Abstract：
:Volunteers were injected im with 100 mg of tripelennamine (pyribenzamine).HCl dissolved in saline. Timed urine was collected. Tripelennamine and its metabolites were identified by GC/MS. Amounts of free tripelennamine excreted in the 0-2-, 2-4-, 4-8-, 8-12-, and 12-24-h urine samples were found to be 0.30, 0.56, 0.17, 0.21, and 0.0%, respectively, of the administered dose. In the same time periods, total tripelennamine (free plus conjugated) amounts were found to be 0.92, 1.20, 0.96, 1.30, and 1.31%, respectively, and total amounts 2-[alpha-hydroxybenzyl(2-dimethylaminoethyl)amino]pyridine(alpha- hydroxytripelennamine) plus an unidentified metabolite were found to be 0.16, 3.35, 3.06, 7.46, and 8.85% of the dose, respectively.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Yeh SYdoi
10.1002/jps.2600800902subject
Has Abstractpub_date
1991-09-01 00:00:00pages
815-9issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48652-6journal_volume
80pub_type
杂志文章abstract：:A new polymorphic form of Alprazolam (Xanax), 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo-[4,3-alpha][1,4]benzodiazepine, C(17)H(13)ClN(4), has been investigated by means of X-ray powder diffraction (XRPD), single crystal X-ray diffraction, and differential scanning calorimetry (DSC). This polymorphic form (form III...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.20930
更新日期：2007-05-01 00:00:00
abstract：:Gender and immune status can considerably impact on the pharmacokinetics (PK) of macromolecular and small molecule drugs. However, these effects are often not considered in drug development. We aimed to quantitatively evaluate effects of gender and immune status on the PK of PEGylated interferon in frequently used mur...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.24412
更新日期：2015-05-01 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
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doi：10.1002/jps.23546
更新日期：2013-06-01 00:00:00
abstract：:The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24137
更新日期：2014-11-01 00:00:00
abstract：:The stereoselective pharmacokinetics of suprofen enantiomers has been studied in humans by means of stable isotope-labeled pseudoracemate-diastereomer methodology. After a single oral dose of a near equimolar mixture of unlabeled-(R)-(-)- and [2H3]-(S)-(+)-suprofen [or unlabeled-(S)- and [2H3]-(R)-suprofen] to three h...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600801116
更新日期：1991-11-01 00:00:00
abstract：:Sodium salicylate improves the rectal absorption of drugs which exhibit molecular self-association; it is suggested that salicylate may improve drug bioavailability by altering the drug self-association pattern. Methylene blue was chosen as a model molecule for investigating the interference of salicylate with drugs u...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600750413
更新日期：1986-04-01 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...
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doi：10.1002/jps.2600721025
更新日期：1983-10-01 00:00:00
abstract：:We report the preparation and structural characterization of a family of primary alcohol solvates of a small-molecule hydrochloride salt. The structures of the solvates are probed by powder and single crystal X-ray diffraction, and the compounds were additionally characterized by polarized light microscopy, thermograv...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.01.020
更新日期：2018-06-01 00:00:00
abstract：:The single pass mean residence time in peripheral tissues, tp1, is a characteristic constant of linear pharmacokinetic systems and nonlinear systems with linear distribution kinetics. It is descriptive of distribution kinetics in such systems and is not dependent on elimination kinetics as are other related parameters...
