Thermodynamic Estimate of the Number of Solvent Molecules Displaced by a Solute Molecule for Enthalpy-Driven Adsorption: Phenobarbital and Activated Carbons as the Model System.

abstract：:A mathematical model based on convective diffusion was developed to describe the rate of dissolution form the surface of a compressed compact. Experimental studies were carried out to test the model. The basic experimental apparatus consisted of a modified rotating-filter-stationary basket dissolution test apparatus. ...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Shah AC

更新日期：1975-04-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:Clinical lots of recombinant human platelet-activating factor acetylhydrolase (rhPAF-AH) were prepared in a lyophilized formulation. After reconstitution with sterile water for injection to form an aqueous solution (10 mM sodium citrate, 7.5 w/v% sucrose, and 0.1 w/v% Pluronic-F68, pH 6.5), a few visible, slowly growi...

journal_title：Journal of pharmaceutical sciences

authors： Chi EY,Weickmann J,Carpenter JF,Manning MC,Randolph TW

更新日期：2005-02-01 00:00:00

abstract：:A series of substituted 3-(benzylideneamino) coumarins was synthesized and evaluated for anti-inflammatory activity against carrageenan-induced edema in rats. Halogenated derivatives 4g and 4c, at oral doses of 100 mg/kg, showed 75 and 60% antiedmatous activity, respectively (phenylbutazone antiedematous activity, 58%...

journal_title：Journal of pharmaceutical sciences

authors： Maddi V,Raghu KS,Rao MN

更新日期：1992-09-01 00:00:00

abstract：:Alkyl esters of ketorolac were synthesized as potential prodrugs for transdermal delivery and evaluated to determine the relationship between their skin permeation characteristics and their physicochemical properties. Solubility of the prodrugs in various vehicles was determined at room temperature while lipophilicity...

journal_title：Journal of pharmaceutical sciences

authors： Doh HJ,Cho WJ,Yong CS,Choi HG,Kim JS,Lee CH,Kim DD

更新日期：2003-05-01 00:00:00

abstract：:Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

journal_title：Journal of pharmaceutical sciences

authors： Loftsson T,Bodor N

更新日期：1981-07-01 00:00:00

abstract：:The concept of cosolvent exclusion was developed by a group of Timasheff's laboratory in 1970-1990 and is currently used widely to explain the effects of a variety of cosolvents on the stability and solubility of macromolecules. Not surprisingly, these concepts have had substantial influence in the fields of formulati...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Gagnon P

更新日期：2018-09-01 00:00:00

abstract：:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It ...

journal_title：Journal of pharmaceutical sciences

authors： Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf H

更新日期：1996-04-01 00:00:00

abstract：:Glasses were prepared from a number of barbiturates. The viscosities and glass transition temperatures of the glasses were dependent on the structure of the groups present on the C-5 and N-1 atoms. Solid dispersions were prepared from three selected barbiturates formulated with citric acid. The glass transition temper...

journal_title：Journal of pharmaceutical sciences

authors： Summers MP

更新日期：1978-11-01 00:00:00

abstract：:The placental and nonplacental clearances of metoclopramide were studied in nine chronically instrumented, near-term pregnant sheep using a two-compartment open model. Metoclopramide was administered to the ewe and fetus on separate occasions as an initial iv bolus loading dose followed by a constant-rate infusion, wi...

journal_title：Journal of pharmaceutical sciences

authors： Riggs KW,Rurak DW,Taylor SM,McErlane BA,McMorland GH,Axelson JE

更新日期：1990-12-01 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：:Uncharged, lipophilic, low molecular weight copper complexes labeled with generator-produced copper-62 are of interest as potential radiopharmaceutials for imaging the brain with positron emission tomography (PET). We report here the synthesis and biodistribution of a series of [67Cu]copper(II) complexes with tetraden...

journal_title：Journal of pharmaceutical sciences

authors： John EK,Bott AJ,Green MA

更新日期：1994-04-01 00:00:00

abstract：:Patients with burn wounds are susceptible to wound infection and sepsis. This research introduces a novel burn wound dressing that contains silver nanoparticles (SNPs) to treat infection in a 2-acrylamido-2-methylpropane sulfonic acid sodium salt (AMPS-Na(+) ) hydrogel. Silver nitrate was dissolved in AMPS-Na(+) solut...

journal_title：Journal of pharmaceutical sciences

authors： Boonkaew B,Barber PM,Rengpipat S,Supaphol P,Kempf M,He J,John VT,Cuttle L

更新日期：2014-10-01 00:00:00

abstract：:Because the ionized species is more polar than its un-ionized counterpart, it is often assumed that the ionized species of the drug does not make a meaningful contribution to solubilization by either cosolvents or surfactants. This report extends previous studies on solubilization of the ionic species by a combination...

journal_title：Journal of pharmaceutical sciences

authors： Li P,Tabibi SE,Yalkowsky SH

更新日期：1999-05-01 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：:Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

journal_title：Journal of pharmaceutical sciences

authors： Banerjee PK,Amidon GL

更新日期：1981-12-01 00:00:00

abstract：:Injectable microcapsules containing 75% (w/w) cyclazocine, a narcotic antagonist, were prepared with dl-poly(lactic acid) as the coating material. Capsule fractions falling between 105 and 295 mum released about 90% of their cyclazocine in 8 days of rotating-bottle extraction at 37 degrees in pH 7.4 phosphate buffer. ...

