The influence of bile acids on cefotaxime pharmacokinetics after oral application
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1
University of Novi sad, Department of Pharmacy, Serbia
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2
University of Novi sad, Department of Pharmacology and Toxicology, Serbia
Cefotaxime is poorly absorbed after oral application. The aim of this study was to investigate the pharmacokinetics of cefotaxime sodium (CEF) pharmacokinetics after oral application in the form of sodium 3α,7α-dihydroxy-12-keto-5β-cholanate (MKC) microvesicules (MV) in rat. Thirty Male Wister rats were divided into six groups (n=5 per group). Groups were treated orally with: 1. CEF (15 mg/kg) saline solution (15 mg/kg); 2. CEF (15 mg/kg) saline solution with MKC (2mg/kg); 3. CEF saline solution mixed with blank microvesicules; 4. CEF (15 mg/kg) encapsulated in microvesicules with saline solution; 5. CEF saline solution (15 mg/kg) mixed with blank MKC microvesicules; 6. CEF (15 mg/kg) encapsulated in MKC microvesicules with saline solution. Data were analyzed using noncompartmental model. CEF oral bioavailability was increased twofold when coadministered with MKC and when encapsulated in microvesicules and ninefold when encapsulated in MKC microvesicules compared to the same CEF dose administered orally as saline solution. The increased bioavailability of CEF resulting from the MKC coadministration and CEF encapsulation in microvesicules with MKC suggests that this formulation can extend the application of CEF from parenteral only to oral application.
Keywords:
Bile acids,
Cefotaxime,
pharmacokinetics
Conference:
8th Southeast European Congress on Xenobiotic Metabolism and Toxicity - XEMET 2010, Thessaloniki, Greece, 1 Oct - 5 Oct, 2010.
Presentation Type:
Poster
Topic:
Drug transport
Citation:
Golocorbin-Kon
S,
Mikov
M,
Vukmirovic
M and
Raskovic
A
(2010). The influence of bile acids on cefotaxime pharmacokinetics after oral application.
Front. Pharmacol.
Conference Abstract:
8th Southeast European Congress on Xenobiotic Metabolism and Toxicity - XEMET 2010.
doi: 10.3389/conf.fphar.2010.60.00125
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Received:
05 Mar 2011;
Published Online:
04 Nov 2010.
*
Correspondence:
Dr. Svetlana Golocorbin-Kon, University of Novi sad, Department of Pharmacy, Novi Sad, Serbia, mr.phkon@eunet.rs