冬凌草甲素粉雾剂的制备及其对大鼠急性肺损伤的治疗

Preparation of oridonin dry powder for inhalation and its therapeutic effect on acute lung injury of rats

目的制备冬凌草甲素粉雾剂并考察其治疗大鼠急性肺损伤的疗效。方法沉淀法制备冬凌草甲素纳米混悬剂。筛选葡萄糖、蔗糖、乳糖和甘露醇4种保护剂,经冷冻干燥制成粉雾剂。盐酸吸入制备大鼠急性肺损伤模型,考察冬凌草甲素粉雾剂对急性肺损伤的疗效。结果冬凌草甲素纳米混悬剂粒径约100 nm,多分散系数为0.115,分布均匀。甘露醇为保护剂,经冷冻干燥制备得到流动性较好的冬凌草甲素粉雾剂。粉雾剂的有效部位沉积率可达31.55%。肺组织解剖和病理学结果显示冬凌草甲素粉雾剂对大鼠急性肺损伤的疗效显著。结论冬凌草甲素粉雾剂有望用于急性肺损伤的治疗。

Objective To prepare the dry powder of oridonin for inhalation and to investigate its pharmacodynamies on rat a- cute lung injury（ALI）. Methods Oridonin nanosuspensions were prepared using the precipitation method, and then freeze-dried to obtain the dry powder with glucose, sucrose, lactose or mannitol as the lyophilization protectants. The rat ALI model was established by inhaling hydrochloric acid. The therapeutic effect of oridonin was explored on the model. Results The oridonin nanosuspensions were small to 100 nm in size and the polydispersing index was 0. 115. The fluidity, containing mannitol was good and the deposition rate in effective parts of the dry powder was 31.55%. The therapeutic effect of oridonin dry powder on the ALI model was good according to the anatomy and pathology. Conclusion Oridonin dry powder might be a promising formulation for the treatment of ALI.