N-hydroxymethyl derivatives of nitrogen heterocycles as possible prodrugs II: possible prodrugs of allopurinol, glutethimide, and phenobarbital.

abstract：:The dependency of metformin in vivo disposition on the rate and extent of dissolution was studied. The analysis includes the use of fundamental principles of drug input, permeability, and intestinal transit time within the framework of a compartmental absorption transit model to predict key pharmacokinetic (PK) parame...

journal_title：Journal of pharmaceutical sciences

authors： Crison JR,Timmins P,Keung A,Upreti VV,Boulton DW,Scheer BJ

更新日期：2012-05-01 00:00:00

abstract：:A spectrophotofluorometric assay for coralyne sulfoacetate was developed. Caralyne was extracted from serum samples with n-butyl alcohol, and the drug concentrations were determined fluorometrically at 475 nm when the extract was excited at 325 nm. A biphasic serum decay curve for coralyne was observed for both dogs a...

journal_title：Journal of pharmaceutical sciences

authors： Finkel JM,Hill DL

更新日期：1978-09-01 00:00:00

abstract：:The pre-equilibrium capillary zone electrophoretic (pre-eq CZE) method to determine association constants of active anionic forms of antithyroid drugs: 6-n-propyl-2-thiouracil (PTU), 6-methyl-2-thiouracil (MTU), 2-thiouracil (TU) with bovine serum albumin (BSA) under physiological pH 7.4 has been developed for the fir...

journal_title：Journal of pharmaceutical sciences

authors： Chernov'yants MS,Dolinkin AO,Chernyshev AV,Khohlov EV,Golovanova EG

更新日期：2010-03-01 00:00:00

abstract：:Crystallization of polymorphs still has a touch of art, as even prior observations of polymorphs do not guarantee their crystallization. However, once crystals of various polymorphs have been obtained, their relative stabilities can be established with a straightforward thermodynamic approach even if the conclusion wi...

journal_title：Journal of pharmaceutical sciences

authors： Rietveld IB,Céolin R

更新日期：2015-12-01 00:00:00

abstract：:The synthesis of the diethyl analog of neostigmine, its preliminary pharmacology, and its use as an internal standard for the GLC assay of neostigmine are described. Both the diethyl analog and neostigmine undergo thermal demethylation in the injection port. The column selected produced satisfactory resolution and sho...

journal_title：Journal of pharmaceutical sciences

authors： Ward HE Jr,Freeman JJ,Sowell JW,Kosh JW

更新日期：1981-04-01 00:00:00

abstract：:The particle sizing performance of a Next Generation Pharmaceutical Impactor (NGI) was compared to that of an Andersen cascade impactor (ACI). A single lot of Vanceril MDIs containing beclomethasone dipropionate (BDP) was used throughout. MDIs were sampled into NGI and ACI in accordance with USP recommendations, at 30...

journal_title：Journal of pharmaceutical sciences

authors： Kamiya A,Sakagami M,Hindle M,Byron PR

更新日期：2004-07-01 00:00:00

abstract：:The chemical stability of the novel anticancer agent carzelesin in aqueous buffer/acetonitrile (1:1, v/v) mixtures has been investigated utilizing a stability-indicating reversed-phase high-performance liquid chromatographic assay. The degradation kinetics of carzelesin has been studied as a function of pH, buffer com...

journal_title：Journal of pharmaceutical sciences

authors： Vries JD,Doppenberg WG,Henrar RE,Bult A,Beijnen JH

更新日期：1996-11-01 00:00:00

abstract：:The equilibrium kinetics of triazolam in aqueous solution was investigated in the pH range of 1-11 at body temperature. The quantitative study indicated that it forms equilibrium mixtures consisting of ring-opened and closed forms with the composition being dependent on pH. The equilibrium constants of the two species...

journal_title：Journal of pharmaceutical sciences

authors： Konishi M,Hirai K,Mori Y

更新日期：1982-12-01 00:00:00

abstract：:A column-switching high-performance liquid chromatographic assay combined with a heart-cutting technique and UV detection (LC/LC/UV) was developed to determine ceftibuten, a new oral cephalosporin, in human plasma. Plasma samples were directly injected into the first chromatographic column for sample cleanup and extra...

journal_title：Journal of pharmaceutical sciences

authors： Pan HT,Kumari P,Lim J,Lin CC

更新日期：1992-07-01 00:00:00

abstract：:With the introduction of Quality by Design (QbD) to the pharmaceutical industry, there has been an increased focus on understanding the nature of particles and composites, with the aim of understanding and modeling how they interact in complex systems, leading to robust dosage forms. Particle characterization tools ha...

journal_title：Journal of pharmaceutical sciences

authors： Gamble JF,Tobyn M,Hamey R

更新日期：2015-05-01 00:00:00

abstract：:Both nonequilibrium and equilibrium models were proposed to explain the optimal biological response to a set of congeners with respect to the oil-water partition coefficient (P). A detailed analysis of the kinetic model proposed by Hansch demonstrates the bilinear form of the model, with the initial slope of the logar...

journal_title：Journal of pharmaceutical sciences

authors： Cooper ER,Berner B,Bruce RD

更新日期：1981-01-01 00:00:00

abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...

journal_title：Journal of pharmaceutical sciences

authors： Jasti BR,Berner B,Zhou SL,Li X

更新日期：2004-08-01 00:00:00

abstract：:Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...

journal_title：Journal of pharmaceutical sciences

authors： MacIntyre AC,Cutler DJ

更新日期：1986-11-01 00:00:00

abstract：:Iontophoretic transdermal delivery of sumatriptan was investigated in vitro. Among the conditions tested, 0.25 mA/cm2 and low ionic strength (NaCl 25 mM) was the best experimental condition to increase its transport across the skin. The flux increased 385-fold respective to passive diffusion, thus resulting in a trans...

