黄芩苷固体分散体的制备及其体外溶出行为考察

Preparation of Baicalin Solid Dispersions and Investigation of Its Dissolution Behavior

摘要:

目的：考察不同溶出条件对黄芩苷固体分散体溶出特性的影响。方法：采用溶剂蒸发法制备黄芩苷-聚乙二醇（PEG）6000固体分散体，利用差示扫描量热法及X-射线衍射法鉴别固体分散体的形成，考察不同溶出条件对其体外溶出特性的影响。结果：黄芩苷以非晶形态分散在固体分散体中；纯水介质中15 min时释放65%，之后释放平缓增加，330 min时释放>70%；人工胃液中，15 min释放30%，330 min约释放56%；在模拟胃肠道介质中，胃内环境中释放较慢，15~120 min释放30%~54%，小肠环境中释放较快，120~330 min释放54%~69%。结论：黄芩苷-PEG6000固体分散体在不同溶出方法中的溶出性质存在差异，动态溶出介质值得推广应用。

Abstract:

Objective: To investigate effects of different dissolution conditions on dissolution characteristics of baicalin solid dispersions. Method: Baicalin-PEG6000 solid dispersions was prepared by solvent evaporation method, DSC and X-ray diffraction method were adopted to identify its formation, and effects of different conditions on its in vitro dissolution were investigated. Result: Baicalin was in amorphous form dispersed in solid dispersions;Stripping properties of baicalin solid dispersions in different kinds of stripping method were different;In pure water medium, release of baicalin was 65% in 15 min, then release slow increased, released more than 70% in 330 min;In artificial gastric juice, it released 30% in 15 min and 56% in 330 min;In simulated gastrointestinal medium, it released slowly in the stomach environment (released 30%-54% in 15-120 min) and released quickly in the small intestine environment (released 54%-69% in 120-330 min). Conclusion: Dissolution properties of baicalin-PEG6000 solid dispersions in different dissolution methods were different, dynamic dissolution medium should be widely applied.