Division of Pharmaceutical Technology, University of Hamburg, Bundesstr. 45, 20146 Hamburg, Germany.
Division of Pharmaceutical Technology, University of Hamburg, Bundesstr. 45, 20146 Hamburg, Germany.
Eur J Pharm Biopharm. 2018 Jul;128:107-118. doi: 10.1016/j.ejpb.2018.04.004. Epub 2018 Apr 7.
In the present study, the sticking tendencies of ibuprofen and ibuprofen sodium dihydrate as model substances for a lipophilic and a hydrophilic sticky API to differently coated punches were investigated. Increased sticking was observed with the more polar ibuprofen sodium dihydrate than with the less polar ibuprofen. Interestingly, the anti-sticking performance of the punch coatings proved to be independent of the APIs' polarity. To understand this phenomenon, key properties of the punches were investigated. The AFM adhesive forces of both APIs to the differently coated punches as well as the surface free energies and the surface texture of these punches were determined. Separately evaluating these properties revealed only a partial correlation with the sticking observed during tableting. Consistent results with the tableting data could only be achieved if evaluating the surface texture in context with the chemical composition of the respective punch surfaces. It was concluded that each punch tip coating represents an entirely different system, which were described in detail as a result of the performed investigations. Particularly, chromium nitride-coated punches resulted in excellent anti-sticking performances because of a low chemical interaction with the APIs combined with a smooth and homogeneous surface texture.
在本研究中,以布洛芬和布洛芬二水合物为模型物质,考察了亲脂性和亲水性粘性 API 对不同涂层冲头的粘附倾向。与非极性布洛芬相比,极性更强的布洛芬二水合物表现出更强的粘附性。有趣的是,冲头涂层的抗粘性性能与 API 的极性无关。为了理解这一现象,研究了冲头的关键性质。确定了两种 API 对不同涂层冲头的 AFM 粘附力,以及这些冲头的表面自由能和表面纹理。单独评估这些性质仅与压片过程中的粘附观察到部分相关。只有在将表面纹理与相应冲头表面的化学成分结合起来进行评估时,才能得到与压片数据一致的结果。结论是,每个冲头尖端涂层代表一个完全不同的系统,由于进行了详细的研究,因此对其进行了详细描述。特别是,氮化铬涂层冲头由于与 API 之间的化学相互作用低,再加上表面光滑且均匀,因此表现出出色的抗粘性。