2-羟丙基-β-环糊精对氯诺昔康的增溶作用

The Solubilization Effect of 2-hydroxypropy1-β-cyclodextrin on Lornoxicam

目的考察不同pH条件下不同浓度的2-羟丙基-β-环糊精溶液对氯诺昔康的增溶作用。方法在室温下运用相溶解度法对氯诺昔康的溶解性进行实验,采用紫外分光光度法测定氯诺昔康在溶液中的浓度。包合物的表观稳定常数由回归方程求得:K=斜率/截距(1-斜率)。结果随着2-羟丙基-β-环糊精浓度的增加和pH的增大,氯诺昔康的溶解度显著提高,在pH7、pH8、pH9条件下HPCD对氯诺昔康的增溶量分别为0.499、1.791、2.405mg·ml-1。计算了不同pH下包合物的表观稳定常数,在pH7、pH8、pH9条件下表观稳定常数分别为132.42、66.53、38.60。结论难溶性药物氯诺昔康与2-羟丙基-β-环糊精可形成1∶1包合物,2-羟丙基-β-环糊精对于难溶性药物氯诺昔康是较理想的增溶剂。

Aim To study the solubilization effect of 2-hydroxypropyl-β-cyclodextrin, （HPCD） of various pH and concentrations on lomoxicam. Methods The solubization experiment was done by the phase-solubility method, and the concentration of lomoxicam was determined by the UV method. The stability constants（K） of the conclusion complex could be calculated from the regression equation： K = slope/intercept（ 1-slope）. Results The solubility of lomoxicam was enhanced rapidly with the increase of HPCD concentration and increase of pH. The solubilization effect on lomoxicam is 0.499, 1.791,2.405mg·ml^-1 at pH7, pH8, pH9. The stability constants were calculated at various pH. The stability constants（K） were 132.42,66.53,38.60 at pH7, pH8, pH9. Conclusion Lomoxicam-HP-CD conclusion complex could be formed,HPCD is a desirable solubilizer for lomoxicam.