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目的制备干扰素α-2b(IFNα-2b)干粉吸入剂,并评价其体外性质以及大鼠体内的药动学性质。方法冷冻干燥并研磨后制备IFNα-2b干粉吸入剂,同时考察了IFNα-2b干粉吸入剂的形态、粒径、吸湿性、排空率及雾粒分布,并以细胞病变抑制法(CPE法)测定了干粉吸入剂中IFNα-2b的效价及活性保持率。此外,还以皮下注射IFNα-2b溶液为对照,考察了IFNα-2b干粉吸入剂在大鼠体内的药动学性质。结果IFNα-2b干粉吸入剂形态为近圆形,粒径为6.78μm,敲击密度为0.35g·mL-1,排空率为95.16%,吸湿率为5.80%,雾粒分布实验中一级和二级瓶中的分布总量为58.32%,干粉吸入剂中IFNα-2b的活性保持率为99.58%;IFNα-2b干粉吸入剂在大鼠体内cmax有所降低,tmax有所减小,相对生物利用度为46.76%;结论本实验所制备的IFNα-2b干粉吸入剂体外各项指标均符合要求,IFNα-2b的活性损失小,而且体内生物利用度高。
Objective To prepare an interferon α-2b (IFNα-2b) dry powder inhaler and evaluate its in vitro properties and pharmacokinetic properties in rats. Methods IFNα-2b dry powder inhalers were prepared by freeze-drying and grinding. Meanwhile, the morphology, particle size, hygroscopicity, emptying rate and fog particle distribution of IFNα-2b dry powder inhalers were investigated. The cytopathic effect (CPE) The potency and activity retention of IFNα-2b in dry powder inhalers were determined. In addition, the IFNα-2b solution was also injected subcutaneously as a control to investigate the pharmacokinetics of IFNα-2b dry powder inhaler in rats. Results The morphology of the inhaled IFNα-2b powder was nearly round with a particle size of 6.78μm, a tap density of 0.35g · mL-1, an emptying rate of 95.16% and a moisture absorption rate of 5.80% And the total amount of two-stage flask distribution was 58.32%, the activity of IFNα-2b in dry powder inhaler was maintained at 99.58%; the cmax of IFNα-2b dry powder inhaler decreased in rats, tmax decreased, The bioavailability was 46.76%. CONCLUSION The IFNα-2b dry powder inhaler prepared in this study meets the requirements in vitro. The activity of IFNα-2b is low, and its bioavailability in vivo is high.