罗红霉素片剂人体生物等效性研究

Bioequivalence of Roxithromycin Tablets in Healthy Volunteers

目的与已上市罗红霉素片为对照,考察另一国产制剂的人体生物等效性。方法18例健康受试者随机交叉单剂量口服两种制剂后,采用微生物法测定血浆中的药物浓度。结果经3P97程序拟合处理,二者的体内过程符合一室模型;试验制剂及参比制剂的罗红霉素实测平均血药峰浓度Cmax分别为(10.869±2.671)μg/ml和(11.250±3.097)μg/ml;实测平均达峰时间Tmax分别为(1.7±0.8)h和(1.6±0.8)h;t1/2(ke)分别为(13.407±2.391)和(12.496±2.231)h;血药浓度-时间曲线下面积AUC0-tn平均值分别为(127.097±32.971)μg·ml-1·h和(134.429±35.783)μg·ml-1·h;AUC0-∞平均值分别为(136.556±33.958)μg·ml-1·h和(143.483±38.052)μg·ml-1·h;试验制剂及参比制剂比较,罗红霉素的相对生物利用度F0-tn、F0-∞分别为(95.79±17.46)%、(96.58±16.66)%;对药动学参数AUC、Cmax、Tmax进行单因素方差分析及双单侧t检验,结果表明两制剂在处方与周期间P>0.05。结论试验与参比制剂的药动学参数具有生物等效性。

OBJECTIVE To study the relative bioequivalence of two sorts of domestic roxithromycin tablets. METHODS The randomized and crossover study was conducted in 18 healthy volunteers. After a single dose of the drugs given, their plasma drug concentration was determined by microbioassay. RESULTS Both the two sorts of domestic roxithromycin tablets were fitted to one compartment model. The main pharmacokinetic parameters of the tested and reference roxithromycin were as follows： Cmax （10. 869±2. 671 ） μg/ml and （11. 250±3. 097）μg/ml; Tmax（1.7±0.8）h and （1.6±0.8） h; t1/2（13.407±2.391）h and （12. 496±2. 231） h; AUC0-tn （127.097±32.971）/μg·ml^-1·h and （134.429±35. 783）μg·ml^-1·h ;AUC0-∞（136. 556±33. 958）μg·ml^-1·h and （143. 483±38. 052） μg·ml^-1·h; F0-tn and F0-∞ were （95.79±17.46）% and （96.58±16.66）%, respectively. CONCLUSIONS The results of analysis showed that the tested and reference formulations are bioequivalent.