Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier.

abstract：:The progress in continuous downstream manufacturing of oral solid doses demands effective real-time process management, with monitoring at its core. This study evaluates the feasibility of using a commercial sensor to measure the mass flow rate of the particulates, a critical process variable in continuous manufacturi...

journal_title：Journal of pharmaceutical sciences

authors： Ganesh S,Troscinski R,Schmall N,Lim J,Nagy Z,Reklaitis G

更新日期：2017-12-01 00:00:00

abstract：:Some fused pyridazino[4,5-b]indoles (7) were synthesized. These new compounds present a planar topography and some resemblance to carbazeram, imadozan, and other pyridazino agents with cardiotonic activity. These compounds also possess a complementary effect as inhibitors of platelet aggregation. 6-(3,5-Dimethylpyrazo...

journal_title：Journal of pharmaceutical sciences

authors： Monge A,Aldana I,Losa MJ,Font M,Castiella E,Frechilla D,Cenarruzabeitia E,Martinez de Irujo JJ,Lopez-Unzu J,Alberdi E

更新日期：1993-05-01 00:00:00

abstract：:The concentrations of antipyrine in plasma and saliva were equivalent in normal volunteers and in patients with acute viral hepatitis following oral doses of antipyrine. Estimates of clearance, volume of distribution, and half-life made from either plasma or saliva samples were not statistically different in these sub...

journal_title：Journal of pharmaceutical sciences

authors： Meffin PJ,Williams RL,Blaschke TF,Rowland M

更新日期：1977-01-01 00:00:00

abstract：:The solubility of a series of compounds was determined in a wide polarity spectrum of normal aliphatic alcohols over a limited temperature range. The solutes chosen were the methyl through n-butyl p-hydroxybenzoates, several of these being useful preservatives. Solubility profiles were determined for these compounds, ...

journal_title：Journal of pharmaceutical sciences

authors： Alexander KS,Mauger JW,Petersen H Jr,Paruta AN

更新日期：1977-01-01 00:00:00

abstract：:In this contribution, we present an analysis of the main parameters influencing the efficiency of the (1)H → (13)C multiple-contact cross-polarization nuclear magnetic resonance (NMR) experiment in the context of solid pharmaceutical materials. Using the optimum experimental conditions, quantitative (13)C NMR spectra ...

journal_title：Journal of pharmaceutical sciences

authors： Saïdi F,Taulelle F,Martineau C

更新日期：2016-08-01 00:00:00

abstract：:Meglumine labeled with carbon-14 was administered orally as 14C-meglumine salicylate to rats and dogs to study its distribution and excretion. The compound was incompletely absorbed; that which was absorbed was rapidly excreted in the urine. Peak blood levels were about 5-10 mug/ml in rats and 2-8 mug/ml in dogs. Tiss...

journal_title：Journal of pharmaceutical sciences

authors： Heeg JF,Born GS,Kessler WV,Shaw SM,Lange WE

更新日期：1977-01-01 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：:Partial molal volumes (Vi infinity) of physostigmine, ranging from 232.9 to 239.8 cm3.mol-1, and its mole fraction solubilities (Xi), ranging from 0.051 to 0.009, were determined at 25 degrees C in solutions of isopropanol (IPA), isopropyl myristate (IPM), and their mixtures. An inverse relation was found between Vi i...

journal_title：Journal of pharmaceutical sciences

authors： Pardo A,Shiri Y,Cohen S

更新日期：1991-06-01 00:00:00

abstract：:A sensitive high-performance liquid chromatographic (HPLC) assay for N-acetylcysteine in human plasma and urine has been developed. The method employs a prechromatographic stage to produce the dinitrophenyl derivative of N-acetylcysteine, which is chromatographed on a 5-microns C18 bonded reverse-phase column using an...

journal_title：Journal of pharmaceutical sciences

authors： Lewis PA,Woodward AJ,Maddock J

更新日期：1984-07-01 00:00:00

abstract：:Thiamine hydrochloride (Vitamin B(1), THCl) can exist as a nonstoichiometric hydrate (NSH) and as a hemihydrate (HH). NSH can contain up to approximately 1 molar equivalent of water and be dehydrated to an isomorphic desolvate (ID) with minimal change in lattice structure. Crystallographic and spectroscopic techniques...

journal_title：Journal of pharmaceutical sciences

authors： Chakravarty P,Berendt RT,Munson EJ,Young VG Jr,Govindarajan R,Suryanarayanan R

更新日期：2010-02-01 00:00:00

abstract：:Review of the current literature on racial differences in pharmacokinetics of drugs supports the premise that only pharmacokinetic processes which are biologically or biochemically mediated have the potential to exhibit differences between racial or ethnic groups. Thus, the pharmacokinetic factors which can be expecte...

journal_title：Journal of pharmaceutical sciences

authors： Johnson JA

更新日期：1997-12-01 00:00:00

abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

journal_title：Journal of pharmaceutical sciences

authors： Rayfield WJ,Kandula S,Khan H,Tugcu N

更新日期：2017-08-01 00:00:00

abstract：:The present work employs recent advances in high-resolution real-time magnetic resonance imaging (MRI) to investigate the disintegration process of tablets containing disintegrants. A temporal resolution of 75 ms and a spatial resolution of 80 × 80 µm with a section thickness of only 600 µm were achieved. The histogra...

journal_title：Journal of pharmaceutical sciences

authors： Quodbach J,Moussavi A,Tammer R,Frahm J,Kleinebudde P

更新日期：2014-01-01 00:00:00

abstract：:The degradation of batanopride hydrochloride, an investigational antiemetic drug, was studied in aqueous buffer solutions (pH 2-10; ionic strength, 0.5; 56 degrees C) in an attempt to improve drug stability for parenteral administration. Degradation occurs by two different mechanisms depending on the pH of the solutio...

