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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。
The double-crossover design was used to determine the plasma concentration in different phases by HPLC-UV method and the pharmacokinetics analysis was carried out. The results showed that 10 healthy volunteers received oral administration of 200 mg of the test preparation and reference tablets respectively The drug-time curves are in line with the one-room open model. The main pharmacokinetic parameters of nimesulide capsules and tablets were T1 / 2K (h), 4.25 ± 0.58 and 4 67 ± 0.45, Cmax (mg.L-1) and 928 ± 220 and 8.92 ± 2.48; Tmax (h), 2.88 ± 0.51 and 2.79 ± 0.55; MRT (h), 9.30 ± 0.92 and 950 ± 060; AUC0- 24 (mg · h · L-1), 87.02 ± 26.88 and 86.98 ± 25.33, respectively. There was no significant difference between these parameters by ANOVA (P <0.05). The relative bioavailability (F%) of nimesulide capsules to the tablets was: 100.54 ± 11.01. The AUC, Cmax, Tmax and lnAUC, lnCmax, lnTmax showed no significant difference by ANOVA under the cross test. The bioavailability of nimesulide capsules and tablets was proved by double unilateral test.