【摘要】 采用双交叉试验设计，用ＨＰＬＣ－ＵＶ法测定不同时相的血药浓度，进行药代动力学分析，结果表明：１０名健康志愿者分别一次口服受试制剂及参比片剂 ２００ ｍｇ后所得的药时曲线均符合一室开放模型。尼美舒利胶囊与片剂的主要药动学参数分别为：Ｔ１／２Ｋ（ｈ），４．２５±０．５８和４ ６７±０．４５；Ｃｍａｘ（ｍｇ．Ｌ－１），９２８±２２０和８．９２±２．４８；Ｔｍａｘ（ｈ），２．８８±０．５１和２．７９±０．５５；ＭＲＴ（ｈ），９．３０±０．９２和９５０±０６０；ＡＵＣ０－２４（ｍｇ·ｈ·Ｌ－１），８７．０２±２６．８８和８６．９８±２５．３３；这些参数经方差分析法证明无显著性差异（Ｐ＜０．０５）。尼美舒利胶囊对片剂的相对生物利用度（Ｆ％）为：１００·５４±１１．０１。两者的ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ 及ｌｎＡＵＣ、ｌｎＣｍａｘ、ｌｎＴｍａｘ经交叉试验下的方差分析法证明无显著性差异，经双单侧检验证明尼美舒利胶囊与片剂具有生物等效性。更多还原

【Abstract】 Objective: to compare the pharmacokinetics and bioavailability of nimesulide capsules with nimesulide tablets. Method: a single 200 mg oral dose of nimesulide capsule or tablet was given to 10 healthy male volunteers in a randomized double cross-over study. Plasma levels of nimesulide were detected by HPLC-U V method. Results: The pharmacokinetic parameters of nimesulide capsules and tablets were as follewed: T1/2K (h):4. 25 ±0. 58 and 4. 67 ±0. 45;Cmax (mg. L -1 ):9. 28 ± 2. 20 and 8. 92 ± 2. 48;Tmax (h):2. 88 ± 0. 51 and 2. 79 ±0. 55;MRT(h):9. 30 ± 0. 92 and 9. 50 ± 0. 60; AUC0-24 (mg. h. L - 1 ): 87. 02 ± 26. 88 and 86. 98 ± 25. 33 respectively. The relative bioavailability of nimesulide capsule was 100. 54 ± 11. 01 %. There were no significant differences between pharmacokinetic parameters for the two formulations of nimesulide(P > 0. 05 ). The nimesulide capsules showed bioequivalence compared with the tablets.更多还原