Simonsson Anna, Bramer Tobias, Wimbush Alex, Alderborn Göran
Department of Pharmaceutical Biosciences and the Swedish Drug Delivery Center, Uppsala University, Box 591, SE-751 24 Uppsala, Sweden.
Inhalation Product Development, Pharmaceutical Technology & Development, AstraZeneca Gothenburg, Sweden.
Int J Pharm X. 2025 Jul 17;10:100358. doi: 10.1016/j.ijpx.2025.100358. eCollection 2025 Dec.
The aim of this study was twofold. First, to examine the mechanical properties (packing and flow) of a series of adhesive mixtures, consisting of two different lactose carriers and varying concentrations of budesonide, using a range of test methods. Second, to investigate if any of the test methods correlate with the dispersibility of the mixtures, i.e. the fine particle fraction and mass median aerodynamic diameter. The mechanical properties assessed included packing, shearing, permeability and compressibility. Dispersion data were generated using an impactor operated at two pressure drops (0.5 and 4 kPa). To explore correlations between the mixture properties, Principal Component Analysis and Pearson correlation were used as statistical tools. The different test methods yielded different property-drug load relationships, which can be classified into two groups: First, packing density and shearing properties, and second, permeability and compressibility. The methods in the first group produced markedly fluctuating property-drug load relationships, characterised by two distinct waves. This type of property-drug load relationship was similar to that observed in the dispersion experiments, and significant correlations were found between shearing properties and dispersibility. Thus, any correlations between mechanical and dispersion properties depend on the choice of the test method used. The underlying cause of this co-variation is the parallel effect of both the blend architecture and the structure of the adhesion layer on mechanical and dispersion properties.
本研究有两个目的。其一,使用一系列测试方法,研究由两种不同乳糖载体和不同浓度布地奈德组成的一系列粘合剂混合物的机械性能(堆积和流动性)。其二,研究是否有任何测试方法与混合物的分散性相关,即细颗粒分数和质量中值空气动力学直径。评估的机械性能包括堆积、剪切、渗透性和可压缩性。使用在两种压降(0.5和4 kPa)下运行的冲击器生成分散数据。为了探索混合物性质之间的相关性,主成分分析和皮尔逊相关被用作统计工具。不同的测试方法产生了不同的性质-药物负载关系,可分为两组:第一,堆积密度和剪切性能;第二,渗透性和可压缩性。第一组方法产生的性质-药物负载关系明显波动,其特征是有两个明显的波峰。这种性质-药物负载关系与分散实验中观察到的相似,并且发现剪切性能与分散性之间存在显著相关性。因此,机械性能和分散性能之间的任何相关性取决于所使用的测试方法的选择。这种共变的根本原因是共混物结构和粘附层结构对机械性能和分散性能的平行影响。