Department of Pharmaceutics and Biopharmaceutics, Christian Albrecht University, Gutenbergstrasse 76, Kiel, Germany.
Eur J Pharm Biopharm. 2012 Oct;82(2):417-23. doi: 10.1016/j.ejpb.2012.07.018. Epub 2012 Aug 9.
Dry powder inhalers play a major role in today's treatment of various respiratory diseases. A lot of effort has been put into the optimization of a device and the appropriate formulation regarding its local lung deposition. However, the complexity and interactions of different factors governing powder dispersion and, therefore, its inhalable fraction challenge research groups around the world. In the current work, binary lactose blends and adhesive ternary powder mixtures containing additional budesonide fines were produced and analyzed with dispersion measurements on the one hand and permeability and aeration measurements conducted with a powder rheometer on the other hand. By comparing the results of the bulk property and dispersion tests, it was expected to gain a better understanding about the effect of excipient fines addition to an adhesive powder mixture. It could be observed that with permeability testing it was possible to clearly differentiate between different amounts of fines within mixtures. However, no correlation between permeability or aeration test values and drug fine particle fraction could be determined for the observed range. Nevertheless, the use of different characterization techniques led to a clearer understanding about the influence of fines addition to an adhesive mixture. It could be demonstrated that after the surface of carrier crystals had been fully saturated, drug particles got incorporated in more stable fines' agglomerates, which resulted in a decrease in fine particle fraction upon dispersion.
干粉吸入器在当今治疗各种呼吸道疾病方面发挥着重要作用。人们在设备优化和适当制剂方面付出了大量努力，以提高其肺部局部沉积率。然而，控制粉末分散的各种因素的复杂性和相互作用，以及由此产生的可吸入部分，给世界各地的研究小组带来了挑战。在当前的工作中，生产了含有额外布地奈德细粉的二元乳糖混合物和粘性三元粉末混合物，并通过分散测量一方面和使用粉末流变法进行的渗透性和通气性测量另一方面进行了分析。通过比较体积性质和分散测试的结果，希望能够更好地了解赋形剂细粉添加到粘性粉末混合物中的影响。可以观察到，通过渗透性测试，可以清楚地区分混合物中不同量的细粉。然而，对于观察到的范围，无法确定渗透性或通气性测试值与药物细颗粒分数之间的相关性。尽管如此，使用不同的表征技术可以更清楚地了解赋形剂细粉添加到粘性混合物中的影响。可以证明，在载体晶体的表面完全饱和后，药物颗粒被纳入更稳定的细粉团聚体中，这导致分散后细颗粒分数降低。