journal_title：Journal of pharmaceutical sciences

authors： Nassar MN,House CA,Agharkar SN

更新日期：1992-11-01 00:00:00

abstract：:High pressure liquid chromatography using reversed-phase and/or ion-pair techniques was used to optimize resolution of aspirin-containing muscle relaxant mixtures as well as other therapeutic agents commonly found in muscle relaxant-analgesic mixtures. The compounds were chromatographed on an octadecylsilane column us...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Honigberg IL,Coldren JW

更新日期：1979-01-01 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

abstract：:The kinetics of decomposition of the following conformationally restricted N-chloro-alpha-amino acids were studied: 1-amino-1-cyclopentanecarboxylic acid (2), 1-amino-1-cyclohexanecarboxylic acid (4), 2-amino-2-norbornanecarboxylic acid (6), and 2-amino-2-benzonorbornanecarboxylic acid (8). The first-order rate consta...

journal_title：Journal of pharmaceutical sciences

authors： Awad R,Hussain A,Crooks PA

更新日期：1990-12-01 00:00:00

abstract：:The ratio between ocular and systemic drug concentrations describes the relative safety of ophthalmic dosage forms of the same drug in terms of its systemic side effects. In this study, we evaluated the effects of epinephrine pretreatment and solution pH on the aqueous humor:plasma and iris-ciliary body:plasma ratios ...

journal_title：Journal of pharmaceutical sciences

authors： Kyyrönen K,Urtti A

更新日期：1990-08-01 00:00:00

abstract：:Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...

journal_title：Journal of pharmaceutical sciences

authors： Wong SM,Oshima Y,Pezzuto JM,Fong HH,Farnsworth NR

更新日期：1986-03-01 00:00:00

abstract：:It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

journal_title：Journal of pharmaceutical sciences

authors： Carstensen JT,Rodriguez-Hornedo N

更新日期：1985-12-01 00:00:00

abstract：:Organic anion transporting polypeptides (OATP) 1B1 and OATP1B3 are important determinants of transporter-mediated drug-drug interactions (DDIs). Current studies assessed the OATP1B1 and OATP1B3-mediated DDI potential of vemurafenib, a kinase inhibitor drug with high protein binding and low aqueous solubility, using R-...

journal_title：Journal of pharmaceutical sciences

authors： Kayesh R,Farasyn T,Crowe A,Liu Q,Pahwa S,Alam K,Neuhoff S,Hatley O,Ding K,Yue W

更新日期：2021-01-01 00:00:00

abstract：:The hydrolysis of acetylcholine and acetylcholine mustard by acetylcholinesterase was compared over a substrate concentration range of 1-10 mM. Reactions were allowed to proceed for 2 min at 25 degrees. Results of these experiments reveal that the substrates have similar affinities for the enzyme, whereas the maximum ...

journal_title：Journal of pharmaceutical sciences

authors： Hudgins PM,Stubbins JF

更新日期：1975-08-01 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：:This investigation was designed to quantitate and compare in the rat the oral absorption characteristics of micronized griseofulvin from a corn oil-in-water emulsion dosage form containing suspended drug and a control aqueous suspension after single-dose (50 mg/kg) and multiple-dose (50 mg/kg every 12 hr for five dose...

journal_title：Journal of pharmaceutical sciences

authors： Bates TR,Carrigan PJ

更新日期：1975-09-01 00:00:00

abstract：:The synthesis and antibacterial evaluation of a number of 2-(substituted phenylureido)-4-thiocyanatobenzothiazoles are described. The more active compounds against the test organisms in vitro generally were those substituted with halogens on the phenyl and benzothiazole rings. ...

journal_title：Journal of pharmaceutical sciences

authors： Alaimo RJ,Pelosi SS,Freedman R

更新日期：1978-02-01 00:00:00

abstract：:Twelve 6,8-disubstituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid derivatives were prepared and evaluated for their antibacterial activity. Among these, only the 6,8-difluoroquinolinone-3-carboxylic acid showed moderate activity. ...

journal_title：Journal of pharmaceutical sciences

authors： Krishnan R,Lang SA Jr

更新日期：1986-12-01 00:00:00

abstract：:Packing behavior and flowability of particulate material have long been acknowledged as important parameters for the processing of pharmaceutical materials. When properly understood, these properties can provide insight into weight uniformity, tableting performance and process design. The aim of this study was to meas...

journal_title：Journal of pharmaceutical sciences

authors： Sandler N,Wilson D

更新日期：2010-02-01 00:00:00

abstract：:In this study the relationships between previously reported connectivity indices described by Kier and Hall and steric contributions to the rate constants for several series of reactions are examined. Rate data were examined for four different series of reactions, which were chosen to represent a range of different re...

journal_title：Journal of pharmaceutical sciences

authors： Schug JC,Viers JW,Seeman JI

更新日期：1984-10-01 00:00:00

abstract：:Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barr...

journal_title：Journal of pharmaceutical sciences

authors： Chan JG,Duke CC,Ong HX,Chan JC,Tyne AS,Chan HK,Britton WJ,Young PM,Traini D

更新日期：2014-05-01 00:00:00

abstract：:A fully automated system for dissolution rate analysis of potassium in slow release tablets is described. Aliquots are removed after 1, 2, and 4 hr from six samples, and potassium is analyzed in a flame photometer at 768 nm. A complete study of six samples takes 5.5 hr. The system may be run overnight. During the time...

journal_title：Journal of pharmaceutical sciences

authors： Engdahl A,Karlberg B,Thelander S

更新日期：1976-03-01 00:00:00