萘哌地尔胶囊和片剂在中国健康男性志愿受试者的生物等效性比较

目的: 以萘哌地尔片剂为对照, 研究萘哌地尔胶囊的人体药动学过程和生物等效性。方法: 18 名健康成年男性志愿者采用随机分组自身交叉对照试验设计方法, 采用HPLC-荧光检测, 血样最低定量限为1 μg ·L^-1, 平均绝对回收率85.2 %~ 89.9 %, 日内、日间变异系数(RSD) 小于8.05 %。血浆标准曲线在1.56 ~ 400 μg·L^-1 范围内相关性良好, r =1 。结果: 萘哌地尔胶囊和片剂的主要药动学参数为:T_max:0.63±0.24 和0.57±0.21 h ;C_max:129.1±60.7和138.3±72.5 μg·L^-1 ;T1 2:5.9±1.7 和6.4±2.1 h ;AUC_0-24:295.6±90.9 和291.6±89.3 μg·L^-1 ·h-1 ;AUC_0-∞:320±97.2 和318.0±98.3 μg·L^-1 ·h^-1 。萘哌地尔胶囊的相对生物利用度F_0-24 、F_0-∞分别为101.9 %±12.9 %和101.2 %±12.3 %。结论: 两种制剂生物等效。

Bioequivalence of naftopidil capsule vs tablet in Chinese healthy male volunteers

AIM: To study the pharmacokinetics and relative bioavailability of naftopidil in healthy male volunteers .METHODS: The naftopidil concentrations in plasma were determined by HPLC.The test and reference formulations of naftopidil were given to 18 healthy male volunteers .The calibration curve was linearwithin the range of 1.6-400 μg·L^-1, r =1.The minimum detection limit was 1 μg·L^-1.The mean recovery rate was 85.2 % -89.9 %, RSDs of inter-day and intra-day were no more than 8.0 %.RESULTS: After a single oral dose of 50 mg naftopidil test capsules or reference tablets, the main pharmacokinetic parameters AUC_0-24:295.6±90.9 and 291.6±89.3 μg·L^-1 ·h-1 ;AUC_0-∞:320.0±97.2 and 318.0±98.3 μg·L^-1·h^-1 ;T_max:0.6±0.2 and 0.6±0.2 h ;C_max:129.1±60.7 and 138.3±72.5μg·L^-1 ;T1 2:5.9±1.7 and 6.4±2.1 h, respectively.The relative bioavailability F_0-24, F_0-∞ were 101.9±12.9 % and 101.2±12.3 %, respectively.CONCLUSION: No significant difference exists among the pharmacokinetic parameters for the test capsules and the reference tablets of naftopidil.The two formulations were bioequivalent.