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目的研究磺丁基醚-β-环糊精和羟丙基-β-环糊精对普拉格雷的增溶作用,以提高普拉格雷的溶解度。方法采用相溶解度法考察磺丁基醚-β-环糊精和羟丙基-β-环糊精对普拉格雷的增溶机制。结果磺丁基醚-β-环糊精和羟丙基-β-环糊精可明显改善普拉格雷的水溶性。结论羟丙基-β-环糊精普拉格雷的平衡相溶解图为AL型,磺丁基醚-β-环糊精普拉格雷的平衡相溶解图为AN型,二者对普拉格雷均有较好的增溶作用,但磺丁基醚-β-环糊精的增溶作用更强。
Objective To study the solubilization of prasugrel with sulfobutyl ether-β-cyclodextrin and hydroxypropyl-β-cyclodextrin to improve the solubility of prasugrel. Methods Solubilization mechanism of prasugrel with sulfobutyl ether-β-cyclodextrin and hydroxypropyl-β-cyclodextrin was investigated by phase-solubility method. Results Sulfobutyl ether-β-cyclodextrin and hydroxypropyl-β-cyclodextrin significantly improved the water solubility of prasugrel. Conclusion The equilibrium phase-resolved solution of hydroxypropyl-β-cyclodextrin prasugrel is AL type. The equilibrium phase-resolved solution of sulfobutyl ether-β-cyclodextrin prasugrel is AN type. Have better solubilization, but sulfobutyl ether-β-cyclodextrin stronger solubilization.