The Effect of Genetic Polymorphism on the Inhibition of Azole Antifungal Agents Against CYP2C9-Mediated Metabolism.

abstract：:The purpose of this work was to study the permeability of two relatively lipophilic sulfenamide prodrugs of linezolid (clogP 0.85), N-(phenylthio)linezolid (1, clogP 2.77) and N-[(2-ethoxycarbonyl)ethylthio]linezolid (2, clogP 1.43), across Caco-2 cell monolayers. Both prodrugs were found to convert to linezolid in th...

journal_title：Journal of pharmaceutical sciences

authors： Nti-Addae KW,Guarino VR,Dalwadi G,Stella VJ

更新日期：2012-09-01 00:00:00

abstract：:Health authorities require that suitable stability of the drug substance be shown in relevant materials of construction. ICH Q1A(R2) explicitly states that "stability studies should be conducted on drug substance packaged in a container closure system that is the same as or simulates the packaging proposed for storage...

journal_title：Journal of pharmaceutical sciences

authors： Klair N,Kim MT,Lee A,Xiao NJ,Patel AR

更新日期：2020-10-07 00:00:00

abstract：:The location and conformation of fosinopril sodium (FS) in a lamellar liquid crystal of water, sodium dodecyl sulfate, and decanol was studied by low-angle X-ray diffraction. The result showed the FS molecule to be located within the amphiphilic part of the liquid crystalline structure with the polar parts anchored at...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Moaddel T,Morris KR,Abramowitz R,Amsberry KL

更新日期：1994-05-01 00:00:00

abstract：:The purpose of this study was to investigate the phase-sensitive delivery systems (D,L-polylactide in triacetin) for controlled delivery of insulin at basal level. The effect of varying concentration of zinc, polymer, and insulin on the in vitro release of insulin was evaluated. Stability of released insulin was inves...

journal_title：Journal of pharmaceutical sciences

authors： Al-Tahami K,Oak M,Singh J

更新日期：2011-06-01 00:00:00

abstract：:A rapid and accurate method for the quantitative determination of the extent and ratio of amino and carboxyl group trimethylsilylation of 6-aminopenicillanic acid, 7-amino-3-methyl-delta3-cephem-4-carboxylic acid, and 7-amino-3-acetoxymethyl-delta3-cephem-4-carboxylic acid is presented. The method utilizes NMR spectro...

journal_title：Journal of pharmaceutical sciences

authors： Bortesi F,Cavalli S,Mangia A

更新日期：1977-12-01 00:00:00

abstract：:Methadyl acetate was metabolized by microsomal preparations of rat liver to yield nor-methadyl acetate and 6-(dimethylamino)-4,4-diphenyl-3-heptanol. The identification and separation of these three compounds was established by TLC, using iodoplatinate spray as a visualizing agent. ...

journal_title：Journal of pharmaceutical sciences

authors： Kochhar MM,Hamrick ME,Bavda LT

更新日期：1976-01-01 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：:Dissolving microneedle patches offer promise as a simple, minimally invasive method of drug and vaccine delivery to the skin that avoids the need for hypodermic needles. However, it can be difficult to control the amount and localization of drug within microneedles. In this study, we developed novel microneedle design...

journal_title：Journal of pharmaceutical sciences

authors： Chu LY,Choi SO,Prausnitz MR

更新日期：2010-10-01 00:00:00

abstract：:The objective of this study was to propose novel surface-modified nanostructured lipid carriers with partially deacetylated water-soluble chitosan (NLC-PDSC) as an efficient ocular delivery system to improve its transcorneal penetration and precorneal retention. PDSC with a deacetylation degree of around 50% was synth...

