甲磺酸溴隐亭自微乳的研制及其质量评价  

Preparation and quality evaluation of bromocriptine mesylate self-emulsion preparation

作　　者：谷筱雅 胡贝贝 姚军[2] 霍杨梅 仝恬卓 GU Xiaoya;HU Beibei;YAO Jun;HUO Yangmei;TONG Tianzhuo(Handan First Hospital,Handan 056004,China;School of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang 050000,China)

机构地区：[1]邯郸市第一医院,河北邯郸056004 [2]河北科技大学化学与制药工程学院,河北石家庄050000

出　　处：《沈阳药科大学学报》2024年第11期1451-1458,1530,共9页Journal of Shenyang Pharmaceutical University

基　　金：河北省自然科学基金资助项目(H2020208001)。

摘　　要：目的制备甲磺酸溴隐亭自微乳制剂,并进行质量评价。方法通过饱和溶解度测定筛选油相、乳化剂、助乳化剂;通过配伍试验、绘制伪三元相图确定处方;再以粒径、载药量为指标,应用星点设计-响应曲面法优化处方;最后对自微乳的显微形态、自乳化时间、粒径和载药量的影响因素、溶出度、稳定性进行质量评价。结果最优处方三乙酸甘油酯21.33%,PEG 40氢化蓖麻油41.74%,PEG 40036.93%。经优处方制备的自微乳,显微形态为内相规整且分布均匀的球形,自乳化时间22.7 s,粒径为16.81 nm,载药量为19.79 mg·g^(-1),且并未因稀释倍数、温度和离心改变发生较大变化,溶出度有大幅度提高,在4、25℃和冷热循环系统下贮藏稳定。结论研制出的甲磺酸溴隐亭液体自微乳工艺较好,粒径分布均匀,载药量较高,体系稳定。Objective To prepare bromocriptine mesylate self-microemulsion and evaluate its quality.Methods The oil phase,emulsifier and coemulsifier were selected by the determination of saturated solubility;The prescription was determined by compatibility test and pseudo ternary phase diagram;Then,with the particle size and drug loading as indicators,the formulation was optimized by using the star point design response surface method;Finally,the micromorphology,self-emulsifying time,particle size,drug loading,dissolution and stability of the self-microemulsion were evaluated.Results The optimal formulation was glyceryl triacetate 21.33%,PEG 40 hydrogenated castor oil 41.74%,PEG 40036.93%.The micro morphology was spherical with regular inner phase and uniform distribution.The self-emulsification time was 22.7 s,the particle size was 16.81 nm,and the drug loading was 19.79 mg·g^(-1).The self-emulsion prepara-tion did not change greatly due to the dilution factor,temperature and centrifugation.The dissolution was greatly improved,and the preparation was stable at 4℃,25℃,cold and hot circulation storage.Conclusion The developed bromocriptine liquid self-microemulsion process is good,with uniform particle size distribu-tion,high drug loading and stable system.

关 键 词：甲磺酸溴隐亭 液体自微乳 伪三元相图 星点设计-响应面优化法 质量评价 

分 类 号：R94[医药卫生—药剂学]