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

The aim of ths study was to investigate the pharmacokinetics of cefotaxime sodium (CEF) pharmacokinetics after oral application in the form of sodium 3alpha,7alpha-dihydroxy-12-keto-5beta-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 encapsulated 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.