摘要
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。
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, AUC0-60h：（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, F0-60h was （97±13）%. Conclusion The test roxithromycin tablet was bioequivalent to the reference tablet.
出处
《中国药物与临床》
CAS
2006年第5期340-342,共3页
Chinese Remedies & Clinics
关键词
罗红霉素
药代动力学
生物利用度
Roxithromycin tablet
Pharmacokinetics
Relative bioavailability
