【摘要】 本文研究了七元瓜环（Q[7]）,八元瓜环（Q[8]）与抗癌药物二甲苯磺酸拉帕替尼（LD）之间的主客体相互作用,以及瓜环对LD溶解度及溶出度的影响,研究结果表明:Q[7],Q[8]两种瓜环均可与LD形成稳定的1∶1配合物。其作用平衡常数分别为:2.43×105L·mol^-1,1.02×106L·mol^-1两种瓜环的加入对LD具有较好的增溶效果,且对LD的溶出度均有一定程度的改善,该实验结果为瓜环促进难溶药物溶解度提供了一定的理论依据。更多还原

【Abstract】 The interaction of cucurbit[7,8]urils（ Q[7,8]） with anti-cancer drug lapatinib ditosylate（ LD） was studied and the effects of cucurbit[7,8]urils on solubility and dissolution rate of lapatinib ditosylate were also investigated. The results show that inclusion complex between Q[7,8]and LD informed at molar ratios of 1: 1. The formation constant were 2.43×105 L·mol^-1 and 1.02×106 L·mol^-1 for the Q[7]-LD and Q[8]-LD complex,respectively. Our results indicate that the complexation of lapatinib ditosylate with Q[7,8]could enhance the solubility and dissolution rate of drug in aqueous solution.更多还原