硝苯地平β－环糊精包合物的研究

STUDY ON INCLUSION COMPLEX OF NIFEDIPINE WITH β-CYCLODEXTRIN

研究了β－环糊精（ＣＤ）对硝苯地下的包合作用及包合物的溶解性，并比较了硝苯地平ＣＤ包合物与硝苯地平片的体内吸收差异。结果表明，硝苯地平与ＣＤ以１：１的摩尔比形成包含物，络合常数为１９１．４ｍｏｌ^（－１）·Ｌ；硝苯地平在包合后其水中溶解度由包含前的７．０５μｇ／ｍｌ提高到１５．６０μｇ／ｍｌ；硝苯地平ＣＤ包合物的生物利用度优于硝苯地平片。

The inclusion complex of nifedipine with β-cyclodextrin was prepared by coprecipitation method or grinding method. The experimental data of the inclusion compound fitted well to the molar ratio of 1 :1 with the association constant of 191.4 mol/L-1 . The solubility of nifedipine in inclusion form increased from 7.05μg/ml to 15. 60μg/ml. As to bioavailability, nifedipine in inclusion state was better than the free form.