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目的:进行受试制剂盐酸安非他酮缓释片与市售参比制剂盐酸安非他酮缓释片的人体生物等效性研究。方法:20例健康男性志愿者采用自身交叉给药方案,分别口服单次给予和连续多次(18例)给予2种盐酸安非他酮缓释制剂,采用HPLC-MS/MS法测定其血药浓度,计算药动学参数,并判定2种制剂的生物等效性。结果:口服单次给予受试制剂和参比制剂安非他酮缓释片的主要药动学参数为Cmax分别为(174.0±55.5),(175.1±56.2)μg.L-1,tmax分别为(2.0±0.5),(2.0±0.6)h,t1/2分别为(11.1±5.0),(11.8±8.2)h,AUC0-72分别为(952.9±423.4),(901.6±372.5)μg.h.L-1,AUC0-∞分别为(968.2±441.0),(918.8±375.8)μg.h.L-1;以AUC0-72计,单次口服受试制剂的相对生物利用度为(106.0±24.3)%。口服连续多次给予的主要药动学参数为Cmax分别为(149.1±45.1),(149.2±38.4)μg.L-1,tmax分别为(2.1±0.9),(1.8±0.3)h,t1/2分别为(12.7±4.6),(12.2±5.3)h,AUCSS分别为(717.9±195.7),(666.9±186.6)μg.h.L-1;以AUCSS计,多次口服试验药的相对生物利用度为(109.0±19.5)%。结论:2种制剂的盐酸安非他酮缓释片具有人体生物等效性。
OBJECTIVE: To study the bioequivalence of bupropion hydrochloride sustained release tablets and the commercial reference bupropion hydrochloride sustained-release tablets. Methods: Twenty healthy male volunteers were given oral crossover regimen. Two kinds of sustained-release preparations of bupropion hydrochloride were given orally and in multiple consecutively (18 cases) respectively. The blood samples were determined by HPLC-MS / MS Drug concentration, calculate pharmacokinetic parameters, and determine the bioequivalence of the two formulations. Results: The main pharmacokinetic parameters of bupropion sustained-release tablets were (174.0 ± 55.5), (175.1 ± 56.2) μg.L-1 and tmax (2.0 ± 0.5) and (2.0 ± 0.6) h respectively, and the values of t1 / 2 were (11.1 ± 5.0) and (11.8 ± 8.2) h respectively. The AUC0-72 values were (952.9 ± 423.4) and (901.6 ± 372.5) -1 and AUC0-∞ were (968.2 ± 441.0) and (918.8 ± 375.8) μg.hL-1, respectively. The relative bioavailability of AUC0-72 was (106.0 ± 24.3)%. The main pharmacokinetic parameters of continuous oral administration for multiple times were (149.1 ± 45.1), (149.2 ± 38.4) μg.L-1 and tmax were (2.1 ± 0.9), (1.8 ± 0.3) h and t1 / 2 were (12.7 ± 4.6), (12.2 ± 5.3) h and AUCSS were (717.9 ± 195.7) and (666.9 ± 186.6) μg.hL-1 respectively. The relative bioavailability of AUCSS (109.0 ± 19.5)%. Conclusion: The two kinds of preparations of bupropion hydrochloride sustained-release tablets have human bioequivalence.