1987-10-01 00:00:00

abstract：:A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B

更新日期：1985-10-01 00:00:00

abstract：:A new three-step synthesis of 4-amino-3-hydroxybutyric acid from an inexpensive starting material and under mild reaction conditions is described. Crotonic acid was brominated by the Wohl-Ziegler reaction to 4-bromocrotonic acid, which, in turn, was converted with ammonium hydroxide into 4-aminocrotonic acid. This com...

journal_title：Journal of pharmaceutical sciences

authors： Pinza M,Pifferi G

更新日期：1978-01-01 00:00:00

abstract：:A stability-indicating reversed-phase high-performance liquid chromatographic method using a refractive index detector is described for the determination of propylene carbonate in pharmaceutical formulations. Good precision and accuracy of the method was demonstrated using an aqueous formulation. This method is also a...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Gadde RR

更新日期：1985-06-01 00:00:00

abstract：:Amorphous nifedipine (NFD), which has a smooth surface immediately after preparation, was shown to have structures resembling clusters of curling and branching fibers approximately 1 μm wide by atomic force microscopy (AFM) after storage at 25°C. The size of the cluster-like structures increased with storage over time...

journal_title：Journal of pharmaceutical sciences

authors： Miyazaki T,Aso Y,Kawanishi T

更新日期：2011-10-01 00:00:00

abstract：:A new extraction-spectrophotometric method for the determination of hydralazine, based on its reaction with 2-hydroxy-1-naphthaldehyde at 25 degrees C, is described. The calibration curve was linear between 0.4 and 6 mg/mL of hydralazine. The molar absorbtivity of the product at 408 nm is 40,900 L.mol-1.cm-1. The meth...

journal_title：Journal of pharmaceutical sciences

authors： Mari-Buigues J,Mañes-Vinuesa J,Garcia-Domenech R,Pous-Miralles G

更新日期：1991-07-01 00:00:00

abstract：:To reduce the inherent variability in serum uric acid levels of animals allowed ad libitum exposure to food containing potassium oxonate and uric acid, male Sprague-Dawley rats were trained to eat their daily food allotment in a 1.25-hr period each morning. After training the rats were fed a food mixture containing 5%...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Hsu TF,Combs AB

更新日期：1979-05-01 00:00:00

abstract：:The chromatographic retention behavior of dextromethorphan hydrobromide on an octadecylsilane column was investigated as a function of the pairing ion and the mobile phase composition. Dramatic increases in the capacity factor were observed with pairing ions containing more than eight carbons and with decreasing organ...

journal_title：Journal of pharmaceutical sciences

authors： Kubiak EJ,Munson JW

更新日期：1980-12-01 00:00:00

abstract：:Photoprotective potential and biological consequences (mutagenic potential) of octyl-dimethyl-PABA (ODP), titanium dioxide (TiO2 ), and montmorillonite (MMT) upon ultraviolet B (UVB) irradiation, alone and in different associations [physical mixtures (PMs)], were evaluated using a Saccharomyces cerevisiae ogg1 mutant ...

journal_title：Journal of pharmaceutical sciences

authors： Paiva JP,Santos BA,Kibwila DM,Gonçalves TC,Pinto AV,Rodrigues CR,Leitão AC,Cabral LM,De Pádula M

更新日期：2014-08-01 00:00:00

abstract：:2 closely related prostaglandins (PGs), A2 and B2, were separated by ion-exchange liquid chromatography. PGA2 and PGB2 are an isomeric pair of PGs which show little resolution on thin-layer chromatography; the pair can be resolved as gas-liquid chromatography, but use of this method requires protection of the C9-carb...

journal_title：Journal of pharmaceutical sciences

authors： Morozowich W

更新日期：1974-05-01 00:00:00

abstract：:This paper traces the academic genealogy of Professor Takeru Higuchi, who is considered "The Father of Physical Pharmacy" because of his contributions to the science of drug formulation and delivery and his impact in mentoring a whole generation of post-World War II pharmaceutical scientists. As one who was mentored b...

journal_title：Journal of pharmaceutical sciences

authors： Stella VJ

更新日期：2001-08-01 00:00:00

abstract：:During the drying process of a wet granulate, water-soluble compounds can migrate to the outer layers of the granule with the evaporating solvent. This migration can affect structural and mechanical characteristics of the granules as the solute accumulates on the granule's outer crust. The objective of this study was ...

journal_title：Journal of pharmaceutical sciences

authors： Poutiainen S,Honkanen M,Becker J,Nachtweide D,Järvinen K,Ketolainen J

更新日期：2012-04-01 00:00:00

abstract：:A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...

journal_title：Journal of pharmaceutical sciences

authors： Purdie N,Province DW,Johnson EA

更新日期：1999-07-01 00:00:00

abstract：:The metabolic fate of aprophen hydrochloride (2-diethylaminoethyl 2,2-diphenylpropionate) was studied in rats after intravenous administration. Both 14C-labeled and unlabeled aprophen were used in these studies. Blood samples were collected and analyzed to determine the identities of the metabolites formed. Utilizing ...

journal_title：Journal of pharmaceutical sciences

authors： Brown ND,Smejkal RM,Breuer E,Doctor BP,Chiang PK

更新日期：1988-02-01 00:00:00

abstract：:A method has been developed for the estimation of the distribution coefficient (D), which considers the microspecies of a compound. D is calculated from the microscopic dissociation constants (microconstants), the partition coefficients of the microspecies, and the counterion concentration. A general equation for the ...

journal_title：Journal of pharmaceutical sciences

authors： Csizmadia F,Tsantili-Kakoulidou A,Panderi I,Darvas F

更新日期：1997-07-01 00:00:00

abstract：:Melphalan (30 microgram/ml) is completely hydrolyzed in water at 37 degrees after 8 hr. At lower temperatures, hydrolysis proceeds at slower rates. The presence of bovine serum albumin retards hydrolysis of melphalan (30 microgram/ml) in water. The melphalan hydrolysis rate is directely releated to the bovine serum al...

journal_title：Journal of pharmaceutical sciences

authors： Chang SY,Alberts DS,Farquhar D,Melnick LR,Walson PD,Salmon SE

更新日期：1978-05-01 00:00:00