甲磺酸雷沙吉兰醇脂质体的制备、评价及优势  

Preparation,Evaluation and Advantages of Rasagiline Mesylate Ethosome

作　　者：吴密 余瑜[1] 张涛 Wu Mi;Yu Yu;Zhang Tao(School of Pharmacy Chongqing Medical University Chongqing 400016,China;Fuan Pharmaceutical Group Chongqing Libang Drug Development Co.,Ltd.,Chongqing 401121,China)

机构地区：[1]重庆医科大学药学院,重庆400016 [2]福安药业集团重庆礼邦药物开发有限公司,重庆401121

出　　处：《广东化工》2024年第7期7-10,共4页Guangdong Chemical Industry

摘　　要：目的:本文旨在提供一种甲磺酸雷沙吉兰经皮给药系统的制剂中间体即醇脂质体,目的是通过该载体将水溶性药物甲磺酸雷沙吉兰包裹其中,借助该载体与皮肤的亲和性,使药物透过皮肤。方法:用溶剂注入法制备雷沙吉兰醇脂质体,单因素考察制备过程中的处方以及工艺,选出影响最大的4个因素设计正交实验优化处方,以粒径、包封率为参考指标,透皮累积量为决定性指标筛选出最佳处方和工艺。结果:雷沙吉兰醇脂质体透过速率和累积透过率(24 h)更高,处方优化后的甲磺酸雷沙吉兰醇脂质体粒径为138.73 nm,包封率为58.80%,单位时间内(24 h)累积透皮量在600 ug左右。结论:说明了醇脂质体作为给药载体的优越性。Objective:The purpose of this paper is to provide a preparation intermediate of Rasagiline mesylate transdermal drug delivery system,namely ethosomes.The purpose is to wrap the water-soluble drug Rasagiline mesylate in the carrier,and make the drug penetrate the skin by the affinity between the carrier and the skin.Methods:The preparation of Rasagiline Mesylate ethsomes were investigated by solvent injection method.Orthogonal experiments were designed to optimize the formulation by selecting the four factors that had the greatest influence.The optimal formulation and process were selected by using particle size and encapsulation rate as reference indexes and cumulative transdermal volume as decisive indexes.Results:The transmission rate and cumulative transmission rate(24 h)of Rasagiline Mesylate ethsomes were higher.After optimized formulation,the particle size of Resagiline mesylate was 138.73 nm and the encapsulation rate was 58.80%.The cumulative transdermal volume per unit time(24 h)was about 600 ug.Conclusion:The advantages of ethosomes as drug delivery carrier were explained.

关 键 词：甲磺酸雷沙吉兰 醇脂质体 粒径 包封率 透皮累积量 

分 类 号：TQ[化学工程]