丙泊酚纳米乳的制备、质量评价及安全性  

Preparation,quality evaluation and security analysis of propofol nanoemulsion

作　　者：郝朝双 欧阳五庆[1] 杨鸣琦[1] 李红连 王波臻[2] 魏云鹏[1] 

机构地区：[1]西北农林科技大学动物医学院,陕西杨凌712100 [2]石河子大学动物科技学院,新疆石河子832003

出　　处：《中国兽医学报》2017年第12期2389-2396,共8页Chinese Journal of Veterinary Science

基　　金：农业科技成果转化资金资助项目(2013GB2G-000475)

摘　　要：本研究制备了丙泊酚纳米乳注射液,并对其理化性质及安全性进行了分析。通过考察纳米乳的载药量、稳定性,结合伪三元相图,筛选出纳米乳的最佳配方:丙泊酚1.0%、盐酸利多卡因0.1%、泊洛沙姆188为10.0%、1,2-丙二醇10.0%、生理盐水78.8%;通过透射电镜、激光粒度分析仪观察,发现纳米乳注射液的乳滴呈圆球形,平均粒径为86.82nm,稳定性良好;用高效液相色谱仪检测药物含量,建立了纳米乳中丙泊酚、盐酸利多卡因含量测定的专属性方法;血管刺激性试验和溶血性试验表明纳米乳的安全性与市售力蒙欣相比无明显差异。结果表明,丙泊酚纳米乳注射液制备成功,且该纳米乳安全、稳定。This research prepared propofol nanoemulsion and its physical, chemical and security properties were evaluated. According to the drug loading, stability and pseudo-ternary phase diagram of the nanoemulsion, the optimum formula of nanoemulsion was composed of propofol（1. 0%）, lidocaine hydrochloride （0. 1%）, pluronic F68 （ 10.0%）, 1,2-propylene glycol （ 10.0%） and saline （78.8%）. The configuration and particle size of nanoemulsion were measured by TEM and LPSA, the results showed that the droplet shape of this nanoemulsion was spherical, with the average diameter of 86.82 nm,and its stability was good. The high performance liquid chromatography （HPLC） method had strong specificity and can be used for content measurement of propofol and lidocaine hydrochloride. Hemolysis and vascular stimulation assay showed that the security of nanoemulsion had no significant difference with commercial lipid emulsion. In conclusion, a safe and stable propofol nanoemulsion was prepared successfully.

关 键 词：丙泊酚 盐酸利多卡因 纳米乳 质量评价 安全性 

分 类 号：S859.791[农业科学—临床兽医学]