Vehicle effects in percutaneous absorption: in vitro study of influence of solvent power and microscopic viscosity of vehicle on benzocaine release from suspension hydrogels.

abstract：:Pharmaceutical scientists are often asked to assess the impact of modifications to the illumination in the manufacturing and product packaging environment on product quality. To assess the impact of switching light sources, four model compounds were exposed to standard fluorescent light, LED, and "yellow light" and th...

journal_title：Journal of pharmaceutical sciences

authors： Wasylaschuk W,Pierce B,Geng X,Socia A,Kim D,Wuelfing WP,Abend A

更新日期：2020-11-01 00:00:00

abstract：:Although significant progress had been made in developing general scale-up rules for an aqueous pan-coating process, there are often scenarios where small-scale experiments are not found to be truly reflective of what may be observed at the large scale. This article reviews some of the methods traditionally used for s...

journal_title：Journal of pharmaceutical sciences

authors： Pandey P,Bindra DS

更新日期：2014-11-01 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：: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：:Determination of the kinetics of water-soluble degradation products inside poly(lactide-co-glycolide) (PLGA) delivery systems during polymer degradation is important to evaluate the polymer microclimate conditions, particularly microclimate pH changes for optimization of encapsulated drug stability. A pre-derivatizati...

journal_title：Journal of pharmaceutical sciences

authors： Ding AG,Schwendeman SP

更新日期：2004-02-01 00:00:00

abstract：:A new synthesis is described for 10alpha-methoxy-delta8,9-lysergaldehyde involving the oxidation of elymoclavine with manganese dioxide in methanol. Lysergol and agroclavine provide no reaction under the same conditions. ...

journal_title：Journal of pharmaceutical sciences

authors： Choong TC,Thompson BL,Shough HR

更新日期：1977-09-01 00:00:00

abstract：:Baclofen, a widely used antispastic agent, has been found to exist in two crystalline forms, the anhydrate and monohydrate. The aim of this study was (1) to identify and characterize these two solid phases of baclofen, and (2) to examine the processing-induced phase transformations associated with wet granulation of b...

journal_title：Journal of pharmaceutical sciences

authors： Mirza S,Miroshnyk I,Rantanen J,Aaltonen J,Harjula P,Kiljunen E,Heinämäki J,Yliruusi J

更新日期：2007-09-01 00:00:00

abstract：:The significance of factors such as drug solubility, polymer molecular weight, drug loading dose, compression force, and hydrodynamic conditions on drug release from a swellable hydrophilic delivery system was investigated. Hydroxypropyl methylcellulose (HPMC) and pectin were major polymeric constituents of the delive...

journal_title：Journal of pharmaceutical sciences

authors： Kim H,Fassihi R

更新日期：1997-03-01 00:00:00

abstract：:The aim of the study was to determine and compare the degree of swelling and the swelling kinetics of poly(ethylene oxide) (PEO) hydrophilic matrix tablets without any additives for matrixes with different molecular weight polydispersities. A wide range of "mixed" polydisperse PEO tablets were obtained by mixing two P...

journal_title：Journal of pharmaceutical sciences

authors： Körner A,Larsson A,Andersson A,Piculell L

更新日期：2010-03-01 00:00:00

abstract：:The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...

journal_title：Journal of pharmaceutical sciences

authors： Nauha E,Bernstein J

更新日期：2015-06-01 00:00:00

abstract：:Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...

journal_title：Journal of pharmaceutical sciences

authors： Li W,Worosila GD,Wang W,Mascaro T

更新日期：2005-12-01 00:00:00

abstract：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:Dabrafenib is a small-molecule inhibitor of BRAF kinase activity that is currently being developed for the treatment of BRAF V600 mutation-positive melanoma. This clinical, open-label, two-cohort (n = 14 per cohort), randomized study was designed to evaluate the effect of drug substance particle size, and food on the ...

journal_title：Journal of pharmaceutical sciences

authors： Ouellet D,Grossmann KF,Limentani G,Nebot N,Lan K,Knowles L,Gordon MS,Sharma S,Infante JR,Lorusso PM,Pande G,Krachey EC,Blackman SC,Carson SW

更新日期：2013-09-01 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：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

journal_title：Journal of pharmaceutical sciences

authors： Schieffer GW,Palermo PJ,Pollard-Walker S

更新日期：1984-01-01 00:00:00

abstract：:A sensitive and specific GLC method is described to determine therapeutic levels of tilidine and its two main metabolites, nortilidine and bisnortilidine, in plasma and urine. The method involves the extraction of the compounds and an internal standard with cyclohexane from alkalinized samples, followed by back-extrac...

journal_title：Journal of pharmaceutical sciences

authors： Hengy H,Vollmer KO,Gladigau V

更新日期：1978-12-01 00:00:00

abstract：:Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...

journal_title：Journal of pharmaceutical sciences

authors： Davies NM,Wright MR,Russell AS,Jamali F

更新日期：1996-11-01 00:00:00

abstract：:Repeated acetaminophen (AP) administration modulates intestinal P-glycoprotein (P-gp) expression. Whether AP can modulate P-gp activity in a short-term fashion is unknown. We investigated the acute effect of AP on rat intestinal P-gp activity in vivo and in vitro. In everted intestinal sacs, AP inhibited serosal-mucos...

