替莫唑胺多晶型胶囊的溶出度及其在家兔体内的生物利用度研究

目的：研究三种不同形态替莫唑胺(TM)胶囊［TM(A)、TM(B)、TM(C)］的溶出度及其在家兔体内的生物利用度。方法：将三种TM分别制成胶囊剂，测定其在0.1?mol/L盐酸中的溶出度。以家兔为实验动物，分别测定三种TM胶囊的绝对生物利用度，评价其生物等效性。结果：TM(C)胶囊溶出最快，TM(A)次之，TM(B)最慢；TM(A)与TM(B)的生物利用度不存在显著性差异(P＞0.05)，而TM(C) 的生物利用度明显低于TM(A)和TM(B) (P＜0.01)。结论：TM(A)与TM(B)在家兔体内具有生物等效性, 而TM(C)为低效的一种形态。

Dissolutions and bioavailabilities of temozolomide capsules

To study three morphological temozolomide (TM) capsules′ dissolutions and absolute bioavailabilities in rabbits. Methods: The dissolution of differently morphological TM capsules was determined by UV spectrophotometry. The pharmacokinetics and bioavailability of three morphologies (A, B and C) in rabbits were studied. Results: The results from Weibull′s analysis showed that the dissolutions of TM capsules were very different, the dissolution rate of TM(C) was the fastest and that of TM(B) was the slowest; The bioavailability of TM(A) and TM(B) were bioequivalent (P＞0.05), but that of TM(C) was obvious lower than the others (P＜0.01). Conclusion: TM capsule A and B are bioequivalent and TM(C) is lower in the bioavailability in rabbits.