中山大学学报自然科学版 ›› 2018, Vol. 57 ›› Issue (1): 1-6.

• 论文 •    下一篇

尖吻蝮蛇凝血酶在大鼠体内的药代动力学

邓沁,刘宏,苏薇薇,彭维,吴忠,王永刚,姚宏亮   

  1. 中山大学生命科学学院∥广东省中药上市后质量与药效再评价工程技术研究中心,广东 广州 510275
  • 收稿日期:2017-07-21 出版日期:2018-01-25 发布日期:2018-01-25
  • 通讯作者: 姚宏亮(1988 年生) ,男;研究方向:创新药物的研究开发; E-mail: yhlsysu@126.com

Pharmacokinetics of Haemocoagulase Acutus in rats

DENG Qin, LIU Hong, SU Weiwei, PENG Wei, WU Zhong, WANG Yonggang, YAO Hongliang   

  1. Guangdong Engineering & Technology Research Center for Quality and Efficacy Re-Evaluation of Post-Market TCM, School of Life Sciences, Sun Yatsen University, Guangzhou 510275, China
  • Received:2017-07-21 Online:2018-01-25 Published:2018-01-25

摘要:

尖吻蝮蛇凝血酶是从尖吻蝮蛇蛇毒中分离纯化得到的一种类凝血酶,是本团队研发的止血一类新药。采用125Ⅰ-标记的放射性同位素法和三氯醋酸沉淀结合放射性检测法研究尖吻蝮蛇凝血酶在大鼠体内的药代动力学。结果表明两种方法测定的AUC值与剂量均呈正相关,相关系数分别为0.999 8和0.999 0;肝、脾、心在给药后5 min药物含量最高,其他绝大部分组织在给药后 30 min药物含量最高,以后逐渐降低;在各时间点,肝组织含药量显著高于其他组织;此外,尖吻蝮蛇凝血酶排泄较完全,主要由尿排泄。

关键词: 尖吻蝮蛇凝血酶, 药代动力学, 大鼠

Abstract:

Haemocoagulase Acutus (Halase), a new hemostatic in halase development, is a highperformance thrombinlike enzyme (TLE) derived from snake venom of Agkistrodon acutus. To study the pharmacokinetics of Halase, 125Ⅰlabeled radioisotope method and radioassay combined with TCA precipitate were applied in rats. Results showed that AUC values were positively correlated with doses under both used methods, and the correlation coefficients were 0.999 8 and 0.999 0 respectively; drug concentration in liver, spleen and heart reached its peak after 5 minutes of administration while most of other organs reached it in 30 minutes,and then gradually decreased; in each time point, drug concentration in the liver was significantly higher than that in other tissues; Halase was completely excreted and mainly in urine.

Key words: Haemocoagulase Acutus, pharmacokinetics, rat

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