醛糖还原酶抑制剂依帕司他胶囊和片剂的人体生物等效性

Bioequivalence of aldose reductase inhibitor epalrestat capsule and tablet in human

目的 :评价依帕司他胶囊和片剂的人体生物等效性。方法 :2 0名健康男性受试者 ,随机分为 2组 ,分别于早晨空腹一次口服依帕司他胶囊或片剂5 0mg。 1wk后再交叉服药。用HPLC法测定依帕司他血药浓度。结果 :依帕司他胶囊和片剂的主要药动学参数 ,Tmax为 (1.7±s 0 .4 )h和 (1.6± 0 .6 )h ,Cmax为 (4 .0± 0 .9)mg·L- 1和 (4 .3± 1.1)mg·L- 1,MRT为 (1.6± 0 .3)h和 (1.6± 0 .4 )h ,T1/2 为(1.7± 0 .6 )h和 (1.4± 0 .3)h ,AUC0 8为 (10 .9±2 .1)mg·h·L- 1和 (11.4± 2 .8)mg·h·L- 1,AUC0 ∞为 (11.1± 2 .2 )mg·h·L- 1和 (11.5± 2 .8)mg·h·L- 1。依帕司他胶囊相对生物利用度为 (10 0±2 2 ) %。结论

AIM: To evaluate bioequivalence of epalrestat between capsule and tablet in human. METHODS: The study was performed with 20 healthy male volunteers according to a randomized 2-way crossover design. The plasma samples were collected at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8 h after taking 50 mg of epalrestat capsule or tablet. The plasma-drug concentrations were determined by HPLC assay. RESULTS: The plasma concentration-time curves of epalrestat capsule and tablet took a nearly identical course. The main pharmacokinetic parameters of epalrestat capsule and tablet were as follows:( 1.7±s 0.4)h and (1.6±0.6)h for T max, (4.0±0.9)mg·L -1 and (4.3±1.1)mg·L -1 for C max, (1.6±0.3)h and (1.6±0.4)h for MRT, (1.7±0.6)h and (1.4±0.3)h for T 1/2, (10.9± 2.1)mg·h·L -1 and (11.4±2.8)mg·h·L -1 for AUC 0-8, (11.1±2.2)mg·h·L -1 and (11.5±2.8)mg·h·L -1 for AUC 0-∞, respectively. The relative bioavailability of epalrestat capsule was (100±22)%. CONCLUSION: The above results show that epalrestat capsule and tablet are bioequivalent.