| 引用本文: | 刘一欢,顾王文,陆振举,刘怡,孙考祥.基于HPMCAS载体的依非韦伦固体分散体溶出模式研究[J].中国现代应用药学,2020,37(9):1096-1101. |
| LIU Yihuan,GU Wangwen,LU Zhenju,LIU Yi,SUN Kaoxiang.Study on the Dissolution Model of Efavirenz in Solid Dispersion Based on HPMCAS Carrier[J].Chin J Mod Appl Pharm(中国现代应用药学),2020,37(9):1096-1101. |
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| 基于HPMCAS载体的依非韦伦固体分散体溶出模式研究 |
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刘一欢1,2, 顾王文3, 陆振举4, 刘怡4, 孙考祥1
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1.烟台大学药学院, 山东 烟台 264000;2.中国科学院上海药物研究所药物制剂研究中心, 上海 201203;3.烟台药物研究所, 山东 烟台 264003;4.亚什兰(中国)投资有限公司, 上海 200233
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| 摘要: |
| 目的 以依非韦伦为原料药、不同规格（L、M、H）HPMCAS为载体，采用喷雾干燥法制备固体分散体并对其溶出模式进行初步探究。方法 通过X射线粉末衍射（XRPD）、扫描电子显微镜（SEM）对固体分散体理化性质进行制剂学表征；以动力溶解度为指标考察不同药载比、不同规格HPMCAS固体分散体的溶出情况；通过粒度分析仪和透射电子显微镜（TEM）、SEM探讨固体分散体溶出时的不同模式。结果 XRPD分析显示，固体分散体中药物以无定形的形态分散在HPMCAS中；SEM分析显示，L、M、H规格HPMCAS与依非韦伦形成的固体分散体均具有"萎缩葡萄干"形态；在pH 6.8磷酸缓冲盐溶液中溶出时，药载比1：6的固体分散体溶出好，药载比1：1.5的固体分散体溶出差且相同药载比时L规格HPMCAS的固体分散体溶出更快。结论 以不同规格HPMCAS为载体制备的依非韦伦固体分散体在pH 6.8磷酸缓冲盐溶液中溶出时，存在多种溶出模式。药载比1：6时，L、M规格HPMCAS的固体分散体以药物纳米颗粒的形式溶出；药载比1：1.5时，L、M规格HPMCAS的固体分散体存在类似溶蚀的溶出模式，药物从载体骨架中释放。 |
| 关键词: 依非韦伦 醋酸羟丙甲纤维素琥珀酸酯 固体分散体 动力溶解度 药物纳米颗粒 溶蚀 |
| DOI：10.13748/j.cnki.issn1007-7693.2020.09.014 |
| 分类号:R917 |
| 基金项目: |
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| Study on the Dissolution Model of Efavirenz in Solid Dispersion Based on HPMCAS Carrier |
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LIU Yihuan1,2, GU Wangwen3, LU Zhenju4, LIU Yi4, SUN Kaoxiang1
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1.School of Pharmacy, Yantai University, Yantai 264000, China;2.Center for Formulations System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;3.Yantai Institute of Materia Medica, Yantai 264003, China;4.Ashland(China) Holding Co., Ltd., Shanghai 200233, China
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| Abstract: |
| OBJECTIVE To prepare the solid dispersion of efavirenz by spray drying with different grades(L, M, H) HPMCAS as the carrier, and the different dissolution models based on 3 grades of HPMCAS were preliminarily explored. METHODS The physicochemical properties of solid dispersion were characterized by X-ray powder diffraction(XRPD) and scanning electron microscope(SEM), the dissolution of solid dispersion with different drug loading ratios and different grades of HPMCAS was determined with dynamic solubility, the different dissolution models were determined by particle size analyzer and transmission electron microscope(TEM) and SEM. RESULTS XRPD analysis showed that efavirenz in the solid dispersion exhibited an amorphous form in HPMCAS. The morphology of efavirenz-HPMCAS observed by SEM exhibiting "shriveled raisin". Compared with 1:1.5, the solid dispersion with drug loading ratio of 1:6 displayed faster dissolution in pH 6.8 phosphate buffer solution. Furthermore, the solid dispersion of HPMCAS L dissolved faster at the same drug loading ratio. CONCLUSION Various dissolution models are determined in the solid dispersions with various grades of HPMCAS under pH 6.8 phosphate buffer solution. Efavirenz in the solid dispersion with HPMCAS L and M is dissolved in nanoparticles at the drug loading ratio of 1:6, while in 1:1.5, the drugs were released from the skeleton of carrier, similar to erosion dissolution model. |
| Key words: efavirenz hypromellose acetate succinate solid dispersion dynamic solubility drug nanoparticles erosion |
