阿奇霉素分散片人体药动学及生物等效性研究

Study on Pharmacokinetics and Bioequivalence of Azithromycin Dispersible Tablets in Healthy Volunteers

关键词:  阿奇霉素  药动学  生物等效性  高效液相色谱-质谱法

Key words:  azithromycin  pharmacokinetics  bioequivalence  LC-MS

摘要:

目的 研究阿奇霉素分散片健康人体的药动学与生物等效性。方法 20名男性健康志愿者随机交叉口服阿奇霉素分散片受试制剂和参比制剂各500 mg，采用高效液相色谱-质谱法(LC-MS)测定血药浓度。以DAS 2.0软件计算其药动学参数，考察其生物等效性。结果 受试制剂和参比制剂阿奇霉素AUC_0-168分别为(8.98±1.74) mg·h·mL^-1和(8.75±1.60) mg·h·mL^-1，C_max分别为(0.81±0.14) mg·mL^-1和(0.80±0.14) mg·mL^-1，t_1/2分别为(48.16±11.10) h和(51.1±7.60) h，T_max分别为(1.80±0.86) h和(1.82±0.92) h，受试制剂相对于参比制剂的生物利用度为(103.4±20.2)%。结论 阿奇霉素分散片受试制剂和参比制剂具有生物等效性。

Abstract:

OBJETIVE To study the pharmacokinetics and bioequivalence of azithromycin dispersible tablets in healthy volunteers. METHODS A single oral dose of 500 mg test or reference formulations was given to 20 male healthy volunteers in a randomized cross-over design. The concentration of azithromycin in plasma was determined by HPLC-MS. Pharmacokinetic parameters and relative bioavailability were calculated by DAS 2.0 software. RESULTS The main pharmacokinetic parameters of test and reference azithromycin were as the followings: AUC_0-168 (8.98±1.74) mg·h·mL^-1 and (8.75±1.60) mg·h·mL^-1; C_max (0.81±0.14) mg·mL^-1 and (0.80±0.14) mg·h·mL^-1; t_1/2 (48.16±11.10) h and (51.1±7.60) h; Tmax (1.80±0.86) h and (1.82±0.92) h. The relative bioavailability of test to reference preparation was (103.4±20.2)%. CONCLUSION The test and reference formulations were bioequivalent.