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中国临床药理学与治疗学 ›› 2004, Vol. 9 ›› Issue (12): 1357-1360.

• 研究原著 • 上一篇    下一篇

内皮素受体拮抗剂CPU-0213 血药浓度的HPLC 测定法和药动学研究

杜荣辉, 管立, 戴德哉, 张媛, 吉民1   

  1. 中国药科大学药理研究室, 南京 210009, 江苏;
    1东南大学, 南京 210009, 江苏
  • 收稿日期:2004-10-18 修回日期:2004-12-08 出版日期:2004-12-26 发布日期:2020-11-19
  • 通讯作者: 戴德哉, 男, 教授, 博士生导师, 研究方向:心脑血管药理。Tel:025-83271270 E-mail:dezaidai@vip.sina.com
  • 作者简介:杜荣辉, 女, 博士生, 研究方向:心脑血管药理。Tel:025-83271453 E-mail:rhdu@163.com
  • 基金资助:
    国家自然科学基金重点项目资助(No30230170, No30171078)

Pharmacokinetics of CPU-0213 in mice and rats after intravenous injection

DU Rong-Hui, GUAN Li, DAI De-Zai, ZHANG Yuan, JI Min1   

  1. Department of Pharmacology, China Pharmaceutical University, Nanjing 210009, J iangsu, China;
    1South East University, Nanjing 210009, Jiangsu, China
  • Received:2004-10-18 Revised:2004-12-08 Online:2004-12-26 Published:2020-11-19

摘要: 目的: 建立内皮素受体拮抗剂CPU-0213 在小鼠和大鼠血清中的检测方法, 测定单次静脉注射(iv) CPU-0213 80 mg·kg-1后在小鼠和大鼠体内的药代动力学。方法: 用HPLC 测定小鼠和大鼠血清中的药物浓度, 3P97 程序拟合药动学参数。结果: CPU-0213 在0.4~200 μg·L-1的范围内呈良好的线性关系(r=0.9998), 最低检测浓度为35 μg·L-1。日内差小于2.7 %, 日间差小于6.3 %, 方法回收率大于95.9 %。CPU-0213 在小鼠和大鼠体内的药-时数据均符合二室模型, 消除半衰期分别为83.0±1.8 min 和96.6±11.5 min 。结论: 该方法灵敏、简单, 专属性强, 重现性好。单次iv CPU-021380 mg·kg-1后, 在小鼠和大鼠体内的药代动力学未见种属差异性。

关键词: 内皮素受体拮抗剂, CPU-0213, HPLC, 小鼠, 大鼠, 单次静脉给药, 血药浓度, 3P97, 药代动力学, 二室模型

Abstract: AIM: To establish a method in determination of CPU-0213 in serum of mice and rats and to investigate the pharmacokinetics parameters after a single injection at the dose of 80 mg·kg-1.METHODS: The concentration of CPU-0213 in serum was assayed by HPLC and the pharmacokinetics parameters were calculated by the program of 3P97.RESULTS: The linearity of CPU-0213 ranged from 0.4 to 200 mg·L-1(r=0.9998) and the limit of quantity was 35 μg·L-1.The RSD of intra-day was less than 2.7 %and that of inter-day was less than 6.3 %.The recovery was more than 95.9 %.The disposition was conformed to a two-compartment model. The T1/2β of CPU-0213 in mice and rats were 83.0±1.8 and 96.6±11.5 min, respectively.CONCLUSION: The study provides a simple, stable and special method for determining of concentrations of CPU-0213 in serum of mice and rats.After intravenously injection of CPU-0213 at a single dose, there is no significantly difference in the pharmacokinetics patterns of CPU-0213 in mice and rats.

Key words: endothelin receptor antagonist, CPU-0213, HPLC, mice, rats, single intravenous injection, drug concentration in the serum, 3P97, pharmacokinetics, two-compartment model

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