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. Dosing regimens are usually based on plasma concentration, however, concentrations at the target site are better correlated with the effect. For each antibiotic, three different i.v. bolus doses were administered to three female rabbits according to a randomized cross-over design and plasma samples were collected serially. Skin concentrations were obtained by continuous microdialysis. Skin and unbound plasma concentrations were fitted simultaneously using a semi-physiological model and the transfer constants plasma/skin (K(in)) and skin/plasma (K(out)) were estimated. K(in) and K(out) were then used to predict skin concentrations from the plasma levels obtained from an oral administration of AMX or from an i.v. bolus of CFX. The predicted skin profiles were similar to those measured by microdialysis during the actual experiments. In conclusion, this study shows that it is possible to generate a reasonable prediction of skin pharmacokinetics from any plasma level once a careful characterization of the transfer process between plasma and skin has been made.

journal_name

Biopharm Drug Dispos

authors

Shukla C,Patel V,Juluru R,Stagni G

doi

10.1002/bdd.658

subject

Has Abstract

pub_date

2009-09-01 00:00:00

pages

281-93

issue

6

eissn

0142-2782

issn

1099-081X

journal_volume

30

pub_type

杂志文章
  • Pharmacokinetics and tissue distribution of intravenous pefloxacin for antibiotic prophylaxis in biliary surgery.

    abstract::The plasma levels and tissue penetration of pefloxacin were studied after prophylactic administration to patients undergoing elective biliary surgery. Pefloxacin was administered as a single dose of 800 mg given intravenously as an infusion 1 h before surgery. Over a period of two years, cultures of bile and stone wer...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.321

    authors: Gascón AR,Campo E,Olea E,Hernández RM,Calvo B,Errasti J,Pedraz JL

    更新日期:2002-10-01 00:00:00

  • Effect of dehydration on the disposition kinetics of erythromycin in rabbits.

    abstract::The effect of water deprivation on the physiologic, biochemical, and disposition parameters of erythromycin was investigated in rabbits. The packed cell volume, plasma glucose, and total lipid concentration increased significantly in dehydration. The pharmacokinetic parameters of erythromycin after intravenous adminis...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510130202

    authors: Ahmad M,Niazi SK,Ahmad T,Muzaffar NA,Nawaz M

    更新日期:1992-03-01 00:00:00

  • In vivo predictive release methods for medicated chewing gums.

    abstract::Understanding the performance of a drug product in vivo plays a key role in the development of meaningful in vitro drug release methodology. In case of functional chewing gums, the mode and the mechanism of release and the site of application differ significantly from other conventional solid oral dosage forms and req...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.1796

    authors: Gajendran J,Kraemer J,Langguth P

    更新日期:2012-10-01 00:00:00

  • The pharmacokinetics of ethosuximide enantiomers in the rat.

    abstract::A chiral gas chromatographic assay previously developed for quantitative analysis of ethosuximide and its major metabolites in rat urine has been adapted for the analysis of the drug in plasma. Ethosuximide, both as a racemic mixture and as the individual enantiomers, was administered to conscious rats by the intraven...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.266

    authors: Mifsud J,Collier PS,Millership JS

    更新日期:2001-03-01 00:00:00

  • Acyl glucuronides: the good, the bad and the ugly.

    abstract::Acyl glucuronidation is the major metabolic conjugation reaction of most carboxylic acid drugs in mammals. The physiological consequences of this biotransformation have been investigated incompletely but include effects on drug metabolism, protein binding, distribution and clearance that impact upon pharmacological an...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,评审

    doi:10.1002/bdd.720

    authors: Regan SL,Maggs JL,Hammond TG,Lambert C,Williams DP,Park BK

    更新日期:2010-10-01 00:00:00

  • p-Hydroxymethamphetamine enantiomer pharmacokinetics and metabolism in rats: absence of N-demethylation.

    abstract::p-hydroxymethamphetamine (OHMAP) is one of the major metabolites of the widely abused drug methamphetamine (MAP). The demethylation of OHMAP to p-hydroxyamphetamine (OHAP) has been shown in vitro but has never been reported in vivo. The disposition kinetics as well as the metabolism of OHMAP was investigated employing...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199707)18:5<423::aid-bdd30

    authors: Hutchaleelaha A,Mayersohn M

    更新日期:1997-07-01 00:00:00

  • Influence of coptis Chinensis on pharmacokinetics of flavonoids after oral administration of radix Scutellariae in rats.

    abstract::Radix Scutellariae (RS) and Coptis Chinensis (CC) are the most popular components in traditional Chinese medicine prescriptions. Flavonoids are the main effective ingredients in RS and berberine is the main effective ingredient in CC. The aim of this study was to determine the influence of CC on the pharmacokinetics o...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.674

    authors: Shi R,Zhou H,Liu Z,Ma Y,Wang T,Liu Y,Wang C

    更新日期:2009-10-01 00:00:00

  • Pharmacokinetics of stobadin and of the sum of its metabolites in rats during repeated administration.

