Abstract:
:Plasma binding of chlordiazepoxide, diazepam, loraxepam, and oxazepam was determined by equilibrium dialysis in 20 male, healthy volunteers, 25-86 years old. A wide range of binding was observed, with the free fraction varying twofold for lorazepam, fourfold for chlordiazepoxide and diazepam, and over 20-fold for oxazepam. Statistically significant linear relationships were not observed between the degree of binding and age, serum albumin, or total protein for any of the drugs. There was, however, a correlation between the extent of binding for the four drugs. Because of the importance of unbound benzodiazepine levels in eliciting any pharmacological response and also in disposition, consideration of the wide interindividual variability in plasma binding must be made in interpreting pharmacodynamic and pharmacokinetic data.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Johnson RF,Schenker S,Roberts RK,Desmond PV,Wilkinson GRdoi
10.1002/jps.2600681034subject
Has Abstractpub_date
1979-10-01 00:00:00pages
1320-2issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)42858-8journal_volume
68pub_type
杂志文章abstract::Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.10.001
更新日期:2016-03-01 00:00:00
abstract::The crystal structure of the common therapeutic agent, the pentahydrated sodium salt of L-thyroxine hormone (3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]-L-alanine), has been determined and discussed in relation to the drug's stability. The stoichiometry and absolute configuration (-)-C(8)S-[C15H10I4NO4]-.Na+....
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20155
更新日期:2004-12-01 00:00:00
abstract::A swellable matrix tablet is described which is partially coated with cellulose acetate (CA) to obtain a film having the shape of a cup, whose permeability to water and solutes was altered by mixing increasing amounts of poly(ethylene glycol) 400 (PEG). The drug-release mechanism from such systems was assessed by carr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js9800026
更新日期:1998-06-01 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
pub_type: 杂志文章
doi:10.1002/jps.2600750608
更新日期:1986-06-01 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::Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has received considerable attention as a potential anticancer agent. However, recombinant Apo2L/TRAIL has several limitations, which include a weak pharmacokinetic profile, namely, a short biological half-life and rapid renal clearance, and an inability t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22298
更新日期:2011-02-01 00:00:00
abstract::This study determines the enhancing effects of 2-n-nonyl-1,3-dioxolane on the penetration of econazole, an antifungal drug, into the deeper layers of the human nail where fungal infection resides. Aliquots (10 microL) of Econail lacquer formulation containing 0.45 mg of [(14)C]-econazole with 18% 2-n-nonyl-1,3-dioxola...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10291
更新日期:2003-01-01 00:00:00
abstract::Electron donor-acceptor complexes for a group of quinolines and naphthalenes with 9-(dicyanomethylene)-2,4,7-trinitrofluorene in 1,2-dichloroethane were studied by optical absorption methods. Association constants, molar absorptivities, and charge-transfer transition energies were evaluated for each system, together w...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670211
更新日期:1978-02-01 00:00:00
abstract::A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690318
更新日期:1980-03-01 00:00:00
abstract::Uptake of the fluorescent probe, 1-anilino-8-naphthalene-sulfonate (I) into isolated rat liver cells was studied using both fluorescence and filtration methods. The time course of the fluorescence enhancement of I after addition to the isolated liver cells was analyzed in terms of rapid, medium, and slow phases. The s...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600720809
更新日期:1983-08-01 00:00:00
abstract::The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650931
更新日期:1976-09-01 00:00:00
abstract::The development of sustained-release lithium (Li) tablets, intended to release the active principle at a rate of 1.0 mM/h for 10 h, was undertaken. The parameters used for the control of the release were the glyceril palmite-stearate content, the carboxypolymethylene content, and the compression force. The experimenta...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600801103
更新日期:1991-11-01 00:00:00
abstract::A radioimmunoassay procedure was developed for the antihistamine terfenadine (alpha[4-(1,2-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol). The keto analog of terfenadine was converted to its O-carboxymethyloxime derivative, which was conjugated to bovine thyroglobulin by a mixed anhydride techniq...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600691218
更新日期:1980-12-01 00:00:00
abstract::As part of a series of articles in this special issue evaluating model IgG1-Fc glycoforms for biosimilarity analysis, 3 well-defined IgG1-Fc glycoforms (high mannose-Fc, Man5-Fc, and N-acetylglucosamine-Fc) and a nonglycosylated Fc protein (N297Q-Fc) were examined in this work to elucidate chemical degradation pathway...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2015.10.024
更新日期:2016-02-01 00:00:00
