【摘要】 不同撞击器尽管设计原理类似，但由于内部结构不同，对相同产品的评价结果常常有差异。本研究尝试探究3种不同撞击器在不同吸气体积下对1种载体型粉雾剂(DPI)体外评价结果的差异及原因，同时讨论3种撞击器在DPI体内外相关性研究中的适用性。以微粉化马来酸氯苯那敏与载体乳糖颗粒的混合物作为处方模型，Breezhaler~?为分散装置；在60 L/min吸气流速下，采用快速筛分撞击器(FSI)、安德森级联撞击器(ACI)和新一代撞击器(NGI)分别在5种吸气体积(0.5、1、2、4和5 L)下对该DPI模型进行体外测试。结果表明，FSI、ACI和NGI能准确评价DPI药物递送表现的吸气体积阈值分别为1、2和2 L。此外，在吸气体积小于2 L的条件下，FSI的评价结果更趋近于制剂处方经Breezhaler~?递送后的实际分散情况，而ACI的评价结果更能表现颗粒分布的全貌。当吸气体积不小于2 L时，NGI得到的微细颗粒沉积总量与FSI基本一致，而与ACI存在较大差异，这可能与ACI固有结构所造成的级间损失有关。本研究为不同撞击器在DPI体外评价和可能的体内外相关性模型建立中的选择和应用提供了参考。更多还原

【Abstract】 Despite cascade impactors have similar design principles, different impactors do not always provide comparable data for the same product in some cases due to their diverse internal structures. This study aimed to investigate the cause of the differences in the results derived from the three different impactors testing a carrier-based dry powder inhaler(DPI) at different sampling inhalation volumes, and discuss the applicability of the three impactors in in vitro-in vivo correlation(IVIVC) studies. The formulation was prepared by mixing micronized chlorpheniramine maleate with coarse lactose carrier particles, and Breezhaler~? was adopted as the inhalation device. The measurement was performed at the flow rate of 60 L/min using fast screening impactor(FSI), Andersen cascade impactor(ACI), and next generation impactor(NGI) at five sampling volumes of 0.5, 1, 2, 4 and 5 L, respectively. The results indicated that the minimum sampling volumes to ensure accurate delivery performance assessment of the DPI by FSI, ACI and NGI were 1, 2 and 2 L,respectively. However, when the sampling volumes were less than 2 L, the FSI provided more reliable results reflecting the real dispersive condition of the formulation delivered by Breezhaler~?, while the ACI presented a relatively complete particle size distribution. When the sampling volumes were no less than 2 L, the fine particle dose(FPD) measured by the NGI was almost the same as that measured by the FSI. Nevertheless, a significant difference in FPD values was observed between the ACI and the other two impactors, which might relate to the considerable interstage losses in the ACI. This study might provide a reference for selecting and applying different impactors in the DPI in vitro evaluation and the possible IVIVC model establishment.更多还原