    abstract::Stobadin dihydrochloride was administered p.o. to rats at a dose of 1 mg kg-1 once daily for 25 consecutive days. The peak and trough concentrations of the sum of stobadin metabolites, determined from Days 6-16 of treatment, demonstrated a steady-state. The mean daily excretion of 3H-radioactivity during this period w...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510120304

    authors: Kállay Z,Soltés L,Trnovec T

    更新日期:1991-04-01 00:00:00

  • Relative lung and systemic bioavailability of sodium cromoglycate inhaled products using urinary drug excretion post inhalation.

    abstract::The relative lung and systemic bioavailability of sodium cromoglycate following inhalation by different methods have been determined using a urinary excretion pharmacokinetic method. On three separate randomised study days, 7 days apart, subjects inhaled (i) 4x5 mg from an Intal metered dose inhaler (MDI), (ii) 4x5 mg...

    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.308

    authors: Aswania O,Chrystyn H

    更新日期:2002-05-01 00:00:00

  • Effect of concomitant colestipol hydrochloride administration on the bioavailability of diltiazem from immediate- and sustained-release formulations.

    abstract::Effects of concomitant colestipol administration on plasma concentrations of diltiazem and desacetyldiltiazem from immediate-release (IR) and sustained-release (SR) formulations were assessed in two studies. In the first study, 12 subjects received 120-mg diltiazem hydrochloride (diltiazem) SR capsules or 120-mg dilti...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.330

    authors: Turner SW,Jungbluth GL,Knuth DW

    更新日期:2002-12-01 00:00:00

  • 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

  • Effects of proton pump inhibitors and famotidine on elimination of plasma methotrexate: Evaluation of drug-drug interactions mediated by organic anion transporter 3.

    abstract::Methotrexate (MTX) is an antifolate agent used in the treatment of numerous types of cancer, and eliminated by active tubular secretion via organic anion transporter 3 (OAT3). Gastric antisecretory drugs, such as proton pump inhibitors (PPIs) and histamine H2 receptor antagonists, are widely used among patients with c...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2091

    authors: Narumi K,Sato Y,Kobayashi M,Furugen A,Kasashi K,Yamada T,Teshima T,Iseki K

    更新日期:2017-12-01 00:00:00

  • Exploring the compatibility mechanism of ShengDiHuang Decoction based on the in situ single-pass intestinal perfusion model.

    abstract::Affecting the absorption of active ingredients in the intestine serves as one of the important compatibility mechanisms of traditional Chinese medicine. The aim of this study was to investigate the compatibility mechanism of ShengDiHuang Decoction (SDHD) by using the single-pass intestinal perfusion in situ model. The...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2211

    authors: Yang H,Hao Q,Cheng J,Wang M,Zou J,Zhang X,Guo D

    更新日期:2020-02-01 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

  • Influence of leucine on intestinal baclofen absorption as a model compound of neutral alpha-aminoacids.

    abstract::The inhibitory effect of the essential alpha-aminoacid L-leucine on the intestinal absorption of the antispastic drug baclofen was examined by means of an in situ rat gut perfusion technique. When 0.5 mM baclofen solutions were perfused in the presence of increasing concentrations of the aminoacid (5-100 mM), the appa...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510160705

    authors: Cercós-Fortea T,Polache A,Nácher A,Cejudo-Ferragud E,Casabó VG,Merino M

    更新日期:1995-10-01 00:00:00

  • Aspects of the clinical pharmacology of nifedipine, a dihydropyridine calcium-entry antagonist.

    abstract::Although nifedipine has been characterized in terms of its general vasodilatory effects, this dihydropyridine must still be regarded as investigational with regard to available pharmacokinetic and pharmacodynamic data. Although limited studies are available, it is clear that the pharmacokinetic and pharmacodynamic dat...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,评审

    doi:10.1002/bdd.2510070102

    authors: Hamann SR,Piascik MT,McAllister RG Jr

    更新日期:1986-01-01 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

  • The effect of caffeine on the pharmacokinetics of acetaminophen in man.

    abstract::The influence of caffeine (60 mg) was studied on the pharmacokinetic characteristics of acetaminophen (500 mg single dose) in ten healthy male human volunteers in a complete cross-over design. A high-performance liquid chromatography (HPLC) method was used to analyse serum drug concentrations. Caffeine caused a highly...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.2510160606

    authors: Iqbal N,Ahmad B,Janbaz KH,Gilani AU,Niazi SK

    更新日期:1995-08-01 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 effect of administration of propranolol on the pharmacokinetics of isoxicam.

    abstract::In order to examine a potential interaction between isoxicam and propranolol, single 200 mg doses of isoxicam were administered to ten healthy male volunteers before and during treatment with propranolol, gradually attaining a dose of 80 mg t.i.d. for 11 days. The pharmacokinetic profiles of the isoxicam plasma concen...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510070109

    authors: Caillé G,Larivière L,Lacasse Y,Vézina M,Besner JG

    更新日期:1986-01-01 00:00:00

  • Simultaneous modelling of mexiletine and hydroxy-methyl-mexiletine data after single- and multiple-dose administration of a sustained-release mexiletine formulation.

