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目的建立LC-MS-MS法测定人血浆中克拉霉素的浓度,研究克拉霉素片剂的人体药动学和生物等效性。方法 24名健康受试者单剂量交叉口服受试制剂和参比制剂500mg,采用LC-MS-MS法测定血浆中不同时间点克拉霉素的药物浓度,计算主要药代动力学参数及相对生物利用度,评价两种制剂的生物等效性。结果受试制剂和参比制剂的主要药动学参数分别为:T1/2(5.271±1.835)h和(5.032±1.257)h,Tmax为(2.24±1.41)h和(1.81±1.20)h,Cmax为(1831±539)ng/ml和(2085±582)ng/ml,AUC0-24为(14172±3125)ng·h/m l和(15169±3548)ng·h/m l,AUC0-inf为(15339±2989)ng·h/ml和(15730±3586)ng·h/ml,试验制剂克拉霉素相对生物利用度F为93.43%。结论两种克拉霉素片剂具有生物等效性。
Objective To establish a LC-MS-MS method for the determination of clarithromycin in human plasma and to study the pharmacokinetics and bioequivalence of clarithromycin in human plasma. Methods Twenty-four healthy subjects received a single dose of 500 mg of the test preparation and reference preparation. The plasma concentrations of clarithromycin in different time points were determined by LC-MS-MS. The main pharmacokinetic parameters and relative bioavailability Utilization, the bioequivalence of both formulations was evaluated. Results The main pharmacokinetic parameters of test and reference preparations were T1 / 2 (5.271 ± 1.835) h and (5.032 ± 1.257) h, Tmax (2.24 ± 1.41) h and (1.81 ± 1.20) h, Cmax was (1831 ± 539) ng / ml and (2085 ± 582) ng / ml, AUC0-24 was (14172 ± 3125) ng · h / ml and (15169 ± 3548) ng · h / (15339 ± 2989) ng · h / ml and (15730 ± 3586) ng · h / ml, respectively. The relative bioavailability of test compound clarithromycin F was 93.43%. Conclusions Both clarithromycin tablets are bioequivalent.