伊维菌素微乳的研制及质量评价

Preparation and Quality Evaluation of Ivermectin Microemulsion

研制伊维菌素微乳剂,并对其特性、稳定性进行评定。依据伊维菌素的溶解度,选择适宜的油相和表面活性剂;依据维持微乳体系稳定性的能力,筛选助表面活性剂;利用伪三元相图,确定表面活性剂与助表面活性剂的质量比(Km值),筛选伊维菌素微乳剂的配方,并进行微乳的特性和稳定性分析。结果表明,伊维菌素微乳剂各组分质量分数为伊维菌素5%(50 mg/mL)、油6.79%、乳化剂13.58%、辅助乳化剂54.27%、超纯水20.36%,运动黏度为610.50 mm^2/s,动力黏度为714.28 mPa·s,乳滴平均粒径为6.30nm,光照试验、加速试验、长期试验等证实,微乳剂外观性状未见异常变化,药物含量符合质量规定,伊维菌素微乳剂稳定性良好,说明伊维菌素微乳剂是一种稳定性良好的制剂。

In order to preparae the ivermectin microemulsion,its physicochemical properties and stability were evaluated.The oil and surfactant were chosen according to the solubility of ivermectin and the cosurfactant was chosen according to the ability of maintaining stability of the microemulsion system.The mass ratio of surfactant to the cosurfactant was determined and the formulations of ivermectin microemulsion were screened according to pseudo-ternary phase diagram.Its physicochemical properties and stability were evaluate.The result showed that mass scores of ivermectin microemulsion components are 5%ivermectin,11.43%oil phase,emulsifier and auxiliary emulsifier 42.86%,ultrapure water 37.86%.Kinematic viscosity is 610.50 mm 2/s,dynamic viscosity is 714.28 mPa·s,emulsion droplet average particle size is 6.30 nm.Exposure test,accelerated test and long-term test showed that physicochemical properties of ivermectin microemulsion have no change,ivermectin content matches the requirement of quality.The experimental results indicated that the 5%ivermectin microemulsion was of reliable quality and steady character.