非洛地平纳米混悬液固化方法的考察

Investigation of Two Kinds of Solidification Methods for Felodipine Nanosuspension: Flocculation Versus Lyophilization

目的非洛地平纳米混悬液存在物理不稳定性,本实验旨在采用固化方法提高其物理稳定性。方法分别采用絮凝法和冷冻干燥法对非洛地平纳米混悬液进行固化。结果非洛地平纳米混悬液的平均粒径为151 nm,呈单峰分布。絮凝后仅有76.7%小于1μm,且呈三峰分布;以20%甘露醇-甘氨酸(1∶1,W/W)组对混悬剂的保护作用冻干效果最好,平均粒径在375 nm左右的粒子占80%左右,其余粒径更小。结论选择冷冻干燥法固化非洛地平纳米混悬液,并且采用20%的甘露醇-甘氨酸(1∶1,W/W)溶液为保护剂时,冻干效果最好。

OBJECTIVE To solve the stability problem of felodipine nanosuspension which is a physically unstable colloidal dispersion by solidification method. METHODS Two different methods, flocculation and lyophilization, were applied to solidi- fy the felodipine nanosuspension. RESULTS The mean particle size of the felodipine nanosuspension was 151 nm and was uni- modally distributed, but only 76.7% particulates were smaller than 1 p,m following flocculation. For lyophilization, it was shown that 20% （W/V） of mannitol-glycine （ 1 ： 1, W/W） could stabilize the colloidal system best. CONCLUSION Lyophilization is considered to be superior to flocculation in the aspects of redispersed particle size, and 20% （W/V） of mannitol-glycine （ 1 ： I , W/W） is selected as the optimal cryoproteetant.