波棱瓜子木脂素纳米混悬剂的制备

Preparation of nanosuspensions of lignans in Herpetospermum caudigerum seeds

目的制备波棱瓜子木脂素(波棱甲素、波棱素、波棱酮、波棱内酯A)纳米混悬剂。方法微量介质研磨法制备纳米混悬剂,考察研磨速度、研磨介质用量、研磨时间对平均粒径、多分散指数、稳定系数的影响,扫描电镜下观察形态,测定体外溶出度。结果波棱甲素、波棱素、波棱酮、波棱内酯A最佳研磨速度分别为1 000、800、1 000、1 000r/min,研磨介质用量分别为4.0、4.0、5.0、5.0mL,研磨时间分别为2.0、1.0、6.0、6.0h,平均粒径小于300nm,多分散指数小于0.30(波棱甲素除外),稳定系数大于0.80。纳米混悬剂明显提高了波棱甲素、波棱酮体外溶出度。结论该方法简单、稳定、可行,可用于制备波棱瓜子木脂素纳米混悬剂。

AIM To prepare the nanosuspensions of lignans(herpetrione, herpetin, herpetone, herpetolide A) in Herpetospermum caudigerum Wall. seeds. METHODS Miniaturized media milling method was applied to preparing the nanosuspensions. The effects of milling speed, milling media consumption and milling time on average particle size, polydispersity index and stability coefficient were investigated, the micromorphology was observed under scanning electron microscopy, and the in vitro dissolution rate was determined. RESULTS Herpetrione, herpetin, herpetone, herpetolide A demonstrated the optimal milling speeds of 1 000, 800, 1 000, 1 000 r/min, milling media consumption of 4.0, 4.0, 5.0, 5.0 mL, and milling time of 2.0, 1.0, 6.0, 6.0 h, respectively,whose average particle sizes were less than 300 nm, polydispersity indices were less than 0.30(except for herpetrione), stability coefficients were more than 0.80. The nanosuspensions could obviously improve the in vitro dissolution rates of herpetrione and herpetone.CONCLUSION This simple, stable and feasible method can be used for the preparation of nanosuspensions of lignans in H. caudigerum seeds.