    abstract::The pharmacokinetics of mexiletine and its metabolite hydroxy-methyl-mexiletine have been investigated following single-dose and during multiple-dose administration of a sustained-release form of mexiletine to six post-myocardial infarct patients. Comparison of single-dose and washout pharmacokinetics, after short-ter...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510130702

    authors: Bruno R,Santoni Y,Iliadis A,Djiane P,Serradimigni A,Cano JP

    更新日期:1992-10-01 00:00:00

  • Gender differences in pharmacokinetics of lumefantrine and its metabolite desbutyl-lumefantrine in rats.

    abstract::Lumefantrine has been reported to be mainly bio-transformed by cytochrome P450 isozyme 3A4 to desbutyl-lumefantrine (DLF) in human liver microsomes. Since CYP3A is expressed in a sex specific manner in rats, it could be expected that the pharmacokinetics of lumefantrine would be changed in male rats compared with thos...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.1786

    authors: Wahajuddin,Singh SP,Jain GK

    更新日期:2012-05-01 00:00:00

  • The relative bioavailability of a commercial propranolol hydrochloride tablet in man.

    abstract::A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation. Based on plasma levels of propranolol for the 24 h following administration of 2 x 40 mg oral propranolol hydrochlo...

    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.2510030204

    authors: Roscoe R,Cooper J,Wilson TW,Joshi NN,Midha KK

    更新日期:1982-04-01 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

  • Pharmacokinetics of dihydroartemisinin in Artekin tablets for single and repeated dosing in Chinese healthy volunteers.

    abstract::Aim. To study the pharmacokinetics of dihydroartemisinin (DHA) in Artekin (compound dihydroartemisinin) tablets in Chinese healthy volunteers. Methods. Eighteen healthy volunteers (9 males, 9 females) received Artekin tablets for oral administration. The plasma samples of DHA were analysed by liquid-liquid extraction ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.607

    authors: Hong X,Liu CH,Huang XT,Huang TL,Ye SM,Ou WP,Wang NS,Mi SQ

    更新日期:2008-05-01 00:00:00

  • The effect of oral dose volume on the absorption of a highly and a poorly water-soluble drug in the rat.

    abstract::The influence of dose volume on drug absorption following oral administration of a highly and a poorly water soluble drug was examined in male Sprague-Dawley rats. A constant mass of each 14C-labeled compound was given via gavage in dose volumes of 1, 5, 10, and 20 mL kg-1. Blood levels, as well as the quantitative ex...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510150508

    authors: Nickerson DF,Weaver ML,Tse FL

    更新日期:1994-07-01 00:00:00

  • Transport characteristics of candesartan in human intestinal Caco-2 cell line.

    abstract::The intestinal absorptive characteristics and the efflux mechanisms of candesartan (CDS), a novel angiotensin II type 1 receptor blocker, were investigated. The Caco-2 cells were used as models of the intestinal mucosa to assess uptake and transport of CDS. The determination of CDS was performed by HPLC-Flu. In the Ca...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.664

    authors: Zhou L,Chen X,Gu Y,Liang J

    更新日期:2009-07-01 00:00:00

  • Pharmacokinetics of controlled-release verapamil in healthy volunteers and patients with hypertension or angina.

    abstract:AIMS:To study the dose-ranging population pharmacokinetics of controlled release verapamil in healthy subjects and patients with angina or hypertension. To characterize the pharmacodynamics of controlled-release verapamil in patients with hypertension. METHODS:Dose-ranging studies were conducted in healthy volunteers ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.289

    authors: Gupta S,Modi NB,Sathyan G,Ho Pl PL,Aarons L

    更新日期:2002-01-01 00:00:00

  • Comparative bioavailability and steady state fluctuations of Tegretol commercial and carbamazepine OROS tablets in adult and pediatric epileptic patients.

    abstract::The comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients. Tegretol commercial tablets were dosed according to previously esta...

    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.2510130802

    authors: Thakker KM,Mangat S,Garnett WR,Levy RH,Kochak GM

    更新日期:1992-11-01 00:00:00

  • Bioactivation of loxoprofen to a pharmacologically active metabolite and its disposition kinetics in human skin.

    abstract::Loxoprofen (LX) is a prodrug-type non-steroidal anti-inflammatory drug which is used not only as an oral drug but also as a transdermal formulation. As a pharmacologically active metabolite, the trans-alcohol form of LX (trans-OH form) is generated after oral administration to humans. The objectives of this study were...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.1945

    authors: Sawamura R,Sakurai H,Wada N,Nishiya Y,Honda T,Kazui M,Kurihara A,Shinagawa A,Izumi T

    更新日期:2015-09-01 00:00:00