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微环境pH对吲哚美辛固体分散体溶出行为的影响及评价
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引用本文:曹杰,朱志凌,袁梦,柯学.微环境pH对吲哚美辛固体分散体溶出行为的影响及评价[J].中国药科大学学报,2019,50(6):686-693.
Cite:CAO Jie,ZHU Zhiling,YUAN Meng,KE Xue.Effect and evaluation of microenvironment pH on dissolution behavior of indomethacin solid dispersion[J].J China Pharm Univ,2019,50(6):686-693.
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作者单位
曹杰 中国药科大学药学院药剂系 
朱志凌 江苏省科学技术情报研究所 
袁梦 中国药科大学药学院药剂系 
柯学 中国药科大学药学院药剂系 
中文摘要:研究和评价微环境pH对无定型固体分散体溶出行为的影响及其可能的机制。以吲哚美辛(IND)为模型药物,Kollidon®; VA64为载体材料,通过热熔挤出法制备IND无定型固体分散体(SD),使用差示扫描量热法(DSC)与X射线粉末衍射法(PXRD)进行表征。考察微环境pH调节剂葡甲胺(MEG)加入前后对固体分散体在不同溶出介质中溶出行为的影响。设计实验从溶出介质浸润速度、微环境pH、药物溶出后再结晶等多角度评价溶出行为的差异。结果发现,MEG提供的碱性微环境加速IND的溶出,但是在不同溶出介质中,pH调节剂产生的微环境强度和持续时间、局部药物再结晶情况和介质浸润粉末速度均存在明显差异,且以上多种因素共同作用影响固体分散体中药物的溶出行为。
中文关键词:微环境  pH调节剂  固体分散体  溶出  浸润
 
Effect and evaluation of microenvironment pH on dissolution behavior of indomethacin solid dispersion
Abstract:In this study, the effect of pH regulator meglumine(MEG)on the dissolution behavior of indomethacin(IND)amorphous solid dispersions was evaluated. The amorphous solid dispersion was prepared by hot-melt extrusion using IND and Kollidon® VA64 at a weight ratio of 1∶4, and extrudates were characterized using differential scanning calorimetry(DSC)and X-ray powder diffraction(PXRD). The dissolution behaviors of solid dispersions with or without MEG were investigated in three kinds of pH media. The effect of infiltration rate of media, microenvironmental pH(pHM)and recrystallization of drugs on drug dissolution were evaluated by designing the appropriate experiments. The results showed that the presence of MEG could accelerate the dissolution of IND from solid dispersions through providing an alkaline microenvironment, but in different dissolution media, the intensity and duration of alkaline microenvironment, recrystallization of local drug molecules and infiltration rate of media showed an obvious difference, and the above factors simultaneously affected the dissolution behavior of drugs from solid dispersions.
keywords:microenvironment  pH regulators  solid dispersion  dissolution  infiltration
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