Liquid chromatographic assay and disposition of carvedilol in healthy volunteers.


:Quantitative determination of serum concentrations of carvedilol [(+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl) amino]-2-propanol], a combined alpha- and beta-adrenergic receptor antagonist, was obtained using HPLC with spectrofluorometric detection. Carvedilol was extracted from alkalinized serum with ether and was subsequently back extracted with diluted phosphoric acid. This method proved to be sensitive and reproducible (mean coefficient of variation of 6.1% for 0.25 to 150 nanograms per milliliter of serum). A single dose of carvedilol (5, 10, or 15 mg) was given as an intravenous infusion to three healthy volunteers. Carvedilol serum concentration-time profiles were fitted best to a three-compartment model and the pharmacokinetic data revealed the following mean values: Vdss of 1.97 L/kg, mean residence time (MRT) of 4.66 h, and CL of 0.437 L X h-1 X kg-1.


J Pharm Sci


Varin F,Cubeddu LX,Powell JR




Has Abstract


1986-12-01 00:00:00














  • A multiphase microscopic diffusion model for stratum corneum permeability. II. Estimation of physicochemical parameters, and application to a large permeability database.

    abstract::The full parameterization for the stratum corneum biphasic microtransport model presented previously in this Journal [95:620-648 (2006)] is developed through a combination of fundamental transport theory and calibration with existing data. Of the five microscopic transport properties, four (D(cor), K(cor/w), D(lip), K...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wang TF,Kasting GB,Nitsche JM

    更新日期:2007-11-01 00:00:00

  • Viscosity and surface tension of dilute salicylic acid-cetrimide systems.

    abstract::The viscosity and surface tension of systems containing small amounts of salicylic acid in aqueous solutions of cetrimide were determined. An abrupt increase in viscosity was observed, and the molar ratio of salicylic acid to certrimide at which this viscosity increase occurred was 1:2. The surface tension of these sy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Wan LS

    更新日期:1977-12-01 00:00:00

  • 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones: a series with stimulant and depressant activities.

    abstract::A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ellis KO,Schwan TJ,Wessels FL,Miles NJ

    更新日期:1980-10-01 00:00:00

  • The Disintegration Process in Microcrystalline Cellulose Based Tablets, Part 1: Influence of Temperature, Porosity and Superdisintegrants.

    abstract::Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

    更新日期:2015-10-01 00:00:00

  • Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine over a 2-year period.

    abstract::Hydrazine levels in formulations of hydralazine, isoniazid, and phenelzine have been measured over a 2-year period under ambient conditions and under temperature and humidity stress. Hydralazine tablets are stable under ambient conditions, but the hydrazine level in an injectable formulation increased from 4.5 to 10 m...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lovering EG,Matsui F,Curran NM,Robertson DL,Sears RW

    更新日期:1983-08-01 00:00:00

  • Inclusion complexation of heptakis(2,6-di-O-ethyl)-beta-cyclodextrin with tiaprofenic acid: pharmacokinetic consequences of a pH-dependent release and stereoselective dissolution.

    abstract::beta-Cyclodextrin was ethylated at the 2- and 6-hydroxyl positions. Diethyl sulfate was employed as an alkylating reagent. NMR spectra data indicate that heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (DCD) is the principal component of the product obtained. In addition, the FAB mass spectra obtained in nitrobenzyl alcoho...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Vakily M,Pasutto FM,Daneshtalab M,Jamali F

    更新日期:1995-08-01 00:00:00

  • Molecular complexing ability of quinoline and its simple derivatives.

    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


    authors: Webb NE,Thompson CC

    更新日期:1978-02-01 00:00:00

  • A novel method for the preparation of liposomes: freeze drying of monophase solutions.

    abstract::A novel method is described for the preparation of sterile and pyrogen-free submicron liposomes of narrow size distribution. The method is based on the formation of a homogeneous dispersion of lipids in water-soluble carrier materials. To obtain the lipid-containing solid dispersion, liposome-forming lipids and water-...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Li C,Deng Y

    更新日期:2004-06-01 00:00:00

  • Autoxidation of tetrazepam in tablets: prediction of degradation impurities from the oxidative behavior in solution.

    abstract::The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxy...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JP

