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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

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【作者】 吴文娟梁月迎关玉群

【Author】 WU Wen juan 1,LIANG Yue ying 1, GUAN Yu qun 2(1. Department of Physical Chemistry, Guangdong College of Pharmacy,Guangzhou 510224;2. Department of Hygienic Chemistry, Zhongshan Medical University, Guangzhou 510089 China)

【机构】 广东药学院物理化学教研室中山医科大学卫生化学教研室 广东广州510224广东广州510224广东广州510089

【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 ,促进了包合作用的进行

【Abstract】 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.

  • 【文献出处】 西北药学杂志 ,Northwest Pharmaceutical Journal , 编辑部邮箱 ,2002年02期
  • 【分类号】R944
  • 【被引频次】21
  • 【下载频次】403
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