混合水分散体肠溶迟释薄膜性能研究

目的 采用肠溶型水分散体Eudragit?L30D-55和控释型水分散体Kollicoat?SR30D混合制备一种全新的对周围环境pH值具有响应的，同时具有迟释性能的聚合物薄膜。方法 采用铸膜法制备L30D-55∶SR30D混合水分散体游离膜，采用差示扫描量热法(DSC)测定薄膜玻璃化转变温度(glass transition temperature，Tg)，万能材料试验机测试薄膜拉伸性能，杯法考察薄膜透湿性能。考察聚合物比例、附加剂种类和用量对薄膜性能的影响，并以制备泮托拉唑钠(PAZ-Na)肠溶迟释微丸考察包衣膜特性。结果 随着SR30D的增加，薄膜的Tg逐渐降低，强度和刚性变弱，韧性变强，透湿性能先不变后增加。随着增塑剂增加，薄膜刚性减弱，渗透性能增强。不溶性成分的加入可不同程度降低薄膜的渗透性。制备的肠溶迟释微丸在0.1 mol·L^-1盐酸中2 h药物损失量<5%，在pH 6.8缓冲液中可延迟10~20 min开始释放，并至90 min释放完全。结论 L30D-55∶SR30D混合水分散体制备的游离膜和包衣膜具有良好的理化性能，可用于肠溶调释制剂的研究和开发。

Studies on Delayed-release Enteric Film Using Blends of Aqueous Dispersion

OBJECTIVE To prepare new polymer film using blends of enteric Eudragit?L30D-55 and sustained-release Kollicoat?SR30D which can provide drug delayed-release profiles that triggered by the pH of the surrounding environment along the gastrointestinal tract. METHODS Free film of polymer blends was prepared by casting technique. Properties of the cast film including glass transition temperature(Tg), mechanical properties and permeability were investigated. Effect of polymer blend ratio and additive on properties of the cast film was evaluated. Pantoprazole sodium(PAZ-Na) was selected as a model drug to prepare delayed-release enteric pellets. RESULTS With an increasing content of SR30D, properties of the cast films varied Tg decreased; strength and stiffness of film weakened, tenacity enhanced; water vapor permeability remained at a certain level firstly, and then increased. With an increasing amount of plasticizer, stiffness of free film weakened and water vapor permeability increased. With the addition of insoluble additive, water vapor permeability decreased at different level. Less than 5% drug degradation occurred after pellets exposed to 0.1 mol·L^-1 HCl solution for 2 h. The delayed-release enteric pellets began to release the drug after 10-20 min and released completely after 90 min in phosphate buffer of pH 6.8. CONCLUSION Free film and coating of polymer blends offers favorable physical characteristics. Blends of aqueous dispersion of Eudragit?L30D-55 and Kollicoat?SR30D can be used for R&D of modified-release enteric preparations.