Abstract：
:Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic carvedilol after oral administration. In this study, a sensitive, stereospecific high-performance liquid chromatographic assay was used to determine the plasma concentration of each enantiomer. The assay involves the diastereomeric derivatization of racemic carvedilol with 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl isothiocyanate as a chiral reagent. After oral administration of racemic carvedilol to humans, the mean Cmax and AUC infinity values for R(+)-enantiomer were 2.6 and 2.8 times greater, respectively, than those for the more active S(-)-enantiomer. Similarly, in monkeys, the respective R:S enantiomer ratios for Cmax and AUC infinity were 1.5 and 1.2. The difference in AUCoral between these enantiomers is ascribed to the greater intrinsic clearance of S(-)-enantiomer than that of the R(+)-enantiomer in the liver, and to a lower plasma protein binding of the S(-)-enantiomer.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Fujimaki M,Murakoshi Y,Hakusui Hdoi
10.1002/jps.2600790704subject
Has Abstractpub_date
1990-07-01 00:00:00pages
568-72issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48299-1journal_volume
79pub_type
杂志文章abstract：:The objective of the current study was to develop and evaluate VLDL-resembling phospholipid-submicron emulsion (PSME) as a carrier system for new cholesterol-based compounds for targeted delivery to cancer cells. BCH, a boronated cholesterol compound, was originally developed in our laboratory to mimic the cholesterol...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.10117
更新日期：2002-06-01 00:00:00
abstract：:The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug:egg albumin solid dispersions have been studied in comparison with those of the drug alone. The interaction of drug with egg albumin in aqueous solution and solid state were examined by solubility analysis, dia...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600800517
更新日期：1991-05-01 00:00:00
abstract：:Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.10.022
更新日期：2019-03-01 00:00:00
abstract：:We have used rheological and thermal methods to study the colloidal characteristics of a widely used technical latex. The dispersions of poly(methacrylic acid-ethyl acrylate) (Eudragit L100-55) were found to be stabilized by a combination of electrostatic and steric mechanisms termed as electrosteric stabilization. Th...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js9803555
更新日期：1999-04-01 00:00:00
abstract：:The aim of this study was to prepare and characterize thiolated chitosan (TC) nanoparticles (NPs) of tizanidine HCl (TZ) and to evaluate its transport across monolayer of RPMI 2650 cells (Human nasal septum carcinoma cell line) followed by assessment of their pharmacokinetic and pharmacodynamic attributes, after intra...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.22780
更新日期：2012-02-01 00:00:00
abstract：:The effect of chemical penetration enhancers (e.g., fatty acids) in combination with iontophoresis was examined on the in vitro permeability of luteinizing hormone releasing hormone (LHRH) through porcine skin. Porcine epidermis was pretreated with either ethanol (EtOH) or 10% fatty acid/EtOH. The permeability coeffic...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js970301f
更新日期：1998-04-01 00:00:00
abstract：:Dynamic imaging analysis instruments are used for sizing particles of different types that might appear in a biopharmaceutical. These instruments are calibrated using polystyrene latex microspheres in water, which is a significantly different system than the typical particles imaged in a formulation. We show how the i...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.10.017
更新日期：2020-01-01 00:00:00
abstract：:The physical stability of an immunoglobulin G4 monoclonal antibody (mAb) upon dilution into intravenous (i.v.) bags containing 0.9% saline was examined. Soluble aggregates and subvisible particles were observed by size-exclusion high-performance liquid chromatography (SE-HPLC) and light obscuration when formulated wit...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.23224
更新日期：2012-10-01 00:00:00
abstract：:The described simple, accurate, and precise reversed-phase high-pressure liquid chromatographic procedure is in excellent agreement with 1-octanol shake-flask partition or distribution coefficients over a 3.5 log range. A chemically bonded octadecylsilane support is persilated and coated with 1-octanol. With 1-octanol...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600671008
更新日期：1978-10-01 00:00:00
abstract：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600720822
更新日期：1983-08-01 00:00:00
abstract：:Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2020.06.017
更新日期：2020-10-01 00:00:00
abstract：:To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.1033
更新日期：2001-06-01 00:00:00
abstract：:This paper traces the academic genealogy of Professor Takeru Higuchi, who is considered "The Father of Physical Pharmacy" because of his contributions to the science of drug formulation and delivery and his impact in mentoring a whole generation of post-World War II pharmaceutical scientists. As one who was mentored b...
