Analysis and prediction of partition coefficients of meta- and para-disubstituted benzenes in terms of substituent effects.

abstract：:The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg 2 or 3 times daily and to evaluate the dosing regimens by using Monte-Carlo p...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo Y,Ishibashi T,Matsumoto S,Katsube T,Wajima T

更新日期：2019-09-01 00:00:00

abstract：:A previous report detailed the derivation and validation of an equation for calculating the Gibbs free energy of liquid-solid adsorption via high-performance liquid chromatography (HPLC). This study utilizes an improved form of that equation in conjunction with an in vitro model of solute adsorption to give an ordered...

journal_title：Journal of pharmaceutical sciences

authors： Kleeman WP,Bailey LC

更新日期：1988-06-01 00:00:00

abstract：:Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

journal_title：Journal of pharmaceutical sciences

authors： Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

更新日期：1976-03-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 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：:The estimates of infinity values obtained using Prony's method are shown to be subject to significant error arising from small errors in the assigned sample times. The error of the estimate may be reduced by increasing the time interval between samples. ...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Stavchansky S,Pearlman RS

更新日期：1980-10-01 00:00:00

abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...

journal_title：Journal of pharmaceutical sciences

authors： Lakhani NJ,Sparreboom A,Xu X,Veenstra TD,Venitz J,Dahut WL,Figg WD

更新日期：2007-07-01 00:00:00

abstract：:Compact strength and the particle-size distribution of milled roller compacted compacts were correlated to the slope of the best-fit line through near-infrared spectra for samples prepared under different roll speeds and feed rates. The above correlations were found to hold for compacts prepared from microcrystalline ...

journal_title：Journal of pharmaceutical sciences

authors： Gupta A,Peck GE,Miller RW,Morris KR

更新日期：2004-04-01 00:00:00

abstract：:Solvent-induced 3 frameworks (the monohydrate, methanol solvate, and dimethyl formamide [DMF] solvate) of an anticancer drug, 7-ethyl-10-hydroxycamptothecin (SN38), were constructed. The crystal structures of the 3 pseudopolymorphs were characterized by single-crystal X-ray diffraction technique for the first time. Cr...

journal_title：Journal of pharmaceutical sciences

authors： Fang L,Wang L,Yao C,Song S,Wu Z,Tao X

更新日期：2017-10-01 00:00:00

abstract：:Microparticles are of considerable interest for drug delivery, vaccination and diagnostic imaging. In order to obtain microparticles with long circulation times, or to provide the prerequisite for tissue specific targeting through decoration with suitable ligands, their surfaces need to be modified such that they beco...

journal_title：Journal of pharmaceutical sciences

authors： Wattendorf U,Merkle HP

更新日期：2008-11-01 00:00:00

abstract：:The effects of the granule size and density on the drying rate kinetics of tablet granulations were studied using lactose and sulfathiazole granules prepared with acacia mucilage and providone solution. The drying rate kinetics consisted of three distinct phases of drying when the drying rate was platted against remai...

journal_title：Journal of pharmaceutical sciences

authors： Opankunle WO,Bhutani BR,Bhatia VN

更新日期：1975-06-01 00:00:00

abstract：:Maintaining good content uniformity (CU) is a significant challenge for low-dose oral tablets in particular when using direct compression (DC). Using 6 model active pharmaceutical ingredients, we show that a platform DC tablet formulation suitable for developing low-dose API with excellent CU can be developed. This pl...

journal_title：Journal of pharmaceutical sciences

authors： Sun WJ,Aburub A,Sun CC

更新日期：2017-07-01 00:00:00

abstract：:A physically based method for arriving at topological indexes is described. The derived indexes correlate with molecular surface areas and with the molecular connectivity index. The newly derived index seems to account better for the expected distinctions among primary, secondary, and tertiary alcohol aqueous solubili...

journal_title：Journal of pharmaceutical sciences

authors： Cammarata A

更新日期：1979-07-01 00:00:00

abstract：:Different approaches for the colorimetric determination of acetaminophen, based on its coupling with diazotized o-nitroaniline, are described. Copper(II) chelation with the coupled compound makes the method highly selective. Sensitivity is increased when the acetaminophen assay is carried out indirectly through the de...

