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双氯芬酸钠缓释微丸型片剂的制备及其药动学 被引量:2

Preparation and Pharmacokinetics of Diclofenac Sodium Multiple-unit Tablets with Sustained-release Pellets
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摘要 采用挤出滚圆法制备双氯芬酸钠微丸,以Eudragit NE30D为包衣材料、流化床包衣得到缓释微丸,考察了滑石粉用量及包衣增重对缓释微丸释放行为的影响;通过调整缓释微丸与辅料的比例,筛选润滑剂的种类,优化制备工艺,将缓释微丸压制成多单元缓释微丸型片剂。通过测定家兔血药浓度,考察其体内药动学行为。结果表明,当双氯芬酸钠∶微晶纤维素∶一水乳糖为2∶3∶5(w/w)时,以适量0.2%羟丙甲纤维素E15溶液作黏合剂,可得到粒径450μm的含药微丸;滑石粉∶包衣材料(固含物)为1∶1(w/w)、包衣增重为27%时包衣微丸的缓释效果良好。双氯芬酸钠缓释微丸∶辅料以4∶6(w/w)混合后,加入适量聚乙烯吡咯烷酮K30水溶液,制粒,烘干后压制的微丸片与市售缓释胶囊的体外释放行为较相似。家兔单剂量给予自制的双氯芬酸钠普通片和缓释微丸片后,二者在家兔体内的t1/2分别为2.01和4.00 h,AUC0→∞分别为277.92和477.98μg·L^(-1)·h,可见缓释微丸片的半衰期以及生物利用度均得到显著提高。 This study aimed to prepare diclofenac sodium (DS) sustained-release pellets and compress the pellets into tablets while maintaining the sustained-release property of the pellets. The DS pellets with mean particle diameter of 450 μm were fabricated by extrusion-spheronization method. Sustained-release pellets were obtained by coating of Eudragit NE30D to raw pellets via fluidized bed. The drug release of the coating pellets was optimized by adjusting proportion of talcum powder in the coating solution and controlling weight gain of the pellets. The pellets were subsequently compressed into tablets with cushioning excipients. Formulations of pellet-based tablets were optimized by adjusting proportion of the sustained-released pellets and the excipients, screening the kinds of lubricant, adjusting the process and the pressure of fabrication. Finally, pharmacokinetics of pellet-based tablets was investigated in rabbit model. The pellets containing DS (20%, w/w), microcrystalline cellulose (MCC) 101 (30%, w/w) and lactose monohydrate (50%, w/w) were prepared with 0.2 % hypromellose E15 solution as an adhesive. When the ratio of talcum powder and coating material was 1 : 1 (w/w) and the weight gain was 27%, the coated pellets demonstrated a desired sustainedrelease profile. Innovation of this study was to improve the homogeneity of the materials. Three methods, namely, direct pressure, wet granulation with the excipients of lactose and MCC PH200, and wet granulation with the excipients of lactose and MCC 101 were adopted to prepare the title tablets. Although there was no record on wet granulation in literature, wet granulation resulted in optimal product. Blending sustained-release coated pellets and excipients at the ratio of 4 : 6 (w/w), followed by adding appropriate amount of polyvinyl pyrrolidone (PVP) K30 aqueous solution, granulation, drying and tabletting, the title tablets were obtained. The results showed that the release behaviors between the above self-made tablets and
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2018年第1期74-81,共8页 Chinese Journal of Pharmaceuticals
关键词 双氯芬酸钠 多单元片 缓释 微丸 体外释放 药动学 diclofenac sodium multiple-unit tablet sustained-release pellet in vitro release pharmacokinetics
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