Preparation of m-Nisoldipine Solid Dispersion / 中国药房

ABSTRACT

OBJECTIVE:To prepare m-nisoldipine solid dispersion from poorly-soluble m-nisoldipine so as to improve its solubility and dissolution rate in vitro. METHODS: Solid dispersions of m-nisoldipine were prepared by coprecipitation method with poloxamer as carrier; Differential scanning calorimetry (DSC) was used to determine the status of nimodipine in carrier. The solubility and the dissolution rate of the solid dispersion in vitro were studied. RESULTS: DSC analysis indicated that eutectic mixture was formed from m-nisoldipine and poloxamer. The solubility of m-nisoldipine and the its solid dispersions prepared from m-nisoldipine and poloxamer at different ratio (1∶3, 1∶5, 1∶7) were 0.89, 4.50, 15.35, and 23.03 mg?L-1, respectively, and their 120 min dissolution rates were 26.80%, 38.57%, 41.38%, and 45.92%, respectively. In the same ratio, the dissolution rates of the solid dispersions were higher than those of their physics mixtures. CONCLUSIONS: The solid dispersion of m-nisoldipine prepared with poloxamer as carrier can increase the solubility and dissolution rate in vitro.