A high-performance liquid chromatographic method for the determination of stobadin pharmacokinetics in serum.

Abstract:

:A high-performance liquid chromatographic method was developed to determine stobadin pharmacokinetics in dog and man. The relative bioavailability of stobadin dipalmitate compared with dihydrochloride was 46.4 per cent in dog. In man peak serum concentrations ranged from 12 to 289 ng ml-1 after a single oral dose of stobadin dipalmitate (0.79 to 2.5 mgkg-1).

journal_name

Biopharm Drug Dispos

authors

Soltés L,Kállay Z,Bezek S,Fedelesová V

doi

10.1002/bdd.2510120104

subject

Has Abstract

pub_date

1991-01-01 00:00:00

pages

29-35

issue

1

eissn

0142-2782

issn

1099-081X

journal_volume

12

pub_type

杂志文章
  • Role of ABC transporters in trans-epithelial transport of vitamin K antagonists.

    abstract::Vitamin K antagonists (VKAs) remain the oral anticoagulant of choice in venous thromboembolic disease. These drugs are characterized by a large inter-individual variability requiring frequent dose tailoring. Genetic polymorphisms for cytochrome CYP2C9 and VKORC1 explain some of the variability, especially in warfarin ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2055

    authors: Espana B,Couturier S,Prouillac C

    更新日期:2017-01-01 00:00:00

  • Influence of dose on the distribution kinetics of ciprofloxacin and ofloxacin in the isolated hindlimb of the rat.

    abstract::The aim of this study was to determine whether the dose influences the distribution kinetics of ciprofloxacin and ofloxacin in muscle- bone- and skin-tissues included in the isolated hindlimb of the rat. Experiments were carried out in the isolated perfused hindlimb of the rat, administering a single dose of 45, 450 o...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.245

    authors: Casquero-Dorado AC,Colino CI,Martínez MS,Sánchez-Navarro A

    更新日期:2000-11-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of mivacurium stereoisomers in beagle dogs using twitch height and train-of-four response.

    abstract::Mivacurium, a non-depolarizing neuromuscular blocking agent, consists of three isomers; trans-trans (57%), cis-trans (36%) and cis-cis (7%). The purpose of this study was to characterize the pharmacokinetics and pharmacodynamics of mivacurium after various inputs. Four beagle dogs weighing between 7.95 and 9.89 kg wer...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(1998110)19:8<485::aid-bdd1

    authors: Lugo SI,Liang Z,Eddington ND

    更新日期:1998-11-01 00:00:00

  • Inhibition of rat hepatic mitochondrial aldehyde dehydrogenase isozymes by repeated cyanamide administration: pharmacokinetic-pharmacodynamic relationships.

    abstract::The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140508

    authors: Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

    更新日期:1993-07-01 00:00:00

  • Pharmacokinetics and hepatic first-pass effect of (-)-carbovir in the anesthetized rat.

    abstract::Studies were designed to allow an in vivo estimation of the hepatic extraction ratio and to test the hypothesis that the pharmacokinetic parameters of (-)-CBV are significantly different during anesthesia. (-)-CBV was administered as an i.v. bolus followed by i.v. infusion into either the portal (n = 3) or the jugular...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510160407

    authors: Soria I,Zimmerman CL

    更新日期:1995-05-01 00:00:00

  • The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers.

    abstract::Sildenafil is the first oral therapeutic agent for the management of male erectile dysfunction. Its oral bioavailability is only 40% due to extensive presystemic elimination, mainly by CYP3A4. This study examined the effect of coadministration of ciprofloxacin or clarithromycin, which inhibit CYP3A4, on the bioavailab...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.488

    authors: Hedaya MA,El-Afify DR,El-Maghraby GM

    更新日期:2006-03-01 00:00:00

  • Safety, tolerability and pharmacokinetics of 2-pyridylacetic acid, a major metabolite of betahistine, in a phase 1 dose escalation study in subjects with ADHD.

    abstract::Betahistine, a potent histamine H3 receptor antagonist, is being developed for the treatment of attention deficit hyperactivity disorder (ADHD) that manifests with symptoms such as hyperactivity, impulsivity and inattention. This study describes the pharmacokinetics of betahistine in ADHD subjects at doses higher than...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/bdd.1955

    authors: Moorthy G,Sallee F,Gabbita P,Zemlan F,Sallans L,Desai PB

    更新日期:2015-10-01 00:00:00

  • Theophylline controlled-release formulations: in vivo-in vitro correlations.

