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系统评估常用润滑剂以优化片剂配方的使用。

Systematic evaluation of common lubricants for optimal use in tablet formulation.

机构信息

Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, MN 55455, United States.

Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 9-127B Weaver-Densford Hall, 308 Harvard Street S.E., Minneapolis, MN 55455, United States.

出版信息

Eur J Pharm Sci. 2018 May 30;117:118-127. doi: 10.1016/j.ejps.2018.02.013. Epub 2018 Feb 10.

Abstract

As an essential formulation component for large-scale tablet manufacturing, the lubricant preserves tooling by reducing die-wall friction. Unfortunately, lubrication also often results in adverse effects on tablet characteristics, such as prolonged disintegration, slowed dissolution, and reduced mechanical strength. Therefore, the choice of lubricant and its optimal concentration in a tablet formulation is a critical decision in tablet formulation development to attain low die-wall friction while minimizing negative impact on other tablet properties. Three commercially available tablet lubricants, i.e., magnesium stearate, sodium stearyl fumerate, and stearic acid, were systematically investigated in both plastic and brittle matrices to elucidate their effects on reducing die-wall friction, tablet strength, tablet hardness, tablet friability, and tablet disintegration kinetics. Clear understanding of the lubrication efficiency of commonly used lubricants as well as their impact on tablet characteristics would help future tablet formulation efforts.

摘要

作为大规模片剂制造的重要制剂成分,润滑剂通过减少模壁摩擦来保护模具。不幸的是,润滑剂也常常对片剂特性产生不利影响,如崩解时间延长、溶解速度减慢和机械强度降低。因此,润滑剂的选择及其在片剂配方中的最佳浓度是片剂配方开发中的关键决策,既要达到低模壁摩擦,又要将对其他片剂性质的负面影响降至最低。本文系统地研究了三种市售的片剂润滑剂,即硬脂酸镁、硬脂富马酸钠和硬脂酸,在塑性和脆性基质中的作用,以阐明它们在降低模壁摩擦、片剂强度、片剂硬度、片剂脆碎度和片剂崩解动力学方面的作用。对常用润滑剂的润滑效率及其对片剂特性的影响有清晰的认识,将有助于未来的片剂配方研究。

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