甲芬那酸分散片在健康人体的生物等效性评价

Pharmacokinetics and bioequivalence study of mefenamic acid dispersible tablets in health volunteers

目的:研究甲芬那酸分散片和普通片在健康人体的药动学特征和生物等效性。方法:采用标准两周期交叉设计自身对照试验方法,18名健康志愿者单剂量口服500mg甲芬那酸分散片或普通片,用反相高效液相色谱法(RP-HPLC)测定血清中甲芬那酸的浓度,计算其药动学参数并评价两种制剂的生物等效性。结果:甲芬那酸分散片和普通片的主要药动学参数Tmax(实测值)分别为(1.1±0.6)h和(2.1±0.8)h,Cmax(实测值)分别为(5.8±2.2)mg.L-1和(5.9±3.0)mg.L-1,AUC(0-14h)分别为(18.1±3.4)mg.L-1.h和(17.3±5.0)mg.L-1.h,AUC(0-inf)分别为(18.7±3.3)mg.L-1.h和(18.0±4.9)mg.L-1.h,T1/2Ke分别为(2.0±0.8)h和(2.3±1.2)h。除Tmax外,甲芬那酸分散片和普通片各主要药动学参数间差异无显著性(P>0.05);甲芬那酸分散片对普通片的相对生物利用度为(111.3±31.9)%。结论:健康人单剂量口服500mg甲芬那酸分散片与普通片具有生物等效性。

OBJECTIVE To study the pharrnacokinetics and bioequivalence of mefenamic acid dispersible tablets and mefenamic acid tablets. METHODS Mefenamic acid dispersible tablets and mefenamic acid tablets were given to 18 health volunteers in an open randomized two period cross-over test single oral dose 500 mg. The serum levels of mefenamic acid were measured by reversed-phase high performance liquid chromatography（RP-HPLC）. RESULTS The pharmacokinetic parameters of mefenamic acid dispersible tablets and mefenamic acid tablets were as follows： Tmax were （1.1 ± 0. 6）h and （2. 1 ± 0. 8）h, Cmax were （5. 8 ± 2. 2）mg, L^-1 and （5. 9 ± 3. 0）mg.L^-1 , AUC（0-14h） were （18. 1 ±3. 4）mg.L^-1 ·h and （17. 3 ± 5. 0）mg.L^-1·h, AUC（0-∞） were （18. 7 ± 3.3）mg.L^-1·h and （18.0 ± 4. 9） mg·L^-1·h, T1/2Ke were （ 2. 0 ± 0. 8） h and （2.3 ± 1.2） h. Exception of Tmax, the statistical analysis for AUC（0-14h）, AUC（0-inf） and Cmax showed that there was no significant difference between mefenamic acid dispersible tablets and mefenamic acid tablets（P〉0. 05）. The relative bioavailability of mefenamic acid tablets was （111.3 ± 31.9）%. CONCLUSION The two preparations of mefenamic acid were bioequivalent.