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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 investigate the solubilization of carvedilol by 2-hydroxypropyl-β-cyclodextrin under different pH conditions and to prepare 2-hydroxypropyl-β-cyclodextrin inclusion complex of carvedilol. It is structurally characterized. Methods: The solubilization of carvedilol with 2-hydroxypropyl-β-cyclodextrin under different pH conditions was investigated by phase-solubility method. The inclusion complex was prepared by solution agitation. The solubility of carvedilol was determined by differential scanning calorimetry FTIR spectroscopy and X-ray diffraction were used to characterize the inclusion complex. Results: Phase solubility diagram was A L type. Under the same pH condition, the solubility of carvedilol increased with the increase of the concentration of 2-hydroxypropyl-β-cyclodextrin. With the same concentration of 2-hydroxypropyl-β-cyclodextrin, the solubility of carvedilol pH increases and decreases. Differential scanning calorimetry, infrared spectroscopy and X-ray diffraction patterns showed that the drug peak disappeared, indicating that carvedilol and 2-hydroxypropyl-β-cyclodextrin have formed inclusion complexes. Conclusion: 2-hydroxypropyl-β-cyclodextrin is an ideal solubilizer for carvedilol.