Chvatal A, Szabo B, Szabo-Revesz P, Ambrus R
Acta Pharm Hung. 2016;86(3):75-83.
Based on the formulation method the dry powder inhalers (DPIs) can be divided in too types: carrier-based and carrier-free drug delivery systems. The newest researches report about several high potency carrier-free formulations, where the active ingredient and the excipients are together formulated to the DPI form. However, in Hungary the commercially available DPIs are carrier-based (e.g. lactose), which means that only the mic-onized active ingredient reaches the deeper lungs, the big carrier deposits in the upper airways. The present work is about formulating a high efficacy mannitol-based Pulmonary Drug Delivery System (PDDS), which is able to delivery different types of active ingredients to the deeper lungs with higher deposition rate. The present study involves the physico-chemical and aerodynamical characterisation of mannitol-based PDDS. The results demonstrated the use of the appropriate excipients (leucine, poly-vinyl-alcohol, cyclodextrine) and solvent combination (ethanol-water) during the co-spray drying, increases the inhalation properties of the mannitol. Such carrier systems with optimized properties can increase the aerolization efficacy of the active ingredient.
根据制剂方法,干粉吸入器(DPI)可分为两类:基于载体的和无载体的药物递送系统。最新研究报道了几种高效的无载体制剂,其中活性成分和辅料一起制成DPI形式。然而,在匈牙利,市售的DPI是基于载体的(如乳糖),这意味着只有微粉化的活性成分能到达更深的肺部,大的载体沉积在上呼吸道。目前的工作是关于制备一种高效的基于甘露醇的肺部药物递送系统(PDDS),它能够以更高的沉积率将不同类型的活性成分递送至更深的肺部。本研究涉及基于甘露醇的PDDS的物理化学和空气动力学特性。结果表明,在共喷雾干燥过程中使用适当辅料(亮氨酸、聚乙烯醇、环糊精)和溶剂组合(乙醇-水),可提高甘露醇的吸入性能。这种具有优化性能的载体系统可提高活性成分的雾化效率。