    更新日期:1992-02-01 00:00:00

  • Finite dose pharmacokinetics of skin penetration.

    abstract::A model for estimating in vivo skin permeability coefficients for finite doses is presented. The ratio of the maximum value of the excretion rate to the steady-state flux is a function of the thickness of the applied vehicle and the vehicle-skin partition coefficient. The decay rate of the excretion is a function of s...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cooper ER,Berner B

    更新日期:1985-10-01 00:00:00

  • Dissolution studies with a multichannel continuous-flow apparatus.

    abstract::A multichannel continuous-flow apparatus for dissolution rate measurements is described. Typical data are presented to demonstrate its utility for studies with bulk drug powders as well as with tablets and capsules without any change of setup. Procedures are given for the preparation of powder samples for dissolution ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Cakiryildiz C,Mehta PJ,Rahmen W,Schoenleber D

    更新日期:1975-10-01 00:00:00

  • Sensitive radioimmunoassay and enzyme-linked immunosorbent assay for the simultaneous determination of chloroquine and its metabolites in biological fluids.

    abstract::Two new methods for the simultaneous determination of chloroquine and its two main metabolites (monodesethylchloroquine and bisdesethylchloroquine) in biological samples, radioimmunoassay (RIA) and enzyme-linked immunosorbent assay (ELISA), are described. Antiserum is produced in rabbits immunized with N-(2-carboxyeth...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Escande C,Chevalier P,Verdier F,Bourdon R

    更新日期:1990-01-01 00:00:00

  • Quantitative determinations of phenol and resorcinol in pharmaceutical dosage forms by high-pressure liquid chromatography.

    abstract::The quantitative determinations of phenol in phenolated calamine lotion USP and of phenol and resorcinol in phenol-resorcinol-boric acid solution by high-pressure liquid chromatography are reported. The procedures are simple, rapid (no special preliminary treatment is required), and accurate. There is no interference ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Das Gupta V

    更新日期:1976-11-01 00:00:00

  • A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.

    abstract::CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu T,Gobburu JVS

    更新日期:2018-03-01 00:00:00

  • Racemic species of sodium ibuprofen: characterization and polymorphic relationships.

    abstract::Racemic and homochiral sodium ibuprofen were characterized by thermal analysis and powder X-ray diffractometry. The melting point phase diagram was constructed and thermodynamic calculation was performed. In contrast to racemic ibuprofen, which is a racemic compound, racemic sodium ibuprofen forms both a racemic congl...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhang GG,Paspal SY,Suryanarayanan R,Grant DJ

    更新日期:2003-07-01 00:00:00

  • Integrated functions for four basic models of indirect pharmacodynamic response.

    abstract::The integrated solutions (ABEC, area between baseline and effect curve) of four basic models of indirect pharmacodynamic responses are developed. These models assume that drug can inhibit or stimulate the production or loss of the response variable. For two models (I and III) with monoexponential drug disposition, exp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Krzyzanski W,Jusko WJ

    更新日期:1998-01-01 00:00:00

  • Using Image Attributes to Assure Accurate Particle Size and Count Using Nanoparticle Tracking Analysis.

    abstract::Nanoparticle tracking analysis (NTA) obtains particle size by analysis of particle diffusion through a time series of micrographs and particle count by a count of imaged particles. The number of observed particles imaged is controlled by the scattering cross-section of the particles and by camera settings such as sens...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Defante AP,Vreeland WN,Benkstein KD,Ripple DC

    更新日期:2018-05-01 00:00:00

  • Utilizing a novel tandem oral dosing strategy to enhance exposure of low-solubility drug candidates in a preclinical setting.

    abstract::Time and resource constraints necessitate increasingly early decision making to accelerate or stop preclinical drug discovery programs. Early discovery drug candidates may be potent inhibitors of new targets, but all too often exhibit poor pharmaceutical and pharmacokinetic properties that limit the in vivo exposure. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Chiang PC,South SA,Foster KA,Daniels JS,Wene SP,Albin LA,Thompson DC

    更新日期:2010-07-01 00:00:00

  • Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.

    abstract::In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY

    更新日期:2009-02-01 00:00:00

  • Isomeric benzoylpyrroleacetic acids: some structural aspects for aldose reductase inhibitory and anti-inflammatory activities.

