This study aimed to develop hydrophilicmatrix based controlled release gastroretentive drug delivery system of ofloxacin and conducting its in vitro and in vivo evaluations.Effervescent floating gastroretentive drug d...This study aimed to develop hydrophilicmatrix based controlled release gastroretentive drug delivery system of ofloxacin and conducting its in vitro and in vivo evaluations.Effervescent floating gastroretentive drug delivery system of ofloxacin was prepared utilizing Boxe Behnken statistical design with 3 factors,3 levels and 15 experimental trials.Formulation optimization was done by setting targets on selected responses.In vivo studies were carried out for the optimized formulation with 12 healthy human volunteers and obtained pharmacokinetic parameters were compared with themarketed once daily formulation,“Zanocin OD”.Optimized formulation showed satisfactory controlled in vitro drug release for more than 12 h with excellent buoyancy properties(floating lag time<1 min,floating duration>16 h).Optimized and marketed formulations were found to have similar in vitro release profile(f2¼79.22)and also were found to be bioequivalent.Serum ofloxacin concentration was well maintained above its reported minimum inhibitory concentrations for most of the pathogens for sufficiently longer duration.Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product despite their bioequivalence.Bettertherapeutic effect can be expected since ofloxacin exhibits concentration dependent killing.Hence,gastroretention can be a promising approach to enhance bioavailability of ofloxacin with narrow absorption window in upper GIT.展开更多
文摘This study aimed to develop hydrophilicmatrix based controlled release gastroretentive drug delivery system of ofloxacin and conducting its in vitro and in vivo evaluations.Effervescent floating gastroretentive drug delivery system of ofloxacin was prepared utilizing Boxe Behnken statistical design with 3 factors,3 levels and 15 experimental trials.Formulation optimization was done by setting targets on selected responses.In vivo studies were carried out for the optimized formulation with 12 healthy human volunteers and obtained pharmacokinetic parameters were compared with themarketed once daily formulation,“Zanocin OD”.Optimized formulation showed satisfactory controlled in vitro drug release for more than 12 h with excellent buoyancy properties(floating lag time<1 min,floating duration>16 h).Optimized and marketed formulations were found to have similar in vitro release profile(f2¼79.22)and also were found to be bioequivalent.Serum ofloxacin concentration was well maintained above its reported minimum inhibitory concentrations for most of the pathogens for sufficiently longer duration.Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product despite their bioequivalence.Bettertherapeutic effect can be expected since ofloxacin exhibits concentration dependent killing.Hence,gastroretention can be a promising approach to enhance bioavailability of ofloxacin with narrow absorption window in upper GIT.
