尼美舒利分散片临床药代动力学和相对生物利用度研究

目的 进行尼美舒利分散片的药代动力学研究, 并与国产尼美舒利片进行生物等效性比较。方法 20名健康男性志愿者采用自身交叉给药方案, 分别单剂量口服100 mg 供试品或对照品后, 用高效液相色谱紫外检测法测定血浆药物浓度。结果 单剂量口服尼美舒利分散片后体内过程符合开放式血管外一室模型, 其c_max为(3.91 ±0.74) μg·ml^-1, t_(1/2) β为(3.40 ±0.78) h, t_max为(3.15 ±0.67) h, AUC_0~24为(31.92 ±6.36) μg·h·ml^-1, 与对照品的主要药代动力学参数比较无显著性差异(P >0.05)。供试品相对于对照品的生物利用度为(96.43 ±8.41) %。结论 两制剂体内过程相仿, 具有生物等效性。

Pharmacokinetics and bioavialability of nimesulide dispersible tablet

Aim To study the pharmacokinetics and bioequivalence of nimesulide dispersible tablet and its normal tablet. Methods 20 healthy volunteers were treated with a single oral dose of domesticc nimesulide dispersible tablet or normal tablet (control) in a randomized crossover study and the plasma drug concentration was determined by HPLC. Results The plasma concentration-time curve was fitted to the one-compartment model. The pharmacokinetic parameters obtained were: c_max (3.91 ±0.74) μg ·ml^-1, t_(1/2) β (3.40 ±0.78) h, t_max (3.15 ±0.67) h, AUC_0~24 (31.92 ±6.36) μg·ml·h^-1, there was no significant difference between the active and control groups. The relative bioavailability obtained was (96.43 ±8.41) %.Conclusion The pharmacokinetic profile for the 2 tablets was similar so it may be concluded that they are bioequivalent.