磷酸苯丙哌林缓释片人体生物利用度试验

目的 :比较磷酸苯丙哌林缓释片与咳快好普通片单剂与多剂双交叉试验的生物等效性、缓释片特殊释放特点以及体外释放与体内吸收间的相关性。方法 :采用高效液相色谱法测定磷酸苯丙哌林血药浓度 ,计算药代动力学参数和磷酸苯丙哌林的相对生物利用度。结果 :单剂口服磷酸苯丙哌林和咳快好T1/2( β) 分别为 (11 99±1 15)h、(11 91±1 41)h ,Tpeak分别为 (3 80±0 42)h、(2 25±0 26)h ,Cmax 分别为 (0 2787±0 03) μg/ml、(0 4507±0 07) μg/ml,AUC0～48 分别为 (4 1445±0 48) μg/(ml·h)、(3 8981±0 54) μg/(ml·h) ,AUC0～∞分别为 (4 7908±0 42) μg/(ml·h)、(4 3278±0 55) μg/(ml·h) ,磷酸苯丙哌林相对生物利用度为(112 40±0 06) %。多剂口服磷酸苯丙哌林和咳快好T1/2( β) 分别为 (11 68±1 24)h、(10 83±1 01)h ,Tpeak分别为 (3 10±0 32)h、(1 95±0 16)h ,Cmax 分别为 (0 4737±0 32) μg/ml、(0 6163±0 42) μg/ml ,AUC0～48 分别为 (9 3954±0 80) μg/(ml·h)、(8 5223±0 76) μg/(ml·h) ,AUC0～∞分别为 (10 1336±0 87) μg/(ml·h)、(8 8821±0 77) μg/(ml·h) ,波动系数分别为(48 32±16 80) %、(83 10±11 24) %。磷酸苯丙哌林体外释放度和体内吸收分数间相关吸收为0 992

Bioavailability of Benproperine Sustained-release Tablets in Healthy Volunteers

OBJECTIVE:To compare benproperine sustained-release tablet(BP)with cofrel tablet(CF)in respect to the bioequivalence,release characteristics and correlation between in vitro dissolubility and in vivo absorption METHODS:A HPLC method was used to determine the serum benproperine concentration after single and multiple oral administration of 80mg BP and CF in a two-period cross-over test RESULTS:The T1/2(β),Tpeak,Cmax,AUC0～36,AUC0～∞ of BP after single and multiple oral administration were (11 99±1 15)h and (11 91±1 41)h,(3 80±0 42)h and (2 25±0 26)h,(0 2 787±0 03)μg/ml and (0 4 507±0 07)μg/ml,(4 1 445±0 48)μg/(ml·h)and (3 8 981±0 54)μg/(ml·h),(4 7 908±0 42)μg/(ml·h) and (4 3 278±0 55)μg/(ml·h),and those of CF were (11 68±1 24)h and (10 83±1 01)h,(3 10±0 26)h and (1 95±0 16)h,(0 4 737±0 32)μg/ml and (0 6 163±0 42)μg/ml,(9 3 954±0 80)μg/(ml·h) and (8 5 223±0 76)μg/(ml·h),(10 1 336±0 87)μg/(ml·h) and (8 8 821±0 77)μg/(ml·h),respectively The relative bioavailability of BP versus CF was(112 40±0 06)% CONCLUSION:The results show that the benproperine sustained-release tablet and cofrel are bioequivalent