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
Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the ...Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.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.
文摘Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.
