盐酸雷洛昔芬自微乳的制备及其体外评价

发布时间：2018-03-27 23:10

本文选题：盐酸雷洛昔芬自微乳　切入点：伪三元相图　出处：《中国新药杂志》2015年15期

【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。
[Abstract]:Objective: to study the formulation of raloxifene hydrochloride self-microemulsion and evaluate its quality, dissolution and stability. The particle size and stability were selected and optimized for the formulation, and the morphology and particle size after emulsification were analyzed. Results: the prescription composition of the self-microemulsion of raloxifene hydrochloride was as follows: ethyl oleate was 30%, polysorbate was 30%, polyethylene glycol -400 (PEG-400) 400.The drug content was 20.0 mg g ~ (-1), the appearance was yellow, and it was clear and transparent, the content of Raloxifene hydrochloride was 20.0 mg / g ~ (-1). The results of dissolution showed that the cumulative dissolution of raloxifene hydrochloride self-microemulsion in 0.1 mol L-1 hydrochloric acid for 45 min could reach 85.18.The stability of the preparation was affected by high temperature and illumination. Conclusion: the preparation of raloxifene hydrochloride microemulsion is simple, the solubility of the drug in water is increased, and it is beneficial to gastrointestinal absorption, which lays a foundation for further study.
【作者单位】：广东药学院医药化工学院;广东省第一荣军医院;
【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)
【分类号】：R943

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