替硝唑结肠给药系统的研制

Preparation of Colonic Delivery System for Tinidazole

依据时控型结肠给药系统原理 ,以替硝唑为模型药物 ,利用干压包衣和薄膜包衣双层包衣的方法制备了结肠给药系统 ,并对影响药物释放的因素 (如 EC粒度 ,HPMC粘度 ,时控层厚度 ,片剂硬度等 )、肠衣层性能和药物释放稳定性等进行了考查。结果表明 ,HPMC粘度增加使药物释放滞后时间延长 ,但高粘度 HPMC会导致药物释放无明显突跃点 ;包芯片硬度 40～ 6 0 N、片重 0 .2 6～ 0 .2 8g的片剂药物释放较稳定。加速试验 ( 3个月 )结果表明 ,药物释放稳定性良好。

Using tinidazole as the model drug, a colonic delivery system based on time-controlled principles was prepared by employing the techniques of compression coating and enteric coating. Factors such as the particle size of ethylcellulose(EC) and viscosity grade of hydroxypropyl-methylcellulose(HPMC), the thickness of time-controlled layer, the tablet hardness and the properties of the enteric layer were investigated for their possible effects on drug release. The results showed that the lag time before drug release was lengthened with the increase of the viscosity grade of HPMC. Drug release remained stable when weight and hardness of tablets were in the range of 0.26~0.28 g and 40~60 N, respectively. The accelerated test demonstrated the satisfactory stability of drug release from the presented system.