尼莫地平固体分散体的制备及其理化性质表征

Preparation and Characterization of Nimodipine Solid Dispersion

目的考察不同载体材料经双螺杆热熔挤出技术制备尼莫地平固体分散体的工艺参数、理化性质、增溶效果以及物理稳定性。方法以共聚维酮和3个规格(L、M和H)的醋酸羟丙甲纤维素琥珀酸酯作为载体材料,使用双螺杆热熔挤出机制备尼莫地平固体分散体。使用偏光显微镜、差示热扫描量热分析和粉末衍射考察制得固体分散体的理化性质,使用原位光纤技术测定固体分散体的动力溶解度,并考察固体分散体的物理稳定性。结果以共聚维酮为载体材料更容易进行热熔挤出操作,挤出过程螺杆扭矩值<30%,口模内熔体压力<15bar;制得的固体分散体易于粉碎;过饱和度达到6 000μg·mL^(-1),且溶解迅速;同时在2个月加速条件下保持稳定。结论共聚维酮更适合用做热熔挤出制备尼莫地平固体分散体的载体材料。

OBJECTIVE To investigate the performance of different polymers in the preparation of Nimodipine amorphous solid dispersion prepared by hot melt extrusion.METHODS Copovidone and hydroxypropyl methylcellulose acetate succinate (L,M and H grade) were selected as the carrier polymers to prepare nimodipine solid dispersions by hot melt extrusion.Polarized light microscopy,differential scanning calorimetry and powder diffraction were used to test the physiochemical properties,in-situ optical fiber was used to test the dynamics solubility of prepared solid dispersions,the stability test was also studied.RESULTS Copovidone was easier to extruded,the torque value of screw was <30% and the die pressure was <15 bar; the prepared solid dispersion was easier to be crushed,supersaturation reached 6 000 μg·mL^-1 and dissolved quickly,and had good stability in 2 months stress test.CONCLUSION Copovidone is more appropriate for the preparation of nimodipine solid dispersion by hot melt extrusion.