Research & Development Headquarters Self-Medication, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshinocho, Kita-ku, Saitama 331-9530, Japan.
Department of Physical Chemistry, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501 Japan.
Int J Pharm. 2020 Apr 15;579:119165. doi: 10.1016/j.ijpharm.2020.119165. Epub 2020 Feb 18.
In this study, we examined the characteristics of glidant that affect the improvement of the flowability of APIs by using the dry surface modification of ibuprofen. In addition, the screening method of glidant suitable for improving flowability of APIs was examined. As a result of evaluation of mixed powder with surface modification using various inorganic fine particles with different physical properties, it became clear that the packing fraction had the most influence regardless of the component. This was thought to able to coat the surface with small quantities because the smaller the packing fraction, the more it was able to dispersed from the less contacts between the glidant particles. The packing fraction of glidant was correlated with the (SE/CBD) which was calculated value from the results measured with powder rheometer. From this results, when using any excipient as a glidant for dry surface modification, it is now possible to estimate the effect of improving flowability simply by measuring with a powder rheometer. Based on this study, it is possible to select excipients suitable for improving APIs flowability and to estimate the improvement effect, and therefore, it is expected to improve the efficiency of prescription design work.
在这项研究中,我们使用布洛芬的干法表面改性来研究影响 API 流变性改善的助流剂特性。此外,还考察了适合改善 API 流变性的助流剂的筛选方法。通过对具有不同物理性质的各种无机细颗粒进行表面改性的混合粉末进行评估,结果表明,无论成分如何,堆积分数的影响最大。这是因为堆积分数越小,助流剂颗粒之间的接触越少,越能分散,所以能够用少量的助流剂进行涂层。助流剂的堆积分数与(SE/CBD)相关,(SE/CBD)是通过粉末流变仪测量结果计算得出的值。根据这些结果,现在可以通过粉末流变仪测量来简单地估计使用任何赋形剂作为助流剂进行干法表面改性对改善流变性的效果。基于这项研究,有可能选择适合改善 API 流变性的赋形剂并估计改善效果,因此,有望提高处方设计工作的效率。