Understanding the role of magnesium stearate in lowering punch sticking propensity of drugs during compression
Understanding the role of magnesium stearate in lowering punch sticking propensity of drugs during compression
复制标题
了解硬脂酸镁在降低压缩过程中药物冲头粘连倾向方面的作用
DOI：
10.1016/j.ijpharm.2023.123016
复制
发表时间：
2023
影响因子：
5.8
通讯作者：
Sun, Changquan Calvin
中科院分区：
文献类型：
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作者：
Gunawardana, Chamara A.;Kong, Angela;Wanapun, Debbie;Blackwood, Daniel O.;Travis Powell, C.;Krzyzaniak, Joseph F.;Thomas, Myles C.;Kresevic, John E.;Sun, Changquan Calvin
活性药物成分 (API) 粘附在压实工具的表面上（通常称为冲孔粘附）会导致商业片剂制造中代价高昂的停机或产品故障。硬脂酸镁 (MgSt) 是一种常见的片剂润滑剂，已知可以改善粘连问题，但也存在例外情况。 MgSt 通过覆盖 API 表面来降低冲头粘着倾向 (PSP) 的机制是合理的，但尚未经过实验证明。这项工作旨在阐明 PSP 和 MgSt 片剂表面积覆盖率 (SAC) 之间的联系，与一些关键配方特性和工艺参数（即 MgSt 浓度、API 负载量、API 粒径和混合条件）相关。该研究使用两种已知高 PSP 的模型 API：tafamidis (TAF) 和 ertugliflozin-pyroglutamic Acid (ERT)。结果表明，随着 MgSt SAC 的增加，PSP 呈指数下降。还探索了粘在冲头表面的材料成分，以更好地了解冲头粘连的开始以及可能的 MgSt 影响的冲头调节事件的影响。
The sticking of active pharmaceutical ingredient (API) to the surfaces of compaction tooling, frequently referred to as punch sticking, causes costly downtime or product failures in commercial tablet manufacturing. Magnesium stearate (MgSt) is a common tablet lubricant known to ameliorate the sticking problem, even though there exist exceptions. The mechanism by which MgSt lowers punch sticking propensity (PSP) by covering API surface is sensible but not yet experimentally proven. This work was aimed at elucidating the link between PSP and surface area coverage (SAC) of tablets by MgSt, in relation to some key formulation properties and process parameters, namely MgSt concentration, API loading, API particle size, and mixing conditions. The study was conducted using two model APIs with known high PSPs, tafamidis (TAF) and ertugliflozin-pyroglutamic acid (ERT). Results showed that PSP decreases exponentially with increasing SAC by MgSt. The composition of material stuck to punch face was also explored to better understand the onset of punch sticking and the impact of possible MgSt-effected punch conditioning event.