Department of Chemical and Biological Engineering, University of Saskatchewan, Saskatoon, SK, Canada.
Department of Biomedical Engineering, University of Saskatchewan, Saskatoon, SK, Canada.
Int J Pharm. 2024 Nov 15;665:124664. doi: 10.1016/j.ijpharm.2024.124664. Epub 2024 Sep 12.
Drying time, velocity, and temperature are important aspects of the drying process for pharmaceutical granules observed during tablet manufacturing. However, the drying mechanism of single granules is often limited to modelling and simulation, with the internal and physical changes difficult to quantify at an experimental level. In this study, in-situ synchrotron-based X-ray imaging techniques were used for the first time to investigate the dynamic drying of single pharmaceutical granules, quantifying internal changes occurring over the drying time. Two commonly used excipients (lactose monohydrate (LMH) and microcrystalline cellulose (MCC)) were used as pure components and binary mixtures with one of either two active pharmaceutical ingredients of differing hydrophilicity/hydrophobicity (acetaminophen (APAP) and carbamazepine (CBZ)). Water was used as a liquid binder to generate single granules of 25 % to 30 % moisture content. Results showed that for most samples, the drying time and composition significantly influences the pore volume evolution and the moisture ratio, with the velocity and temperature of the drying air possessing mixed significance on increasing the rate of pore connectivity and moisture removal depending on the sample composition. Effects of active ingredient loading resulted in minimal influence on the drying of CBZ and generated binary mixtures, with APAP and its respective mixtures' drying behaviour dominated by the material's hydrophilic nature.
干燥时间、速度和温度是制药颗粒在片剂制造过程中干燥过程的重要方面。然而,单个颗粒的干燥机制通常仅限于建模和模拟,内部和物理变化难以在实验水平上量化。在这项研究中,首次使用基于同步加速器的原位 X 射线成像技术研究了单个药物颗粒的动态干燥,定量了干燥过程中发生的内部变化。使用了两种常用的赋形剂(一水乳糖(LMH)和微晶纤维素(MCC))作为纯成分和两种具有不同亲水性/疏水性的活性药物成分(对乙酰氨基酚(APAP)和卡马西平(CBZ))的混合物。水被用作液体粘合剂,以生成水分含量为 25%至 30%的单个颗粒。结果表明,对于大多数样品,干燥时间和组成显著影响孔体积演化和水分比,干燥空气的速度和温度对增加孔连通率和水分去除率的影响因样品组成而异。活性成分负载的影响对 CBZ 的干燥和生成的二元混合物的影响最小,APAP 及其各自混合物的干燥行为主要由材料的亲水性决定。