依托咪酯胶束溶液的制备及体内麻醉效果  

Preparation of Etomidate Micelle Solution and Its Anesthetic Effects in Vivo

作　　者：吴爱玲[1] 王滢莹 刘浩 WU Ailing;WANG Yingying;LIU Hao(Department of Anesthesiology,the First People’s Hospital of Neijiang City,Sichuan Province,Neijiang 641000,China;Department of Clinical Medicine,School of Clinical Medicine,Southwest Medical University,Luzhou 646000,China;School of Pharmacy,Southwest Medical University,Luzhou 646000,China)

机构地区：[1]四川省内江市第一人民医院麻醉科,内江641000 [2]西南医科大学临床医学院临床医学系,泸州646000 [3]西南医科大学药学院,泸州646000

出　　处：《医药导报》2020年第7期905-909,共5页Herald of Medicine

基　　金：四川省科技计划研究项目(2019YJ0489);四川省卫生和计划生育委员会研究项目(16PJ536)。

摘　　要：目的制备依托咪酯胶束溶液,并研究其对大鼠的麻醉作用。方法采用薄膜水化法制备依托咪酯的普朗尼克胶束溶液(EtoPM),通过透射电镜、动态光散射法和吸光光度法等方法考察胶束的形态、大小、Zeta电位、药物包裹率和体外药物释放等性质,通过大鼠体内实验研究EtoPM的麻醉效果。结果EtoPM胶束颗粒圆整,平均粒径(85.53±10.25)nm,Zeta电位(-4.31±1.04)mV,药物包裹率(73.14±1.85)%。与市售依托咪酯乳状注射液相比,EtoPM能够更快地释放药物(P<0.01)。EtoPM溶液与依托咪酯乳状注射液通过大鼠尾静脉注射后均能迅速起效,但EtoPM麻醉后苏醒所需时间显著缩短(P<0.01)。结论普郎尼克胶束在有效增溶依托咪酯的同时能够快速释药。该实验所制备的EtoPM溶液麻醉作用迅速,麻醉后苏醒所需时间较短,与全麻药物要求相符,是一种很有潜力的依托咪酯注射液。Objective To prepare etomidate micelle solution and to research the sedative effects in rats.Methods Etomidate-loaded Pluronic micelle solution(EtoPM)was prepared using thin-film rehydration method.The morphology,particle size distribution,Zeta potential,encapsulation efficiency of drug-loaded micelles,and in vitro drug release profile of EtoPM were determined using transmission electron microscopy(TEM),dynamic light scattering(DLS),spectrophotometry,etc.The in vivo anesthetic effects of EtoPM were studied by in vivo experiments with rats.Results The drug-loaded micelles in EtoPM showed spherical shape,with the average particle size of(85.53±10.25)nm and Zeta potential of(-4.31±1.04)mV.The drug encapsulation efficiency was(73.14±1.85)%.The drug release of EtoPM was faster than that of the commercially available etomidate emulsion injection(P<0.01).Both EtoPM and the etomidate emulsion injection took effect quickly after tail vein injection into the rats,while the anesthesia recovery of EtoPM group was significantly faster(P<0.01).Conclusion Pluronic micelles can well solubilize etomidate,and can also quickly release the drug.With rapid onset and recovery,EtoPM fits well to the requirement of general anesthetics.Therefore,EtoPM is a promising etomidate injection.

关 键 词：依托咪酯 麻醉 胶束 体内实验 

分 类 号：R971.2[医药卫生—药品] TQ460.1[医药卫生—药学]