IMPROVEMENT OF BIOAVAILABILITY OF CEFUROXIME AXETIL ORAL SUSPENSION BY INCLUSION COMPLEXATION METHOD
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2016, Vol 8, Issue 3
Abstract
Objective: Cefuroxime axetil, a prodrug of Cefuroxime, is a poorly water soluble drug, thus it has got only limited solubility and dissolution rate in gastric fluids. Also, the bioavailability of Cefuroxime axetil oral suspension is only 40-45% when compared to the 60% bioavailability of tablets. The objective of this study was to develop an oral suspension of Cefuroxime axetil with improved oral bioavailability by inclusion complexation method using Hydroxypropyl beta cyclodextrin [HP-Beta-cylcodextrin]Methods: The complexation of Cefuroxime axetil and HP-Beta cyclodextrin was carried out at 1:1, 1:2, 1:2.5 and 1:3 ratios respectively. The prepared suspensions were evaluated for various parameters like pH, viscosity, re-dispersibility, pourability, and assay and in-vitro dissolution profile. A leading marketed product and the optimized formulation were evaluated for the pharmacokinetic parameters like Cmax, AUC0-t, AUC0-∞ and Tmax in healthy adult male rabbits.Results: Considering the in-vitro dissolution profile, formulation with 1:2.5 ratios of Cefuroxime axetil and HP-Beta cyclodextrin was selected as the optimized formulation. The Cmax of Optimized formulation and Marketed product were 148±1.26ng/ml and 126±1.52 ng/ml respectively, and the AUC0-t ofOptimized formulation and Marketed product were 989±16.42 ng. h/ml and 613±24.26 ng. h/ml respectively, which shows a significant improvement in the bioavailability of optimized formulationConclusion: From the results obtained it can be observed that there is a significant improvement in the bioavailability of optimized formulation compared to the marketed product. This demonstrates that the inclusion complexation method with HP-Beta cyclodextrin can significantly improve the oral bioavailability of Cefuroxime axetil.Keywords: Cefuroxime axetil, Bioavailability, Beta cyclodextrin, Inclusion complexation
Authors and Affiliations
Renju Prabhakaran, Janakiraman K. , Jyoti Harindran
Keywords
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