结肠靶向控释片的制备及体外释药性能评价

Preparation of colon-targeted controlled release tablets and evaluation of drug release in vitro

目的 制备结肠靶向控释片,并评价其体外释药性能。方法 以普萘洛尔为模型药物,蒙脱石、魔芋多糖为辅料制备片芯,采用酶降解试验考察肠道微生物对魔芋多糖的分解能力。片芯用Eudragit FS 30D包衣,制成结肠靶向控释片;采用吸水试验考察结肠靶向控释片的吸水能力;转篮法测定其体外释药性能;X线成像观察其在新西兰兔消化道内的运动轨迹和形态。结果 片芯在β-甘露聚糖酶、大鼠结肠物(RCC)溶液中5 d后重量分别减少31.2%、31.9%。结肠靶向控释片在PBS溶液中6 h后重量增加到104.0%。体外释放结果显示:增重15%的片剂延缓药物4.5 h后释放,在RCC溶液中的释药性显著提高。X射线成像观察到片剂进入新西兰兔消化道4.5 h后崩解。结论 制备的结肠靶向控释片能够到达结肠崩解,并延缓药物释放,为结肠靶向给药系统的制备提供了新思路。

OBJECTIVE To prepare colon-targeted controlled release tablets and evaluate their drug release performance in vitro.METHODS The tablet core was prepared with propranolol as model drug and montmorillonite and konjac polysaccharide as excipients.Enzymatic degradation test was used to investigate the decomposition ability of konjac polysaccharides by intestinal microorganisms.The core was coated with Eudragit FS 30D to prepare colon-targeted controlled release tablets.Water absorption test was used to investigate the water absorption ability of colonic targeted controlled release tablets.The in vitro drug release performance was determined by basket turning method.X-ray imaging was used to observe the movement trajectory and morphology in the digestive tract of New Zealand rabbit.RESULTS After 5 days in β-mannanase or rat colonic material(RCC) solution, the weight of the tablet core decreased by 31.2% and 31.9%,respectively.The weight of colon-targeted controlled release tablets increased to 104.0% after 6 h in PBS solution.In vitro release results showed that the tablets with 15% weight gain delayed drug release after 4.5 h, and the drug release in RCC solution was significantly improved.X-ray imaging observed that the tablets disintegrated 4.5 h after entering the digestive tract of New Zealand rabbits.CONCLUSION The colon-targeted controlled release tablets prepared in this study can achieve colon disintegration and delay drug release, which provides a new idea for the preparation of colon-targeted drug delivery system.