DFE Pharma, Kleverstrasse 187, 47568 Goch, Germany.
DFE Pharma, Kleverstrasse 187, 47568 Goch, Germany.
Adv Drug Deliv Rev. 2022 Oct;189:114527. doi: 10.1016/j.addr.2022.114527. Epub 2022 Sep 5.
Lactose is the most commonly used excipient in carrier-based dry powder inhalation (DPI) formulations. Numerous inhalation therapies have been developed using lactose as a carrier material. Several theories have described the role of carriers in DPI formulations. Although these theories are valuable, each DPI formulation is unique and are not described by any single theory. For each new formulation, a specific development trajectory is required, and the versatility of lactose can be exploited to optimize each formulation. In this review, recent developments in lactose-based DPI formulations are discussed. The effects of varying the material properties of lactose carrier particles, such as particle size, shape, and morphology are reviewed. Owing to the complex interactions between the particles in a formulation, processing adhesive mixtures of lactose with the active ingredient is crucial. Therefore, blending and filling processes for DPI formulations are also reviewed. While the role of ternary agents, such as magnesium stearate, has increased, lactose remains the excipient of choice in carrier-based DPI formulations. Therefore, new developments in lactose-based DPI formulations are crucial in the optimization of inhalable medicine performance.
乳糖是载体型干粉吸入剂（DPI）制剂中最常用的赋形剂。已经开发了许多使用乳糖作为载体材料的吸入疗法。有几种理论描述了载体在 DPI 制剂中的作用。尽管这些理论很有价值，但每个 DPI 制剂都是独特的，不能用任何单一理论来描述。对于每种新制剂，都需要特定的开发轨迹，并且可以利用乳糖的多功能性来优化每个制剂。在本文综述中，讨论了基于乳糖的 DPI 制剂的最新发展。综述了改变乳糖载体颗粒的材料特性（如粒径、形状和形态）的影响。由于制剂中颗粒之间的复杂相互作用，用活性成分对乳糖进行粘合混合处理至关重要。因此，还综述了 DPI 制剂的混合和填充工艺。尽管像硬脂酸镁这样的三元试剂的作用增加了，但乳糖仍然是载体型 DPI 制剂中首选的赋形剂。因此，基于乳糖的 DPI 制剂的新发展对于优化可吸入药物的性能至关重要。