journal_title：Journal of pharmaceutical sciences

authors： Novak A,Carpini GD,Ruiz ML,Luquita MG,Rubio MC,Mottino AD,Ghanem CI

更新日期：2013-10-01 00:00:00

abstract：:Quantification analysis with near-infrared (NIR) spectroscopy typically requires utilizing chemometric techniques, such as partial least squares (PLS) method, to achieve the desired selectivity. This article points out a major limitation of these statistical-based calibration methods. The limitation is that the techni...

journal_title：Journal of pharmaceutical sciences

authors： Xiang D,Berry J,Buntz S,Gargiulo P,Cheney J,Joshi Y,Wabuyele B,Wu H,Hamed M,Hussain AS,Khan MA

更新日期：2009-03-01 00:00:00

abstract：:Caco-2 cell monolayers are widely used systems for predicting human intestinal absorption. This study was carried out to develop a quantitative structure-property relationship (QSPR) model of Caco-2 permeability using a novel genetic algorithm-based partial least squares (GA-PLS) method. The Caco-2 permeability data f...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita F,Wanchana S,Hashida M

更新日期：2002-10-01 00:00:00

abstract：:Pharmacokinetic profiles of pentylenetetrazol in the dog were studied following rapid intravenous and oral administrations of a convulsant dose (15-20 mg/kg). Plasma level-time curves after a rapid intravenous injection showed biexponential decline, indicating that the disposition of this drug in the dog follows a two...

journal_title：Journal of pharmaceutical sciences

authors： Jun HW

更新日期：1976-07-01 00:00:00

abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...

journal_title：Journal of pharmaceutical sciences

authors： Wu B,Sun YN

更新日期：2014-01-01 00:00:00

abstract：:The purpose of the present study was to examine whether the intestinal absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of PEPT1, using rebamipi...

journal_title：Journal of pharmaceutical sciences

authors： Kikuchi A,Tomoyasu T,Tanaka M,Kanamitsu K,Sasabe H,Maeda T,Odomi M,Tamai I

更新日期：2009-05-01 00:00:00

abstract：:Poly(D,L-lactide-co-glycolide, 50:50) samples of similar molecular weight were obtained from three commercial sources and were characterized by gel permeation chromatography, differential scanning calorimetry, X-ray powder diffraction, viscometry, and proton nuclear magnetic resonance spectroscopy. Pellets were prepar...

journal_title：Journal of pharmaceutical sciences

authors： Schmitt EA,Flanagan DR,Linhardt RJ

更新日期：1993-03-01 00:00:00

abstract：:Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

journal_title：Journal of pharmaceutical sciences

authors： Hosseini-Yeganeh M,McLachlan AJ

更新日期：2001-11-01 00:00:00

abstract：:The objective of this study was to investigate the permeation-enhancing effect of thiolated polycarbophil (PCP) on peptide drugs. Mediated by a carbodiimide, increasing amounts of cysteine (Cys) were covalently bound to sodium neutralized PCP (NaPCP). The extent of covalently attached Cys was determined by quantifying...

journal_title：Journal of pharmaceutical sciences

authors： Clausen AE,Bernkop-Schnürch A

更新日期：2000-10-01 00:00:00

abstract：:Although many biotech products are successfully stored in the frozen state, there are cases of degradation of biologicals during freeze storage. These examples are discussed in the Perspective to emphasize the fact that stability of frozen biologicals should not be taken for granted. Frozen-state degradation (predomin...

journal_title：Journal of pharmaceutical sciences

authors： Authelin JR,Rodrigues MA,Tchessalov S,Singh SK,McCoy T,Wang S,Shalaev E

更新日期：2020-01-01 00:00:00

abstract：:The absorption-enhancing effects of polyamidoamine (PAMAM) dendrimers with various generations (G0-G3) and concentrations [0.1%-1.0% (w/v)] on the pulmonary absorption of peptide and protein drugs were studied in rats. Insulin and calcitonin were chosen as models of peptide and protein drugs, and their pulmonary absor...

journal_title：Journal of pharmaceutical sciences

authors： Dong Z,Hamid KA,Gao Y,Lin Y,Katsumi H,Sakane T,Yamamoto A

更新日期：2011-05-01 00:00:00

abstract：:We have developed a hydrogel patch, which could promote antigen penetration through stratum corneum (SC), and have demonstrated its safety and efficacy in animals and humans. For the availability improvement of our system, it is important to develop a device, which enhances antigen penetration through SC more efficien...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo K,Ishii Y,Kawai Y,Saiba Y,Quan YS,Kamiyama F,Hirobe S,Okada N,Nakagawa S

更新日期：2013-06-01 00:00:00

abstract：:AZD1175 and AZD2207 are 2 highly lipophilic compounds with a significant risk of not achieving therapeutic plasma concentrations due to solubility-limited absorption. The compounds have the same molecular weight and minimal structural differences. The aim of the present work was to investigate whether salts could be a...

journal_title：Journal of pharmaceutical sciences

authors： Tannergren C,Karlsson E,Sigfridsson K,Lindfors L,Ku A,Polentarutti B,Carlert S

更新日期：2016-11-01 00:00:00