奈妥吡坦/β-环糊精包合物的制备、评价与表征  

Preparation, Evaluation and Characterization of Netupitant/β-cyclodextrin Inclusion Compound

作　　者：和龙 刘玉[2] 温晓燕 张馨予 王玲 舒骁 HE Long;LIU Yu;WEN Xiao-yan;ZHANG Xin-yu;WANG Ling;SHU Xiao(Beijing Funhau Medicine Technology Co.,Ltd.,Beijing,100176,China;Department of Chest Oncology,West China Hospital,Sichuan University,Chengdu,Sichuan,610041,China;College of Basic Medical Sciences Jilin University,Changchun,Jilin,130012,China)

机构地区：[1]北京宽厚医药科技有限公司,北京100176 [2]四川大学华西医院胸部肿瘤科,四川成都610041 [3]吉林大学基础医学院,吉林长春130012

出　　处：《现代生物医学进展》2021年第2期233-238,共6页Progress in Modern Biomedicine

基　　金：北京市科协金桥工程种子资金项目(ZZ19015)。

摘　　要：目的:制备奈妥吡坦/β-环糊精包合物,用以提高奈妥吡坦的水溶性。方法:采用饱和水溶液法,制备奈妥吡坦/β-环糊精包合物;以载药量为指标,考察奈妥吡坦与β-环糊精的质量比(芯壁比)、包合温度、包合时间、搅拌速度的影响。基于单因素试验结果,采用正交设计实验对制备处方和工艺进行优化,得到最优奈妥吡坦/β-环糊精包合物,并对其包封率、载药量及稳定性进行体外评价。采用傅里叶红外光谱和X射线粉末衍射分析法,对最优奈妥吡坦/β-环糊精包合物进行表征。结果:奈妥吡坦/β-环糊精包合物的最佳优制备条件为:芯壁比1:20,包合温度为40℃,包合时间为20 min、搅拌速度为150 r/min。该条件制备制得的奈妥吡坦/β-环糊精包合物的载药量为4.73%,包合率为94.8%且在水溶液中的稳定性良好。傅里叶红外光谱和X射线衍射结果表明奈妥吡坦/β-环糊精包合物的成功制备。结论:成功制备了奈妥吡坦/β-环糊精包合物,奈妥吡坦的水溶性提高了1500倍,为奈妥吡坦水溶性新制剂的研发提供了实验基础。Objective: Preparation of netupitant/β-cyclodextrin inclusion compound, to improve the water solubility of netupitant.Methods: Netupitant/β-cyclodextrin inclusion compound was prepared by saturated aqueous solution method;taking the drug load as the index, the impacts of mass ratio(core-wall ratio), coating temperature, coating time and stirring speed of netupitant and β-cyclodextrin were investigated. The optimal netupitant/β-cyclodextrin inclusion compound was obtained based on the results of single factor experiment, orthogonal designed experiments were used to optimize the preparation formula and process, and the encapsulation rate, drug loading capacity and stability were evaluated in vitro. Fourier transform infrared spectroscopy(FTIR) and X-ray powder diffraction(XRD)were used to characterize the optimal netupitant/β-cyclodextrin inclusion compound. Results: The optimal preparation conditions for the netupitant/β-cyclodextrin inclusion compound are as follows: core-wall ratio 1:20, coating temperature 40℃, coating time 20 min, stirring speed 150 r/min. Under these conditions, the drug loading capacity of the netupitant/β-cyclodextrin inclusion compound was 4.73 %,the inclusion rate was 94.8%, and the stability in aqueous solution was good. Fourier transform infrared spectroscopy(FTIR) and X-ray diffraction(XRD) analysis proved the successful preparation of netupitant/β-cyclodextrin inclusion compound. Conclusion: Netupitant/β-cyclodextrin is successfully prepared, and the water solubility of netupitant increases by more than 1500 times, which provides an experimental basis for the development of new water-soluble pharmaceutics of netupitant.

关 键 词：奈妥吡坦 Β-环糊精 包合技术 水溶性 化疗止吐药 

分 类 号：R944[医药卫生—药剂学]