Powder flow analysis: A simple method to indicate the ideal amount of lactose fines in dry powder inhaler formulations
Powder flow analysis: A simple method to indicate the ideal amount of lactose fines in dry powder inhaler formulations
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DOI：
10.1016/j.ijpharm.2017.10.052
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发表时间：
2018-01-15
影响因子：
5.8
通讯作者：
Scherliess, Regina
中科院分区：
文献类型：
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作者：
Hertel, Mats;Schwarz, Eugen;Scherliess, Regina
许多努力已经作出了在过去，以了解乳糖粉作为一个三元组分给予载体型干粉吸入器配方的功能。毫无疑问，细粉可以显著提高此类配方的性能，但选择适量的细粉是关键，因为浓度过高会对分散性能产生负面影响。本研究的目的是用一种简单的测试方法来确定最佳的细粉浓度。为此，用高剪切混合器制备了硫酸沙丁胺醇和两种不同乳糖载体的混合物，用FT4粉末流变仪进行了测量，并用两种不同的吸入器装置测试了细颗粒的输送。用曝气试验装置测定的流化能与细颗粒分数（FPF）之间存在相关性。这也适用于曝气比，以及粉末样品的渗透性。此外，无药混合物的流变学性质与含有活性药物成分（API）的混合物几乎没有差异，这表明该方法可以适用于节省成本的筛选试验。此外，解释细粒功能的重要方面，如活性位点的饱和、团聚体的形成和流化能量的增加，可以在本研究中得到证明。
Many efforts have been made in the past to understand the function of lactose fines which are given as a ternary component to carrier-based dry powder inhaler formulations. It is undisputed that fines can significantly improve the performance of such formulations, but choosing the right amount of fines is a crucial point, because too high concentrations can have negative effects on the dispersion performance. The aim of this study was to indicate the optimal concentration of fines with a simple test method. For this purpose, mixtures with salbutamol sulfate and two different lactose carriers were prepared with a high shear mixer, measured with a FT4 powder rheometer and tested for fine particle delivery with two different inhaler devices. A correlation between the fluidization energy, measured with the aeration test set up, and the fine particle fractions (FPF) could be proven. This also applied for the aeration ratio, as well as the permeability of the powder samples. In addition, drug-free mixtures hardly differed in their rheological properties from mixtures containing the active pharmaceutical ingredient (API), which indicates that the method could be suitable for cost-saving screening trials. Furthermore, important aspects that explain the function of fines, such as the saturation of active sites, the formation of agglomerates and an increase in fluidization energy, could be shown in this study.