摘要
目的制备依托孕烯和炔雌醇临床处方量的固体分散体,考察载药及药物释放行为。方法将不同量依托孕烯或炔雌醇与Poloxamer188共同溶解在二氯甲烷中后,在玻璃板上浇铸并挥干溶剂。高效液相色谱-紫外分光光度法测定释放介质中从固体分散体中释放的药物的量,并绘制经时释放曲线。差示热分析、热重分析、X-射线衍射等手段评价两种药物在固体分散体中的包裹行为。结果Poloxamer188固体分散体中依托孕烯和炔雌醇载量高则百分释放率少,载量低则百分释放率多。单方固体分散体中依托孕烯的释放较炔雌醇更为完全,但是复方制剂中依托孕烯的释放仅为炔雌醇的1/3。差示热分析曲线上和X-射线衍射图谱上Poloxamer188特征峰明显而药物峰不明显,但是同时载有依托孕烯和炔雌醇的Poloxamer188固体分散体显示特殊峰形。结论Poloxamer188作为依托孕烯和炔雌醇的固体分散体载体可以在一定程度上增溶两种药物,并且在5 h内具有一定的缓释性。复方制剂中呈现了新的复合方式,并且释放行为和单方制剂有明显不同。
Objective To prepare solid dispersion of etonogestrel and ethinylestradiol of the clinical prescription amount,and to investigate the drug loading and release behavior.Methods After different amounts of etonogestrel or ethinylestradiol and Poloxamer188 were dissolved in methylene chloride,the solvent was cast on the glass plate and dried.High performance liquid chromatography-ultraviolet spectrophotometry was used to measure the amount of drug released from the solid dispersion in the release medium and plot the time release curve.Differential thermal analysis,thermogravimetric analysis and X-ray diffraction were used to evaluate the coating behavior of the two drugs in solid dispersions.Results The release percentage of etonogestrel and ethinylestradiol from Poloxamer188 solid dispersion was lower when the drugs loading amounts were higher,meanwhile drugs release percentage was higher when their loading amounts were lower.From the single-prescription solid dispersions,the release of ethinylestradiol was more complete than ethinylestradiol,but the release percentage of ethinylestradiol from the compound-prescription solid dispersion was only 1/3 of ethinylestradiol.The characteristic peaks of Poloxamer188 on the differential thermal analysis curve and the X-ray diffraction patterns were obvious while characteristic peaks of the drugs peak were not obvious,but the Poloxamer188 solid dispersion containing both etonogestrel and ethinylestradiol showed a special peaks pattern.Conclusion Poloxamer188,as a solid dispersion carrier for etonogestrel and ethinylestradiol,can solubilize the two drugs to a certain extent,and has showed certain sustained release profiles within 5 hours.The compound prescription has showed a novel composite behavior,and its release behavior is significantly different from that of the single prescription.
作者
吕蕴麒
高枫
王瑛颖
王浩
LV Yunqi;GAO Feng;WANG Yingying;WANG Hao(School of Pharmacy,Jinzhou Medical University,Jinzhou 121000 China;Department of Medicinal Materials,Fuxin Mining General Hospital of Liaoning Health Industry Group,Fuxin 123000 China)
出处
《锦州医科大学学报》
2025年第1期1-9,共9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:2021-4。
