PDF(Pubmed)
Abstract：
Atenolol (ATE) and propranolol (PRO) inclusion complexes with β-cyclodextrin have been investigated in aqueous solution. The aqueous solution was examined and characterized using UV-vis, fluorescence spectroscopy, and 1H NMR. The physical mixture was characterized using FTIR. The existence of inclusion complexes is confirmed by observing changes in spectroscopic properties. The ATE complex with β-CD exhibited an interaction as host and (β-CD) as a guest in a 1:1 ratio, with an inclusion constant K of 2.09 × 10-3 µM-1, as determined by the typical double-reciprocal graphs. Similarly, the PRO complex with β-CD exhibited an interaction as host and (β-CD) guest in 1:1 and 1:2 stoichiometry at the same time; the inclusion constants were K1 = 5.80 × 10-5 µM-1 and K2 = 4.67 × 10-8 µM-1, as determined by typical double-reciprocal graphs. The variables influencing the formation of the inclusion complexes were investigated and optimized. Based on the enhancement in fluorescence intensity due to the formation of inclusion complexes, spectrofluorometric methods were developed and validated for determination of each drug\'s pharmaceutical formulation. The quantification of the fluorescence intensity for ATE and PRO was conducted at λex/λem 226/302 nm and λex/λem 231/338 nm, respectively. Under the optimal reaction circumstances, linear relationships with good correlation coefficients of 0.9918 and 0.99 were found in the concentration ranges of 0.3-1.7 μM, and 0.1-1.1 μM for ATE and PRO, respectively. The limits of detection (LODs) were found to be 0.13 and 0.01 μM for ATE and PRO, respectively. The suggested approach was effectively applied to the analysis of both drugs\' pharmaceutical formulations.
摘要：
已在水溶液中研究了阿替洛尔（ATE）和普萘洛尔（PRO）与β-环糊精的包合物。使用UV-vis检查和表征水溶液，荧光光谱法，和1HNMR。使用FTIR表征物理混合物。通过观察光谱性质的变化证实了包合物的存在。与β-CD的ATE复合物以1：1的比例表现出作为主体和（β-CD）作为客体的相互作用，包含常数K为2.09×10-3µM-1，由典型的双倒数图确定。同样，具有β-CD的PRO复合物同时以1：1和1：2的化学计量表现出作为主体和（β-CD）客体的相互作用；包涵常数为K1=5.80×10-5µM-1，K2=4.67×10-8µM-1，由典型的双倒数图确定。研究并优化了影响包合物形成的变量。基于由于包合物的形成而导致的荧光强度的增强，开发并验证了荧光分光光度法，用于测定每种药物的药物制剂。在λex/λem226/302nm和λex/λem231/338nm处对ATE和PRO的荧光强度进行定量。分别。在最佳反应情况下，在0.3-1.7μM的浓度范围内发现了良好的相关系数为0.9918和0.99的线性关系，ATE和PRO为0.1-1.1μM，分别。对于ATE和PRO，检测限（LOD）分别为0.13和0.01μM，分别。该方法有效地应用于两种药物的药物制剂分析。
