自制双氯芬酸钠缓释片及其与原研药扶他林缓释片的体外释放一致性研究

In-vitro drug release consistency study between homemade sodium diclofenac extended release tablet and Voltaren Retard

目的 :采用乙基纤维素和羟丙甲纤维素为缓释材料制备双氯芬酸钠缓释片,并与原研药扶他林缓释片(Voltaren Retard,100 mg/片)比较体外释放的一致性。方法 :先将双氯芬酸钠原料药与乳糖混匀,于流化床中以固含量10%乙基纤维素的95%乙醇溶液制粒。干燥后的颗粒再与羟丙甲纤维素混匀,加入硬脂酸镁后压制成双氯芬酸钠缓释骨架片,最后以标准型欧巴代对片剂进行包衣,包衣增重3%(w/w)。分别采用不同pH介质的中国药典篮法和使用生物相关介质的美国药典往复筒法对自制双氯芬酸钠缓释片与扶他林缓释片的体外释放度进行检测和比较。结果与结论 :使用乙基纤维素和羟丙甲纤维素制备的双氯芬酸钠缓释片的体外释放趋势与扶他林缓释片相近。

Objective： To compare the in-vitro drug release consistency between homemade sodium diclofenac extended release tablets prepared by using hypromellose （Methocel K100LV CR） and ethyl cellulose （Ethocel 10cp FP） as drug dissolution rate control polymers and innovator Voltaren Retard （100 mg）. Methods： Sodium diclofenac extended release tablets were manufactured by mixing API with lactose and then granulating with ethyl cellulose containing 10% solid in 95% alcohol in fluid bed. The dried granules were mixed with hypromellose until uniform and sodium diclofenac extended release matrix tablets were pressed into by adding magnesium stearate. The tablets were coated by Opadry with 3% （w/w） weight gain. The drug release profiles in-vitro were determined by a basket method in four different pH media for homemade tablets and a reciprocating tube method in bio-relative media recorded in the Pharmacopeia of the United States for innovator Voltaren Retard and compared. Results ＆ Conclusion： The drug release profile in-vitro of the homemade sodium diclofenac extended release tablets is closed to that of the innovator.