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Improvement of bioavailability of taste masked cefuroxime axetil oral suspension using hydroxy propyl-betacyclodextrin | Abstract
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Abstract

Improvement of bioavailability of taste masked cefuroxime axetil oral suspension using hydroxy propyl-betacyclodextrin

Author(s): Renju Prabhakaran, Janakiraman K. and Jyoti Harindran

Cefuroxime axetil is a prodrug of Cefuroxime, which is a second generation cephalosporin antibiotic with activity against wide range of organisms. Cefuroxime axetil is extremely bitter in taste, which reduces the patient compliance when taken as oral suspension especially in pediatric population. Also the bioavailability of oral suspension is only 40-45% when compared to 60% bioavailability of tablets, therefore the oral suspension and tablets cannot be substituted each other on mg/mg basis. The objective of this study was to improve the bioavailability of oral suspension and also to mask the bitter taste of Cefuroxime axetil using Hydroxy propyl betacyclodextrin by inclusion complexation method. The complexation of Cefuroxime axetil and Hydroxy Propyl betacyclodextrin 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, redispersibility, pourability, Assay, invitro dissolution profile and taste. Considering the invitro dissolution profile and taste evaluation with marketed product, formulation with 1:2.5 ratio of Cefuroxime axetil and Hydroxy propyl betacyclodextrin was selected as the optimized formulation. The marketed product and optimized formulation were evaluated for the pharamacokinietic parameters like Cmax, AUC0-t, AUC0-∞ and Tmax in healthy adult male rabbits. From the results obtained it can be observed that there is significant improvement in the bioavailabvility of optimized formulation, compared to the marketed product. This demonstrates that the inclusion complexation method with Hydroxy Propyl betacyclodextrin can effectively mask the bitter taste and significantly improve the oral bioavailability of Cefuroxime axetil.