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西南医科大学药学院药剂学教研室
纸质出版日期:2020,
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[1]吴依洁,乔珍珍,魏月,缪柯,曹敏杰,陈林,叶茜,钟志容.环吡酮胺-β-环糊精包合物的制备及表征[J].西南医科大学学报,2020,43(06):548-553.
WU Yijie, QIAO Zhenzhen, WEI Yue, et al. Preparation and characterization of ciclopirox olamine-β-cyclodextrin inclusion complex[J]. Journal of Southwest Medical University, 2020,43(6):548-553.
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(R
2
=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 of β-cyclodextrin(β-CD)on ciclopirox olamine(CPX)using the β-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 of β-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 200 μg/mL
an injection volume of 5 μL
and a mobile phase of acetonitrile and 0.1% EDTA-2 Na(v/v
45∶55).The detection concentration of CPX showed a good linear relationship within the range of 20.0 ~ 200.0 μg/mL(R2= 0.9998).Relative standard deviation was < 2% for precision
repeatability
stability
and recovery.At a ratio of 1∶2 for CPX and β-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.
环吡酮胺β-环糊精包合物表征
Ciclopirox olamineβ-CyclodextrinInclusion complexCharacterization
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