Pharmacy and Pharmaceutical Sciences, School of Applied Sciences, University of Huddersfield, Huddersfield HD1 3DH, UK.
Int J Pharm. 2013 Dec 15;458(1):118-27. doi: 10.1016/j.ijpharm.2013.10.004. Epub 2013 Oct 17.
Salt formation is an effective method of improving physicochemical properties of acidic and basic drugs. The selection of a salt form most suitable for drug development requires a well-designed screening strategy to ensure various issues are addressed in the early development stages. Triboelectrification of pharmaceutical powders may cause problems during processing such as segregation of components due to the effects of particle adhesion. However, very little work has been done on the effect of salt formation on triboelectrification properties. In this paper, salts of flurbiprofen were prepared by combining the drug with a selection of closely related amine counter ions. The aim of the work was to investigate the impact of the counter ion on electrostatic charge of the resultant salts to inform the salt selection process. The experimental results show the magnitude of charge and polarity of the flurbiprofen salts to be highly dependent on the type of counter ion selected for the salt formation. Furthermore, particle adhesion to the stainless steel surface of the shaking container and the salts' compression properties were measured. The formed salts had lower electrostatic charges, improved tabletability, and resulted in reduced adhesion of these powders compared with the parent drug.
盐形成是改善酸性和碱性药物理化性质的有效方法。选择最适合药物开发的盐形式需要精心设计的筛选策略,以确保在早期开发阶段解决各种问题。医药粉末的静电现象可能会导致在处理过程中出现问题,例如由于颗粒粘附的影响导致成分分离。然而,对于盐形成对静电现象特性的影响,研究工作很少。在本文中,通过将药物与一系列密切相关的胺抗衡离子结合,制备了氟比洛芬盐。这项工作的目的是研究抗衡离子对所得盐的静电荷的影响,为盐的选择过程提供信息。实验结果表明,氟比洛芬盐的电荷量和极性大小高度取决于用于盐形成的抗衡离子的类型。此外,还测量了对不锈钢容器表面的颗粒粘附以及盐的压缩特性。与母体药物相比,形成的盐具有较低的静电荷,可改善可压性,并减少这些粉末的粘附。