间尼索地平固体分散体的研制

目的:将难溶性药物间尼索地平制备成固体分散体,以增加其溶解度及体外溶出度。方法:以泊洛沙姆为载体,共沉淀法制备间尼索地平固体分散体。采用差示扫描量热分析(DSC)方法鉴别药物在载体中的存在状态,并进行溶解度和体外溶出度研究。结果:DSC显示间尼索地平与泊洛沙姆形成了低共熔物,间尼索地平原料药及其与泊洛沙姆不同比例的固体分散体(1∶3、1∶5、1∶7)的溶解度分别为0.89、4.50、15.35、23.03mg·L-1,120min时的累积溶出百分率分别为26.80%、38.57%、41.38%、45.92%,固体分散体的溶出度高于同比例的物理混合物。结论:以泊洛沙姆为载体制备间尼索地平固体分散体,可增加药物的体外溶出度和溶解度。

Preparation of m-Nisoldipine Solid Dispersion

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 eopreeipitation 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 rain dissolution rates were 26.80%, 38.57%,6, 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.