液质联用法研究罗红霉素在健康人体内的药代动力学及相对生物利用度

目的研究罗红霉素在健康人体内的药代动力学和相对生物利用度。方法20名健康成年男性志愿者采用随机分组自身交叉对照试验设计,单剂量口服150mg罗红霉素片后,用液质联用(LC-MS)法测定血浆中药物浓度。结果罗红霉素线性范围为0.0111～11.14mg/L;提取回收率83.47%～91.68%,日内和日间精密度(RSD)均<10.0%。受试制剂和参比制剂的主要药代动力学参数:峰时(Tmax):(2.1±1.4)和(2.2±1.5)h;峰浓度(Cmax):(5.8±1.8)和(6.1±2.0)mg/L;曲线下面积(AUC)0￣60h:(80±28)和(84±28)mg·L-1·h-1;AUC0￣∞:(83±30)和(87±30)mg·L-1·h-1;消除半衰期(T1/2):(12.4±2.3)和(12.3±1.6)h。以AUC0￣60h计算的受试制剂的相对生物利用度为(97±13)%。结论两种制剂生物等效。

Pharmacokinetics and relative bioavailability study of roxithromycin tablet in Chinese healthy volunteers by LC-MS

Objective To study the pharmacokinetics and relative bioavailability of roxithromycin in Chinese healthy volunteers. Methods 20 male healthy volunteers randomly received a single crossover oral dose of 150 mg test tablet or reference tablet. The concentration of roxithromycin in plasma was determined by LC-MS. Results The method was linear in the range from 0.0111 mg/L to 11.14 μg/ml (r=0.9991). The relative bioavalability was more than 93% and the absolute bioavalability was more than 81%.The inter-day and intra-day RSD were less 10%.The main pharmacokinetic parameters of test and reference roxithromycin tablets were as following:Tmax:(2.1±1.4) and (2.2±1.5)h, Cmax:(5.8±1.8) and (6.1±2.0)μg/ml, AUC0~60 h:(80±28) and (84±28)mg·L-1·h-1, AUC0~∞:(83±30) and (87±30)mg·L-1·h-1, T1/2:(12.4±2.3) and (12.3±1.6)h, F0~60 h was (97±13)%. Conclusion The test roxithromycin tablet was bioequivalent to the reference tablet.