Effect of hydroxypropyl-β-cyclodextrin and pH on the solubility of levemopamil HCl

Effect of hydroxypropyl-β-cyclodextrin and pH on the solubility of levemopamil HCl
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羟丙基-β-环糊精和pH对盐酸左莫帕米溶解度的影响

DOI:
10.1021/js9802143
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发表时间:
1998
影响因子:
3.8
通讯作者:
S. Yalkowsky
S. Yalkowsky
中科院分区:
医学3区
文献类型:
--
作者:
Richard McCandless;S. Yalkowsky

文献摘要

被引文献

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通过改变羟丙基-β-环糊精 (HPβCD) 的浓度和改变 pH 值来溶解左旋帕米。该药物分子有两个可能与 HPβCD 络合的位点,从而产生 1:1 或 1:2 络合的可能性。带电荷和不带电荷形式的药物的溶解度与 HPβCD 浓度的关系分别遵循 AL 和 AP 络合模型。这表明带电药物形成 1:1 复合物,而中性药物形成 1:1 和 1:2 复合物。
Levemopamil was solubilized by varying the concentration of hydroxypropyl-β-cyclodextrin (HPβCD) and by the alteration of pH. The drug molecule has two sites for possible complexation with HPβCD, creating the possibility of either 1:1 or 1:2 complexation. The solubility as a function of HPβCD concentration of the charged and uncharged forms of the drug follows the AL 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.