尼美舒利分散片临床药代动力学和相对生物利用度研究

Pharmacokinetics and bioavialability of nimesulide dispersible tablet

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 2 0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 10 0mg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cmax为 (3.91± 0 .74 ) μg·ml- 1,t( 1/2 ) β为 (3.4 0± 0 .78)h ,tmax为 (3.15± 0 .6 7)h ,AUC0～ 2 4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 .0 5 )。供试品相对于对照品的生物利用度为 (96 .4 3± 8.4 1) %。结论 两制剂体内过程相仿 。

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 domestic 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.