Department of Pharmaceutical Technology and Biopharmacy, Faculty of Science and Engineering, University of Groningen, Groningen, The Netherlands.
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Science and Engineering, University of Groningen, Groningen, The Netherlands.
Int J Pharm. 2018 Sep 5;548(1):325-336. doi: 10.1016/j.ijpharm.2018.07.008. Epub 2018 Jul 2.
In recent years there is an increasing interest in the pulmonary delivery of large cohesive powder doses, i.e. drugs with a low potency such as antibiotics or drugs with a high potency that need a substantial fraction of excipient(s) such as vaccines stabilized in sugar glasses. The pulmonary delivery of high powder doses comes with unique challenges. For low potency drugs, the use of excipients should be minimized to limit the powder mass to be inhaled as much as possible. To achieve this objective the inhaler design should be adapted to the properties of the API in order to achieve a compatible combination of the drug formulation and inhaler device. The inhaler should have an appropriate powder dosing principle for which prefilled compartments seem most appropriate. The drug formulation should not only allow for accurate filling of these compartments but also enable efficient compartment emptying during inhalation. The dispersion principle must have the capacity to disperse considerable amounts of powder in a short time frame that allows the powder to reach the deep lung. Last, but not least, the inhaler should be simple and intuitive in use, be cost-effective and exhibit accurate and consistent, preferably patient independent, pulmonary delivery performance.
近年来，人们对大剂量粘性粉末的肺部给药越来越感兴趣，即那些药效低的药物，如抗生素，或药效高的药物，需要用大量赋形剂（如稳定在糖玻璃中的疫苗）来稳定药物。高剂量粉末的肺部给药带来了独特的挑战。对于低效力的药物，应尽量减少赋形剂的使用，以尽可能减少吸入的粉末质量。为了实现这一目标，吸入器的设计应适应 API 的特性，以实现药物配方和吸入器装置的兼容组合。吸入器应采用适当的粉末给药原理，预填充隔室似乎是最合适的。药物配方不仅应允许准确填充这些隔室，而且在吸入过程中还应能够有效地排空隔室。分散原理必须能够在短时间内分散大量粉末，以使粉末到达肺部深处。最后但同样重要的是，吸入器的使用应简单直观，具有成本效益，并具有准确且一致的、最好是患者独立的肺部输送性能。
