肝能滴丸纳米混悬剂的制备

Preparation of Ganneng Dropping Pill-Nanosuspension

目的制备肝能滴丸(波棱瓜子总木脂素)纳米混悬剂。方法沉淀法制备纳米混悬剂,以15%甘露醇为保护剂进行冻干,滴加二甲基硅油制备滴丸。在单因素试验基础上,以药液温度、滴速、冷凝液温度、滴距为因素,正交试验法优化制备工艺。通过含有量均匀度试验、粒径分析及形态观察,评价所得滴丸的稳定性。结果最佳条件为PEG4000与PEG6000比例4∶5,药物与基质比例1∶9,药液温度90℃,滴速40滴/min,冷凝液温度4℃,滴距9 cm。肝能滴丸纳米混悬剂的含有量均匀度为7.04%,在90 d内粒径无明显变化,形态稳定。结论波棱瓜子总木脂素纳米化后,可有效改善肝能滴丸的稳定性。

AIM To prepare Ganneng Dropping Pills（ total lignans from Herpetospermum caudigerum） into pill-nanosuspension dosage form. METHODS The nanosuspension was prepared by precipitation method and then freeze-dried with 15% mannitol as a lyoprotectant. Dimethicone was added dropwise to prepare the dropping pills. On the basis of single factor test,with reference to a range of parameters of drug fluid temperature,drop rate,condensate liquid temperature and dropping distance,the preparation was optimized by orthogonal test. The evaluation on the stability of obtained dropping pills was by content uniformity test,particle size analysis and morphology observation. RESULTS The optimal conditions were 4 ∶ 5 for ratio of PEG4000 to PEG6000,1 ∶ 9 for ratio of drug to matrix,90 ℃ for drug fluid temperature,40 drops / min for drop rate,4 ℃ for condensate liquid temperature,and 9 cm for dropping distance. The content uniformity of Ganneng Dropping Pills-Nanosuspension was7. 04%,whose particle size showed no obvious change within 90 d,and was morphologically stable. CONCLUSION The stability of Ganneng Dropping Pills can be effectively improved after nanocrystallization of total lignans from Herpetospermum caudigerum.