abstract::It is shown that tricalcium phosphate follows a simple Heckel relationship in pressures of usual tablet compression, only if a density of 1.92 g/mL is used. This coincides with the density obtained by wet pycnometry, whereas the crystallographical density is 3.1 g/mL. The interpretation is that some of the pore space ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600740419
更新日期:1985-04-01 00:00:00
abstract::A rapid and sensitive GLC method was developed for the quantitative determination of methenamine in tablets. The method was shown to possess several advantages over the official NF assay. After dissolution of the whole tablet in absolute ethanol and addition of an internal standard (pentylenetetrazol), an aliquot was ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660435
更新日期:1977-04-01 00:00:00
abstract::Poly(D,L-lactide-co-glycolide, 50:50) samples of similar molecular weight were obtained from three commercial sources and were characterized by gel permeation chromatography, differential scanning calorimetry, X-ray powder diffraction, viscometry, and proton nuclear magnetic resonance spectroscopy. Pellets were prepar...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600820322
更新日期:1993-03-01 00:00:00
abstract::Parsley cigarettes containing [3H]phencyclidine were machine smoked, and the mainstream smoke was trapped in glass wool filters. Radioactivity was extracted from these filters with chloroform. The average recoveries of radioactivity were 76, 85, 70, and 69% for cigarettes containing 3, 10, 30, and 50 mg of [3H]phencyc...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600700908
更新日期:1981-09-01 00:00:00
abstract::Judicious choice of the salt form of a drug can greatly affect the aqueous solubility and formulation of the compound. The objective of this work was to demonstrate the effect of various counteranions on the aqueous solubility of the antimalarial agent alpha-(2-piperidyl)-3, 6-bis(trifluoromethyl)-9-phenanthrenemethan...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650533
更新日期:1976-05-01 00:00:00
abstract::Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2017.03.012
更新日期:2017-07-01 00:00:00
abstract::The biphasic degradation of delta9-tetrahydrocannabinol (I), as monitored by flame-ionization GLC, produced delta8-tetrahydrocannabinol (II), cannabidiol (X), 9-hydroxyhexahydrocannabinol (VI), 9,10-dihydro-9-hydroxyisocannabidiol (VI), and and 6,12-dihydro-6-hydroxycannabidiol (VIII) in acidic solutions. Further iden...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670108
更新日期:1978-01-01 00:00:00
abstract::Tablet characteristics of tensile strength and disintegration time were predicted using residual stress distribution, simulated by the finite element method (FEM). The Drucker-Prager Cap (DPC) model was selected as the method for modeling the mechanical behavior of pharmaceutical powders composed of lactose (LAC), cor...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23675
更新日期:2013-10-01 00:00:00
abstract::Nonionic block copolymers are surfactants synthesized using propylene oxide and ethylene oxide, and they can be designed so that individual copolymers have unique vaccine adjuvant properties. We have designed and produced nonionic block copolymers based on high molecular weight (MW), 9-15 kDA, cores of poly(oxypropyle...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980072c
更新日期:1998-11-01 00:00:00
abstract::Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章,评审
doi:10.1016/j.xphs.2017.08.009
更新日期:2017-12-01 00:00:00
abstract::Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural an...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600800404
更新日期:1991-04-01 00:00:00
abstract::The previous paper in this series introduced an X-ray diffraction quantitation method for the polymorphic content in tablets made of pure components. Before the method could be transferred, further studies were required to explain the commonly observed X-ray intensity variation in analyzing compacts. The literature ty...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10480
更新日期:2003-12-01 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
pub_type: 杂志文章
doi:10.1002/jps.2600650134
更新日期:1976-01-01 00:00:00
abstract::The dissolution kinetics of theophylline monohydrate and anhydrous theophylline were investigated with a rotating-disk apparatus in buffer solutions at 298 K under sink conditions. The observed dissolution rate of theophylline monohydrate under various conditions agreed well with predictions based on the Extended Simu...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600750515
更新日期:1986-05-01 00:00:00
abstract::A rapid approach for estimating the pK(a) value of small organic molecules was developed using vacuum-assisted multiplexed capillary electrophoresis (VAMCE) with ultraviolet detection. The VAMCE method employed a 96-capillary array, arranged in a standard 8 x 12 microtiter plate configuration, with each row of capilla...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20275
更新日期:2005-03-01 00:00:00
abstract::The aims of the present study were to formulate stable onion phases of the biodegradable surfactant PEG-8 Distearate (PEG8DS) and evaluate application of the onion phases in encapsulating sumatriptan succinate, a BCS class III potent antimigraine drug. Drug loaded and placebo onion phases were prepared by shearing lyo...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20863
更新日期:2007-09-01 00:00:00