| 引用本文: | 高显峰,高建青.热熔挤出技术制备硝苯地平固体分散体[J].中国现代应用药学,2012,29(11):1002-1006. |
| GAO Xianfeng,GAO Jianqing.Preparation of Nifedipine Solid Dispersion by Hot-melt Extrusion Technology[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(11):1002-1006. |
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| 摘要: |
| 目的 利用热熔挤出技术制备难溶性药物硝苯地平固体分散体，提高其溶出度，并进一步制成控释片剂。方法 以丙烯酸树脂Ⅳ号、醋酸羟丙甲基纤维素琥珀酸酯、聚乙烯吡咯烷酮共聚物、高取代羟丙基纤维素为载体，采用同向双螺杆热熔挤出机制备硝苯地平固体分散体，考察不同载体挤出物在不同介质中的累积溶出度，为筛选合适的固体分散体，进一步制备控释片做准备。结果 利用热熔挤出技术制备的固体分散体均显著提高了硝苯地平的溶出度，通过羟丙基甲基纤维素骨架材料的控制作用，制成了符合零级释放的控释制剂。结论 热熔挤出技术制备固体分散体能够提高难溶性药物硝苯地平的溶出度，并能进一步制成符合零级释放的控释片。 |
| 关键词: 热熔挤出 硝苯地平 固体分散体 |
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| Preparation of Nifedipine Solid Dispersion by Hot-melt Extrusion Technology |
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GAO Xianfeng1,2, GAO Jianqing3
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1.Institute of Pharmaceutics, Zhejiang University, Hangzhou 310058, China;2.Zhejiang Pharmaceutical College, Ningbo 315100, China;3.Institute of Pharmaceutics, Zhejiang University, Hangzhou 310058, China
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| Abstract: |
| OBJECTIVE Hot-melt extrusion technology was used to prepare solid dispersion of nifedipine for improving its dissolution, and moreover controlled-release tablets were prepared based on the solid dispersion. METHODS Acrylic resin Ⅳ, hydroxypropylmethylcellulose acetate succinate (HPMCAS), polyethylene pyrrole copolymer(PVP-VA64) and high replace hydroxypropyl cellulose(H-HPC) were selected as carriers. The homonymous double screw extrusion method was used for prepare nifedipine solid dispersion. The dissolution of various extrudates in different mediums were studied. Furthermore, nifedipine tablets were prepared. RESULTS The dissolution of nifedipine was improved significantly by solid dispersion technology and the tablets made by hydroxypropyl methyl cellulose matrix showed the zero order release controlled-release. CONCLUSION Solid dispersion using hot-melt extrusion technology can improve the dissolution of poorly water soluble drug nifedipine, and further form the controlled-release formulation. |
| Key words: hot-melt extrusion nifedipine solid dispersion |
