β-环糊精与福尼地平包合物的分光光度法和电化学研究

Spectrophotometric and electrochemical study of the inclusion complex between beta-cyclodextrin and furnidipine.

作者信息

Yáñez C, Salazar R, Núñez-Vergara L J, Squella J A

机构信息

Bioelectrochemistry Laboratory, Chemical and Pharmaceutical Sciences Faculty, University of Chile, P.O. Box 233, Santiago 1, Chile.

出版信息

J Pharm Biomed Anal. 2004 Apr 1;35(1):51-6. doi: 10.1016/j.jpba.2003.12.015.

DOI:10.1016/j.jpba.2003.12.015

PMID:15030879

Abstract

Inclusion complexation between furnidipine (2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-tetrahydrofurfuryl 5-methyl diester), a calcium-channel antagonist, and beta-cyclodextrin (beta-CyD) was studied in aqueous solution by using both spectrophotometric and electrochemical measurements. The phase solubility profile was classified as A(L)-type, indicating the formation of 1:1 stoichiometric inclusion complex of furnidipine with beta-CyD. Based on the spectrophotometric absorbance's variations, a formation constant value, K(f), of 156 M(-1) was determined. Electrochemical measurements using chronocoulometric experiments were used for the determination of the diffusion coefficients. In absence of beta-CyD, a diffusion coefficient value of 4.32 x 10(-6) cm2 s(-1) was obtained for furnidipine. The addition of beta-CyD produced a decrease of 30% for the diffusion coefficient. Formation of inclusion complexes of furnidipine with beta-CyD was proved to increase more than three times the solubility of furnidipine.

摘要

采用分光光度法和电化学测量方法，在水溶液中研究了钙通道拮抗剂福尼地平（2,6 - 二甲基 - 4 - (2 - 硝基苯基) - 1,4 - 二氢吡啶 - 3,5 - 二羧酸3 - 四氢糠醇酯5 - 甲酯）与β - 环糊精（β - CyD）之间的包合络合作用。相溶解度曲线归类为A(L)型，表明福尼地平与β - 环糊精形成了化学计量比为1:1的包合络合物。基于分光光度法吸光度的变化，测定了形成常数K(f)值为156 M⁻¹。使用计时电量实验的电化学测量用于测定扩散系数。在不存在β - 环糊精的情况下，福尼地平的扩散系数值为4.32×10⁻⁶ cm² s⁻¹。加入β - 环糊精后，扩散系数降低了30%。已证明福尼地平与β - 环糊精形成包合络合物后，福尼地平的溶解度增加了三倍多。