    abstract::Four experimental controlled-release oral solid dosage formulations were developed and the in vitro dissolution characteristics of theophylline from these formulations were studied in USP apparatus I. Pharmacokinetic evaluation of these formulations was carried out in eight beagle dogs under fasting conditions. Theoph...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(SICI)1099-081X(199604)17:3<259::AID-BDD95

    authors: Yu Z,Schwartz JB,Sugita ET

    更新日期:1996-04-01 00:00:00

  • Non-clinical characterization of the disposition of EMA401, a novel small molecule angiotensin II type 2 receptor (AT2R) antagonist.

    abstract::EMA401, (the S-enantiomer of 5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid), also known as Olodanrigan, is an orally active selective angiotensin II type 2 receptor (AT2 R) antagonist that is in Phase IIb clinical development as a novel analgesic for the relief of chro...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2226

    authors: Murgasova R,Carreras ET,Suetterlin-Hachmann M,da Silva Torrao LR,Kittelmann M,Alexandra V,Fredenhagen A

    更新日期:2020-04-01 00:00:00

  • Oxidative versus conjugative biotransformation of temazepam.

    abstract::Twenty-four healthy volunteers, aged 21-59 years, received single 30 mg oral doses of the benzodiazepine hypnotic temazepam. Levels of intact temazepam were determined in multiple plasma samples drawn during 48 h after dosage. Intact temazepam, its direct glucuronide conjugate, and the conjugate of its demethylated (o...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510110604

    authors: Locniskar A,Greenblatt DJ

    更新日期:1990-08-01 00:00:00

  • Disposition of WR-1065 in the liver of tumor-bearing rats following regional vs systemic administration of amifostine.

    abstract:PURPOSE:Amifostine is a prodrug in which selectivity is largely determined by the preferential formation and uptake of its cytoprotective metabolite, WR-1065, in normal tissues as a result of differences in membrane-bound alkaline phosphatase activity. It was hypothesized that amifostine may be a good candidate for reg...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.380

    authors: Levi M,DeRemer SJ,Dou C,Ensminger WD,Smith DE

    更新日期:2004-01-01 00:00:00

  • Bioavailability of phenylbutazone from a new enteric-coated formulation with superior dissolution characteristics.

    abstract::The bioavailability of an improved formulation of enteric-coated phenylbutazone with faster dissolution, more consistent in vitro rate of drug release and improved stability was compared in 8 normal subjects at doses of 100 and 200 mg with commercially available Butacote. Phenylbutazone was more rapidly absorbed from ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510030109

    authors: John VA,Goldsborough S,Morrison PJ,Rogers HJ,Spector RG,Bradbrook ID

    更新日期:1982-01-01 00:00:00

  • Pharmacokinetic studies with atenolol in the dog.

    abstract::The pharmacokinetics of the cardioselective beta-adrenoreceptor blocking agent atenolol have been determined following intravenous and oral dosing to the dog. After intravenous administration at 200 mg the blood levels of parent drug were found to decay tri-exponentially with a final elimination phase half-life of abo...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510040306

    authors: McAinsh J,Holmes BF

    更新日期:1983-07-01 00:00:00

  • A quantitative threshold for high/low extent of urinary excretion of compounds in humans.

    abstract::In this study, a quantitative threshold was determined for the high/low extent of urinary excretion (UE) of compounds in humans, using a straightforward but robust statistical method known as receiver operating characteristic curve (ROC) analysis, and also 18 potential physicochemical determinants of UE were evaluated...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2013

    authors: Dave RA,Morris ME

    更新日期:2016-07-01 00:00:00

  • Effect of dietary fibers on losartan uptake and transport in Caco-2 cells.

    abstract::The objective of this study was to assess the effect of dietary fibers on the transport of losartan, an angiotensin II type 1 receptor blocker, in small intestinal cells. Using Caco-2 cells in vitro, losartan uptake and transport were evaluated in the presence of various fibers (cellulose, chitosan, sodium alginate an...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2004

    authors: Iwazaki A,Takahashi N,Miyake R,Hiroshima Y,Abe M,Yasui A,Imai K

    更新日期:2016-05-01 00:00:00

  • Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats.

    abstract::Beta-adrenoceptor blocking drugs are widely used as effective antihypertensive and antianginal agents. We have determined the effect of beta-blockade in the rat to ascertain whether there are differences between metoprolol (MET) and acebutolol (AC) with respect to regional blood flow (RBF). Both AC and MET were admini...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/1099-081x(200005)21:4<121::aid-bdd216>3.0.

    authors: Mostafavi S,Lewanczuk R,Foster R

    更新日期:2000-05-01 00:00:00

  • Quantification and prediction of skin pharmacokinetics of amoxicillin and cefuroxime.

    abstract::The purpose of this project was to develop and validate a pharmacokinetic model and to quantify the rate and extent of distribution between plasma and skin of two beta-lactam antibiotics, amoxicillin (AMX) and cefuroxime (CFX), which are frequently administered systemically to treat skin and skin structure infections....