journal_title：Journal of pharmaceutical sciences

authors： Tian B,Luo Q,Song S,Liu D,Pan H,Zhang W,He L,Ma S,Yang X,Pan W

更新日期：2012-03-01 00:00:00

abstract：:Three dimensional terahertz pulsed imaging (TPI) was evaluated as a novel tool for the nondestructive characterization of different solid oral dosage forms. The time-domain reflection signal of coherent pulsed light in the far infrared was used to investigate film-coated tablets, sugar-coated tablets, multilayered con...

journal_title：Journal of pharmaceutical sciences

authors： Zeitler JA,Shen Y,Baker C,Taday PF,Pepper M,Rades T

更新日期：2007-02-01 00:00:00

abstract：:The objective of this study was to identify the important factors that determine plasma concentrations of diphenhydramine (DPHM) in the mother and the fetus after maternal as well as fetal steady-state drug administration. Inter-relationships were evaluated between maternal and fetal placental and nonplacental clearan...

journal_title：Journal of pharmaceutical sciences

authors： Kumar S,Tonn GR,Riggs KW,Rurak DW

更新日期：1999-12-01 00:00:00

abstract：:The plasma protein binding of drugs has been shown to have significant effects on the quantitative relationship between clinical pharmacokinetics and pharmacodynamics. In many clinical situations, measurement of the total drug concentration does not provide the needed information concerning the unbound fraction of dru...

journal_title：Journal of pharmaceutical sciences

authors： Musteata FM,Pawliszyn J,Qian MG,Wu JT,Miwa GT

更新日期：2006-08-01 00:00:00

abstract：:To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...

journal_title：Journal of pharmaceutical sciences

authors： Aso Y,Yoshioka S,Kojima S

更新日期：2001-06-01 00:00:00

abstract：:After having been used in treating HIV infection for a decade, zidovudine (AZT) continues to be an essential component of antiretroviral regimens. Because antiviral responses and toxicity of AZT seem to be related to cells in specific target tissues, being able to understand and predict the distribution of AZT into di...

journal_title：Journal of pharmaceutical sciences

authors： Chow HH

更新日期：1997-11-01 00:00:00

abstract：:The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid ch...

journal_title：Journal of pharmaceutical sciences

authors： Yamana T,Tsuji A

更新日期：1976-11-01 00:00:00

abstract：:Two novel series of steroidal derivatives containing various thiourea and substituted thiazoline moieties attached to the 2- or 4-position of estrone were synthesized and examined for in vitro effect on bovine pancreatic ribonuclease activity. All compounds studied exhibited a catabolic activity. The steroidal thiazol...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim ES,Omar AM,Habib NS,Aboulwafa OM,El-Sewedy SM,Bourdais J

更新日期：1983-10-01 00:00:00

abstract：:The α-keto carboxylic acid, pyruvic acid (1) was found to be a very effective peroxide scavenger but is subject to an aldol-like self-condensation/polymerization reaction. The purpose of this study was to evaluate the hydrogen peroxide, H2O2, scavenging ability of 3-methyl-2-oxobutanoic acid (2), 4-methyl-2-oxopentano...

journal_title：Journal of pharmaceutical sciences

authors： Lopalco A,Stella VJ

更新日期：2016-09-01 00:00:00

abstract：:Circular dichroism (CD) spectroscopy is routinely used in the biopharmaceutical industry to study the effects of manufacturing, formulation, and storage conditions on protein conformation and stability, and these results are often included in regulatory filings. In this context, the purpose of CD spectroscopy is often...

journal_title：Journal of pharmaceutical sciences

authors： Li CH,Nguyen X,Narhi L,Chemmalil L,Towers E,Muzammil S,Gabrielson J,Jiang Y

更新日期：2011-11-01 00:00:00

abstract：:Mixing Fungizone with a fat emulsion used for nutritional purpose (Intralipid or Lipofundin ) was reported to decrease Amphotericin B (AmB) toxicity in clinical use. In an effort to understand the reason for this phenomenon, spectral and morphological analyses were done for the Fungizone and Fungizone /Lipofundin admi...

