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中国临床药理学与治疗学 ›› 2005, Vol. 10 ›› Issue (4): 417-420.

• 研究原著 • 上一篇    下一篇

替米沙坦在中国健康人体内的药代动力学和相对生物利用度研究

余俊先, 张银娣, 卓海通, 沈建平, 印晓星   

  1. 南京医科大学临床药理研究所,南京 210029,江苏
  • 收稿日期:2004-12-08 接受日期:2005-03-05 出版日期:2005-04-26 发布日期:2020-11-19

Pharmacokinetics and relative bioavailability of telmisartan in male healthy Chinese volunteers

YU Jun-xian, ZHANG Yin-di, ZHUO Hai-tong, SHEN Jian-ping, YIN Xiao-xing   

  1. Institute of Clinical Pharmacology, Nanjing Medical University, Nanjing210029, Jiangsu, China
  • Received:2004-12-08 Accepted:2005-03-05 Online:2005-04-26 Published:2020-11-19
  • Contact: ZHANG Yin-di, female, professor, tutor of doctor,specialized in clinical pharmacology. Tel:025-86863159  E-mail:ydzhang @njmu.edu.cn
  • About author:YU Jun-xian, male, PhD candidate.E-mail:yujunxian@sohu.com

摘要: 目的: 研究替米沙坦在中国人体内的药代动力学和相对生物利用度。方法: 20 名男性健康志愿者单剂量随机交叉口服 80 mg 国产替米沙坦胶囊(试验片)和进口替米沙坦片(参比片), 采用 HPLC-荧光检测法测定受试者 96 h 的血药浓度, 生物等效性采用双侧 t 检验。结果: 国产和进口的替米沙坦血药浓度-时间曲线符合二室开放模型, 其主要药代动力学参数:Cmax 分别为 456.28 ±252.56 和 759.54±313.54 μg°L-1, Tmax 分别为 1.61±0.71 和 1. 08 ±0.36 h, T1/2β 分别为 22.39 ±6.29 和 21.08 ±5.24,MRT 分别为 27.02±6.23 和 24.27±5.79 h, AUC0-t分别为 3454±1050 和 3636±1300 μg°h°L-1,统计分析, 试验片与参比片的 Cmax 、Tmax 有统计学差异(P<0.05),而 AUC0-t 没有显著性差异(P>0.05), 试验片相对生物利用度为97.28%±12.74%。结论: 国产替米沙坦胶囊和进口片剂具有生物等效性。

关键词: 替米沙坦, 药代动力学, 相对生物利用度, 高效液湘色谱法

Abstract: AIM: To compare pharmacokinetics and relative bioavailability of telmisartan capsule (T)and telmisartan tablet (R).METHODS: 20 male healthy Chinese volunteerswere enrolled in a randomized two-way crossover designs with a single-oral dose study (80 mg once per day for each preparation).The plasma telmisa-tan concentration was determined by HPLC-fluorescence detector.Plasma levels of telmisatan were followed up to 96 h. Area under the telmisartan concentration time curve was calculated by variance analysis and the bioequivalent was determined by two one-side t-test. RESULTS: A two-compartment model was adopted in telmisartan plasma concentration-time data analysis.The pharmacokinetic parameters of T and Rin single-dose study including C max (μg°L-1), Tmax (h), T1/2β (h), MRT(h), AUC0-92 (μg°h°L-1)were as following:456 ±253 and 760 ± 314, 1.61±0.71 and 1.08 ±0.36, 22. 39 ±6.29 and 21.08±5.24, 27. 02 ±6. 23 and 24.27 ±5.79, 3454 ±1050 and 3635±1300, respectively. Statistically sig-nificant differences were observed between the parameter values of the two products in C max and T max;whereas there was no statistically significant difference between AUC0 -∞ μg°h°L-1 (3601 ±1095 and 3767 ±1399). The relative bioavailability for T was 97.28% ± 12.74%.CONCLUSION: The test telmisartan capsule is bioequivalent to the reference tablet.

Key words: telmisartan, pharmacokinetics, bioavailability, HPLC

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