非诺贝特缓释胶囊栓的制备及其生物利用度研究

刘羽 孙备 王贺 李姜晖

中国药学杂志 ›› 2011, Vol. 46 ›› Issue (15) : 1173-1178.

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中国药学杂志 ›› 2011, Vol. 46 ›› Issue (15) : 1173-1178.
论著

非诺贝特缓释胶囊栓的制备及其生物利用度研究

  • 刘羽,孙备,王贺,李姜晖
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Preparation of Sustained-Release Capsule-Suppositories of Fenofibrate with Emulsified-Solid Dispersing Technology

  • LIU Yu, SUN Bei, WANG He, LI Jiang-hui
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摘要

目的 采用乳化固体分散技术制备非诺贝特缓释胶囊栓。并以非诺贝特为模型药物来说明制剂方法及原理。方法 混合存在极性差异的低熔点原辅料,加热使混合物液化,在乳化剂的作用下,使原本分离的两相混合,形成分散相和连续相,所形成的乳液灌装胶囊,冷却后形成乳化固体分散体胶囊栓。考察该胶囊栓的溶出及所形成的微粒粒径。并与市售缓释品种进行生物利用度比较。并探讨该制剂方法的制剂原理。结果 该胶囊栓具有缓释特征;电镜检查结果显示,该胶囊栓中所形成的微粒粒径可达到1 μm左右;与市售产品相比,生物利用度有了大幅度提高。结论 该制剂方法可以以低成本制备高生物利用度的非诺贝特缓释胶囊栓。

Abstract

OBJECTIVE To establish a simple method for preparing sustained-release capsule suppositories of fenofibrate with the emulsified-solid dispersing technology (ESD). METHODS Low melting point materials with the different polarity were used.The mixture was melted into liquid form. With the help of emulsifying agent(s), the seperated phases were mixed. The "Continuous phase" and "dispersed phase" were obtained. Capsules were filled with the emulsion,While cooling down,the "emulsion" of mixture was solidified. The fenofibrate sustained-release capsule-suppositories were generated. The dissolution of the capsule suppository , the size of solid lipid microparticles and the comparison of bioavailability between self-made sustained-release capsule-suppositories and commercially available sustained-release capsules were studied. The principles of the preparation were explored. RESULTS The size of particles formed in this preparation were 1 μm which was confirmed by the electron microscope examination. Compared with the commercially available products, bioavailability was improved significantly. CONCLUSION The preparation method could be used to prepare the high bioavailable sustained-release capsules suppositories of fenofibrate cost-effectively.

关键词

非诺贝特 / 乳化固体分散技术 / 缓释 / 生物利用度

Key words

fenofibrate / the emulsified-solid dispersing technology(ESD) / sustained-release / bioavailability

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导出引用
刘羽 孙备 王贺 李姜晖 . 非诺贝特缓释胶囊栓的制备及其生物利用度研究[J]. 中国药学杂志, 2011, 46(15): 1173-1178
LIU Yu;SUN ei;WNG He;LI Jing-hui. Preparation of Sustained-Release Capsule-Suppositories of Fenofibrate with Emulsified-Solid Dispersing Technology[J]. Chinese Pharmaceutical Journal, 2011, 46(15): 1173-1178

参考文献


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