Faculty of Pharmaceutical Sciences, Toho University.
Pharmaceutical Technology Development Department, Nippon Chemiphar Co., Ltd.
Chem Pharm Bull (Tokyo). 2024;72(9):817-825. doi: 10.1248/cpb.c24-00303.
The triboelectric properties of active pharmaceutical ingredients (APIs) contribute to problems during the manufacturing of pharmaceuticals. However, the triboelectric properties of APIs have not been comprehensively characterized. In this study, the effect of salt formulation on the triboelectric properties of APIs was investigated. The triboelectric properties of three groups of amines, namely tertiary amines, purine bases, and amino acids, and their hydrochlorides were evaluated using a suction-type Faraday cage meter. Most of the hydrochloride salts exhibited more negative charges than the corresponding free bases, and the degree by which the triboelectric property changed upon hydrochlorination depended on the structural groups of the compounds. In the case of tertiary amines, the change in the zero-charge margin upon hydrochlorination was negatively correlated with the zero-charge margin of the free base. In contrast, hydrochlorination of the amino acids led to a significant change in the zero-charge margin. In most cases, salt formation also affected the triboelectric properties of API powders. Controlling the triboelectric properties of APIs solves various problems caused by the electrification of raw material powders and granules during the production of pharmaceuticals, thereby increasing the quality of produced pharmaceuticals.
活性药物成分（APIs）的摩擦带电特性会导致药物制造过程中的问题。然而，API 的摩擦带电特性尚未得到全面的表征。在这项研究中，研究了盐形式对 API 摩擦带电特性的影响。使用抽吸式法拉第笼仪评估了三组胺类物质（叔胺、嘌呤碱基和氨基酸）及其盐酸盐的摩擦带电特性。大多数盐酸盐表现出比相应游离碱更负的电荷，并且氯化对摩擦带电性质的改变程度取决于化合物的结构基团。对于叔胺，氯化时零电荷间隙的变化与游离碱的零电荷间隙呈负相关。相比之下，氨基酸的氯化会导致零电荷间隙发生显著变化。在大多数情况下，盐形成也会影响 API 粉末的摩擦带电特性。控制 API 的摩擦带电特性可以解决原料药粉末和颗粒在药物生产过程中因带电而产生的各种问题，从而提高所生产药物的质量。