    abstract::A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Demopoulos VJ,Rekka E

    更新日期:1995-01-01 00:00:00

  • Pharmacokinetics of polychlorinated biphenyl components in swine and sheep after a single oral dose.

    abstract::Single-dose oral administration of a commercial polychlorinated biphenyl product containing 54% chlorine provided data with which to plot the time course of total polychlorinated biphenyl and individual components in the blood of swine and sheep. Pharmacokinetic parameters describing absorption from the gut and elimin...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Borchard RE,Welborn ME,Wiekhorst WB,Wilson DW,Hansen LG

    更新日期:1975-08-01 00:00:00

  • Release of polyionizable compounds from submicrometer oil-in-water emulsions.

    abstract::A novel, general, theoretical equation that describes the release of polyionizable compounds from submicrometer emulsions was derived and evaluated. The model accounts for simultaneous partitioning, interfacial activity, and adsorption to surfactant for n independent drug species and j surfactant species in a single e...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Silvestri S,Wu LL,Bowser B

    更新日期:1992-05-01 00:00:00

  • Bioequivalence of long half-life drugs--informative sampling determination--using truncated area in parallel-designed studies for slow sustained-release formulations.

    abstract::A simulation study was done to determine if 72 h is the most informative sampling duration for bioequivalence (BE) determination in parallel-designed BE studies with drugs that have half-lives of at least 30 h. The impact of absorption and elimination half-lives on informative sampling was evaluated. Two-treatment par...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: El-Tahtawy A,Harrison F,Zirkelbach JF,Jackson AJ

    更新日期:2012-11-01 00:00:00

  • Inulin hydrogels as carriers for colonic drug targeting. Rheological characterization of the hydrogel formation and the hydrogel network.

    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

    pub_type: 杂志文章


    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

  • In vitro iontophoretic studies using a synthetic membrane.

    abstract::In vitro iontophoretic administration of drugs through a microporous polyolefin membrane with hydrophilic urethane polymerfilled pores was done for the ionized drugs dexamethasone sodium phosphate, hydrocortisone sodium phosphate, and prednisolone sodium succinate, and for a nonionizable drug cortisone acetate. Curren...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tu YH,Allen LV Jr

    更新日期:1989-03-01 00:00:00

  • Estimation of the aqueous solubility I: application to organic nonelectrolytes.

    abstract::The estimation of aqueous solubilities of organic nonelectrolytes by the General Solubility Equation (GSE) as proposed by Valvani and Yalkowsky (1980) is used in this study. The data and assumptions on which the GSE are based are reevaluated, and the equation is revised. The revised GSE is validated on a set of 580 ph...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Jain N,Yalkowsky SH

    更新日期:2001-02-01 00:00:00

  • Dissolution profiles for finely divided drug suspensions.

    abstract::A suspension of micronized prednisolone acetate was separated into four fractions by the technique of centrifugal elutriation. Data showed that each fraction had a narrow particle size. The dissolution experiments were carried out under sink conditions (less than 10% of saturation concentration) in a dissolution appar...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mauger JW,Howard SA,Amin K

    更新日期:1983-02-01 00:00:00

  • Automated in vitro dissolution rate analysis of potassium in plastic matrix slow release tablets.

    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

    pub_type: 杂志文章


    authors: Engdahl A,Karlberg B,Thelander S

    更新日期:1976-03-01 00:00:00

  • Modeling of transmitted X-ray intensity variation with sample thickness and solid fraction in glycine compacts.

    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


    authors: Cao W,Mullarney MP,Hancock BC,Bates S,Morris KR

    更新日期:2003-12-01 00:00:00

  • Cactus alkaloids XXXIII: beta-phenethylamines from the Guatemalan cactus Pilosocereus maxonii.

    abstract::TLC analysis of extracts of Pilosocereus maxonii (Rose) Byles and Rowley detected six identifiable alkaloids. Preparative TLC aided in the crystallization of the hydrochlorides of N-methyl-3,4-dimethoxyphenethylamine, N-methyl-3-methoxytyramine, and N,N-dimethyl-3-methoxytyramine. Traces of 3,4-dimethoxyphenethylamine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Pummangura S,Nichols DE,McLaughlin JL

    更新日期:1977-10-01 00:00:00