曾东向 任华益 李坤艳 曹丽芝 宋剑萍 (湖南省肿瘤医院药剂科临床药学室 长沙 410006)
摘 要 目的：研究国产（受试制剂）与进口（参比制剂）替米沙坦片的人体生物等效性。方法：采用LC-MS法，测定18名健康男性单次交叉口服参比制剂及受试制剂80 mg后血浆中不同时间点的药物浓度，计算其药动学参数和相对生物利用度。结果：受试制剂及参比制剂的主要药物动力学参数Cmax分别为(428.8±108.6)和(420.7±93.0) ng•h-1•ml-1；tmax分别为(1.0±0.3)和(1.3±0.5)h；AUC0→96分别为(3 041.8±409.4)和(3 144.1±260.4)ng•h-1•ml-1。受试制剂相对生物利用度为96.8%±10.6%。结论：受试制剂与参比制剂具有生物等效性。
关键词 替米沙坦；片剂； LC-MS法；生物等效性；药物动力学
中图分类号：R969.1
文献标识码：A
文章编号：1008-049X(2007)07-0644-03
Bioequivalence Evaluation of Two Telmisartan Tablets in Healthy Volunteers
Zeng Dongxiang,Ren Huayi, Li Kunyan,Cao Lizhi，Song Jianping(Department of Pharmacy, Hunan Tumor Hospital, Changsha 410006,China)
ABSTRACT Objective: To study the pharmacokinetics and relative bioavailability of two preparations of telmisartan tablets. Method: The open randomized crossover design was used, the plasma concentrations of telmisartan were determined by LC-MS after 18 healthy male volunteers were given test or reference tables of telmisartan with a single oral dose of 80 mg.Result:AUC0→96 of test and reference drugs were 3 041.8±409.4ng•h-1•ml-1 and 3 144.1±260.4ng•h-1•ml-1respectively, Cmaxwere 428.8±108.6ng•h-1•ml-1and 420.7±93.0 ng•h-1•ml-1,tmax were1.0±0.3 h and 1.3±0.5 h,respectively. The relative bioavailability of the test drug was 96.8%±10.6%.Conclusion: Two preparations are bioequivalent.
KEY WORD Telmisartan；Bioequivalence；LC-MS；Pharmacokinetics
参 考 文 献
1 朱珠.抗高血压新药替米沙坦［J］.中国药学杂志，1999，34（12）:27-28
2 孙忠实.新型AT拮抗剂替米沙坦［J］.中国新药杂志，1998,12（12）:801-802
3 陶达人，孙黎，沈金芳.高效液相色谱法测定血浆中替米沙坦的浓度［J］.中国药师，2006，9（3）：221-222
4 Lacourciere Y, Lenis J, Orchard R，et al. A comparison of the efficacies and duration of action of the angiotensin II receptor blockers telmisartan and amlodipine［J］. J Blood Press Monit，1998,3(5):295-302
5 Bajcetic M, Benndorf R A, Appel D，et al. Pharmacokinetics of Oral Doses of Telmisartan and Nisoldipine, Given Alone and in Combination, in Patients With Essential Hypertension［J］. J Clin Pharmaco., 2007,47(3):295-304
6 朱赛楠，马林茂.生物利用度生物等效性评价方法概述［J］.中国临床药理学杂志,2003，22（5）：388-391
7 刘玉秀，姚晨.多交叉设计生物利用度试验的等效性分析［J］.中国临床药理学杂志,2002，12（3）：219-223
8 Stangier J, Su CA, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients［J］. J Int Med Res，2000,28(4):149-167 资料来自:中国药师-专业站 |