阿昔洛韦药代动力学及相对生物利用度研究

Study on pharmacokjnetics and relative bioavailability of Aciclovir

目的:对阿昔洛韦药代动力学及相对生物利用度进行研究。方法:用HPLC法研究10名健康男性受试者口服400mg供试制剂阿昔洛韦(无环鸟苷片)和400mg参比制剂阿昔洛韦(甘泰片)后,研究血浆中阿昔洛韦浓度及药代动力学指标,并对阿昔洛韦(无环鸟苷片)生物利用及生物等效性进行评价。结果:受试者口服阿昔洛韦(甘泰片)后tmax为(1.2±0.5)h,Cmax(906.71±188.95)ng·ml-1,t1/2为(2.59±0.53)h。口服阿昔洛韦(无环鸟苷片)后,tmax为(1.8±0.5)h,Cmax为(847.72±180.32)ng·ml-1,t1/2为(2.41±0.58)h。方差分析表明两种制剂药代动力学参数AUC0-∞、AUC0-r以及Cmax生物等效。结论:两种制剂的吸收程度相同,生物利用度符合要求。

Objectives: To study the pharmacokinetics and relative bioavailability of acyclovir. Method: A single dose of 400 mg aciclovir or controlled preparation-aciclovir( Gantai) was given to ten healthy male adults in a crossover study. The blood concentration of both acyclovir and their parameters of pharmacokinetics were analyzed, the relative bioavailability and bioequivalence were evaluated byHPLC. Result: tmax was (1.2±0.5)h, Cmax was (906.71± 188. 95)ng·ml-1, t1/2 was (2. 59 ± 0. 53)h in receiving Gantai, while it were (1.8± 0. 45)h, (847. 72±180. 32)ng·mg-1, (2. 41 ±0. 58)h in receiving aciclovir, respectively. The analysis of variance showed that there were no significant differences in pharmacokinetic parameters( AUC0-∞ , AUC0-r) Cmax between the two a-gents. The two-one sided test showed that AUC0-∞, AUC0-r and Cmax of the two agents were bioequivalent. Conclusion: It was suggested that the two agents had the same absorptivity, which met the requirement of bioavailability.