曲尼司特在人体内的药动学及生物利用度研究

 目的：测定曲尼司特(Tra)在人体内的药动学及生物利用度。方法：健康志愿者12人，随机、交叉、单剂量poTra片剂或胶囊400 mg,采用反相高效液相色谱法测定不同时间血药浓度，在计算机上以3P87程序拟合处理，计算药动学参数。结果：Tra片剂和胶囊的T_1/2K,K,T_max,c_max和AUC分别为7.31和9.44 h,0.114和0.085 6 h^-1,5.11和4.84 h,74.92和77.40 μg/ml,1 339和1 544 (μg·h)/ml。结论：经统计学分析表明，片剂与胶囊剂之间的药动学参数无显著性差异(P＞0.05)，片剂相对于胶囊的生物利用度为99.66%。

Pharmacokinetics and relative bioavailability of tranilast in healthy volunteers

OBJECTIVE:To investigate the pharmacokinetics and relative bioavailability of tranilast in healthy volunteers.METHOD:The blood level of tranilast at different times after single oral administration of 400 mg of tranilast tablets and capsules was determined by reversed-phase HPLC.The 3P87 program was used for the calculation of pharmacokinetic parameters on computer.RESULTS:The T_1/2K,K,T_max,c_max and AUC of the tranilast tablet and capsule were 7.31 and 9.44 h,0.114 0 and 0.085 6 h^-1,5.11 and 4.84 h,74.92 and 77.40 μg/ml,1 339 and 1 544 (μg·h)/ml,respectively.CONCLUSION:The statistical analysis for the pharmacokinetic parameters showed that there was no significant difference between tablet and capsule(P＞0.05).The relative bioavailability of tablets was 99.66%.