journal_title：Journal of pharmaceutical sciences

authors： Egito ES,Araújo IB,Damasceno BP,Price JC

更新日期：2002-11-01 00:00:00

abstract：:Site I of human serum albumin is an important and complex region for high-affinity binding of drugs. Equilibrium dialysis showed independent binding of dansyl-L-asparagine (DNSA) and n-alkyl p-aminobenzoates (p-ABEs) to regions Ib and Ic, respectively, in the pH range 6.0-9.0. However, individual binding of DNSA incre...

journal_title：Journal of pharmaceutical sciences

authors： Yamasaki K,Maruyama T,Takadate A,Suenaga A,Kragh-Hansen U,Otagiri M

更新日期：2004-12-01 00:00:00

abstract：:Spectrophotometric assay for cycloserine based on the interaction of the drug with 9-methoxyacridine as a chromogenic agent is described. The highly colored substituted acridine product was identified as 9-(d-4-imino-3-isoxazolidinone)acridine. Color development was affected by time and temperature of heating and by t...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Yoo GS

更新日期：1988-05-01 00:00:00

abstract：:Two new methods for the simultaneous determination of chloroquine and its two main metabolites (monodesethylchloroquine and bisdesethylchloroquine) in biological samples, radioimmunoassay (RIA) and enzyme-linked immunosorbent assay (ELISA), are described. Antiserum is produced in rabbits immunized with N-(2-carboxyeth...

journal_title：Journal of pharmaceutical sciences

authors： Escande C,Chevalier P,Verdier F,Bourdon R

更新日期：1990-01-01 00:00:00

abstract：:A method for the measurement, in human plasma, of all tertiary and secondary tricyclic antidepressants prescribed in the United States is described. The method uses electron beam ionization GLC-mass spectrometry, employing a computer-controlled multiple-ion detector. This method, mass fragmentography, is used with int...

journal_title：Journal of pharmaceutical sciences

authors： Biggs JT,Holland WH,Chang S,Hipps PP,Sherman WR

更新日期：1976-02-01 00:00:00

abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

journal_title：Journal of pharmaceutical sciences

authors： Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

更新日期：2018-07-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:Previous studies have shown that protein storage stability in freeze-dried l-arginine-based systems improved in the presence of chloride ions. However, chloride ions reduced the glass transition temperature of the freeze concentrate (Tg') and made freeze drying more challenging. In this study, l-arginine was freeze dr...

journal_title：Journal of pharmaceutical sciences

authors： Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach P

更新日期：2016-10-01 00:00:00

abstract：:The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

更新日期：1992-02-01 00:00:00

abstract：:(+-)-Carbovir [(+-)-9-[4 alpha-(hydroxymethyl)-cyclopent-2-ene-1 alpha-yl]guanine; NSC 614846] is a novel carbocyclic nucleoside analogue which has been shown to be a potent and selective inhibitor of HIV in vitro. As part of an effort to develop a parenteral formulation for subsequent clinical and toxicological evalu...

journal_title：Journal of pharmaceutical sciences

authors： Anderson BD,Chiang CY

更新日期：1990-09-01 00:00:00

abstract：:The release of potassium chloride from hydroxypropyl methylcellulose matrices was investigated for tablets prepared with several different compression forces. It was determined that the release kinetics for these systems deviates significantly from the classical t1/2 dependence. This behavior was attributed to air ent...

journal_title：Journal of pharmaceutical sciences

authors： Korsmeyer RW,Gurny R,Doelker E,Buri P,Peppas NA

更新日期：1983-10-01 00:00:00

abstract：:Vaults, at 13 MDa, are the largest ribonucleoprotein particles known. In vitro, expression of the major vault protein (MVP) alone in Sf9 insect cells results in the production of recombinant particles with characteristic vault structure. With the ultimate goal of using recombinant vaults as nanocapsules for the delive...

journal_title：Journal of pharmaceutical sciences

authors： Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

更新日期：2009-04-01 00:00:00