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阿司匹林磷脂复合物脂微球的制备及评价 预览

Preparation and Evaluation of Aspirin Phospholipid Compound Lipid Microsphere
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摘要 目的:制备阿司匹林磷脂复合物脂微球(ASP-PC-LM),并评价其性质。方法:采用高速剪切法制备初乳,高压均质法对初乳进行二次乳化,以离心稳定常数(Ke)及平均粒径为考察指标,单因素试验考察处方和制备工艺,并对其外观、粒径、Zeta电位及包封率进行考察。结果:ASP-PC-LM最佳处方和工艺是橄榄油与辛癸酸甘油酯(MCT)以1∶1配比(15%),油酸(0.3%)、大豆磷脂(1.2%)于70℃混合作为油相,Kolliphor HS 15(2.0%)同温度下溶解于注射用水作为水相,油水两相在70℃下混合,10 000 r/min高速剪切5 min,然后在110 MPa高压均质3次,所得ASP-PC-LM外观呈圆形,平均粒径为(180.2±12.8)nm,Zeta电位为(-41.23±1.53)mV,包封率为(81.03±0.797)%,Ke为32.93±0.08。结论:最佳工艺制备ASP-PC-LM的粒径适宜、包封率高,工艺稳定性好。 Objective:To prepare aspirin phospholipid compound lipid microspheres(ASP-PC-LM)and evaluate its properties.Methods:The crude emulsion was prepared by high speed shear method and secondary emulsification was performed by high pressure homogenization method.The centrifugal stability constant(Ke)and mean particle size were taken as the evaluation indexes.The single-factor test examined the formulation and preparation process;its appearance,particle size,Zeta potential and encapsulation rate were also investigated.Results:The optimized prescription process was as follows:olive oil and MCT were mixed at 1∶1 ratio(15%)with oleic acid(0.3%)and soybean phospholipid(1.2%)at 70°C as oil phase.Kolliphor HS 15(2.0%)was dissolved with water for injection at the same temperature and then the oil-water two-phase mixed under 70℃;high-speed shear 5 minutes at 10 000 r/min,high pressure homogenization was performed for 3 times at 110 MPa.The appearance of ASP-PC-LM presented as round,the average particle size was(180.2±12.8)nm,the Zeta potential was(-41.23±1.53)mV,the encapsulation rate was(81.03±0.797)%and the centrifugal stability constant was(32.93±0.08).Conclusion:The optimum process preparation of ASP-PC-LM has the advantages of suitable particle size,high encapsulation rate and good process stability.
作者 贺智勇 姜丰 李婉蓉 杨佳佳 周雪 吴林菁 肖婷 沈祥春 陶玲 HE Zhiyong;JIANG Feng;LI Wanrong;YANG Jiajia;ZHOU Xue;WU Linjing;XIAO Ting;SHEN Xiangchun;TAO Ling(State Key Laboratory on Efficacy and Utilization of Medicinal Plants,Guizhou Engineering Center for Efficient Utilization of Natural Drug Resources,High Educational Key Laboratory of Natural Medicinal Pharmacology and Drug Ability,Guizhou Medical University-Guiyang Key Laboratory of Natural Medicine Resources,Key Lab of Excellent and Effective Utilization of Natural Drug Resources,Guizhou Medical University,Guiyang 550025,Guizhou,China)
机构地区 贵州医科大学
出处 《贵州医科大学学报》 CAS 2019年第7期786-791,共6页 Journal of Guizhou Medical University
基金 贵州省高等教育科技创新团队项目[黔教合人才团队字(2014)31] 贵州省科技创新团队项目[黔科合人才团队(2015)4025号] 贵州省科技厅[黔科合人才(2015)4029号] 贵州省科技计划项目[黔科合SY字(2015)3032] 贵阳市科技计划项目[筑科合同(20141001)12号] 大学生创新创业项目(201710660032).
关键词 阿司匹林 磷脂复合物 脂微球 制备工艺 评价 asipirin phosphlipid complex lipid microsphere preparation process evaluation
作者简介 通信作者:沈祥春,shenxiangchun@126.com;通信作者:陶玲,E-mail:649511230@qq.com.
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