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目的:研究国产班布特罗口腔崩解片在人体的相对生物利用度,并与进口片比较,评价两者生物等效性。方法:20例健康男性志愿者随机交叉单剂量口服国产盐酸班布特罗口腔崩解片(受试制剂)或进口盐酸班布特罗片(参比制剂)20 mg后,采用液相色谱串联质谱法测定血浆中班布特罗及其代谢产物特布他林的血药浓度,用DAS 2.0软件计算药代动力学参数,并评价其生物等效性。结果:受试制剂和参比制剂药代动力学参数为:Cmax(6.22±1.51)和(5.96±1.39)ng.mL-1;Tmax(2.52±0.72)和(2.70±0.86)h;t1/2(11.06±3.60)和(10.64±2.24)h;AUC0～72 h(56.69±16.82)和(52.86±14.57)ng.h.mL-1。特布他林药代动力学参数:Cmax(10.04±2.92)和(9.38±2.87)ng.mL-1;Tmax(4.35±1.04)和(4.60±1.14)h;t1/2(19.60±4.26)和(18.27±4.22)h;AUC0～72 h(199.60±68.89)和(179.55±50.18)ng.h.mL-1。国产盐酸班布特罗口腔崩解片单次给药后的相对生物利用度为(107.4±16.9)%(班布特罗),(110.9±18.6)%(特布他林)。结论:国产班布特罗口腔崩解片与进口班布特罗片在人体内生物等效。
OBJECTIVE: To study the relative bioavailability of domestic bambuterol orally disintegrating tablets in human body and evaluate the bioequivalence of the two products in comparison with imported tablets. Methods: A total of 20 healthy male volunteers were randomized to receive a single oral dose of bambuterol hydrochloride orally disintegrating tablets (test preparation) or imported bambuterol hydrochloride tablets (reference preparation) 20 mg. Plasma concentrations of bambuterol and its metabolite terbutaline in plasma were determined by mass spectrometry. Pharmacokinetic parameters were calculated using the DAS 2.0 software and their bioequivalence was evaluated. Results: The pharmacokinetic parameters of the tested and reference preparations were as follows: Cmax (6.22 ± 1.51) and (5.96 ± 1.39) ng.mL-1, Tmax (2.52 ± 0.72) and (2.70 ± 0.86) 2 (11.06 ± 3.60) and (10.64 ± 2.24) h respectively; AUC0 ~ 72 h (56.69 ± 16.82) and (52.86 ± 14.57) ng.h.mL-1. The pharmacokinetic parameters of terbutaline were: Cmax (10.04 ± 2.92) and (9.38 ± 2.87) ng.mL-1; Tmax was 4.35 ± 1.04 and 4.60 ± 1.14 respectively; t1 / 2 was 19.60 ± 4.26, And (18.27 ± 4.22) h respectively; AUC0 ~ 72 h (199.60 ± 68.89) and (179.55 ± 50.18) ng.h.mL-1. The relative bioavailability of domestic bambuterol hydrochloride buccal tablets after oral administration was (107.4 ± 16.9)% (bambuterol), (110.9 ± 18.6)% (terbutaline). Conclusion: Domestic bambuterol orally disintegrating tablets are bioequivalent to imported bambuterol tablets in the human body.