聚氧丙烯聚氧乙烯共聚物作为片剂润滑剂的系统评价。

A systematic evaluation of poloxamers as tablet lubricants.

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.

Product and Technical Development, Biogen, 225 Binney St., Cambridge, MA 02142, United States.

出版信息

Int J Pharm. 2020 Feb 25;576:118994. doi: 10.1016/j.ijpharm.2019.118994. Epub 2019 Dec 29.

DOI:10.1016/j.ijpharm.2019.118994

PMID:31893543

Abstract

Lubricants are important for both preserving the tooling of high-speed tablet presses and attaining quality tablets. Magnesium stearate (MgSt) is most commonly used due to its superior lubrication efficiency; however, it can lead to negative effects on tabletability and dissolution. In this study, we have systematically evaluated two poloxamers, P188 and P407, for their suitability as alternative tablet lubricants. For two excipients with different mechanical properties, i.e., microcrystalline cellulose and lactose, both poloxamers exhibit acceptable lubrication efficiency without negatively impacting tabletability. Compared to 1% MgSt, the performance of 2% of both poloxamers in an experimental tablet formulation of ritonavir led to better lubrication, higher tabletability, and enhanced in vitro drug release. Thus, the use of P188 and P407 as alternative tablet lubricants deserves further evaluations.

摘要

润滑剂对于保护高速压片机的模具和获得高质量的片剂都很重要。硬脂酸镁（MgSt）由于其优越的润滑效率而被广泛使用；然而，它可能会对可压性和溶出度产生负面影响。在这项研究中，我们系统地评估了两种泊洛沙姆，即 P188 和 P407，以评估它们作为替代片剂润滑剂的适用性。对于两种机械性能不同的赋形剂，即微晶纤维素和乳糖，两种泊洛沙姆都表现出可接受的润滑效率，而不会对可压性产生负面影响。与 1%的 MgSt 相比，在利托那韦的实验片剂配方中使用 2%的两种泊洛沙姆都能实现更好的润滑效果、更高的可压性和增强的体外药物释放。因此，使用 P188 和 P407 作为替代片剂润滑剂值得进一步评估。