达沙替尼纳米结构脂质载体的制备与体外评价  

Preparation and in Vitro Evaluation of Dasatinib Nanostructured Lipid Carriers

作　　者：侯甲福[1] 刘世娟 耿艳萌[1] 杨琦[1] 胡泽香 谢舒 张颖 HOU Jia-fu;LIU Shi-juan;GENG Yan-meng;YANG Qi;HU Ze-xiang;XIE Shu;ZHANG Ying(Mudanjiang Medical College,Mudanjiang 157011,China;Hongqi Hospital Aff iliated to Mudanjiang Medical College,Mudanjiang 157011,China)

机构地区：[1]牡丹江医学院,黑龙江牡丹江157011 [2]牡丹江医学院附属红旗医院,黑龙江牡丹江157011

出　　处：《化工管理》2022年第20期138-140,共3页Chemical Engineering Management

基　　金：黑龙江省省属高等学校基本科研业务费科研项目(2019-KYYWFMY-0062)。

摘　　要：文章论述了采用热熔乳化超声法制备达沙替尼(DST)纳米结构脂质载体(NLC)的方法。采用正交试验法,对固-液比、乳化剂用量、药脂比、超声时间因素进行了考察,采用高校液相色谱法(HPLC)测定含量,以包封率为指标,筛选最佳工艺,体外透析法模拟药物释药情况。实验结果显示,制备的DST-NLC最优处方为,单硬脂酸甘油酯与新癸酸甘油酯比为8∶2,乳化剂用量为6%,药/脂比为1∶30,超声时间为4 min,DST-NLC在体外释药具有显著的缓释特性。实验制备的DST-NLC工艺简单,重复性好,体外释药具有缓释特征,为进一步研究奠定了基础。In this paper,the method of preparing dasatinib(DST)nanostructured lipid carriers(NLC)by hot melt emulsif ication ultrasound was discussed.The factors such as solid-liquid ratio,emulsif ier dosage,drug lipid ratio and ultrasound time were investigated by orthogonal test.The content was determined by high performance liquid chromatography(HPLC).The best process was selected with the entrapment eff iciency as the index.In vitro dialysis was used to simulate the drug release.The experimental results show that the optimal formulation of DST-NLC was as follows:the ratio of monostearate to neodecanoic acid glyceride was 8∶2,the dosage of emulsif ier was 6%,the drug/lipid ratio was 1∶30,and the ultrasonic time was 4 min.DST-NLC had signif icant sustained-release characteristics in vitro.The DST-NLC prepared in this experiment has simple process and good repeatability.The drug release in vitro has the characteristics of sustained release,which can lay a foundation for further research.

关 键 词：达沙替尼 纳米结构脂质体 体外释药 热熔乳化超声 

分 类 号：TQ469[化学工程—制药化工]