齐墩果酸β-环糊精包合物的制备

Inclusion of Oleanolic Acid with β-Cyclodextrin

目的提高齐墩果酸(OA)的水溶性,制备其β-环糊精(β-CD)包合物,并且研究药物成盐和加入水溶性高分子聚乙烯吡咯烷酮(PVP)对包合效率和药物水溶性的影响。方法采用饱和水溶液法制备包合物,采用HPLC测定药物在水中的溶解度,通过红外光谱对包合物验证,并初步探讨PVP的影响机制。结果形成包合物后,OA在水中的溶解度提高3.4倍,成盐可提高包合效率,并使药物溶解度进一步提高,达107倍。制备包合物时加入浓度较高的PVP,反而使药物溶解度减少。红外光谱研究结果表明,OA与β-CD确实形成了包合物,OA与PVP、β-CD均存在分子间相互作用。结论制备包合物时加NaOH成盐可以大幅提高OA的水溶性。

Objective To improve the water solubility of oleanolic acid（OA）by preparing the inclusion complex of OA andβ-cyclodextrin（β-CD）,and to investigate the effects of salt formation of OA and addition of water-soluble polyvinylpyrrolidone（PVP）on complexation efficiency and drug solubility.Methods The inclusion complexes were prepared by saturated water solution method.Aqueous solubility of OA was determined using HPLC,and inclusion complexes were validated using infrared spectroscopy.Furthermore,the effect mechanism of PVP was investigated preliminarily.Results The water solubility of OA was increased by 3.4-times after inclusion withβ-CD.The complexation efficiency was improved and drug solubility was further increased to 107-fold by salt formation of OA.However,the water solubility of OA was reduced by the addi-tion of high concentrations of PVP during the inclusion process.Infrared spectrum analysis indica-ted that the inclusion complex was formed between OA andβ-CD and there was strong molecular interaction between OA and PVP or between OA andβ-CD.Conclusion The water solubility of OA can be obviously increased by salt formation with the addition of NaOH during the prepara-tion of inclusion complex.