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目的比较单独和联合使用辅料对丹参提取物物理性质和其水溶性和脂溶性成分溶出的影响。方法分别以聚乙烯吡咯烷酮(PVP10)、帕洛沙姆(F127)及二者联用(PVP10-F127)为载体,采用喷雾干燥法制备丹参提取物的固体分散体,并对其物理性质进行表征。选取水溶性成分丹参素、迷迭香酸、丹酚酸B和脂溶性成分隐丹参酮、丹参酮ⅡA作为指标成分,采用相似因子法分别对其脂溶性和水溶性成分的体外溶出行为进行评价。结果扫描电镜和粉末X射线衍射结果显示喷雾干燥制得的样品为无特征晶体峰的球形颗粒。无论在原提取物还是在制得的固体分散体中,水溶性成分均可完全溶出;而脂溶性成分均无法在使用单一辅料制备的固体分散体中完全释放。联用辅料时,当PVP10-F127的质量比为5∶4时,丹参脂溶性和水溶性成分均可完全快速释放。提取物原药和不同辅料制备的剂型中无晶体峰出现。而辅料联用可增加粉体的润湿角,但不能增加其比表面积。结论辅料联用能显著提高丹参固体分散体中脂溶性成分的溶出,其原因可能是增加了粉体的润湿性。相似因子评价结果显示,丹参提取物中的多组分分别达到了同步完全释放,符合《中国药典》体外溶出的要求。
Objective To compare the effects of single and combined excipients on the physical properties of Salvia miltiorrhiza extract and the dissolution of its water-soluble and fat-soluble components. Methods The solid dispersions of Salvia miltiorrhiza extracts were prepared by spray drying with polyvinylpyrrolidone (PVP10), Palladium (F127) and PVP10-F127 as their carriers respectively, and their physical properties were characterized . Water-soluble components of Danshensu, rosmarinic acid, salvianolic acid B and fat-soluble components of cryptotanshinone and tanshinone Ⅱ A were selected as index components, and the dissolution factors of water-soluble and water-soluble components were evaluated by similarity factor method. Results Scanning electron microscopy and powder X-ray diffraction results showed that the spray-dried samples were spherical particles with no characteristic crystal peak. Both the original extract and the solid dispersions obtained were completely soluble in the water-soluble components, whereas the fat-soluble components were not completely released in the solid dispersions prepared with the single excipients. When used together with excipients, when the mass ratio of PVP10-F127 is 5: 4, fat-soluble and water-soluble components of Salvia miltiorrhiza can be completely and rapidly released. No crystalline peak appeared in the formulation of the extract original drug and different excipients. The auxiliary materials can increase the wetting angle of the powder, but can not increase its specific surface area. Conclusions The combination of auxiliary materials can significantly improve the dissolution of fat-soluble components in Danshen solid dispersions, which may be due to the increased wettability of powders. Similarity factor evaluation results show that the components of the Salvia extract to achieve simultaneous complete release, in line with “Chinese Pharmacopoeia” in vitro dissolution requirements.