薄膜分散法制备格列本脲类脂质体的工艺研究与质量评价  

Technical study and quality evaluation of Glibenclamide liposmes prepared by Thin-film dispersion method

作　　者：白彩萍[1] 孙敬蒙 张晓晨[1] 王丹[1] 张炜煜[1] BAI Caiping;SUN Jingmeng;ZHANG Xiaochen;WANG Dan;ZHANG Weiyu(Changchun University of Chinese Medicine,Changchun,Jilin,130017 P.R.China;The First Hospital of Jilin University,Changchun,Jilin,130000,P.R.China)

机构地区：[1]长春中医药大学,吉林长春130117 [2]吉林大学第一医院,吉林长春130000

出　　处：《华西药学杂志》2019年第2期125-130,共6页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备格列本脲类脂质体,并对其进行质量评价。方法采用薄膜分散法制备格列本脲类脂质体,以包封率为考察指标,采用单因素实验法,对HLB值、载体与药物比值等7种因素进行考察,确定其制备工艺的影响因素和水平;进一步采用正交实验法,优化其制备工艺参数;通过差示热量扫描法(DSC)测定,验证格列本脲类脂质体是否形成;并就最佳处方制备的格列本脲类脂质体的粒径、形态、包封率、载药量、释放度等性质进行评价。结果最佳制备工艺为:表面活性剂与胆固醇的摩尔比为1∶1. 4,载体与药物比值为100∶28,水合温度为65℃,乙醇用量为180 m L; DSC证明了类脂质体的形成。电镜观察格列本脲类脂质体形态为圆形或椭圆形,粒径为0. 776μm,跨距PDI为1. 229,载药量为58. 40%,包封率为82. 50%,12 h释放度为90. 86%。结论成功制备了格列本脲类脂质体,其质量符合2015年版《中国药典》中微粒制剂指导原则项下要求,为后续新药开发提供了参考。OBJECTIVE To prepare the Glibenclamide liposome and to evaluate its quality.METHODST The Glibenclamide liposomes were prepared using Thin-film dispersion method.The encapsulation efficiency of the Glibenclamide was measured by single factor method.The HLB value,carrier and drug ratio were investigated to determine the influencing factors and levels of preparation process.The preparation process parameters were optimized by Orthogonal experiment method.The formation of Glibenclamide liposome by DSC(differential calorimetry),and the optimal prescription preparation was determined.The particle size,morphology,encapsulation efficiency,drug loading amount,and release degree of the leukuria liposome were evaluated.RESULTS The optimal preparation process was as follow:a molar ratio of surfactant to cholesterol of1∶1.4,a carrier to drug ratio of 100∶28,a hydration temperature of 65℃,and an ethanol dosage of 180 m L.DSC demonstrated the formation of liposomes.Electron microscopy showed that the morphology of glibenclamide liposomes was round or elliptical.The particle size was 0.776μm;span PDI was 1.229;drug loading was 58.4%;encapsulation efficiency was 82.50%;and the12 h release was 90.86%.CONCLUSION Glibenclamide liposome has been successfully prepared,and its quality meets the requirements of the Chinese Pharmacopoeia 2015 edition,which provides a reference for the development of new drugs.

关 键 词：格列本脲 类脂质体 薄膜分散法 单因素 正交实验 包封率 质量评价 工艺参数 

分 类 号：R94[医药卫生—药剂学]