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中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (5): 505-509.

• 研究原著 • 上一篇    下一篇

地塞米松当归多糖前体药在大鼠体内的结肠靶向释药研究

刘新友, 周四元, 程建峰1, 冉玉华, 滕增辉, 杨润涛, 杨茜, 梅其炳   

  1. 第四军医大学药学系药理学教研室, 西安 710032, 陕西;
    1第四军医大学唐都医院药剂科, 西安 710038, 陕西
  • 收稿日期:2006-03-31 修回日期:2006-06-04 出版日期:2006-05-26 发布日期:2020-12-09
  • 通讯作者: 梅其炳, 男, 博士, 教授, 博士生导师, 研究方向:分子药理学。 Tel:029-83374555   E-mail:qbmei@fmmu.edu.cn
  • 作者简介:刘新友, 男, 硕士生, 主管药师, 研究方向:药代动力学。 Tel:029-83374555   E-mail:lxylxywy @163.com
  • 基金资助:
    国家“863”计划资助项目(No2004AA2Z3160)

Colon-targeted delivery system of dexamethasone-angelica sinensis po-lysaccharides prodrug in rats

LIU Xin-you, ZHOU Si-yuan, CHENG Jian-feng1, RAN Yu-hua, TENG Zeng-hui, YANG Run-tao, YANG Xi, MEI Qi-bing   

  1. Department of Pharmacology, the Fourth Military Medical University, Xi'an 710032, Shanxi, China;
    1Department of Pharmacy of Tangdu Hospital, the Fourth Military Medical University, Xi'an 710038, Shanxi, China
  • Received:2006-03-31 Revised:2006-06-04 Online:2006-05-26 Published:2020-12-09

摘要: 目的: 探讨以当归多糖为载体的地塞米松前 体药在大鼠胃肠道内的转运及活性药物的释放情况。方法: 地 塞 米 松 及其 当 归 多 糖 前 体 药 按 1.96 mg·kg-1 (以地塞米松量计) 给大鼠灌胃, 采用 高效液相色谱法检测地塞米松在大鼠胃肠道不同部位的分布及血药浓度变化。 结果: 地塞米松当归多 糖前体药灌胃后, 释放出的地塞米松只分布在盲肠 和结肠的内容物及粘膜中, 在胃和小肠的内容物及 粘膜中未检测到地塞米松释放;释放出的地塞米松 吸收缓慢, 达峰时间(tmax) 为 7.2 h, 血浆药物峰浓度 (Cmax)为 42 μg·L-1, 曲 线 下 面 积 (AUC) 为 334 μg·h·L-1。 地塞米松灌胃后, 药物主要分布在 胃、小肠近端及小肠远端的内容物和粘膜中, 药物吸 收迅速, tmax 为 2.2 h, Cmax 为 2 120 μg·L-1, AUC 为 11 875 μg·h·L-1结论: 以当归多糖为载体的地塞 米松前体药具有良好的结肠定位转释作用, 有可能 成为一种具有良好应用前景的结肠炎治疗药物。

关键词: 结肠靶向释药, 前体药, 地塞米松, 当归多糖, 结肠炎

Abstract: AIM: To explore the transport and deliv-ery of active drug from dexamethasone-angelica sinensis polysaccharides prodrug in the gastrointestinal tract of rats.METHODS: Dexamethasone and the prodrug were orally administered to rats at the dose of 1.96 mg·kg-1 (calculated by carried dexamethasone).The drugs in the plasma and contents of different parts of the rats' gastroi-ntestinal tract were determined by high performance liquid chromatography (HPLC).RESULTS: Dexamethasone carried by the prodrug wasmainly released in the contents andmucosa of cecum and colon after oral administration of the prodrug.The absorption of released dexamethasone was reduced significantly.The peak time, peak concen-tration and AUC were 7.2 h, 42 μg·L-1 and 334 μg·h·L-1, respectively.However, free dexamethasone was found mainly in the contents and mucosa of the stom-ach, proximal and distal small intestine after oral admin-istration.The peak time, peak concentration and AUC were 2.2 h, 2 120 μg·L-1 and 11 875 μg·h·L-1, re-spectively.CONCLUSION: Dexamethasone can be spe-cifically delivered to the cecum and colon by using dexam-ethasone-angelica sinensis polysaccharides prodrug.The absorption of dexamethasone was reduced significantly and the drug concentration in colon was increased significant-ly.The prodrug has a potential in the treatment of colitis.

Key words: colon-targeted delivery system, pro-drug, dexamethasone, angelica sinensis polysaccharides, colitis

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