Cediranib is a tyrosine kinase inhibitor that is used to treat ovarian cancer. The drug is administered as tablets containing the somewhat water-soluble salt cediranib maleate. However, the oral bioavailability is low and variable due to first-pass elimination. Enhanced solubilization and stabilization of cediranib can allow for alternative route of administration. The purpose of this study was to investigate the aqueous solubility of cediranib and its chemical stability in aqueous solutions. The aqueous solubility of cediranib maleate is strongly dependent on the ionization of both cediranib and the maleate counterion showing maximum at pH where the monovalent cediranib cation can form an ion pair with the monovalent maleate anion. The monovalent cediranib cation also had the highest affinity for the γ-cyclodextrin central cavity resulting in optimum solubilization. Cyclodextrin complexation did enhance the cediranib stability in aqueous solution and addition of small amount of riboflavin increased the stability even further. The degradation pathway of cediranib in acidic aqueous solutions was determined.

Cediranib是一种酪氨酸激酶抑制剂，用于治疗卵巢癌。该药物以含有某种水溶性马来酸西地尼布盐的片剂形式给药。但是，口服生物利用度低且由于首过清除而变化。西地尼布的增强的增溶作用和稳定性可以允许替代的给药途径。这项研究的目的是研究西地尼布的水溶性及其在水溶液中的化学稳定性。马来酸西地尼布的水溶性很大程度取决于西地尼布和马来酸抗衡离子的电离，在单价西地尼布阳离子可以与马来酸单价阴离子形成离子对的pH下显示出最大。单价西地拉尼阳离子也对γ-环糊精中央腔具有最高的亲和力，从而导致最佳的增溶作用。环糊精络合确实增强了西地尼布在水溶液中的稳定性，加入少量核黄素则进一步提高了稳定性。确定了西地尼布在酸性水溶液中的降解途径。