Stancanelli R, Mazzaglia A, Tommasini S, Calabrò M L, Villari V, Guardo M, Ficarra P, Ficarra R
Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
J Pharm Biomed Anal. 2007 Aug 15;44(4):980-4. doi: 10.1016/j.jpba.2007.03.025. Epub 2007 Mar 30.
The improvement of isoflavones bioavailability by complexation with chemically modified cyclodextrins (CyDs) has been exploited to analyse the drug/macrocycle binding affinity by a conventional method with new useful measures. Genistein (Gen) and daidzein (Daidz) were investigated in aqueous medium and in presence an amount of (2-hydroxypropyl)-beta-cyclodextrin (HP-beta-CyD) at different host/guest molar ratios. The solubility in pure water, approximately 3 x 10(-6)M for Gen and approximately 10 x 10(-6)M for Daidz, was obtained by distributing the of guest molecule between water and the organic solvent. The stoichiometric ratios and stability constants describing the extent of formation of the complexes have been determined by phase-solubility UV-vis measurements and confirmed by circular dichroism data. These results have implications in the determination of the carrier's capacity for the complexation of the drug in water solution.
通过与化学修饰的环糊精(CyDs)络合来提高异黄酮的生物利用度,已被用于通过一种具有新的有用测量方法的传统方法来分析药物/大环化合物的结合亲和力。在水介质中以及存在不同主/客体摩尔比的一定量(2-羟丙基)-β-环糊精(HP-β-CyD)的情况下,对染料木黄酮(Gen)和大豆苷元(Daidz)进行了研究。通过将客体分子分布在水和有机溶剂之间,得到了在纯水中的溶解度,Gen约为3×10⁻⁶M,Daidz约为10×10⁻⁶M。通过相溶解度紫外-可见测量确定了描述络合物形成程度的化学计量比和稳定常数,并通过圆二色性数据得到了证实。这些结果对于确定载体在水溶液中络合药物的能力具有重要意义。