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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (20): 2439-2444. 上一篇    下一篇

研究论文

辅以时滞的pH-敏感介孔膦酸锆对双氯芬酸钠的可控结肠靶向释放

李建平，石鑫*   

  1. (辽宁师范大学化学化工学院， 功能材料化学研究所 大连 116029)
  • 投稿日期:2011-04-27 修回日期:2011-06-02 发布日期:2011-06-16
  • 通讯作者: 石鑫 E-mail:xinshi@lnnu.edu.cn
  • 基金资助:

    辽宁省高等学校科研计划项目

Diclofenac Sodium Loaded pH-Sensitive Mesoporous Zirconium Diphosphonate Coated with Lag-time Films for Controlled Colon-targeted Release

LI Jian-Ping, SHI Xin   

  1. (Institute of Chemistry for Functionalized Materials, College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029)
  • Received:2011-04-27 Revised:2011-06-02 Published:2011-06-16
  • Contact: Xin SHI E-mail:xinshi@lnnu.edu.cn

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944

被引次数

11

以pH-敏感介孔膦酸锆作为药物载体, 选用治疗时辰节律性疾病(风湿性关节炎)的药物双氯芬酸钠作为药物模型, 利用蘸涂的方法对载药的pH-敏感介孔膦酸锆进行时滞膜的包覆, 建立起一个时滞型和pH-敏感型相结合的口服结肠靶向给药系统. 在系统研究pH-敏感介孔膦酸锆对双氯芬酸钠吸附和释放的基础之上, 通过调控时滞膜的厚度控制释放双氯芬酸钠的时滞时间约为6 h. 该给药系统在人工模拟胃液中3 h内完全不释放双氯芬酸钠, 而在人工模拟肠液中最初的3 h(可以看成发生在小肠)所释放的双氯芬酸钠仅为全部释放量的9%, 在之后的46 h内(可以看成发生在结肠)缓慢释放的双氯芬酸钠则占全部释放量的90%以上. 这样, pH-敏感介孔膦酸锆作为新型药物载体与时滞效应相结合, 通过时滞和pH-敏感双重控制实现了治疗时辰节律性疾病药物在结肠的定位释放.

关键词: pH-敏感介孔膦酸锆, 时滞, 双氯芬酸钠, 结肠靶向给药

pH-Sensitive mesoporous zirconium diphosphonate as drug carrier and diclofenac sodium for diseases susceptible to the circadian rhythm (rheumatic arthritis) as model drug, a lag-time combined with pH-sensitive colon-targeted drug delivery system was successfully prepared by coating lag-time films on diclofenac sodium loaded pH-sensitive mesoporous zirconium diphosphonate tablet. Based on the investigations of diclofenac sodium adsorbed onto and released from pH-sensitive mesoporous zirconium diphosphonate, a lag time of 6 h can be controlled through adjusting the thickness of lag-time film. The diclofenac sodium loaded pH-sensitive mesoporous zirconium diphosphonate tablet coated by lag-time films released no diclofenac sodium within 3 h in the simulated gastric solution, released diclofenac sodium less than 10% of gross released amount of diclofenac sodium within the first 3 h (thinked as occurring in small intestine) and slowly released diclofenac sodium more than 90% of gross released amount of diclofenac sodium within the following 46 h (considered as happening in colon) in the simulated intestinal solution. Thus, drugs for treatment of diseases susceptible to the circadian rhythm can be colon-specifically released in such dual controll of lag-time and pH-sensitive colon-targeted drug delivery system.

Key words: pH-sensitive mesoporous zirconium diphosphonate, lag time, diclofenac sodium, colon-targeted drug delivery