journal_title：Journal of pharmaceutical sciences

authors： Belal S,Elsayed MA,El-Waliely A,Abdine H

更新日期：1979-06-01 00:00:00

abstract：:Condensations of carbon disulfide were carried out with amino, chloro, and diamino heterocycles to give condensed ring thiazoline-2-thiones and imidazoline-2-thiones, with cyanomethyl heterocycles to give dithio acid derivatives, and with heterocyclic sulfonamides to give sulfonyldithiocarbamates. Of several examples ...

journal_title：Journal of pharmaceutical sciences

authors： Foye WO,Kauffman JM,Lanzillo JJ,LaSala EF

更新日期：1975-08-01 00:00:00

abstract：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...

journal_title：Journal of pharmaceutical sciences

authors： Acree WE Jr,McHan DR,Rytting JH

更新日期：1983-08-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 00:00:00

abstract：:Simple and sensitive enzyme immunoassays (EIAs), discriminating a new angiotensin-converting enzyme (ACE) inhibitor, cilazapril [9(s) - [1(s)-(ethoxycarbonyl)-3-phenylpropylamino]-octahydro-10-oxo-6H- pyridazo[1,2-a] [1,2]diazepine-1(s)carboxylic acid] and its active metabolite [9(s)-[1(s)-carboxy-3-phenylpropylamino]...

journal_title：Journal of pharmaceutical sciences

authors： Tanaka H,Yoneyama Y,Sugawara M,Umeda I,Ohta Y

更新日期：1987-03-01 00:00:00

abstract：:An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...

journal_title：Journal of pharmaceutical sciences

authors： Severin G

更新日期：1987-03-01 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：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:Two human bioavailability studies were conducted to assess the in vivo performances of recently marketed 200-, 300-, and 400-mg ibuprofen capsules relative to the innovator's 300- and 400-mg tablets when administered as single oral 300- or 400-mg doses. An ibuprofen oral solution was also administered in each trial. W...

journal_title：Journal of pharmaceutical sciences

authors： Gillespie WR,DiSanto AR,Monovich RE,Albert KS

更新日期：1982-09-01 00:00:00

abstract：:Nosocomial diarrhea and pseudomembranous colitis causing toxins A and B from Clostridium difficile were studied at pH 5-8 and over the temperature range of 10-85 degrees C. The proteins were crosslinked with formaldehyde to inactivate them to toxoid forms and permit their use as vaccines. Structural changes and aggreg...

journal_title：Journal of pharmaceutical sciences

authors： Salnikova MS,Joshi SB,Rytting JH,Warny M,Middaugh CR

更新日期：2008-09-01 00:00:00

abstract：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00

abstract：:The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

journal_title：Journal of pharmaceutical sciences

authors： Halasz I,Dinnebier RE

更新日期：2010-02-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 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：:A number of biopharmaceuticals are available as lyophilized formulations along with a prefilled syringe (PFS) containing water for injection (WFI). Submicron- and micron-size droplets of lubricating silicone oil (SO) applied to the inner surface of the PFS barrel might migrate into the WFI, to which protein pharmaceut...

journal_title：Journal of pharmaceutical sciences

authors： Krayukhina E,Yokoyama M,Hayashihara KK,Maruno T,Noda M,Watanabe H,Uchihashi T,Uchiyama S

更新日期：2019-07-01 00:00:00

abstract：:The purpose of this paper was to investigate the relaxation behavior of amorphous hesperetin (HRN), using dielectric spectroscopy, and assessment of its crystallization kinetics above glass transition temperature (Tg ). Amorphous HRN exhibited both local (β-) and global (α-) relaxations. β-Relaxation was observed belo...

journal_title：Journal of pharmaceutical sciences

authors： Shete G,Khomane KS,Bansal AK

更新日期：2014-01-01 00:00:00

abstract：:In this paper, we establish a mechanistic model for the prediction of amorphous solid dispersion (ASD) stability. The novel approach incorporates fundamental physical parameters, principally supersaturation, diffusivity, and interfacial energy, to model crystallization in ASDs accounting for both kinetic and thermodyn...

journal_title：Journal of pharmaceutical sciences

authors： Ojo AT,Lee PI

更新日期：2020-08-18 00:00:00