结肠定位释药双氯芬酸钠包衣片的制备和体外释放

Preparation and in vitro release of coated diclofenac sodium tablet s for colon-specific delivery

目的 以 3种不同包衣材料制备时间依赖型结肠定位释药包衣片 ,并考察其体外释放影响因素。方法 以双氯芬酸钠为模型药物 ,分别以乙基纤维素、Surelease 和醋酸纤维素为包衣材料制备包衣片 ,用释放度测定法考察影响药物释放的因素。结果 膨胀剂种类、包衣增重和包衣液中致孔剂浓度是影响药物释放的关键因素。 3种包衣材料制备的双氯芬酸钠包衣片体外延时时间均可达到 5～ 6h。

OBJECTIVE: Three potential coating materials for time-dependent colon-specific drug delivery were investigated. METHODS: Diclofenac sodium was used as a model drug and ethylcellulose(EC), Surelease&reg and cellulose acetate (CA) as coating materials. The behaviors of colon-specific delivery coated tablets were evaluated in vitro by dissolution test. RESULTS: Three parameters were critical in reducing the beginning release time of diclofenac sodium, the decreasing of the concentration of the pore former, the increasing of the coat weight and the decreasing of swelling agent. All of the tablets coated with EC, Surelease&reg or CA containing certain pore former reached a lag time of 5 h. CONCLUSIONS: It provided the technologies for colon-specific drug delivery using time as the release trigger.