Kaialy Waseem
School of Pharmacy, Faculty of Science and Engineering, University of Wolverhampton, Wolverhampton WV1 1LY, UK.
Int J Pharm. 2016 Apr 30;503(1-2):262-76. doi: 10.1016/j.ijpharm.2016.01.076. Epub 2016 Feb 2.
Pharmaceutical powders are typically insulators consisting of relatively small particles and thus they usually exhibit significant electrostatic charging behaviours. In the inhalation field, the measurement of electrostatic charge is an imperative stage during pharmaceutical formulation development. The electrostatic charge is affected by the interplay of many factors. This article reviews the factors affecting the electrostatic charging of pharmaceutical powders with a focus on dry powder inhalations. The influences of particle resistivity, size distribution, shape distribution, surface roughness, polymorphic form and hygroscopicity, as well as the effects of moisture uptake, environmental conditions, pharmaceutical processing (i.e., milling, sieving, spray drying and blending), and storage on the electrostatic charge behaviours of pharmaceuticals, with focus on inhalation powders, were reviewed. The influence of electrostatic charge on the performance of dry powder inhaler formulations in terms of drug content homogeneity, the passage of drug through the inhaler device, drug-carrier adhesion/detachment, and drug deposition on the respiratory airways were discussed. The understanding gained is crucial to improving the safety, quality, and efficiency of the pharmaceutical inhalation products.
药用粉末通常是由相对较小颗粒组成的绝缘体,因此它们通常表现出显著的静电充电行为。在吸入领域,静电电荷的测量是药物制剂研发过程中必不可少的阶段。静电电荷受到多种因素相互作用的影响。本文综述了影响药用粉末静电充电的因素,重点关注干粉吸入剂。综述了颗粒电阻率、粒径分布、形状分布、表面粗糙度、多晶型和吸湿性等因素,以及吸湿、环境条件、药物加工(即研磨、筛分、喷雾干燥和混合)和储存对药物静电充电行为的影响,重点是吸入粉末。讨论了静电电荷对干粉吸入剂制剂性能的影响,包括药物含量均匀性、药物通过吸入装置的情况、药物与载体的粘附/分离以及药物在呼吸道的沉积。所获得的认识对于提高药物吸入产品的安全性、质量和效率至关重要。