丹参提取物固体分散体的制备与溶出特性  

Preparation and dissolution study of solid dispersions of Danshen extract

作　　者：巫剑峰[1] 邱佩斯[1] 陈彦雯[1] 陈海南[1] 李沙[1,2] 

机构地区：[1]暨南大学药学院,广东广州510632 [2]暨南大学中药药效物质基础及创新药物研究广东省高校重点实验室,广东广州510632

出　　处：《中国医院药学杂志》2010年第11期900-905,共6页Chinese Journal of Hospital Pharmacy

基　　金：暨南大学青年基金项目(编号:51208021);广东省医学科研基金项目(编号:B2009127)

摘　　要：目的:制备丹参提取物固体分散体,考察其中丹参酮ⅡA的溶出效果。方法:选择不同种类的聚乙二醇(PEG)与聚乙烯吡咯烷酮(PVPK30)载体材料,分别采用熔融法和溶剂法制备丹参提取物的固体分散体。用高效液相色谱法对固体分散体中及溶出液中所含丹参酮ⅡA进行测定,色谱柱为Kromasil C18柱(4.6mm×250mm,5μm),流动相为甲醇-水(85:15);流速为1.0mL·min-1;检测波长为270nm。结果:与丹参提取物相比,以PEG和PVP所制备的丹参提取物固体分散体中丹参酮ⅡA的溶出度与溶出速度均明显增加,且有显著性差异(P<0.01或P<0.05)。其中以PEG2000:PEG4000(3:7)为载体材料,药载比为1:9所制备的固体分散体,其丹参酮ⅡA溶出度最优,60min累积溶出百分率达87%,高出丹参提取物32%。结论:采用PEG与PVPK30成功制备了丹参提取物固体分散体,其中丹参酮ⅡA的溶出较原料提取物有明显改善。采用固体分散技术可为更有效地利用丹参提取物中脂溶性成分提供一种新的制剂手段。OBJECTIVE To prepare solid dispersions of Danshen extract and to investigate their dissolution behaviour by using tanshinone ⅡA as index component. METHODS Using different types of PEG and PVP K30 as carriers, the solid dispersions were prepare by melted method and dissolved method respectively. The content of tanshinone ⅡA in solid dispersions and dissolution liquid was assayed by HPLC method with a Kromasil C18 column （4. 6 mm × 250 mm, 5 μm）. The mobile phase was composed of methanol and water in a ratio of 85： 15. The flow rate is 1. 0 mL·min^-1 and the detecting wavelength is 270 nm. RESULTS Compared with Danshen Extract, the dissolution percentage and dissolution rate of tanshinone ⅡA from the solid dispersions prepared with PEG and PVP increased obviously, and the improvement showed statistical significant difference （P 〈0. 01 or P〈0. 05）. The solid dispersion, which was prepared with PEG2000：PEG4000（3：7） as carrier at a drug carrier ratio of 1：9, demonstrated the optimal dissolution behaviour. The accumulative dissolution percentage of tanshinone Ⅱ A from the solid dispersion at 60 min reached 87%, which was 32% higher than that from Danshen extract. CONCLUSION The solid dispersions of Danshen extract were successfully prepared with PEG an PVP K30. Compared with Danshen extract, the dissolution of tanshinone ⅡA from the solid dispersions was markedly enhanced. Solid dispersing technique may provide a new pharmaceutical manner for utilizing the liposoluble components in Danshen extract more efficaciously.

关 键 词：丹参提取物固体分散体 丹参酮ⅡA 溶出特性 

分 类 号：R969.1[医药卫生—药理学]