Heidrich Lara, Abdelkader Ayat, Ornik Jan, Castro-Camus Enrique, Keck Cornelia M, Koch Martin
Department of Physics and Material Sciences Center, Philipps-Universität Marburg, Renthof 5, 35032 Marburg, Germany.
Department of Pharmaceutics and Biopharmaceutics, Philipps-Universität Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.
Pharmaceutics. 2023 Jun 21;15(7):1786. doi: 10.3390/pharmaceutics15071786.
(1) Background: Amorphous drug systems are an intensively studied approach to overcome the insufficient bioavailability of poorly soluble drugs. Here, paper tablets were studied, which were made from cellulose-based paper matrices loaded with norfloxacin. Moreover, wet granulation was introduced as an additional processing step for improving the flowability of the solids, which is necessary when considering production on an industrial scale. (2) Methods: The possible impact of the wet granulation on the crystallinity of norfloxacin was studied by examining granulated and non-granulated samples. Crystallinity investigations were performed using X-ray powder diffraction (XRD) and terahertz time-domain spectroscopy (THz TDS). (3) Results: THz TDS allowed for a more straightforward crystallinity assessment than XRD. Moreover, using THz TDS, it was possible to detect minor changes in the crystallinity of the API after the granulation, whereas this was not possible with the XRD analysis. (4) Conclusions: THz TDS results indicate a partial crystallization of norfloxacin due to the wet granulation. Depending on the formulation, THz TDS can serve as a beneficial and advantageous tool to determine the crystallinity of an API.
（1）背景：无定形药物体系是一种用于克服难溶性药物生物利用度不足的深入研究方法。在此，对由负载诺氟沙星的纤维素基纸质基质制成的素片进行了研究。此外，引入湿法制粒作为额外的加工步骤以改善固体的流动性，这在考虑工业规模生产时是必要的。（2）方法：通过检查制粒和未制粒样品，研究了湿法制粒对诺氟沙星结晶度的可能影响。使用X射线粉末衍射（XRD）和太赫兹时域光谱（THz TDS）进行结晶度研究。（3）结果：与XRD相比，THz TDS能够进行更直接的结晶度评估。此外，使用THz TDS，可以检测到制粒后原料药结晶度的微小变化，而XRD分析则无法做到这一点。（4）结论：THz TDS结果表明由于湿法制粒导致诺氟沙星部分结晶。根据配方不同，THz TDS可作为确定原料药结晶度的有益且有利的工具。
