溶剂蒸发-沉积法制备尼群地平固体分散体

Study on preparation of nitrendipine solid dispersion using the solvent evaporation-deposition method

目的:采用溶剂蒸发-沉积法制备尼群地平固体分散体。方法:通过单因素试验和正交设计试验详细考察了影响尼群地平固体分散体中药物释放的处方因素和制备工艺因素,并通过X-射线粉末衍射(XRD)和差示扫描量热(DSC)实验对药物可能存在的状态进行了判断。结果:固体分散体的最优处方与工艺为PVPk30、L-HPC,两者的比例为2∶7,溶剂为二氯甲烷,超声时间10min,水浴温度80℃。XRD和DSC实验表明药物可能以无定型存在于固体分散体中。结论:采用溶剂蒸发-沉积法制备尼群地平固体分散体,简便可行、易于工业化。

OBJECTIVE To prepare nitrendipine solid dispersion using solvent evaporation-deposition method. METHODS By means of the influence factors test and orthogonal design test, formulation and technology factors on drug release from solid dispersion were investigated and optimized by dissolution tests. Physical states in solid dispersion of drug were characterized using X-ray diffraction analysis （XRD） and differential scanning calorimetry （DSC）. RESULTS The optimized formulation and technology factors were as follows： the soluble carrier was PVPk30, insoluble carrier was L-HPC, of which the proportion in solid dispersion was 2 ： 7 and the solvent was dichloromethane, the time of supersonic treating and temperature of water bath were 10 minutes and 80 ℃, respectively. XRD and DSC tests showed the presence of nitrendipine in amorphous form in the solid dispersion. CONCLUSION It is simple, effective and prone to industrialization to prepare nitrendipine solid dispersion using the solvent evaporation-deposition method.