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  

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

作　　者：李建平[1] 石鑫[1] 

机构地区：[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

出　　处：《化学学报》2011年第20期2439-2444,共6页Acta Chimica Sinica

基　　金：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.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 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 con-troll of lag-time and pH-sensitive colon-targeted drug delivery system.

关 键 词：pH-敏感介孔膦酸锆 时滞 双氯芬酸钠 结肠靶向给药 

分 类 号：R943[医药卫生—药剂学]