中国药物警戒 ›› 2012, Vol. 9 ›› Issue (1): 5-7.

• 基础及临床研究 • 上一篇    下一篇

去甲斑蝥素理化性质测定及大鼠在体肠吸收动力学研究

周颖1,成旭东2, 王玉婷2,刘扬2   

  1. 1.江苏省苏州市第四人民医院药剂科,江苏苏州215001；
    2.江苏省苏州大学医学部药学院,江苏苏州215123
  • 收稿日期:2016-03-12 修回日期:2016-03-12 出版日期:2013-01-08 发布日期:2016-03-09
  • 通讯作者: 周颖,女,主管药师,药物质量控制。
  • 作者简介:江苏省普通高校研究生科研创新计划项目（CXZZ11_0114）；苏州市科技计划项目（应用基础研究计划）（SYS201107）。
  • 基金资助:
    刘扬,男,博士,讲师,药物新剂型与新技术。 E-mail:liuyang@suda.edu.cn

Study on the Physicochemical Properties and the Intestinal Absorption Kinetics of Norcantharidin in Rats

ZHOU Ying1, CHENG Xu -dong2, WANG Yu -ting2, LIU Yang2   

  1. 1.Suzhou No.4 People's Hospital, Jiangsu Suzhou 215001, China;
    2.College of Pharmaceutical Science, Soochow University, Jiangsu Suzhou 215123, China
  • Received:2016-03-12 Revised:2016-03-12 Online:2013-01-08 Published:2016-03-09

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摘要： 目的 测定去甲斑蝥素理化性质及在体肠吸收动力学,为设计缓释制剂提供参考依据。方法 测定去甲斑蝥素溶解度、油水分配系数。采用大鼠在体回流方法,利用紫外分光光度法和HPLC 分别测定酚红和去甲斑蝥素的含量,研究去甲斑蝥素在不同浓度和不同小肠区段下的吸收。结果 去甲斑蝥素在十二指肠、空肠、回肠、结肠的吸收速率常数分别为：0.1623,0.1260,0.0084,0.0035h-1；在小肠的吸收速率常数不同药物浓度70、80、90μg·mL-1 时分别为：0.0112,0.0056,0.0071h-1。结论 不同的药物浓度对去甲斑蝥素在大鼠全肠道的吸收无显著影响,药物的吸收呈一级动力学过程,吸收机制为被动扩散,提示适于制备日服一次的缓释给药系统。

关键词: 去甲斑蝥素, 理化性质, 吸收动力学, 在体肠回流法

Abstract: Objective To investigate physicochemical properties and the absorption kinetics of norcantharidin(NCTD) at different intestine segments in rats. Methods The dissolubility and n-octyl alcohol/water partition coefficient were determined. The intestine in rats was cannudated for in situ recirculation, UV and HPLC were respectively used to determine the concentrations of UV spectrums of phenol red and NCTD. The absorption of NCTD was studied at different intestine segments, and with different concentration of NCTD. Results The absorption rate constants (Ka) at duodenum, jejunum, ileum, and colon were 0.1623, 0.1260, 0.0084, 0.0035h -1 respectively. Ka from intestine at NCTD concentration of 70, 80, 90μg·mL-1 were 0.0112, 0.0056, 0.0071h-1 respectively. Conclusion The concentration of NCTD had no distinctive effect on the absorption kinetics. The absorption of NCTD was a first -order process with passive diffusion mechanism, which indicated that NCTD could be prepared as sustained -release dosage form for administration once a day.

Key words: norcantharidin, physicochemical properties, absorption kinetics, intestinal recirculating method in situ

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