2-羟丙基β-环糊精对美洛昔康的包合作用

目的测定美洛昔康在不同浓度 2 羟丙基 β 环糊精溶液中的溶解度曲线 ,以及包合物的组成量比例和稳定性常数。方法在 2 5℃运用相溶解度法进行实验 ,采用紫外分光光度法测定美洛昔康在溶液中的浓度。结果随着 2 羟丙基 β 环糊精浓度增加和 pH的增大 ,美洛昔康的溶解度显著提高。计算了表观稳定常数、确定了不同pH条件下包合物的摩尔比。 结论难溶性药物美洛昔康与 2 羟丙基 β 环糊精可形成 1 :1包合物。

Utilization of 2-hydroxpropy 1-β-cyclodextrin as the solubilizer of meloxicam

Objective To investigate the solubilization effects of the inclusion complex of meloxicam with 2-hydroxypropy1-β-cyclodextrin (HPCD) in aqueous solutions at various pH and to determine the constitutive molar ratio of meloxicam-2-hydroxypropy1-β-cyclodextrin inclusion compound and its stability constant.Methods The solubilization experiment was performed by the phase-solubility method at 25℃.The concentration of meloxicam was determined by the UV spectrophotometric method. Results The apparent solubility of meloxicam was enhanced noticeably with the increase of concentration HPCD and the increasing pH values.The apparent stability constants were calculated respectively.The molar ratio of the inclusion complex at various pH were studied.The application of HPCD to parenteral formulations of meloxicam was discussed preliminarily.Conclusion An inclusion compound of meloxicam and HPCD can be formed.