环吡酮胺-β-环糊精包合物的制备及表征  

Preparation and characterization of ciclopirox olamine-β-cyclodextrin inclusion complex

作　　者：吴依洁 乔珍珍 魏月 缪柯 曹敏杰 陈林 叶茜 钟志容 WU Yijie;QIAO Zhenzhen;WEI Yue;MIU ke;CAO Minjie;CHEN lin;YE Qian;ZHONG Zhirong(Department of Pharmacy,School of Pharmacy,Southwest Medical University,Luzhou 646000,Sichuan Province,China)

机构地区：[1]西南医科大学药学院药剂学教研室,四川泸州646000

出　　处：《西南医科大学学报》2020年第6期548-553,共6页Journal of Southwest Medical University

基　　金：大学生创新创业训练计划项目(S201910715084);四川省科技厅重点研发项目(2020YFS0313);四川省卫计委课题(20PJ174,18PJ547);泸州-西南医大联合项目(2020LZXNYDZ04)。

摘　　要：目的:利用环糊精包合技术研究环糊精对环吡酮胺的增溶作用,改善环吡酮胺的溶解度、吸收度,对环吡酮胺类药物临床制剂进行优化,促进皮肤对药物的吸收,提高该类药物的生物利用度。方法:运用超声法制备环吡酮胺-β-环糊精包合物(CPX-β-CD),通过红外光谱仪和电镜扫描进行物相鉴定;使用高效液相色谱法检测含量并计算包合率与释放度;并通过体外释放度实验考察β-CD包合物对环吡酮胺释药的影响。结果:最优色谱条件为:流速1.0 mL/min,检测波长304 nm,柱温30℃,原药200μg/mL,进样量5μL,流动相乙腈与0.1%EDTA-2Na(体积比,45∶55)。环吡酮胺检测浓度在20.0~200.0μg/mL范围内呈良好线性关系(R2=0.9998);精密度、重复性、稳定性、回收率实验的RSD值均小于2%;环吡酮胺与β-CD的制备比例为1∶2时,超声法制得的包合物包合率最大,为47.72%;包合物在各时间点的药物释放量均大于环吡酮胺原料药的释放量,即包合作用可提高环吡酮胺的释放效率。结论:本实验成功制备了CPX-β-CD包合物,制备工艺简单可行;制得的CPX-β-CD包合物稳定性高,能够有效提高环吡酮胺的释放效率。Objective:To investigate the solubilization effect ofβ-cyclodextrin(β-CD)on ciclopirox olamine(CPX)using theβ-CD inclusion technology,and to improve the solubility and absorption of CPX,optimize the clinical preparation of CPX,promote drug absorption by the skin,and improve the bioavailability of such drugs.Methods:The ultrasonic method was used to prepare CPX-β-CD inclusion complex,and an infrared spectrometer and a scanning electron microscope were used for phase identification.High-performance liquid chromatography was used to measure the content and calculate inclusion rate and release rate,and in vitro release assay was used to observe the effect ofβ-CD inclusion complex on the drug release of CPX.Results:The optimal chromatographic conditions were a flow rate of 1.0 mL/min,a detection wavelength of 304 nm,a column temperature of 30℃,active compound 200μg/mL,an injection volume of 5μL,and a mobile phase of acetonitrile and 0.1%EDTA-2Na(v/v,45∶55).The detection concentration of CPX showed a good linear relationship within the range of 20.0~200.0μg/mL(R2=0.9998).Relative standard deviation was<2%for precision,repeatability,stability,and recovery.At a ratio of 1∶2 for CPX andβ-CD,the inclusion complex prepared by the ultrasonic method had the highest inclusion rate of 47.72%.The inclusion complex had a higher drug release amount than the bulk drug of CPX at each time point,suggesting that the inclusion action can improve the release efficiency of CPX.Conclusion:CPX-β-CD inclusion complex is successfully prepared in this experiment,and the preparation process is simple and feasible.The prepared CPX-β-CD inclusion complex has high stability and can effectively improve the release efficiency of CPX.

关 键 词：环吡酮胺 Β-环糊精 包合物 表征 

分 类 号：R943[医药卫生—药剂学]