磷脂和羟丙基-β-环糊精对葛根素溶解度的影响

Effect of phospholipid and hydroxypropyl-β-cyclodextrin on solubility of puerarin

目的将葛根素制成两相及三相分散体系,以提高葛根素的体外溶出速率。方法分别以磷脂和羟丙基-β-环糊精为载体,制备两相固体分散体和包合物,再将磷脂加入到葛根素-羟丙基-β-环糊精中制备三相分散体,分别进行溶解度和体外溶出度实验。对两相固体分散体、包合物和三相分散体进行红外扫描和差示扫描量热分析。结果当葛根素和磷脂的质量比为1∶2时制备的固体分散体葛根素的溶解度为6.54 g/L,包含物中葛根素溶解度为84.03 g/L,三相分散体中葛根素的溶解度为94.41 g/L。体外溶出结果显示15 min时,三相分散体中葛根素的累积溶出百分率达到98.34%。结论磷脂和羟丙基-β-环糊精对葛根素的溶出度具有协同作用。

AIM To prepare binary and ternary complexes of puerarin to evaluate their dissolution. METH- ODS Phospholipid （PL） and hydroxypropyl-β-cyclodextrin （HP-β-CD） were used as carrier to prepare binary solid dispersion and binary inclusion complex. Ternary complexes systems were obtained by adding phospholipid to puerarin-HP-β-CD （ 1 ： 1 ） systems. All systems were examined for solubility and dissolution properties, and char- acterized by FT-IR and DSC. RESULTS The solubility of puerarin in binary solid dispersion （puerarin ： PL of 1 ： 2, m/m） was 6.54 g/L, and in binary inclusion complex was 84.03 g/L, while in ternary complexes systems reached 94. 41 g/L. The percent of cumulative dissolution of ternary complexes systems in 15 min was 98.34% . CONCLUSION The synergistic effect between cyclodextrin and phospholipid makes the dissolution and solubility of puerarin increase.