Abstract

FORMULATION AND PHARMACOKINETIC (IN-VITRO AND IN-VIVO) EVALUATION OF CEFIXIME MICROSPHERES

Mallikarjun Vasam* and Raja Sridhar Rao Ponugoti

ABSTRACT

Objective: The present study determined the antimicrobial activity and permeability of Cefixime from optimized formulation by comparing with pure drug from prepared microspheres. Method: Microspheres were prepared by ionic gelation technique with different concentrations of polymers to sustain release of drug for 12hrs. The in-vivo studies were done to evaluate various pharmacokinetic parameters like maximum plasma drug concentration (Cmax), area under the plasma concentration-time curve from time zero to infinity (AUC0-∞), area under the plasma concentration-time curve from time zero to time t (AUC0-t), elimination half life (t1/2), time to reach maximum concentration following drug administration (Tmax) and elimination rate constant from central compartment (Kel) for the comparison of optimized formulation and pure drug of Cefixime. Results: From the pharmacokinetic evaluation, the optimized formulation of microspheres produced Cmax of 4.86 ± 1.42 (mcg/ml) and Tmax of 3.00 ± 0.3 at 3h. The 90% confidence intervals for Cmax were 92.99-107.70, for AUC0-t were 93.03-108.10 and for AUC0-∞ were 93.56-118.06. Conclusion: The developed microspheres were evaluated for in-vitro and in-vivo studies and showed good entrapment and bioavailability of drug. The calculated confidence intervals were meeting the bioavailability criteria (within the limit of 80 -125) with respect to the rate and extent of absorption for Cefixime under fasting conditions.

Keywords: Cefixime, Microspheres, ionic gelation technique.