β-环糊精聚合物与药物包合作用的研究  

Study on complexation of β-cyclodextrin polymer with several drugs

作　　者：吴文娟[1] 梁月迎[1] 关玉群[2] 

机构地区：[1]广东药学院物理化学教研室,广东广州510224 [2]中山医科大学卫生化学教研室,广东广州510089

出　　处：《西北药学杂志》2002年第2期71-72,共2页Northwest Pharmaceutical Journal

摘　　要：目的　研究β-环糊精聚合物对几种药物的包合性能 ,并与β-环糊精 (β- CD)单体进行比较。方法　用电子分光光度法研究了药物与 β-环糊精聚合物或 β- CD在不同 p H缓冲溶液中的热力学性质。结果　该聚合物保留了β- CD所原有的包络性能 ,与巴比妥、苯巴比妥和盐酸黄连素均形成 1∶ 1包合物。在 p H4缓冲溶液中 ,中性客体包合物形成常数 Kf 比 p H10时负离子客体大 ;在相同 p H条件下 ,该聚合物形成包合物的 Kf 值大于与β- CD单体形成包合物的 Kf 值。药物的交联疏水增强系数 R均大于 1。结论　交联作用增强了 CD空穴的疏水性 。The complex forming abilities of β cyclodextrin epichlorohydrin po1ymer(β CDP)with several drugs were studied and compared with that of β CD. The results showed that β CDP kept the original character of β CD, forming 1∶1 complexes with barbita1, phenobarbital and hydrochloridum berberini. The association constant K f at pH4(neutra1 guest) was general1y larger than that at pH10(anionic guest); and the K f values of β CDP were larger than that of β CD under the same pH conditions. The R(hydrophobic enchancement coefficient) values for drugs were larger than 1, which indicated that the crosslinking increased the hydrophobicity of the binding site in β CDP and promoted the formation of the complex.

关 键 词：Β-环糊精聚合物 药物包合作用 包合物形成常数 疏水增强系数 环氧氯丙烷 

分 类 号：R944.2[医药卫生—药剂学]