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新型口服活性炭微球对链脲佐菌素诱导的糖尿病模型大鼠治疗作用的研究

沈晴, 高姗姗, 谢毅妮, 凌立成, 高峰*   

  1. 1. 华东理工大学 药学院, 上海 200237
    2. 华东理工大学 上海市功能性材料化学重点实验室, 上海 200237
    3. 上海市食品药品监督管理局 认证审评中心, 上海 200020
    4. 华东理工大学 化工学院, 上海 200237
    5. 华东理工大学 上海市新药设计重点实验室, 上海 200237
  • 收稿日期:2011-12-13 修回日期:2012-03-02 出版日期:2012-05-15 发布日期:2012-05-15
  • 通讯作者: 高峰*

Curative effect of novel oral carbon microspheres on streptozotocin-induced
diabetes mellitus in rats

Qing Shen, Shan-Shan Gao, Yi-Ni Xie, Li-­Cheng Ling, Feng Gao*   

  1. 1. Department of Pharmaceutics, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
    2. Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, China
    3. Center for Certification & Evaluation, SHFDA, Shanghai 200020, China
    4. School of Chemical Engineering, East China University of Science and Technology, Shanghai 200237, China
    5. Shanghai Key Laboratory of New Drug Design, East China University of Science and Technology, Shanghai 200237, China
  • Received:2011-12-13 Revised:2012-03-02 Online:2012-05-15 Published:2012-05-15
  • Contact: Feng Gao*

摘要:

制备并表征了孔径不同的活性炭微球, 考察其对糖尿病模型大鼠的治疗作用。通过制备工艺的改良, 制得了直径在0.2-0.3 mm的活性炭微球。通过对葡萄糖的吸附实验, 筛选最优的活性炭微球。采用雄性Sprague-Dawley大鼠腹腔注射链脲佐菌素诱导制得糖尿病大鼠模型。两组大鼠采用每天两次口服灌胃活性炭微球, 连续给药30天。通过离体肠段外翻实验法, 测定葡萄糖的跨膜透过量。与糖尿病组相比, 在服药2周以后, 活性炭微球治疗组的血糖水平明显降低, 改善血糖耐受量。在肠粘膜侧有活性炭微球存在时, 葡萄糖分子的渗透清除率显著增大, 尤其是当浆膜侧的葡萄糖浓度较高时 (10 mg/mL)。 筛选得到的活性炭微球BET比表面积为1566 m2/g, 微孔含量高 (0.478 cm3/g), 球形良好, 对葡萄糖吸附率高。作为口服微球制剂, 活性炭微球对链脲佐菌素诱导的糖尿病大鼠有治疗作用。

关键词: 活性炭微球, 孔隙结构, 吸附特性, 治疗作用, 糖尿病大鼠

Abstract:

A kind of novel pitch-based activated carbon microsphere (ACM) characterized by its controlled porous structure was developed in this study, the curative effect of this ACM on diabetes mellitus in rats was investigated. ACM 0.2-0.3 mm in diameter was prepared by modified method. The optimal ACM was screened by its adsorption ability for glucose. Diabetes mellitus model was established by streptozotocin injection in male Sprague-Dawley rats. Two groups of rats were orally administrated with ACM twice a day for 30 d. Intestinal glucose transport was determined in vitro using everted rat intestinal sacs technique. Compared with the diabetic mellitus group, the ACM treated group showed significant lower blood glucose level and improved glucose tolerance after two-week treatment. If ACM was applied in the mucosal side, glucose permeation clearance in the ACM treated group was significantly higher than that of the control group, especially at high glucose concentration (10 mg/mL) on the serosal side. The selected ACM possessed a BET specific surface of 1566 m2/g and high volume of micropores (0.478 cm3/g) with fine spherical morphology, and showed more significant adsorption capacity for glucose. As oral microsphere preparations, ACM presented the curative effect on streptozotocin-induced diabetes mellitus in rats.

Key words: Activated carbon microsphere, Porous structure, Adsorption behavior, Protective effect, Diabetes mellitus rats

中图分类号: 

Supporting:

Foundation items: The Ministry of Science and Technology of the People's Republic of China (Contract No. 2010DFA44300) and Shanghai Committee of Science and Technology (Grant No. 10DZ2220500 and 11DZ2260600).
*Corresponding author. Tel.: 86-21-64252449