论文部分内容阅读
目的建立人血浆中阿奇霉素的高效液相色谱/质谱/质谱(HPLC-MS/MS)测定法,测定受试者口服阿奇霉素颗粒后的血药浓度,并对受试制剂与参比制剂的生物等效性进行评价。方法19名健康受试者采用随机双交叉试验设计,单剂量口服阿奇霉素颗粒受试制剂和参比药物各500 mg,用HPLC-MS/MS测定用药后不同时间血药浓度。血药浓度-时间数据经DAS 2.0统计软件处理,计算主要药动学参数,并进行两种制剂的生物等效性评价。结果受试制剂和参比制剂的Tmax分别为(2.5±1.1)h和(2.6±1.7)h,Cmax分别为(574.6±209.2)ng.mL-1和(594.5±229.9)ng.mL-1,t1/2分别为(44.7±15.2)h和(42.0±13.0)h,AUC0-144分别为(5 319.6±2 507.8)h.ng.mL-1和(5 710.7±2 710.1)h.ng.mL-1,AUC0-∞分别为(5 704.2±2 858.7)h.ng.mL-1和(6 010.0±2 808.1)h.ng.mL-1,以AUC0-144计算,相对生物利用度为(94.2±15.7)%。两制剂的主要药动学参数无显著性差异。结论受试制剂与参比药物生物等效。
Objective To establish a HPLC-MS / MS method for the determination of azithromycin in human plasma, and to determine the plasma concentration of azithromycin after oral administration of the test compound. Validity evaluation. Methods Nineteen healthy volunteers were randomized to receive double crossover design. 500 mg of azithromycin was administered orally as a single dose. The plasma concentrations of azithromycin granules and reference drugs were determined by HPLC-MS / MS. Plasma concentration-time data were processed by the DAS 2.0 statistical software to calculate the main pharmacokinetic parameters and to evaluate the bioequivalence of the two formulations. Results The Tmax of test and reference preparations were (2.5 ± 1.1) h and (2.6 ± 1.7) h, with Cmax of (574.6 ± 209.2) ng.mL-1 and (594.5 ± 229.9) ng.mL-1 , t1 / 2 were (44.7 ± 15.2) h and (42.0 ± 13.0) h, AUC0-144 were (5 319.6 ± 2 507.8) h.ng.mL-1 and (5 710.7 ± 2 710.1) h.ng mL-1 and AUC0-∞ were (5 704.2 ± 2 858.7) h.ng.mL-1 and (6 010.0 ± 2 808.1) h.ng.mL-1 respectively. The relative bioavailability (94.2 ± 15.7)%. The main pharmacokinetic parameters of two formulations no significant difference. Conclusion The test preparation is bioequivalent to the reference drug.