熔融高速搅拌法制备双氯芬酸钠缓释胶囊的研究-中国现代应用药学.PDF

熔融高速搅拌法制备双氯芬酸钠缓释胶囊的研究 孟祥磊，王洪光(青岛科技大学药学院，山东 青岛 266042) 摘要：目的 研究熔融高速搅拌法制备双氯芬酸钠缓释胶囊及其体外释药行为。方法 采用 KJZ-10 型熔融高速搅拌制粒机 制备含药微丸，以微丸体外释放度为指标，考察处方工艺因素对微丸体外释放度的影响，通过释放度曲线药动力学拟合确 定微丸缓释机制。结果 双氯芬酸钠微丸体外释放行为符合 Higuchi 方程 Y=35.43t1/2-16.152 3(r=0.998 8) ，释药机制主要是 骨架溶蚀和扩散释放。结论 该技术制备的双氯芬酸钠缓释微丸具有较好的释药性能及良好的缓释效果。 关键词：熔融法；缓释胶囊；骨架溶蚀；双氯芬酸钠 中图分类号：R943.41 文献标志码：A 文章编号：1007-7693(2009)08-0641-04 Studies on Preparation of Diclofenac Sodium Sustained-release Capsules by High-shear Melt Agglomeration MENG Xianglei ，WANG Hongguang (Department of Pharmacy, Qingdao University of Science and Technology, Qingdao 266042, China) ABSTRACT: OBJECTIVE To prepare diclofenac sodium sustained-release pellets by high-shear melt agglomeration technology and study its in vitro drug release. METHODS Drug-contained pellets were prepared in a high-shear granulator, and the influencing factors of formulation and technique on pellets releasing profile were investigated and the mechanism of drug releasing from pellets was also studied. RESULTS The release of the drug from pellet was in accordance with Higuchi equation: Y=35.43t1/2-16.152 3(r=0.998 8). The mechanism of diclofenac sodium releasing from pellets was matrix erosion and diffusion. CONCLUSION The diclofenac sodium sustained-release pellets made by this technique provided a rather good sustained-release profile. KEY WORDS ：melt agglomeration; sustained-release capsule ；matrix erosion ；diclofanc sodium 双氯芬酸钠，又名双氯灭痛，是一种强效非甾 1 仪器与试剂 体类消炎药。临床上用于治疗风湿，类风湿性关节 KJZ-10 型熔融高速搅拌制粒( 上海信谊制药 炎，神经炎以及各种原因引起的发热。由于其半衰 厂) ，YP202N 电子天平(上海精密仪器厂) ，ZRS-12G 期仅为 1～2 h[1]，普通制剂(25 mg 规格)需每天服用 型溶出仪(天津市天大发科技有限公司) ，T6 型紫外 3 次，且一半药物在肝脏被首过代谢，制成缓释剂 分光光度计(上海普析通用仪器有限责任公司) 。 型，可有效解决上述问题。目前国内外已有市售的