盐酸雷洛昔芬自微乳的制备及其体外评价  

Preparation and in vitro evaluation of raloxifene hydrochloride self-microemulsion

作　　者：卢秀霞[1] 李伟镇 何琳[1] 罗海珊 潘育方[1] 

机构地区：[1]广东药学院医药化工学院,中山528458 [2]广东省第一荣军医院,广州510260

出　　处：《中国新药杂志》2015年第15期1777-1785,共9页Chinese Journal of New Drugs

基　　金：广东省医学科研基金立项项目(B2014210);广东省科技计划项目(粤科规划字[2013]137号)

摘　　要：目的:研究盐酸雷洛昔芬自微乳的处方,并对其质量、溶出度以及稳定性进行评价。方法:通过溶解度考察、配伍试验与伪三元相图法,以自乳化时间、外观、粒径与稳定性为指标筛选与优化处方,并对乳化后的形态、粒径、溶出度以及稳定性进行评价。结果:所得盐酸雷洛昔芬自微乳的处方组成:油酸乙酯(30%)、聚山梨酯-80(30%)、聚乙二醇-400(PEG-400,40%),载药量20.0 mg·g-1,外观呈黄色、澄清透明,平均粒径10.37 nm,Zeta电位-17.90 m V。溶出度结果表明,盐酸雷洛昔芬自微乳在0.1 mol·L-1盐酸中45 min累积溶出度可达85.18%。高温与光照影响制剂稳定性,应低温、避光保存。结论:盐酸雷洛昔芬自微乳制备简单,增加药物在水中溶解度,有利于胃肠道吸收,为进一步研究奠定基础。Objective： To study the prescription of raloxifene hydrochloride self-microemulsion and evaluate the quality,dissolution and stability. Methods： The prescription was selected and optimized through solubility experiment,compatibility test and pseudo-ternary phase diagram method,using self-emulsification time,appearance,particle size and stability as selection indexes. The droplet morphology,particle size,dissolution and stability were evaluated. Results： The prescription was composed of aethylis oleas（ 30%）,polysorbate-80（ 30%） and PEG-400（ 40%）. The drug loading was 20. 0 mg·g- 1. The raloxifene hydrochloride self-microemulsion exhibited uniform and transparent appearance,with particle size of 10. 37 nm and zeta potential of- 17. 90 m V. The accumulative dissolution of raloxifene hydrochloride self-microemulsion in 0. 1 mol·L- 1hydrochloric acid was 85. 18% at 45 min.Raloxifene hydrochloride self-microemulsion was affected by high temperature and illumination,indicating that it needs to be stored at low temperature and protected from light. Conclusion： The raloxifene hydrochloride self-microemulsion developed in this study is simple to prepare and has increased solubility in water and better absorption in stomach and intestine,which lays the foundation for further research of raloxifene hydrochloride.

关 键 词：盐酸雷洛昔芬自微乳 伪三元相图 粒径 溶出度 稳定性 

分 类 号：R977.1[医药卫生—药品]