journal_title：Journal of pharmaceutical sciences

authors： Femenía-Font A,Balaguer-Fernández C,Merino V,López-Castellano A

更新日期：2005-10-01 00:00:00

abstract：:Historically, recovery had been used to evaluate the data quality of plasma protein binding or tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative of high nonspecific binding, instability, or low solubility. This study showed that, when equilibrium was fully established in the d...

journal_title：Journal of pharmaceutical sciences

authors： Di L,Umland JP,Trapa PE,Maurer TS

更新日期：2012-03-01 00:00:00

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 00:00:00

abstract：:Polymethyl [1-14C]methacrylate nanoparticles were administered orally to bile cannulated rats. Ten to fifteen percent of the administered radioactivity was absorbed and found in the bile and urine. Within 48 h, 94-97% of the absorbed radioactivity had been eliminated from the body. After 8 d, the highest residual radi...

journal_title：Journal of pharmaceutical sciences

authors： Nefzger M,Kreuter J,Voges R,Liehl E,Czok R

更新日期：1984-09-01 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：:Jet-milling as the common way for micronization of drugs shows several disadvantages. Drug powder properties are decisive for pulmonary use because, besides a small particle size, a good deagglomeration behavior is required. In this study, several anti-inflammatory drugs [beclomethasone-17,21-dipropionate (BDP), betam...

journal_title：Journal of pharmaceutical sciences

authors： Rasenack N,Steckel H,Müller BW

更新日期：2003-01-01 00:00:00

abstract：:Evaluation of a multiplexed capillary electrophoresis (CE) method for pK(a) measurements of organic compounds, including low solubility compounds, is presented. The method is validated on a set of 105 diverse compounds, mostly drugs, and results are compared to literature values obtained from multiple references. Two ...

journal_title：Journal of pharmaceutical sciences

authors： Shalaeva M,Kenseth J,Lombardo F,Bastin A

更新日期：2008-07-01 00:00:00

abstract：:Free radical polymerization converts aqueous solutions of methacrylated inulin into cross-linked hydrogels. The purpose of this work was to study the hydrogel formation and to characterize the fully cured hydrogels. The gelation process of aqueous solutions of methacrylated inulin was monitored as a function of time b...

journal_title：Journal of pharmaceutical sciences

authors： Vervoort L,Vinckier I,Moldenaers P,Van den Mooter G,Augustijns P,Kinget R

更新日期：1999-02-01 00:00:00

abstract：:Synthetic peptides corresponding to the variable tandem repeat domain of the cancer-associated antigen MUC1 mucin are candidates for cancer vaccines. In our investigation mice were immunized via subcutaneous injection with poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres containing a MUC1 mucin peptide. It was hy...

journal_title：Journal of pharmaceutical sciences

authors： Newman KD,Sosnowski DL,Kwon GS,Samuel J

更新日期：1998-11-01 00:00:00

abstract：:SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 receptor. Ivermectin has shown antiviral activity by inhibiting the formation of the importin-α (IMPα) and IMPβ1 subunits as well as dissociating the IMPα/β1 heterodimer and has in vitro efficacy agains...

journal_title：Journal of pharmaceutical sciences

authors： Jermain B,Hanafin PO,Cao Y,Lifschitz A,Lanusse C,Rao GG

更新日期：2020-12-01 00:00:00

abstract：:The aim of this study was to investigate the effect of divalent metal ions (Ca, Mg(2+) , and Zn(2+) ) on the stability of oxytocin in aspartate buffer (pH 4.5) and to determine their interaction with the peptide in aqueous solution. Reversed-phase high-performance liquid chromatography and high-performance size-exclus...

journal_title：Journal of pharmaceutical sciences

authors： Avanti C,Hinrichs WLJ,Casini A,Eissens AC,Van Dam A,Kedrov A,Driessen AJM,Frijlink HW,Permentier HP

更新日期：2013-06-01 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：:Our objective was to characterize, by DSC and XRD, the equilibrium thermal behavior of frozen aqueous solutions containing polyethylene glycol (PEG) and sucrose. Aqueous solutions of (i) PEG (2.5-50% w/w), (ii) sucrose (10% w/v) with different concentrations of PEG (1-20% w/v), and (iii) PEG (2% or 10% w/v) with diffe...

journal_title：Journal of pharmaceutical sciences

authors： Bhatnagar BS,Martin SM,Teagarden DL,Shalaev EY,Suryanarayanan R

更新日期：2010-11-01 00:00:00

abstract：:Successful development of stable solid protein formulations usually requires the addition of one or several excipients to achieve optimal stability. In these products, there is a potential risk of an inhomogeneous distribution of the various ingredients, specifically the ratio of protein and stabilizer may vary. Such ...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen KTT,Frijlink HW,Hinrichs WLJ

更新日期：2020-01-01 00:00:00

abstract：:As part of a study to examine cocaine disposition and interaction with ethanol, it was necessary to characterize various properties of cocaine in the blood of the experimental animal. All studies were conducted using blood from healthy adult male Sprague-Dawley rats. Cocaine was incubated in whole blood at 37 degrees ...

journal_title：Journal of pharmaceutical sciences

authors： Sukbuntherng J,Martin DK,Pak Y,Mayersohn M

更新日期：1996-06-01 00:00:00

abstract：:A pharmacokinetic model was developed describing the pharmacokinetics of stannous fluoride in human subjects after oral topical application of a stannous fluoride dentifrice. Twenty subjects participated in an investigation of an experimental dentifrice. Subjects rinsed their mouths with the experimental dentifrice sl...

journal_title：Journal of pharmaceutical sciences

authors： Scott DC,Coggan JW,Cruze CA,He T,Johnson RD

更新日期：2009-10-01 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