热熔挤出法制备尼美舒利固体分散体

赵优曼,赵会英,马驰

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (3) : 185-188.

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中国药学杂志 ›› 2013, Vol. 48 ›› Issue (3) : 185-188. DOI: 10.11669/cpj.2013.03.007
论 著

热熔挤出法制备尼美舒利固体分散体

  • 赵优曼,赵会英,马驰
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Preparation of Nimesulide Solid Dispersion by Hot Melt Extrusion Technology

  • ZHAO You-man, ZHAO Hui -ying, MA Chi
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摘要

目的 采用热熔挤出技术制备难溶性药物尼美舒利固体分散体,提高其溶出速率。方法 以共聚维酮(PVP-VA64,Kollidon VA64)、聚维酮(PVPK30)或聚乙烯醇-聚乙二醇(3∶1)接枝共聚物(Kollicoat IR)为亲水性载体材料,使用双螺杆热熔挤出机制备尼美舒利固体分散体,通过差示扫描量热法(DSC)、X射线衍射法(XRD)、傅立叶红外光谱(FTIR)和体外溶出度测定来表征和评价所制备的固体分散体。结果 以共聚维酮为载体制备的尼美舒利固体分散体药物溶出最快,在pH 7.4的磷酸盐缓冲液中10 min溶出达到81%,远快于物理混合物(1 h时只有37%)。X射线衍射图谱显示药物晶体衍射峰消失,差示扫描量热图谱显示药物晶体吸热峰消失,提示药物是以无定形态分散在载体材料中。结论 热熔挤出加工技术适用于制备尼美舒利-共聚维酮固体分散体,药物是以无定形态分散在载体中,溶出度得到显著提高。

Abstract

OBJECTIVE To improve the in vitro dissolution of nimesulide by preparing nimesulide solid dispersion with hot melt extrusion (HME) technology. METHODS Using PVP-VA64,PVP K30 or PVA-PEG (Kollicoat IR) as hydrophilic carrier,nimesulide solid dispersion was prepared by hot melt extrusion and characterized by drug dissolution, DSC, XRD and FTIR. RESULTS Nimesulide exhibited rapid in vitro dissolution from the solid dispersion using PVP-VA64 as carrier. The cumulative release rate was 81% in 10 min, much faster than its physical mixture (only 37% in 1 h). The results of DSC and FTIR showed that nimesulide was amorphously dispersed in the carrier.CONCLUSION Hot melt extrusion technology is suitable for preparing nimesulide-PVP-VA64 solid dispersion, which can significantly increase drug dissolution.

关键词

热熔挤出技术 / 固体分散体 / 尼美舒利 / 共聚维酮 / 溶出度

Key words

hot melt extrusion / solid dispersion / nimesulide / PVP-VA64 / dissolution

引用本文

导出引用
赵优曼,赵会英,马驰. 热熔挤出法制备尼美舒利固体分散体[J]. 中国药学杂志, 2013, 48(3): 185-188 https://doi.org/10.11669/cpj.2013.03.007
ZHAO You-man, ZHAO Hui -ying, MA Chi. Preparation of Nimesulide Solid Dispersion by Hot Melt Extrusion Technology[J]. Chinese Pharmaceutical Journal, 2013, 48(3): 185-188 https://doi.org/10.11669/cpj.2013.03.007
中图分类号: R944   

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基金

基金项目北京市自然科学基金资助项目(7092052)
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