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目的:以阿司匹林为模型药制备壳聚糖pH敏感结肠定位给药系统,并考察其体外释药行为。方法:以N-磷酸化壳聚糖衍生物(NPCP)作为药物载体,利用戊二醛交联制备了固载模型药物的凝胶,并研究该载药凝胶在模拟人体胃肠道环境中的释放情况。结果:在人工胃液中药物释放较少,在pH6.8和pH7.8的磷酸盐缓冲液中缓慢释放,且pH越高,释药速度越快,无交联pH7.8在7h内释药完全,交联的载药凝胶86h释放完毕。结论:NPCP有望作为药物载体用于开发具有pH敏感性的口服定位给药系统。
OBJECTIVE: To prepare chitosan pH-sensitive colon-targeted delivery system using aspirin as a model drug and investigate its in vitro release behavior. METHODS: N-Phosphorylated chitosan derivatives (NPCP) were used as drug carriers and glutaraldehyde cross-linked gels were prepared to immobilize the model drugs. The drug-loaded gels were studied in a simulated human gastrointestinal environment Release situation. Results: There was less drug release in the artificial gastric juice, which was slowly released in phosphate buffer solution of pH6.8 and pH7.8. The higher the pH value was, the faster the drug release was. No cross-linked pH7.8 was released within 7h Complete, cross-linked drug-loaded gel 86h release is completed. CONCLUSIONS: NPCP is expected to be used as a drug carrier for the development of pH-sensitive oral drug delivery systems.