枸橼酸莫沙必利胶囊剂人体药动学及相对生物利用度

 目的了解枸橼酸莫沙必利胶囊剂的人体药动学及相对生物利用度。方法采用随机交叉自身对照试验设计,对23名健康男性自愿受试者分别单剂量口服试验制剂枸橼酸莫沙必利胶囊和日本进口的对照制剂枸橼酸莫沙必利片各10 mg,进行人体相对生物利用度研究;采用HPLC测定血浆中莫沙必利浓度,用DAS ver1.0程序进行生物等效性分析。结果受试制剂枸橼酸莫沙必利胶囊与参比制剂枸橼酸莫沙必利片的AUC_0～7分别为(117.31±44.92)及(123.70±44.88)μg·h·L^-1,ρ_max分别为(51.70±20.57)及(65.86±29.96)μg·L^-1,t_max分别为(1.03±0.42)及(0.67±0.33)h,t_1/2分别为(1.63±0.45)及(1.70±0.43)h。结论枸橼酸莫沙必利胶囊与参比制剂经双单侧t检验AUC_0～7和ρ_max检验无显著差异(P<0.05),t_max经非参数法检验差异有统计学意义。受试制剂枸橼酸莫沙必利胶囊与参比制剂的相对生物利用度为(96.7±23.4)%。

Pharmacokinetics and Relative Bioavailability of Mosapride Citrate Capsule in Healthy Volunteers

OBJECTIVE To study the pharmacokinetics and relative bioavailability of mosapride citrate capsule.METHODS A single oral dose of 10 mg mosapride citrate test capsule and reference tablet was given to 23 healthy male volunteers according to a randomized cross-over design. The mosapride citrate concentration in plasma was determined by HPLC method.The pharmacokinetics and bioavailability of the test capsule were compared with the reference tablet.RESULTS The main pharmacokintic parameters of test capsule and reference tablet were as follows: AUC_0～7(117.31±44.92) and(123.70±44.88)μg·h·L^-1,ρ_max(51.70±20.57) and(65.86±29.96) μg·L^-1,t_max(1.03±0.42) and(0.67±0.33) h,respectively.CONCLUSION Through the one two-sided test and the analysis of covariance,no significant difference of the AUC_0～7 and ρ_max between the two formulations is found.The relative bioavailability of the test mosapride citrate capsule is(96.7±23.4)% compared with the reference tablet.The two formulations are bioequivalent.However,the t_max of the test mosapride citrate capsule is longer than the reference tablet.