驱动器的规格与吸入辅助装置对气雾剂体外沉积性质的影响

摘要

目的 考察驱动器的规格——孔径、孔长以及吸入辅助装置的使用对气雾剂体外沉积性质的影响.方法 以自制丙酸氟替卡松混悬型气雾剂为模型药物,装配不同规格的驱动器,使用Andersen多级撞击器(Andersen cascade impactor,ACI)测定体外沉积率;将丙酸氟替卡松气雾剂装配筛选好的特定规格的驱动器,分别在不使用吸入辅助装置与使用吸入辅助装置的情况下,对体外沉积性质进行对比研究.结果 在孔径固定的情况下,随着孔长的延长,驱动器的残留量降低,Andersen多级撞击器装置的L型连接管沉积量增加,微细粒子剂量降低.在孔长固定的情况下,随着孔径的增加,驱动器的残留量降低,Andersen多级撞击器装置的L型连接管沉积量增加,微细粒子剂量降低.根据试验结果、混悬型气雾剂本身的剂型特点以及驱动器的实际使用情况,最终,将0.42 mm孔径、0.70 mm孔长的驱动器作为优选驱动器;在使用吸入辅助装置的情况下,Andersen多级撞击器装置L型连接管的沉积量极大地降低,微细粒子剂量增加,原来沉积在L型连接管的大粒子很大一部分被截留在吸入辅助装置当中.结论 驱动器的规格会对吸入气雾剂的体外沉积产生一定的影响,在药品研发的过程中,可根据气雾剂产品的具体特点(溶液型或混悬型,原料药的粒径大小等)进行驱动器的筛选;吸入辅助装置的使用可以提高气雾剂的药物利用率,推荐患者用药时使用.%Objective To investigate effects of actuator dimensions(the aperture and the hole length)and add-on devices for inhalation on the deposition of metered dose inhaler in vitro.Methods Self-made metered dose inhalers(MDI) of fluticasone propionate were selected as the model drug,and then assembled different dimensions of actuators.The deposition of metered dose inhaler in vitro was determined by Andersen cascade impactor(ACI).Fluticasone propionate aerosols were loaded on specific actuator.Thus,a comparative study was conducted in vitro deposition with and without add-on devices.Results When the value of aperture was fixed,increasing the hole length could reduce the amount of residue in the actuator and increase the drug deposited in the L type connection tube.Moreover,the deposition of fine particle distribution decreased slightly.Likewise,when the value of the hole length was fixed,increasing the diameter could reduce the amount of residue in the actuator and increase the amount of drug deposited in the L type connection tube.At the same time,the value of fine particle distribution was decreased.According to the experiment results,the characteristic of suspension aerosol and the actual use,actuator of 0.42 mm aperture and 0.70 mm hole length can be chosen as the priority.Add-on device can hold back the big particle,thus the drug deposition in the L type connection tube was greatly reduced,and the value of fine particle distribution is increased.Conclusion Actuator dimensions can affect the deposition of metered dose inhaler in vitro.According to the specific characteristics of aerosol products(solution or suspension,raw material particle size),actuators can be chosen in the drug research.The use of add-on devices can improve the drug utilization of aerosol,and it was recommend that patients use the add-on devices for inhalation.