journal_title：Journal of pharmaceutical sciences

authors： Mason N,Thies C,Cicero TJ

更新日期：1976-06-01 00:00:00

abstract：:Each of three harmala alkaloids, harmine, harmaline, and harmalol, decreased heart rate and increased pulse pressure, peak aortic flow, and myocardial contractile force in intact normotensive anesthetized dogs. Harmine reduced systemic arterial blood pressure and total peripheral vascular resistance; harmaline-evoked ...

journal_title：Journal of pharmaceutical sciences

authors： Aarons DH,Rossi GV,Orzechowski RF

更新日期：1977-09-01 00:00:00

abstract：:Ketoconazole (KTZ) has 2 chiral centers with the therapeutically active form being a racemic mixture of 2 cis-enantiomers, namely, (2R,4S)-(+)-KTZ and (2S,4R)-(-)-KTZ. The aims of the present study were to examine the effects of (+)-KTZ, (-)-KTZ, and (±)-KTZ on aryl hydrocarbon receptor activation and subsequently CYP...

journal_title：Journal of pharmaceutical sciences

authors： Anwar-Mohamed A,El-Sherbeni AA,Hamdy DA,Korashy HM,Brocks DR,El-Kadi AO

更新日期：2016-03-01 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：:The pharmacokinetics of atropine in three healthy male volunteers after intravenous administration of 1.35 and 2.15 mg of the drug was determined. Pharmacodynamic effects of atropine were measured simultaneously. All the data were fitted to a novel integrated kinetic-dynamic model. Plasma concentrations of atropine an...

journal_title：Journal of pharmaceutical sciences

authors： Hinderling PH,Gundert-Remy U,Schmidlin O

更新日期：1985-07-01 00:00:00

abstract：:Responses from the second Product Quality Research Institute (PQRI) Blend Uniformity Working Group (BUWG) survey of industry have been reanalyzed to identify potential links between formulation and processing variables and the measured uniformity of blends and unit dosage forms. As expected, the variability of the ble...

journal_title：Journal of pharmaceutical sciences

authors： Hancock BC,Garcia-Munoz S

更新日期：2013-03-01 00:00:00

abstract：:Minitablets are an appealing option for an age-appropriate pediatric dosage form. In particular, for combination therapies where multiple active ingredients are dosed simultaneously, the use of minitablets will enable independent adjustments of each dose. The work presented describes the development of Compound A and ...

journal_title：Journal of pharmaceutical sciences

authors： Zhang D,Rumondor ACF,Zhu W,Colace T,Marota M,Mora J,Liu Z,Li Y

更新日期：2020-12-01 00:00:00

abstract：:The degradation kinetics of phentolamine hydrochloride in aqueous solution over a pH range of 1.2 to 7.2 and its stability in propylene glycol- or polyethylene glycol 400-based solutions were investigated. The observed rate constants were shown to follow apparent first-order kinetics in all cases. The pKa determinatio...

journal_title：Journal of pharmaceutical sciences

authors： Wang DP,Tu YH,Allen LV Jr

更新日期：1988-11-01 00:00:00

abstract：:Antisense phosphorodiamidate Morpholino oligomers (PMO) are resistant to degradation by cellular hydrolases, DNases, RNases, and phosphodiesterases, but remain sensitive to prolonged exposure to low pH. The present studies evaluate the oral fractional bioavailability, stability, and efficacy of two distinct PMO sequen...

journal_title：Journal of pharmaceutical sciences

authors： Arora V,Knapp DC,Reddy MT,Weller DD,Iversen PL

更新日期：2002-04-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:The synthesis, hydrolysis rate, and bioavailability of 1-(p-acetaminophenoxy)-1-ethoxyethane, an acetaminophen prodrug, are described. The prodrug is less soluble than acetaminophen and stable at neutral pH. However, in an acidic environment, the compound cleaves rapidly, generating acetaminophen. When both the prodru...

journal_title：Journal of pharmaceutical sciences

authors： Hussain A,Kulkarni P,Perrier D

更新日期：1978-04-01 00:00:00

abstract：:Protein immunogenicity is intensively researched by academics, biopharmaceutical companies, and authorities as it can compromise the safety and efficacy of a biopharmaceutical drug. So far, the exact protein aggregate properties inducing immune responses are not known. Possible protein-related factors could be size, c...

journal_title：Journal of pharmaceutical sciences

authors： Werner BP,Winter G

更新日期：2018-11-01 00:00:00

abstract：:Upon exposure to shaking stress, an IgG1 mAb formulation in both the liquid and lyophilized state formed subvisible particles. Because freeze-drying was expected to minimize protein physical instability under these conditions, the extent and nature of aggregate formation in the lyophilized preparation were examined us...

journal_title：Journal of pharmaceutical sciences

authors： Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

更新日期：2015-02-01 00:00:00

abstract：:The objective of this study was to establish the optimal blood concentrations of the potent P-glycoprotein (P-gp) inhibitor GF120918 (Elacridar) required to achieve maximal knockout of this efflux transporter in the blood-brain barrier (BBB) of mice, rats, and guinea pigs. Genetic mdr1a/b(-/-) knockout mice and "chemi...

journal_title：Journal of pharmaceutical sciences

authors： Cutler L,Howes C,Deeks NJ,Buck TL,Jeffrey P

更新日期：2006-09-01 00:00:00