奥硝唑片在健康人体的生物等效性

Bioequivalence of ornidazole tablets in Chinese healthyvolunteers

目的评价奥硝唑片(抗厌氧菌药)试验制剂与国产上市剂型在健康人体的生物等效性。方法 22例健康男性受试者随机分组,按照自身对照单次口服奥硝唑片1500 mg后,用高效液相色谱法测定血浆中奥硝唑的浓度,采用DAS软件计算主要药代动力学参数。结果试验制剂和参比制剂的主要药代动力学参数如下:t1/2分别为(13.69±3.20)h和(14.31±4.30)h;tm ax分别为(1.89±1.26)h和(1.73±1.10)h;Cm ax分别为(29.13±3.57)μg·mL-1和(28.22±4.19)μg·mL-1;AUC0-t分别为(619.3±98.9)μg·h·mL-1和(601.1±92.9)μg·h·mL-1;AUC0-∞分别为(626.4±102.0)μg·h·mL-1和(609.0±94.3)μg·h·mL-1。试验制剂对于参比制剂的平均相对生物利用度F按照AUC0-t与AUC0-∞计算分别为(103.4±10.1)%,(103.2±10.1)%。结论试验制剂和参比制剂为生物等效性制剂。同时2种制剂服用安全,耐受性良好。

Objective To assess the pharmacokinetics and bioequiva- lence of test and domestic marketed ornidazole tablets in healthy volunteers. Methods A single dose of 1500 mg ornidazole was orally given to 22 healthy volunteers in a randomized cross -over study. The concentrations of ornidazole in plasma was determined by high performance liquid chromatography （HPLC）. The pharmacokinetic parameters were calculated by DAS. Results The main pharmacokinetic parameters were as follows： t1/2 were （13. 69 ±3.20） h and （14.31 ±4.30） h, tmax were （1.89±1.26） hand （1.73 ±1.10） h, Cmax were（29.13±3.57）μg· mL^-1 and （28.22 ±4. 19） μg·mL^-1, AUC0-t were （619.3 ±98.9） μg·h·mL^-1 and （601.1 ±92.9） μg·h·mL^-1, AUC0-∞ were （626. 4±102. 0）μg·h·mL^-1 and （609.0 ±94. 3）μg·h·mL^-1, re- spectively. The relative bioavailability were （103.4 ± 10. 1 ）% for AUC0-t and （ 103.2 ± 10. 1 ） % for AUC0-∞ , respectively. Conclusion The test and reference preparations were bioequivalent. Both preparations were well tolerated.