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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
引用本文:李建平,石鑫.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[J].化学学报,2011,69(20):2439-2444.
作者姓名:李建平  石鑫
作者单位:(辽宁师范大学化学化工学院, 功能材料化学研究所 大连 116029)
基金项目:辽宁省高等学校科研计划(No.2008367)资助项目
摘    要: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  

Diclofenac Sodium Loaded pH-Sensitive Mesoporous Zirconium Diphosphonate Coated with Lag-time Films for Controlled Colon-targeted Release
Li,Jianping Shi,Xin.Diclofenac Sodium Loaded pH-Sensitive Mesoporous Zirconium Diphosphonate Coated with Lag-time Films for Controlled Colon-targeted Release[J].Acta Chimica Sinica,2011,69(20):2439-2444.
Authors:Li  Jianping Shi  Xin
Institution:(Institute of Chemistry for Functionalized Materials, College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029)
Abstract: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 di-clofenac sodium loaded pH-sensitive mesoporous zirconium diphosphonate tablet.Based on the investiga-tions of diclofenac sodium adsorbed onto and released from pH-sensitive mesoporous zirconium diphos-phonate,a...
Keywords:pH-sensitive mesoporous zirconium diphosphonate  lag time  diclofenac sodium  co-lon-targeted drug delivery  
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