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 investigate the effect of sole and combined utilizing of carriers to prepare solid dispersion for improving dissolution rate of hydrophilic and lipophilic components in extracts of Salviae Miltiorrhizae Radix et Rhizoma (Danshen). Methods Solid dispersions were prepared with PVP10 and F127 as sole carrier or their combinations by Spray Drying (SD) method. The prepared powders were characterized by various methods. Three hydrophilic (danshensu, rosmarinic acid, and salvianolic acid B) and two lipophilic components (cryptotanshinone and tanshinone IIA) of Danshen were determined as bioactive markers. The simulating factor (f2) was utilized to evaluate similarities of dissolution profiles of hydrophilic and lipophilic components, respectively. Results SEM and PXRD results showed that solid dispersion prepared by SD method was amorphous spheroid particles without intensive characteristic peaks. The hydrophilic components were completely released from the bulk Danshen extract and from the prepared solid dispersions. However, no lipophilic components could be completely dissolved from solid dispersions prepared by sole carrier. When combined using carriers (e.g. PVP10-F127 = 5:4), both of the lipophilic and hydrophilic components could be rapidly and completely released from the solid dispersion. Combined use of carriers could increase the wetting angle without changing the specific surface area. Conclusion The combined use of carriers significantly increases the in-vitro release of lipophilic components in Danshen extract, which may be attributed to the increased wettability of powders. The simulating factor evaluation results suggest that the release profiles of either the lipophilic or the hydrophilic components in Danshen extract are complete and similar, which could meet the requirements of Chinese Pharmacopoeia.

澳门科学技术发展基金资助项目(008/2007/A1);澳门大学科研基金资助项目(UL016/09-Y2/CMS/WYT01/ICMS)