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.658

    authors: Shukla C,Patel V,Juluru R,Stagni G

    更新日期:2009-09-01 00:00:00

  • Effect of pH, mucin and bovine serum on rifampicin permeability through Caco-2 cells.

    abstract::Rifampicin, a poorly soluble drug, has great importance in therapeutics as it is the main drug used to treat tuberculosis. The characterization of its permeability and the factors that influence it represent an important tool for predicting its bioavailability. Caco-2 cell monolayers were used as models of the intesti...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.1802

    authors: Gonçalves JE,Ballerini Fernandes M,Chiann C,Gai MN,De Souza J,Storpirtis S

    更新日期:2012-09-01 00:00:00

  • Azimilide pharmacokinetics and pharmacodynamics upon multiple oral dosing.

    abstract::This study assessed steady-state azimilide pharmacokinetics and pharmacodynamics in 119 healthy male and female volunteers. Parallel groups of 18-40-year-old subjects received doses of 35, 100, 150 or 200 mg day(-1) for up to 14 days, with 1, 2 or 3 days of loading. Another group of > 55-year-old subjects received 100...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/(sici)1099-081x(199903)20:2<59::aid-bdd155

    authors: Corey A,Al-Khalidi H,Brezovic C,Marcello S,Parekh N,Taylor K,Karam R

    更新日期:1999-03-01 00:00:00

  • Single dose pharmacokinetics of HEPP, a new anticonvulsant in normal healthy volunteers.

    abstract::The pharmacokinetics and the dose proportionality of a new anticonvulsant compound, HEPP (D,L-3-hydroxy-3-ethyl-3-phenylpropionamide) was studied in healthy male volunteers as part of the pharmacological evaluation for new drugs. Study was performed administering doses of 250, 375, 500 and 625 mg of HEPP to six male v...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/(sici)1099-081x(199812)19:9<583::aid-bdd13

    authors: González-Esquivel DF,Rubio-Donnadieu F,Carvajal-Sandoval G,Jung HC

    更新日期:1998-12-01 00:00:00

  • The development of a population physiologically based pharmacokinetic model for mycophenolic mofetil and mycophenolic acid in humans using data from plasma, saliva, and kidney tissue.

    abstract:BACKGROUND:Mycophenolic acid (MPA) is used widely to prevent graft rejection in kidney-transplant patients. Therapeutic drug monitoring (TDM) in plasma requires an invasive procedure that is inconvenient, especially in pediatric patients. TDM in saliva is a more convenient non-invasive alternative compared with plasma....

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2206

    authors: Alsmadi MM,Alfarah MQ,Albderat J,Alsalaita G,AlMardini R,Hamadi S,Al-Ghazawi A,Abu-Duhair O,Idkaidek N

    更新日期:2019-11-01 00:00:00

  • Fluorouracil Uptake in Triple-Negative Breast Cancer Cells: Negligible Contribution of Equilibrative Nucleoside Transporters 1 and 2.

    abstract::Equilibrative nucleoside transporters (ENTs) 1 and 2 reportedly accept fluorouracil as a substrate. Here, we evaluated ENT1/2 expression at the messenger RNA (mRNA), protein, and functional levels in a panel of four triple-negative breast cancer (TNBC) cell lines, BT-549, Hs578T, MDA-MB-231, and MDA-MB-435, and we exa...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2261

    authors: Noguchi S,Takagi A,Tanaka T,Takahashi Y,Pan X,Kibayashi Y,Mizokami R,Nishimura T,Tomi M

    更新日期:2021-01-10 00:00:00

  • Evaluation of a limited sampling method used to determine the bioequivalence of highly variable drugs with long half-lives.

    abstract::The usefulness of a limited sampling method (LSM) to determine the bioequivalence of highly variable drugs with long half-lives was investigated. The LSM uses multiple linear regression of observed drug plasma concentrations versus area under the curve (AUC) or C(max) (peak plasma concentration) to obtain a best set o...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.275

    authors: Jackson AJ

    更新日期:2001-07-01 00:00:00

  • Screening of non-steroidal anti-inflammatory drugs for inhibitory effects on the activities of six UDP-glucuronosyltransferases (UGT1A1, 1A3, 1A4, 1A6, 1A9 and 2B7) using LC-MS/MS.

