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

山东大学学报(医学版)

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

王海钠¹,庞华²,张君仁¹,纪建波^3/sup>

山东大学 1. 药学院药物分析研究所； 2. 化学院有机化学所3. 药学院新药药理研究所，山东济南 250012

收稿日期:2006-03-29 修回日期:1900-01-01 出版日期:2006-09-24 发布日期:2006-09-24
通讯作者: 王海钠

Dissolutions and bioavailabilities of temozolomide capsules

WANG Hai-Na¹,ZHANG Jun-ren1¹, PANG Hua²,JI Jian-po³

1. Institute of Pharmaceutical analysis, School of Pharmacy, Shandong University, Jinan 250012, Shandong, China;2. Institute of Organic Chemistry, School of Chemistry, Shandong University, Jinan 250012, Shandong, China;

Received:2006-03-29 Revised:1900-01-01 Online:2006-09-24 Published:2006-09-24

摘要/Abstract

摘要： 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。

Abstract: 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.

Key words: Temozolomide, Polymorphism, Capsule, BioavailabilitY

王海钠,庞华,张君仁,纪建波/sup>. 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[J]. 山东大学学报(医学版), 2006, 44(9): 942-945.

WANG Hai-Na,ZHANG Jun-ren,PANG Hua,JI Jian-po. Dissolutions and bioavailabilities of temozolomide capsules[J]. JOURNAL OF SHANDONG UNIVERSITY (HEALTH SCIENCES), 2006, 44(9): 942-945.

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