环孢素A固体自微乳的制备及初步评价  

Preparation and preliminary evaluation of cyclosporin A solid self-emulsifying drug delivery system

作　　者：白中稳[1,2] 胡容峰[1,2,3] 孙备[4] 胡晓[1,2] 朱丽[1,2] 

机构地区：[1]安徽中医学院药学院,合肥230031 [2]安徽省中药研究与开发重点实验室,合肥230038 [3]安徽省"115"现代中药研发创新团队,合肥230038 [4]安徽省药物研究所,合肥230022

出　　处：《中国新药杂志》2013年第12期1455-1461,共7页Chinese Journal of New Drugs

基　　金：国家自然科学基金(81274100);2009年度安徽省高层次人才创新创业基金(2009Z061);2011年度安徽省学术和技术带头人及后备人选学术科研活动项目(皖人社秘[2011]381号-26)

摘　　要：目的:制备环孢素A(CsA)固体自微乳,评价其粉体学性质,并测定其体外溶出度。方法:运用球晶造粒技术制备乙基纤维素多孔微球,并联合其他载体对液体CsA自微乳固化,测定自微乳固化前后粒径及Zeta电位,考察粉体学性质并测定体外溶出度。结果:自制的CsA固体自微乳,流动性、可压性、填充性均较好,载药量较高,固化前后平均粒径及Zeta电位分别为:(27.19±0.54)nm和(-5.71±0.73)mV;(28.82±0.68)nm和(-5.66±0.58)mV,固化前后,粒径、电位变化较小,自微乳固化过程中未被破坏,该制剂30 min释放87.0%以上,90 min释放95.0%以上。结论:球晶造粒技术制备多孔微球,可以用于液体CsA自微乳的固化,且固化后粉体学性质较好,载药量较高,释放较完全。Objective： To prepare cyclosporin A （CsA） solid self-microemulsion, and to evaluate the pow- der properties and determine its dissolution properties. Methods： Porous microspheres of ethyl cellulose were pre- pared by spherical crystallization technique. Liquid CsA microemulsion was solidified in conjunction with other car- riers. The changes in particle size and zeta potential of CsA self-microemulsion were determined by Malvern before the adsorption and after the adsorption. Powder properties and in vitro dissolution were also determined. Results： Self-restraint CsA solid self-microemulsion had better mobility, compressibility, filling and higher drug loading. The particle size and zeta potential of CsA self-microemulsion were （27.19 ± 0.54） nm and （ -5.71 ± 0.73） mV before adsorption, and （28.82 ± 0.68） nm and （ -5.66 ±0.58） mV after adsorption. Self-microemulsion was un- spoiled in the preparing process, and release rate was 〉 87.0% in 30 min and 〉 95.0% in 90 min. Conclusion： Spherical crystallization technique can prepare porous microspheres and can be used for preparing the liquid CsA microemulsion. The solid CsA microemulsion has better powder properties, higher drug loading and more complete release rate.

关 键 词：环孢素A 球晶造粒技术 固体自微乳 粉体学性质 溶出度 

分 类 号：R943.4[医药卫生—药剂学] R979.5[医药卫生—药学]