    abstract::Non-steroidal anti-inflammatory drugs (NSAIDs) are used widely to relieve pain and to decrease inflammation. Several clinical studies have reported that NSAIDs inhibit uridine 5'-diphospho-glucuronosyltransferase (UGT) enzymes. Therefore, the study evaluated the inhibitory potential of 15 NSAIDs on the activities of s...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.1933

    authors: Joo J,Kim YW,Wu Z,Shin JH,Lee B,Shon JC,Lee EY,Phuc NM,Liu KH

    更新日期:2015-05-01 00:00:00

  • The acetylcholinesterase oxime reactivator HI-6 in man: pharmacokinetics and tolerability in combination with atropine.

    abstract::In a double-blind, placebo-controlled, single-dose ascending pharmacokinetics and tolerance study, we evaluated the bispyridinium oxime HI-6 dichloride monohydrate (62.5, 125, 250, and 500 mg), administered intramuscularly with atropine sulphate, 2 mg, in 24 healthy male volunteers. The plasma HI-6 peak concentration ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510160506

    authors: Clement JG,Bailey DG,Madill HD,Tran LT,Spence JD

    更新日期:1995-07-01 00:00:00

  • Pharmacokinetic study of a novel sonosensitizer chlorin-e6 and its sonodynamic anti-cancer activity in hepatoma-22 tumor-bearing mice.

    abstract:PURPOSE:The sonodynamically induced anti-tumor effect of chlorin-e6 (Ce6) was studied in mice bearing hepatoma-22 solid tumors. METHODS:In order to determine the optimum timing of ultrasound exposure after administration of Ce6, the Ce6 concentrations in plasma, skin, muscle and tumor were estimated by measuring the f...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.761

    authors: Shi H,Liu Q,Qin X,Wang P,Wang X

    更新日期:2011-09-01 00:00:00

  • A multiple-dose pharmacokinetic interaction study between didanosine (Videx) and ciprofloxacin (Cipro) in male subjects seropositive for HIV but asymptomatic.

    abstract::The pharmacokinetics of didanosine and ciprofloxacin were evaluated following the administration of multiple oral doses of each drug as a single agent or in combination. Didanosine was dosed as the Videx chewable/dispersible tablet, which contains the antacids dihydroxyaluminum sodium carbonate and magnesium hydroxide...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/(sici)1099-081x(199701)18:1<65::aid-bdd13>

    authors: Knupp CA,Barbhaiya RH

    更新日期:1997-01-01 00:00:00

  • The effect of food on the pharmacokinetics of the bicalutamide ('Casodex') enantiomers.

    abstract::'Casodex' (bicalutamide) is an orally active, non-steroidal, pure antiandrogen; it is a racemate with antiandrogenic activity residing predominantly in the (R)-enantiomer. Healthy male volunteers (n = 15) were administered single oral doses of bicalutamide (50 mg) after food and after fasting as part of a three-treatm...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/(sici)1099-081x(199708)18:6<499::aid-bdd37

    authors: Cockshott ID,Oliver SD,Young JJ,Cooper KJ,DC Jones

    更新日期:1997-08-01 00:00:00

  • Pharmacokinetics of halofantrine in the rat: stereoselectivity and interspecies comparisons.

    abstract::The antimalarial drug, halofantrine, is chiral and is administered clinically as the racemate. In order to define the pharmacokinetic properties of halofantrine enantiomers in the rat, male Sprague-Dawley rats (264-311 g) were given halofantrine HCl orally (n = 5; 14 mg/kg) or intravenously (i.v.) (n = 5; 2 mg/kg). Pl...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199904)20:3<165::aid-bdd17

    authors: Brocks DR,Toni JW

    更新日期:1999-04-01 00:00:00

  • Prednisone and prednisolone interconversion in the rabbit utilizing unbound concentrations.

    abstract::Prednisolone (POH) and prednisone (PO) were both administered via seven different intravenous infusions (three POH and four PO) in each of six rabbits to obtain steady state. Bolus doses of POH and PO were also administered to four of the rabbits. Plasma samples of POH and PO were analyzed by normal phase HPLC. Unboun...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510120608

    authors: Hammarlund-Udenaes M,Benet LZ

    更新日期:1991-08-01 00:00:00