丹参酮ⅡA固体脂质纳米粒缓释凝胶骨架片的制备  

Preparation of the hydrophilic gel-matrix tablets of tanshinone ⅡA sustained-release solid lipid nanoparticles

作　　者：索绪斌[1] 张涵 王文青[3] 徐兴[1] 

机构地区：[1]广东药学院中药学院,广州510006 [2]黑龙江省中医药科学院,哈尔滨150036 [3]湖北省荆州市中心医院药剂科,荆州4340201

出　　处：《中国新药杂志》2015年第5期576-580,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(80303288);国家科技创新基金(国科发计[2013]583号)

摘　　要：目的:为了提高丹参酮ⅡA的溶解度,解决难溶性药物难以持续缓慢释放的问题,制备丹参酮ⅡA缓释固体脂质纳米粒凝胶骨架片,为丹参酮ⅡA缓释制剂的研究提供参考。方法:采用乳化-溶剂挥发法制备丹参酮ⅡA固体脂质纳米粒,将丹参酮ⅡA固体脂质纳米粒分散于凝胶骨架片辅料中制备缓释凝胶骨架片,对影响其体外释放的因素进行了考察,并对丹参酮ⅡA缓释固体脂质纳米粒凝胶骨架片体外释放动力学进行探讨。结果:丹参酮ⅡA缓释固体脂质纳米粒包封率、载药量及粒径分别为(89.81±3.54)%,(6.12±0.32)%及(243±8.5)nm。丹参酮ⅡA缓释固体脂质纳米粒凝胶骨架片药物的释放符合RitgerPappas模型。结论:丹参酮ⅡA缓释固体脂质纳米粒凝胶骨架片通过溶蚀作用持续不断地释放药物,达到丹参酮ⅡA缓释制剂药物设计要求。Objective： To improve the dissolution of tanshinone ⅡA in solution for solving the problem that insoluble drugs cannot sustained-release continually; to prepare the hydrophilic gel-matrix tablets of tanshinone ⅡA sustained-release solid lipid nanoparticles,which will provide references for the development of the new dosage forms of tanshinoneⅡ A. Methods： The solid lipid nanoparticles of tanshinone ⅡA were prepared by emulsification-solvent evaporation method,and then dispersed in the gel-matrix tablet excipients to prepare sustained-release gel-matrix tablets. The influence factors on its release in vitro were studied and the in vitro release kinetics of tanshinone ⅡA from the solid lipid nanoparticles gel-matrix tablets was also explored. Results： The encapsulation efficiency,drug loading and particle size of tanshinone IIA sustained-release solid lipid nanoparticles were（ 89. 81 ±3. 54） %,（ 6. 12 ± 0. 32） % and（ 243 ± 8. 5） nm,respectively. The release of tanshinone IIA from the hydrophilic gel-matrix tablets fit Ritger-Pappas model. Conclusion： The gel-matrix tablets of tanshinone ⅡA solid lipid nanoparticles can sustained release drug through the corrosion of the hydrophilic matrix tablets. It has achieved the design requirements of tanshinone ⅡA sustained-release.

关 键 词：丹参酮ⅡA 固体脂质纳米粒 凝胶骨架片 体外释放 

分 类 号：R943.41[医药卫生—药剂学]