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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 phosphate as a drug carrier, the treatment of rhythmic disease (rheumatoid arthritis) drug diclofenac sodium as a drug model, the use of dip coating method of pH-sensitive mesoporous zirconium phosphate Time lag film and pH-sensitive oral colon-specific drug delivery system was established.Studying the effect of pH-sensitive mesoporous zirconium phosphate on the adsorption and release of diclofenac sodium , The time delay of controlled release diclofenac sodium by controlling the thickness of time-lag membrane was about 6 h.The diclofenac sodium was not released at all within 3 h in artificial simulated gastric fluid, whereas in the first 3 h in artificial simulated intestinal fluid (Which can be thought of as occurring in the small intestine) releases only 9% of the total amount of diclofenac released, while diclofenac released slowly over the next 46 hours (which can be seen in the colon) accounts for more than 90% of total release In this way, pH-sensitive mesoporous zirconium phosphonate as a novel drug carrier combined with the time-lag effect, the time-dependent and pH-sensitive dual control to achieve the treatment of rhythmic disease drug release in the colon positioning.