载多西紫杉醇米替福新固体分散体的表征  

Characterization of Miltefosine Solid Dispersions with Docetaxel Loaded

作　　者：袁燕 王瑛颖 吕蕴麒 王浩 Yuan Yan;Wang Yingying;Lv Yunqi;Wang Hao(School of Pharmacy,Jinzhou Medical University,Jinzhou 121000 China;Section of Pharmaceutical Preparation,Chinese Medicine Hospital of Gao Country,Yibin 644600 China)

机构地区：[1]锦州医科大学药学院,辽宁锦州121000 [2]高县中医医院药剂科,四川宜宾644600

出　　处：《锦州医科大学学报》2024年第2期45-50,共6页Journal of Jinzhou Medical University

基　　金：辽宁省药物作用与质量评价专业技术创新中心与辽宁省海洋生物活性物质重点实验室主任基金项目,项目编号:2020-06,2021-4。

摘　　要：目的考察米替福新固体分散体中多西紫杉醇的载药、增溶和溶出行为。方法以米替福新为载体材料,通过共溶液-溶剂挥发法制备载多西紫杉醇的固体分散体,差示热分析和热重分析考察米替福新和多西紫杉醇的复合行为、X-射线衍射分析考察材料表面的复合情况,高效液相色谱-紫外分光光度法测定多西紫杉醇的增溶和溶出量并绘制累积释放量经时曲线。结果差示热分析-热重分析曲线和X-射线衍射图谱结果均显示随着米替福新中多西紫杉醇的从无到有、从少到多,曲线和图谱中米替福新的特征逐渐减少,而多西紫杉醇的特征逐渐增多。当多西紫杉醇载量为40%以下时,其能够完全被米替福新增溶,当多西紫杉醇载量在50%及以上时,只有部分多西紫杉醇能够被增溶,且增溶过程需要约2 h。结论以米替福新为固体分散体的载体材料可以复合多西紫杉醇,并且可以在一定载量下对多西紫杉醇进行完全或部分增溶。Objective To investigate the loading,solubilization,and dissolution behavior of docetaxel in the solid dispersion of miltefosine.Methods The solid dispersions containing docetaxel were prepared by co-solution-solvent volatilization method using miltefosine as carrier material.The composite behavior of miltefosine and docetaxel was investigated by differential thermal analysis and thermogravimetric analysis,and the surface composite was investigated by X-ray diffraction analysis.The solubilization and dissolution of docetaxel were determined by high performance liquid chromatography-ultraviolet spectrophotometry and the cumulative release curve was plotted.Results The results of DTA curve and X-ray diffraction pattern both showed that the characteristics of miltefosine in the curve and graph gradually decreased,while the characteristics of docetaxel gradually increased with the change of docetaxel from zero to more,from less to more.When docetaxel load is less than 40%,it can be completely dissolved by miltefosine,when docetaxel load is 50%or more,only part of docetaxel can be solubilized,and the solubilization process takes about 2 h.Conclusion Docetaxel can be synthesized with miltefosine as a solid dispersion carrier material,and docetaxel can be completely or partially solubilized in a certain load.

关 键 词：多西紫杉醇 米替福新 固体分散体 载药 增溶 

分 类 号：R965[医药卫生—药理学]