盐酸莫雷西嗪片剂人体生物等效性研究

Study on Bioequivalence of Moricizine Hydrochloride Tablets in Healthy Volunteers

目的评价两种盐酸莫雷西嗪片剂的生物等效性。方法18名健康男性志愿者分别单剂量po受试制剂和参比制剂200mg,采用高效液相色谱-质谱联用法测定血浆中莫雷西嗪的浓度。结果受试制剂和参比制剂在受试者体内的药动学参数如下:血浆中莫雷西嗪的tmax分别为(1.4±0.4)和(1.4±0.5)h,ρmax分别为(595±318)和(589±283)μg·L-1,t1/2分别为(2.4±0.9)和(2.7±1.5)h,用梯形法计算,AUC0-t分别为(1.60±0.89)和(1.57±0.76)mg.h·L-1,AUC0-∞分别为(1.66±0.90)和(1.63±0.76)mg.h·L-1,以AUC0-t计算,莫雷西嗪的相对生物利用度平均为(103.6±28.8)%。结论两种制剂生物等效。

OBJECTIVE To study the relative bioavailability of two moricizine hydrochloride tablets in 18 healthy volunteers, METHODS A single oral dose of 200 mg moricizine hydrochloride tablets was given according to a randomized crossover design. The plasma concentrations of moricizine were determined by a high performance liquid chromatography-mass spectrometry method. RESULTS The main pharmacokinetic parameters of the test and the reference tablets were as follows：tmax were （1.4 ± 0. 4） and （ 1.4 ± 0.5 ） h ;Pmax were （595 ± 318） and （590 ± 283 ）μg·L^-1 ; t1/2 were （ 2.4 ± 0. 9 ） and （ 2.7 ± 1.5 ） h ; AUC0., were （ 1.60 ± 0. 89） and （ 1.57 ± 0. 76） mg·h·L^-1, AUC0-∞ were （ 1.66 ± 0. 90 ） and （ 1.63 ± 0. 76 ） mg ·h·L^-1, respectively. The relative bioavailability of the test formulation was（ 103.6 ±28. 8） %. CONCLUSION The two tablets are bioequivalent.