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压片过程中和压片后片剂结构中的粒度分布及演变

Particle size distribution and evolution in tablet structure during and after compaction.

作者信息

Fichtner Frauke, Rasmuson Ake, Alderborn Göran

机构信息

Department of Pharmacy, Uppsala University, Box 580, SE-751 23 Uppsala, Sweden.

出版信息

Int J Pharm. 2005 Mar 23;292(1-2):211-25. doi: 10.1016/j.ijpharm.2004.12.003. Epub 2005 Jan 26.

Abstract

The objective of this study was to investigate the effect of the distribution in size of free-flowing particles for the evolution in tablet structure and tablet strength. For sucrose and sodium chloride, three powders of different size distributions were prepared by mixing predetermined quantities of particle size fractions. For paracetamol, three batches with varying particle size distributions were prepared by crystallisation. The powders were formed into tablets. Tablet porosity and tensile strength were determined directly after compaction and after short-term storage at two different relative humidities. Tablets were also formed after admixture of a lubricant (magnesium stearate) and the tablet tensile strength was determined. For the test materials used in this study, the spread in particle size had no influence on the evolution in tablet porosity and tensile strength during compression. However, the spread in particle size had a significant and complex influence on the short-term post-compaction increase in tablet tensile strength. The effect of the spread was related to the instability mechanism and the presence of lubricant. It is concluded that the distribution in size of free-flowing particles is not critical for the tablet porosity but may give significant effects on tablet tensile strength due to a post-compaction reaction.

摘要

本研究的目的是调查自由流动颗粒的尺寸分布对片剂结构演变和片剂强度的影响。对于蔗糖和氯化钠,通过混合预定量的粒度级分制备了三种不同尺寸分布的粉末。对于扑热息痛,通过结晶制备了三批具有不同粒度分布的样品。将这些粉末压制成片剂。在压制后以及在两种不同相对湿度下短期储存后,直接测定片剂的孔隙率和抗张强度。在加入润滑剂(硬脂酸镁)后也压制片剂,并测定片剂的抗张强度。对于本研究中使用的测试材料,粒度分布对压制过程中片剂孔隙率和抗张强度的演变没有影响。然而,粒度分布对压制后片剂抗张强度的短期增加有显著且复杂的影响。这种影响与不稳定性机制和润滑剂的存在有关。得出的结论是,自由流动颗粒的尺寸分布对片剂孔隙率并不关键,但由于压制后的反应,可能对片剂抗张强度产生显著影响。

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