journal_title：Journal of pharmaceutical sciences
pub_type： 传,社论,历史文章
doi：10.1002/jps.1049
更新日期：2001-08-01 00:00:00
abstract：:Levetiracetam therapy is often associated with high levels of individual variation in the recommended dose required to achieve preferential treatment. Thus, a reliable and dynamic regulation system to accurately tailor dose is necessary. The main objective of this study is to explore and prepare a dose-flexible contro...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.10.001
更新日期：2019-02-01 00:00:00
abstract：:4,5-Dimethoxykynuramine was synthesized in a three-step sequence originating with veratrole. Indirect evidence indicates that the drug was converted in vivo to the hypotensive agent 6,7-dimethoxy-4-quinolinol by the action of monoamine oxidase. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670344
更新日期：1978-03-01 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
pub_type： 杂志文章
doi：10.1021/js960005n
更新日期：1996-11-01 00:00:00
abstract：:A heparin derivative sufficiently lipophilic to be bound to plastics, forming blood-compatible supports, or to be used as an anticoagulant by transdermal or oral routes would be of great pharmaceutical interest. For such applications, the functional groups within heparin's antithrombin III binding site, responsible fo...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600830721
更新日期：1994-07-01 00:00:00
abstract：:One of the most important challenges for pharmaceutical and cosmetic industries is solubilization and preservation of their active ingredients. Therefore, most of these formulations contain irritant chemical additives to improve their shelf-life and the solubility of hydrophobic ingredients. An interesting alternative...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2019.02.010
更新日期：2019-07-01 00:00:00
abstract：:To date, research on the effect of single nucleotide polymorphisms (SNPs) on P-glycoprotein (P-gp) expression and functionality has rendered inconsistent results. This study systematically evaluates the impact of MDR1 haplotypes (1236/2677, 1236/3435, 2677/3435, 1236/2677/3435) on P-gp functionality compared to indivi...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20717
更新日期：2006-10-01 00:00:00
abstract：:An assay is described for the determination of the H2-receptor antagonist, cimetidine, in human plasma and urine. Alkalinized plasma or urine was extracted with methylene chloride, the organic phase was evaporated, and the reconstituted residue was analysed by high-pressure liquid chromatography (HPLC) using a reverse...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600710528
更新日期：1982-05-01 00:00:00
abstract：:The melting behavior of paracetamol and polyethylene glycol (PEG) 4000, both individually and as binary systems, has been studied using differential scanning calorimetry. The appearance of the PEG peaks was shown to be highly dependent on scanning rate, with evidence for the existence of once-folded and extended chain...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1021/js970137w
更新日期：1997-09-01 00:00:00
abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1016/j.xphs.2018.12.027
更新日期：2019-06-01 00:00:00
abstract：:A series of 4-substituted aminoquinoline-3-carboxylates was prepared and evaluated for antimicrobial activity. Four of the compounds (VIII, XIII, XV, and XXIII) exhibited low activity against Staphylococcus aureus. ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600730828
更新日期：1984-08-01 00:00:00
abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章,评审
doi：10.1002/jps.23783
更新日期：2014-01-01 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
pub_type： 杂志文章
doi：10.1002/jps.22182
更新日期：2010-11-01 00:00:00
abstract：:The comparative pharmacokinetics of free MTP-PE (muramyl tripeptide phosphatidyl ethanolamine) and MTP-PE entrapped in negatively charged multilamellar liposomes (liposomal MPT-PE) was evaluated in rats at a bolus intravenous (i.v.) dose of 0.2 mg/kg and in dogs at a bolus i.v. dose of 0.1 mg/kg. Additional studies we...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600821005
更新日期：1993-10-01 00:00:00
abstract：:In an attempt to explain the triamterene stone diathesis, we studied the excretion and solubility of triamterene, 1, and its metabolite, the sulfate ester of the hydroxy derivative of triamterene, 3. The urinary excretion pattern and metabolism in stone formers was the same as in other chronic users of triamterene or ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600750205
更新日期：1986-02-01 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
pub_type： 杂志文章
doi：10.1002/jps.23789
更新日期：2014-01-01 00:00:00
abstract：:The area under the plasma concentration-time curve (AUC) was measured after an intravenous injection of sodium salicylate and after intragastric administration of aspirin, using either an intermittent sampling and the trapezoid rule (AUC-trapezoid) or the recently introduced constant blood withdrawal method (AUC-integ...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.2600670644
更新日期：1978-06-01 00:00:00
abstract：:The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from...
journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
doi：10.1002/jps.20769
更新日期：2007-01-01 00:00:00
