替米沙坦片在健康人体的药代动力学和相对生物利用度

Pharmacokinetics and relative bioequivalence of telmisartan tablets in Chinese healthy volunteers

目的研究国产和进口替米沙坦片在健康人体的药代动力学并评价2制剂的生物等效性。方法20名健康志愿者单次、交叉口服替米沙坦片80mg后,用高效液相色谱-荧光检测法测定血浆替米沙坦浓度。用3P97药代动力学软件计算药代动力学参数。结果2种替米沙坦片在健康志愿者体内的药-时曲线均符合二室模型,2种制剂的主要药代动力学参数:Cmax分别为(944.71±376.08),(852.72±333.78)ng·mL-1;tmax分别为(0.98±0.60),(1.28±0.65)h;t1/2β分别为(28.78±13.88),(25.83±9.25)h;AUC0-t分别为(4.14±2.44),(3.83±1.97)mg·h·L-1;AUC0-∞分别为(4.64±2.84),(4.17±2.22)mg·h·L-1。国产对进口制剂的平均相对生物利用度F0-t为(99.64±23.93)%,F0-∞为(97.97±26.20)%。结论国产和进口替米沙坦片剂为生物等效制剂。

Objective To study the relative bioavailability of telmisartan tablet in Chinese healthy volunteers and to evaluate its bioequivalence. Methods A single oral dose 80 mg of two telmisartan tablets was given to 20 healthy volunteers in a randomized cross-over study. The concentration of telmisartan in plasma were determined by HPLC method with fluorimetric detection. Results Finding revealed that the data of two formulations were fitted to a two-compartment open model. The main pharmacokinetic parameters of two formulations, reference and test tablets, were as follow: C max were (944.71± 376.08) and (852.72±333.78) ng·mL -1, t max were (0.98±0.60) and (1.28±0.65)h, t 1/2β were (28.78±13.88) and (25.83±9.25)h, AUC 0-twere (4.14±2.44) and (3.83±1.97) mg·h·L -1; AUC 0-∞ were (4.64±2.84) and (4.17±2.22)mg·h·L -1.The relative bioavalability of F 0-t and F 0-∞were (99.64±22.39)% and (97.97± 26.20)%, respectively. Conclusion The domestic and imported telmisartan tablets were bioequivalent .