盐酸丁咯地尔片的生物利用度及药代动力学研究

THE STUDY ON PHARMACOKINETICS OF BUFLOMEDIL HYDROCHLORIDE TABLET IN HEALTHY VOLUNTEERS

为比较国产盐酸丁咯地尔片剂和进口盐酸丁咯地尔（活脑灵）片剂的药代动力学参数，求出国产制剂的生物利用度，将１２ 名健康志愿者随机分为２ 组，分别单次口服国产盐酸丁咯地尔片及进口活脑灵片３００ｍ ｇ，用ＨＰＬＣ法测定血药浓度，采用３Ｐ９７ 程序处理实验数据，进行药代动力学和相对生物利用度研究。结果表明，口服国产和进口两种制剂的药时曲线均符合一室模型，血药峰浓度Ｃｍ ａｘ 分别为（１．９５±０．４２）ｍ ｇ／Ｌ和（２．００±０．５７）ｍ ｇ／Ｌ，达峰时间Ｔｐｅａｋ 分别为（２．４２±０．６３）ｈ 和（２．４８±０．４６）ｈ，药时曲线下面积ＡＵＣ分别为（１６．１６±３．４６）ｍ ｇ／Ｌ·ｈ 和（１６．２１±２．８２）ｍ ｇ／Ｌ·ｈ。两组参数差别均无统计学意义（Ｐ＞０．０５）。国产盐酸丁咯地尔片剂与进口活脑灵片剂相比，相对生物利用度为（１００．７±１９．１）％ 。

In order to compare the pharmacokinetics parameters of the domestic Buflomedil hydrochloride tablet with the imported Fonzylane tablet and obtained the bioavailability of domestic Buflomedil hydrochloride tablet and provide the theoretical basis for the reasonable use of the drug in the clinic, the 12 healthy male volunteers were divided into two groups by the randomized crossover method, the test group and the control group. A single oral dose 300mg of domestic Buflomedil hydrochloride tablet or imported Fonzylane tablet was given to each group respectively. The serum concentrations were determined with HPLC. The serum concentration time parameters were analyzed by 3P97 computer software and obtained the relevant pharmacokinetics parameters and the relative bioavailability. Took domestic buflomedil hydrochloride tablet concentration time curve fitted one compartment model. The main pharmacokinetics parameters of domestic Buflomedil hydrochloride and imported Fonzylane tablets were as follows respectively. Cmax=(1.95±0.42)mg/L and (2.00±0.57)mg/L, Tmax=(2.42±0.63)h and (2.48±0.46)h,AUC=(16.16±3.46)mg/L·h,and (16.21±2.82)mg/L·h. Compared the domestic Buflomedil hydrochloride tablet with the imported Fonzylane tablet and obtained the bioavailability: (100.7±19.1)%. As the result of analysis of variance and (1 2a) confidential interval, two one side test, the AUC values of the two formulations were no significant difference between the formulations, periods and individuals. It proved that domestic Buflomedil hydrochloride tablet and imported Fonzylane tablet were bioequivalent.