国产异丁司特缓释胶囊的人体相对生物利用度研究

目的 考察国产异丁司特缓释胶囊的人体相对生物利用度。方法 12 名男性健康受试者随机分为3组,分别口服单剂量日本产异丁司特缓释胶囊20 mg、国产异丁司特缓释胶囊20 mg、异丁司特原料药10mg,交叉自身对照。于服药后取静脉血,用HPLC 法测定血清异丁司特浓度。结果 三种制剂的Cm ax 分别为(54.9±9.7)、(60.7±9.1)、(62.2±11.5)μg · L^-1,t_max分别为(3.8±0.8)、(3.9±0.8)、(1.75±0.34)h,t_1/2(ke)为(11.5±1.4)、(12.1±1.0)、(3.5±0.5)h,AUC_(0~t)为(618.1±57.7)、(588.2±66.6)、(233.0±46.4)μg ·h·L^-1。以日本杏林公司产品作为参比制剂,国产异丁司特缓释胶囊的人体相对生物利用度为(95.6±11.0)%。结论 经双向单侧t检验,国产和进口缓释胶囊具有生物等效性,与原料药相比具有明显的缓释特性。

Pharmacokinetics and relative bioavailability of domestic ibudilast sustained release capsules in healthy volunteers

Aim The relative bioavailability of domestic ibudilast sustained release capsules in healthy volunteers was observed.Methods A single oral dose of 20 mg of imported and domestic ibudilast sustained release capsules and 10 mg of ibudilast raw material was separately given to 12 healthy volunteers in a randomized crossover study.Ibudilast concentration in plasma was determined by HPLC method.Results The C_max were (54.9±9.7), (60.7±9.1)and (62.2±11.5)μg·L^-1;the t_max were (3.8±0.8), (3.9±0.8)and (1.8±0.3)h; the t_1/2(ke) were (1.5±1.4), (12.1±1.0) and (3.5±0.5)h, and the A UC_(0~t) were (618.1±57.7), (588.1±66.6)and (233.0±46.4)μg·h ·L^-1 in imported capsule group, domestic capsule group and raw material group respectively.The relative bioavailability of domestic sustained release capsules of ibudilast is (95.6±11.0)%.Conclusion The results of statistical analysis demonstrate that the imported and domestic sustained capsules have significant character of significantly sustained release and are bioequivalent.