McCandless R, Yalkowsky S H
Department of Pharmaceutical Sciences, University of Arizona, College of Pharmacy, Tucson 85721, USA.
J Pharm Sci. 1998 Dec;87(12):1639-42. doi: 10.1021/js9802143.
Levemopamil was solubilized by varying the concentration of hydroxypropyl-beta-cyclodextrin (HPbetaCD) and by the alteration of pH. The drug molecule has two sites for possible complexation with HPbetaCD, creating the possibility of either 1:1 or 1:2 complexation. The solubility as a function of HPbetaCD concentration of the charged and uncharged forms of the drug follows the A(L) and Ap complexation models, respectively. This suggests that the charged drug forms a 1:1 complex, whereas the neutral drug forms both 1:1 and 1:2 complexes.
通过改变羟丙基-β-环糊精（HPβCD）的浓度以及调节pH值来增溶乐卡地平。药物分子有两个位点可与HPβCD发生络合，从而产生1:1或1:2络合的可能性。药物的带电形式和不带电形式的溶解度随HPβCD浓度的变化分别遵循A(L)和Ap络合模型。这表明带电药物形成1:1络合物，而中性药物则形成1:1和1:2络合物。
