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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４００ｍｇ，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Ｔ１／２Ｋ，Ｋ，Ｔｍａｘ，ｃｍａｘ和ＡＵＣ分别为７．３１和９．４４ｈ，０．１１４和０．０８５６ｈ－１，５．１１和４．８４ｈ，７４．９２和７７．４０μｇ／ｍｌ，１３３９和１５４４（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％。
OBJECTIVE: To determine pharmacokinetics and bioavailability of Tranilast in humans. Methods: Twelve healthy volunteers were randomized, crossover and single-dose poTra tablets or capsules. The plasma concentrations of poTra tablets and capsules were determined by RP-HPLC. The pharmacokinetics was calculated by 3P87 program on computer parameter. Results: T1 / 2K, K, Tmax, cmax and AUC for Tra tablets and capsules were 7.31 and 9.44 h, 0.114 and 0.0856 h-1, 5.11 and 4.84 h, 74.92, respectively And 77.40 μg / ml, 1339 and 1544 (μg · h) / ml respectively. Conclusion: The statistical analysis shows that there is no significant difference in the pharmacokinetic parameters between tablets and capsules (P> 0.05). The bioavailability of tablets relative to capsules is 99.66%.