GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
Int J Pharm. 2024 May 25;657:124190. doi: 10.1016/j.ijpharm.2024.124190. Epub 2024 May 1.
Lubricants are essential for most tablet formulations as they assist powder flow, prevent adhesion to tableting tools and facilitate tablet ejection. Magnesium stearate (MgSt) is an effective lubricant but may compromise tablet strength and disintegratability. In the design of orodispersible tablets, tablet strength and disintegratability are critical attributes of the dosage form. Hence, this study aimed to conduct an in-depth comparative study of MgSt with alternative lubricants, namely sodium lauryl sulphate (SLS), stearic acid (SA) and hydrogenated castor oil (HCO), for their effects on the tableting process as well as tablet properties. Powder blends were prepared with lactose, sodium starch glycolate or crospovidone as the disintegrant, and a lubricant at different concentrations. Angle of repose was determined for the mixtures. Comparative evaluation was carried out based on the ejection force, tensile strength, liquid penetration and disintegratability of the tablets produced. As the lubricant concentration increased, powder flow and tablet ejection improved. The lubrication efficiency generally decreased as follows: MgSt > HCO > SA > SLS. Despite its superior lubrication efficacy, MgSt is the only lubricant of four evaluated that reduced tablet tensile strength. Tablet disintegration time was strongly determined by tensile strength and liquid penetration, which were in turn affected by the lubricant type and concentration. All the above factors should be taken into consideration when deciding the type and concentration of lubricant for an orodispersible tablet formulation.
润滑剂对于大多数片剂制剂都是必不可少的，因为它们有助于粉末流动、防止与压片工具粘连，并便于片剂推出。硬脂酸镁（MgSt）是一种有效的润滑剂，但可能会影响片剂的强度和崩解性。在口崩片的设计中，片剂的强度和崩解性是剂型的关键属性。因此，本研究旨在深入比较硬脂酸镁与替代润滑剂，即月桂基硫酸钠（SLS）、硬脂酸（SA）和氢化蓖麻油（HCO），以研究它们对压片过程以及片剂性质的影响。将乳糖、交联羧甲基纤维素钠或共聚维酮作为崩解剂，与不同浓度的润滑剂混合制备粉末混合物。测定混合物的休止角。根据生产的片剂的推出力、拉伸强度、液体渗透和崩解性进行比较评估。随着润滑剂浓度的增加，粉末流动性和片剂推出性得到改善。润滑剂的润滑效率通常按以下顺序降低：MgSt > HCO > SA > SLS。尽管硬脂酸镁具有优越的润滑效果，但它是四种评估润滑剂中唯一一种降低片剂拉伸强度的润滑剂。片剂崩解时间主要取决于拉伸强度和液体渗透，而拉伸强度和液体渗透又受到润滑剂类型和浓度的影响。在决定口崩片制剂的润滑剂类型和浓度时，应考虑所有上述因素。
