芦丁-二甲基-β-环糊精包合物的制备、物理化学表征及体外溶出研究  

Preparation,physicochemical characterization and dissolution studies in vitro of rutin- DM- β- CD inclusion complexes

作　　者：艾凤伟[1] 张加伟[1] 钱楠[1] 范春燕[1] 王敏[1] 

机构地区：[1]徐州医学院药学院,江苏徐州221004

出　　处：《药学研究》2015年第11期650-653,共4页Journal of Pharmaceutical Research

基　　金：徐州市科技计划项目(No.KC14SH077)

摘　　要：目的制备芦丁-二甲基-β-环糊精(DM-β-CD)包合物,提高芦丁在水中的溶解度。方法采用相溶解度法进行增溶试验,绘制相溶解度曲线,计算包合稳定常数(KC),利用研磨法制备芦丁-二甲基-β-环糊精包合物,以显微镜法、红外光谱法、体外溶出度法对包合物进行鉴定。结果芦丁与二甲基-β-环糊精相溶解度曲线属于AN型,在一定的二甲基-β-环糊精浓度范围内,芦丁的溶解度随着二甲基-β-环糊精浓度的增加呈线性增加,表明芦丁与二甲基-β-环糊精最佳包合比为1∶1,在线性范围内计算包合稳定常数(KC)为294.58L·mol-1。结论芦丁与二甲基-β-环糊精包合后呈现了新的物相特征,表明芦丁-二甲基-β-环糊精包合物已经形成,且溶解度明显增高,研磨法制备芦丁-二甲基-β-环糊精包合物能明显提高芦丁的溶解度,此法可用于芦丁-二甲基-β-环糊精包合物的制备。Objective To prepare the rutin- DM- β- CD inclusion complex and elevate the solubilization capacity of DM- β- CD for rutin. Methods Phase solubility method was used to perform a soluble experiment of rutin,drew phase solubility curves and calculated the inclusion stability constant( KC). The characteristic of rutin- DM- β- CD inclusion complex was identified by microscopy,FT- IR and dissolution etc. Results Phase solubility curves of rutin in DM- β-CD belong to typical AN. In a certain DM- β- CD concentration range,the solubility of rutin increased linearly as DM- β- CD concentration. Phase solubility profile showed that the molar ratio of rutin and DM- β- CD was 1 ∶ 1. The stability constant of rutin- DM- β- CD was 294. 58 L·mol- 1. Conclusion Rutin was complexed in DM- β- CD,which presents new phase characteristics. It indicated that the inclusion complex was formed and the solubility of rutin was improved significantly. It was a good method to prepare rutin- DM- β- CD inclusion complex.

关 键 词：芦丁 二甲基-β-环糊精 包合物 溶解度 

分 类 号：R944[医药卫生—药剂学]