Haware Rahul V, Shivagari Ramya, Johnson Paul R, Staton Scott, Stagner William C, Gupta Mali Ram
College of Pharmacy & Health Sciences, Campbell University, Buies Creek, North Carolina, 27506.
J Pharm Sci. 2014 May;103(5):1466-77. doi: 10.1002/jps.23920. Epub 2014 Mar 4.
This work distinguishes and quantifies the effects of bovine- and vegetable-derived magnesium stearate (MgSt) molecular and macroscopic properties on lubrication efficiency using multivariate analysis. Principal component analysis (PCA) and partial least-square regression (PLS) were used to evaluate and quantify the lubricant effectiveness on a model tablet formulation. PCA score and loading plots showed a separation of model formulations based on the MgSt sources, which indicated different bovine- and vegetable-derived MgSt lubrication potential. PLS quantified the MgSt molecular [enthalpy of dehydration (ΔHd), enthalpy of melting (ΔHm), percent crystallinity, and moisture content] and macroscopic [particle size (d50 ), specific surface area (SSA-MgSt), and MgSt Hausner ratio (HF-MgSt)] properties, their interactions, and square effects on formulation powder flow and tableting properties relating to MgSt's lubrication effectiveness. For crystalline MgSt, moisture content, HF-MgSt, d50 , and SSA-MgSt showed a major influence on the lubrication efficiency compared with the other MgSt molecular properties (percent crystallinity, ΔHm, and ΔHd). Amorphous MgSt showed poor lubrication, and none of its molecular or macroscopic properties showed significant effects on lubrication efficiency.
本研究通过多变量分析区分并量化了牛源性和植物源性硬脂酸镁（MgSt）的分子及宏观性质对润滑效率的影响。主成分分析（PCA）和偏最小二乘回归（PLS）用于评估和量化模型片剂配方中的润滑剂效果。PCA得分图和载荷图显示，基于MgSt来源，模型配方出现了分离，这表明牛源性和植物源性MgSt具有不同的润滑潜力。PLS量化了MgSt的分子性质[脱水焓（ΔHd）、熔化焓（ΔHm）、结晶度百分比和水分含量]和宏观性质[粒径（d50）、比表面积（SSA-MgSt）和MgSt哈氏比（HF-MgSt）]、它们之间的相互作用以及对与MgSt润滑效果相关的配方粉末流动性和压片性质的平方效应。对于结晶态MgSt，与其他MgSt分子性质（结晶度百分比、ΔHm和ΔHd）相比，水分含量、HF-MgSt、d50和SSA-MgSt对润滑效率有主要影响。非晶态MgSt润滑性较差，其分子或宏观性质对润滑效率均无显著影响。
