十一酸睾酮Ⅲ型脂质制剂体外脂解过程及机制研究  

In vitro lipolysis process and lipolysis mechanism of testosterone undecanoate typeⅢlipid formulations

作　　者：王雅蒙 邹丹璐 李钰 柯学[1] WANG Ya-meng;ZOU Dan-lu;LI Yu;KE Xue(School of Pharmacy,China Pharmaceutical University,Jiangsu Public Technical Service Center for Nanometer Drug Preparation and Biological Evaluation,Nanjing 210009,China)

机构地区：[1]中国药科大学药学院,江苏省纳米药物制备与生物学评价公共服务中心,江苏南京210009

出　　处：《药学学报》2021年第6期1696-1703,共8页Acta Pharmaceutica Sinica

摘　　要：以十一酸睾酮为模型药物,制备Ⅲ型脂质制剂,利用体外脂解模型评价各处方的体外脂解速率及脂解程度,并以光学显微镜和电导率等手段进一步研究其消化机制。结果表明,在以蓖麻油为油相、Transcutol HP为助表面活性剂的十一酸睾酮Ⅲ型脂质制剂中,随着油相比例增加,脂解速率和脂解程度增加;表面活性剂比例过高,脂解过程中可观察到液晶相、脂解速率和脂解程度下降。含有不同表面活性剂的ⅢB型脂质制剂脂解速率排序为Labrasol>Tween 80>Cremophor EL,而ⅢA型的排序在快速消化期和慢速消化期有所不同,但两者脂解程度排序均为Cremophor EL>Tween 80>Labrasol。研究结果提示,处方含油量、表面活性剂比例及其结构对Ⅲ型脂质制剂体外脂解速率和脂解程度均具有较大影响且相互交织,进行处方筛选时需综合考虑各方面因素对制剂体内消化的影响。The study evaluates the lipolysis rate and extent of typeⅢlipid formulations using testosterone undecanoate as a model drug after digestion with in vitro lipolysis model,and studies the digestive regularity with optical microscope and electrical conductivity.The results showed that for testosterone undecanoate typeⅢlipid formulations with castor oil as oil phase and Transcutol HP as latent solvent,the lipolysis rate and extent were increased with the increase of oil phase proportion and were decreased with excessive proportion of surfactant,in which can see liquid crystal phase during lipolysis process.The lipolysis rate of typeⅢB lipid preparations with different surfactant were ordered as Labrasol>Tween 80>Cremophor EL,but the rate of typeⅢA is different in quick digestion phase and slow digestion phase.The lipolysis extent of typeⅢlipid formulations with different surfactant were ordered as Cremophor EL>Tween 80>Labrasol.These may be related to the digestive effect of pancreatic lipase on different surfactants.This study implied that the lipolysis rate and extent of typeⅢlipid formulations are greatly influenced by the proportion of oil phase and surfactant,and the surfactant structure.These factors will affect the in vivo digestion and should be taken into account when screening typeⅢlipid formulations.

关 键 词：Ⅲ型脂质制剂 体外脂解模型 脂解速率 脂解程度 十一酸睾酮 

分 类 号：R943[医药卫生—药剂学]