2-羟丙基-β-环糊精对卡维地洛增溶作用的研究

Study on the Solubilization of 2-Hydroxypropyl-β-cyclodextrin for Carvedilol

目的:考察不同pH条件下2-羟丙基-β-环糊精对卡维地洛的增溶作用,制备卡维地洛的2-羟丙基-β-环糊精包合物并对其进行结构表征。方法:以相溶解度法考察不同pH条件下2-羟丙基-β-环糊精对卡维地洛的增溶作用,采用溶液搅拌法制备包合物,并以差示扫描量热法、红外光谱法和X-射线衍射法对包合物进行结构表征。结果:相溶解度图呈A L型。相同pH条件下,卡维地洛溶解度随2-羟丙基-β-环糊精浓度增大而增大;相同2-羟丙基-β-环糊精浓度下,卡维地洛溶解度随pH增大而减小。差示扫描量热法、红外光谱和X-射线衍射法图谱均显示药物峰消失,表明卡维地洛与2-羟丙基-β-环糊精已形成包合物。结论:2-羟丙基-β-环糊精是卡维地洛的理想增溶剂。

Objective： To study the solubilization effect of 2-hydroxypropyl-β-cyclodextrin（2-HP-β-CD） on carvedilol under different pH values, and to prepare and characterize the carvedilol-2-HP-β-CD inclusion complex. Methods： The phase-solubility method was used to study the aqueous solubility of carvedilol under different pH values. The carvedilol-2-HP-β-CD inclusion complex was prepared by using solution- stirring method. In addition, the carvedilol-2-HP-β-CD inclusion complex was characterized by differential scanning calorimetry （DSC）, Fourier transform infrared spectroscopy （FTIR） and X-ray diffractometry （XRD）. Results： The phase-solubility diagrams of carvedilol were shown as AL type. The solubility of carvedilol increased with the increase of 2-HP-β-CD concentration under the same pH value. The solubility of carvedilol decreased with the increase of pH value under the same concentration of 2-HP-β-CD. The spectra of DSC, FTIR and XRD showed the disappearance of carvedilol peak, suggesting the formation of carvedilol-2-HP-β-CD inclusion complex. Conclusion： 2-HP-β-CD is an ideal solubilizer for carvedilol.