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Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat

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Summary

The aim of ths 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) microvesicles (MV) in rat. Thirty Male Wister rats were divided into six groups (n=5 per group). Groups were treated orally with: i. CEF (15 mg/kg) saline solution (15 mg/kg); ii. CEF (15 mg/kg) saline solution with MKC (2 mg/kg); iii. CEF saline solution mixed with blank microvesicles; iv. CEF (15 mg/kg) encapsulated in microvesicles with saline solution; v. CEF saline solution (15 mg/kg) mixed with blank MKC microvesicules; vi. 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 microvesicles and ninefold when encap-sulated in MKC microvesicles compared to the same CEF dose administered orally as saline solution. The increased bioavailability of CEF resulting from CEF encapsulation in microvesicules with MKC suggests that this formulation can extend the application of CEF from parenteral only to oral application.

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Authors and Affiliations

  1. Department of Pharmacy, Medical Faculty Novi Sad, Haj-duk Veljkova 3, 21000, Novi Sad, Serbia

    Svetlana Golocorbin-Kon

  2. Department of Pharmacology and Toxicology, Medical Faculty Novi Sad, Haj-duk Veljkova 3, 21000, Novi Sad, Serbia

    Momir Mikov, Ivan Mikov, Majda Sahman-Zaimovic & Zdenko Tomic

  3. School of Pharmacy, University of Otago, Dunedin, New Zealand

    Mousab Arafat

  4. Faculty of Chemical Technology, University of Novi Sad, Serbia

    Zika Lepojevic

Authors
  1. Svetlana Golocorbin-Kon
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  2. Momir Mikov
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Golocorbin-Kon, S., Mikov, M., Arafat, M. et al. Cefotaxime pharmacokinetics after oral application in the form of 3α,7α-dihydroxy-12-keto-5β-cholanate microvesicles in rat. Eur. J. Drug Metabol. Pharmacokinet. 34, 31–36 (2009). https://doi.org/10.1007/BF03191381

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  • DOI: https://doi.org/10.1007/BF03191381

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