Tofiq Maryam, Alderborn Göran, Nordström Josefina, Persson Ann-Sofie
Department of Pharmaceutical Biosciences and the Swedish Drug Delivery Center (SweDeliver), Uppsala University, Box 591, SE-751 24 Uppsala, Sweden.
Int J Pharm X. 2025 Jul 2;10:100351. doi: 10.1016/j.ijpx.2025.100351. eCollection 2025 Dec.
Mini-tablets of different proportions of -lactose monohydrate (LAC) and microcrystalline cellulose (MCC) were prepared by uniaxial compaction and served as surrogate granules. The inverted Adams coefficient i.e., was derived from bulk mini-tablet compression data and used as an indication of granule plastic deformation. The correlation of the parameter to single granule deformability assessed from uniaxial single mini-tablet compression and macro-indentation hardness was investigated. Furthermore, the relationship between the plastic deformation parameters and the tabletability of mini-tablets were evaluated. An increased MCC concentration resulted in an increased indentation hardness and deformability of the mini-tablets, but no correlation was found between indentation hardness and the coefficient. Thus, the plastic deformation expressed during powder compression showed no relationship to the single specimen indentation hardness and plastic deformability. An increased indentation hardness tended to correspond to an increased tablet tensile strength, while the opposite applied for the coefficient. The trend of increased tablet tensile strength with higher MCC concentration was broken at the highest MCC concentration, i.e., for mini-tablets showing very limited fragmentation. It was concluded that granule plastic deformation is a key property for granule tabletability. It is suggested that granule plastic deformation should be assessed during granule engineering.
通过单轴压制制备了不同比例的一水乳糖（LAC）和微晶纤维素（MCC）的微型片剂，并将其用作替代颗粒。倒置亚当斯系数，即 ，由块状微型片剂压缩数据得出，并用作颗粒塑性变形的指标。研究了该参数与通过单轴单微型片剂压缩和宏观压痕硬度评估的单个颗粒可变形性之间的相关性。此外，还评估了塑性变形参数与微型片剂可压性之间的关系。MCC浓度的增加导致微型片剂的压痕硬度和可变形性增加，但未发现压痕硬度与 系数之间存在相关性。因此，粉末压制过程中表现出的塑性变形与单个试样的压痕硬度和塑性可变形性无关。压痕硬度的增加往往对应于片剂抗张强度的增加，而 系数则相反。在最高MCC浓度下，即对于显示出非常有限破碎的微型片剂，随着MCC浓度升高片剂抗张强度增加的趋势被打破。得出的结论是，颗粒塑性变形是颗粒可压性的关键特性。建议在颗粒工程过程中评估颗粒塑性变形。