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doi：10.1002/jps.2600751202
更新日期：1986-12-01 00:00:00
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doi：10.1002/jps.2600831019
更新日期：1994-10-01 00:00:00
abstract：:A theory of charge, fluid-mass, and solute (including macromolecular) transport through porous media is applied to describe transport phenomena across the external layer of mammalian skin. Linear relationships are derived between transport fluxes and applied fields. These relationships introduce six effective transder...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600830925
更新日期：1994-09-01 00:00:00
abstract：:An automated two-phase method for the simultaneous fluorometric determination of the spironolactone metabolites canrenone (II) and canrenoic acid (III) in serum is described. The determination is performed by two dichloroethane extractions of the same serum sample at different pH values. The fluorescence developed in ...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600660820
更新日期：1977-08-01 00:00:00
abstract：:This study was aimed to investigate chemical preactivated thiomers for their potential use in mucosal drug delivery. Thiomers--thiolated polymers--are mucoadhesive polymers with sulfhydryl group-bearing side chains. Thiomers are synthesized by covalent attachment of low molecular mass compounds bearing sulfhydryl grou...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.24060
更新日期：2014-08-01 00:00:00
abstract：:Eighteen healthy adult volunteers completed an open-label, four-way crossover study designed to determine the bioequivalency of 160-mg cibenzoline [2-(2,2-diphenylcyclopropyl)-4,5-dihydro-1H-imidazole] capsules and tablets, their relative bioavailability compared with an oral solution of the drug, as well as the absol...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600750915
更新日期：1986-09-01 00:00:00
abstract：:The present work shows that the heated carbamazepine (CBZ) powder form III can be described as purely triclinic form I or a mixture of triclinic form I and monoclinic form III, depending on the resolution of the X-ray diffraction equipment used. Visual identification of the minor phase is possible when high-resolution...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.22482
更新日期：2011-07-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600751015
更新日期：1986-10-01 00:00:00
abstract：:Transcutaneous immunization is the administration of a vaccine on the skin to generate efficient systemic and mucosal immune responses against an antigen. In the present study, reconstituted hepatitis B surface antigen vesicles (HBsAg-REVs) integrated with monophosphoryl lipid A were prepared by the delipidation-recon...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2019.07.007
更新日期：2019-11-01 00:00:00
abstract：:Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.24085
更新日期：2014-10-01 00:00:00
abstract：:A new High-performance liquid chromatographic (HPLC) method for the assay of sodium fusidate (I) or fusidic acid in dosage forms was developed and compared to a microbiological assay. A linear relationship was obtained between absolute peak area and amount of I(r = 0.99+) in the 50-1000-microgram/ml range. In the micr...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600711130
更新日期：1982-11-01 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
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doi：10.1002/jps.20658
更新日期：2006-09-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：
更新日期：1980-10-01 00:00:00
abstract：:This work investigates the use of spray freeze-drying (SFD) to produce protein loaded particles suitable for epidermal delivery. In the first part of the study, the effects of formulation and process conditions on particle properties are examined. Aqueous solutions of trehalose produce SFD particles in the size range ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10204
更新日期：2002-10-01 00:00:00
abstract：:An on-line, high-performance frontal analysis (HPFA)-high-performance liquid chromatographic system was developed for the enantioselective determination of a low level of unbound ketoprofen (KP) that is in equilibrium with KP that is bound to protein. The system consists of three subsystems (HPFA system, preconcentrat...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810725
更新日期：1992-07-01 00:00:00
abstract：:Substance P (SP) was degraded by synaptic membranes of rat spinal cord. Cleavage products were separated by reversed phase high performance liquid chromatography and identified by amino acid composition analyses. Major products of SP were phenylalanine, SP(1-4), SP(1-6), SP(1-7), SP(10-11), and SP(8-9). Both the degra...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js990149c
更新日期：1999-11-01 00:00:00
abstract：:Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform in...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2018.11.038
更新日期：2019-04-01 00:00:00
abstract：:Capillary gas chromatography using an open tubular fused silica column and NP-FID was applied to the simultaneous analysis of the antihistamine, carbinoxamine, and the antitussive, hydrocodone, in human serum. Carbinoxamine and hydrocodone were extracted into methylene chloride-2-propanol (9:1) under alkaline conditio...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600721126
更新日期：1983-11-01 00:00:00
abstract：:Many active pharmaceutical ingredients exhibit a needle-like (acicular) crystal habit, which can significantly complicate their downstream processing. In this study, the acicular crystal habit of a model active pharmaceutical ingredient, 5-aminosalicylic acid (5-ASA), was modified by addition of selected organic solve...
journal_title：Journal of pharmaceutical sciences
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doi：10.1016/j.xphs.2017.12.005
更新日期：2018-04-01 00:00:00
abstract：:The effects of various factors on the adsorption of nicotinic acid onto and desorption from activated charcoal were investigated in vitro. The affinity of nicotinic acid for charcoal was poor both in acidic and neutral media. Adsorption increased with increasing charcoal:drug ratios and decreasing incubation volume:ch...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600810916
更新日期：1992-09-01 00:00:00
abstract：:The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challengi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.08.020
更新日期：2020-11-01 00:00:00
abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...
journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.22188
更新日期：2010-12-01 00:00:00
