GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy and Pharmaceutical Sciences, National University of Singapore, 18 Science Drive 4, Singapore, 117543, Singapore.
Airlangga University, Kampus C Mulyorejo, Surabaya, 60115, Indonesia.
AAPS PharmSciTech. 2024 Nov 5;25(8):262. doi: 10.1208/s12249-024-02980-x.
Magnesium stearate (MgSt) is a common tablet lubricant. As variations in MgSt properties are known to influence tablet attributes, the impact of MgSt fatty acid composition, particularly the significance of the stearate and palmitate contents, and its effects on tablet properties warrant further investigation. This study investigated the effect of MgSt with different stearate and palmitate contents but comparable physical properties (e.g. particle size, crystallinity, specific surface area and morphology) on lubrication performance and resulting tablet quality attributes, including mechanical strength, disintegratability and drug release. The influence of MgSt concentration and blending duration on the resulting tablet properties was also examined. Tablets produced using the lower stearate content MgSt had slightly higher tensile strength. The effect of MgSt stearate content was more apparent in the disintegration time and drug release, whereby MgSt of lower stearate content resulted in tablets with longer disintegration time and slower drug release. The lower stearate content also resulted in a lower lubrication performance, leading to a lesser reduction in tablet ejection force. As expected, a longer blending time of the tablet formulation blend with MgSt yielded tablets with reduced tensile strength, shorter disintegration time and slower drug release. Tablets with higher MgSt concentration showed a greater reduction in tensile strength, longer disintegration time and faster drug release. The study findings reinforced observations by other researchers and provided a better understanding of the fatty acid composition effects of MgSt on lubrication performance and the resulting tablet properties.
硬脂酸镁（MgSt）是一种常用的片剂润滑剂。由于已知 MgSt 性质的变化会影响片剂的特性，因此有必要进一步研究硬脂酸镁脂肪酸组成的影响，特别是硬脂酸和棕榈酸的含量及其对片剂性质的影响。本研究考察了具有不同硬脂酸和棕榈酸含量但具有可比物理性质（例如粒径、结晶度、比表面积和形态）的 MgSt 对润滑性能和由此产生的片剂质量特性的影响，包括机械强度、崩解性和药物释放。还研究了 MgSt 浓度和混合时间对所得片剂性质的影响。使用较低硬脂酸含量的 MgSt 生产的片剂的拉伸强度略高。MgSt 硬脂酸含量的影响在崩解时间和药物释放方面更为明显，其中较低硬脂酸含量的 MgSt 导致片剂的崩解时间更长，药物释放更慢。较低的硬脂酸含量还导致润滑性能降低，从而导致片剂推出力的降低减少。正如预期的那样，更长的片剂配方与 MgSt 的混合时间导致片剂的拉伸强度降低，崩解时间缩短，药物释放速度减慢。较高 MgSt 浓度的片剂表现出更大的拉伸强度降低，崩解时间更长，药物释放更快。研究结果强化了其他研究人员的观察结果，并更好地理解了 MgSt 的脂肪酸组成对润滑性能和由此产生的片剂性质的影响。
