Department of Pharmaceutical Biosciences, Uppsala University, Uppsala, Sweden.
Oasmia Pharmaceutical AB, Uppsala, Sweden.
Pharm Dev Technol. 2022 Mar;27(3):319-330. doi: 10.1080/10837450.2022.2051550. Epub 2022 Mar 23.
In this paper, two types of parameters representing tabletability and compactibility profiles of a series of -lactose monohydrate powders, ranging in particle size from approximately 3.5 to 203 µm, are derived and compared. By approximating the tabletability profiles using a three-stage model and the compactibility profiles using the Ryshkewitch-Duckworth equation, two compaction rate parameters and two compaction endpoint parameters were derived. The original median particle diameter had generally a strong effect on the tablet tensile strength and hence the tabletability and compactibility profiles. The experimental profiles were well approximated by the models used, and the compaction parameters were regarded as representative of the experimental profiles. The compaction endpoint parameters increased with decreased particle size and were controlled by the same structural feature as the compacts. The tabletability rate parameter also increased with decreased particle size and correlated well with the tabletability endpoint parameter. The compactibility rate parameter tended to increase with decreased particle size, but the effect was limited; moreover, no general correlation was obtained with the compactibility endpoint parameter. It is concluded that compactibility and tabletability parameters collectively provide a concentrated description of the compaction properties of a powder.
本文推导并比较了两种参数,分别代表一系列粒径范围在 3.5 至 203μm 之间的 -乳糖一水合物粉末的可压性和压缩性特征。通过使用三阶段模型近似可压性特征,以及使用 Ryshkewitch-Duckworth 方程近似压缩性特征,得出了两个压缩速率参数和两个压缩终点参数。原始的中位粒径通常对片剂拉伸强度有很大影响,从而影响可压性和压缩性特征。实验特征曲线与所使用的模型很好地吻合,并且压缩参数被认为是实验特征曲线的代表。压缩终点参数随着粒径的减小而增加,并且受与压块相同的结构特征控制。可压性速率参数也随着粒径的减小而增加,并且与可压性终点参数相关性良好。压缩性速率参数有随着粒径减小而增加的趋势,但效果有限;此外,与压缩终点参数没有得到一般的相关性。结论是,压缩性和可压性参数共同提供了粉末压缩性能的集中描述。