Hooper D, Clarke F C, Docherty R, Mitchell J C, Snowden M J
Faculty of Engineering and Science, University of Greenwich, Medway, ME4 4TB, UK; Pfizer Ltd., Ramsgate Road, Sandwich, CT13 9NJ, UK.
Pfizer Ltd., Ramsgate Road, Sandwich, CT13 9NJ, UK.
Int J Pharm. 2017 Oct 5;531(1):266-275. doi: 10.1016/j.ijpharm.2017.08.091. Epub 2017 Aug 24.
This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regularity. The surface energy of the extreme habits were shown to be different where particles that were more regular in shape exhibited surface energies of 9mJ/m higher than those that were needle-like in habit. Computational and experimental data reveals that the increase in surface energy of the regular shaped particles can be attributed to the increase in the specific (polar) component, which is due to greater presence of faces which contain the carboxylic acid functionality at the surface. The increase in the specific energy component is shown to correlate with the sticking propensity of ibuprofen. It is proposed that investigation of the chemical causality of sticking, for this API and others, using the techniques demonstrated in this paper will be of increasing importance.
本研究证明了活性药物成分（API）颗粒习性对布洛芬黏附倾向的影响。报告了四种具有相似物理化学性质的不同晶体习性，且发现黏附倾向随形状规则性的增加而增大。研究表明，极端习性的表面能不同，形状更规则的颗粒的表面能比针状习性的颗粒高9mJ/m²。计算和实验数据表明，规则形状颗粒表面能的增加可归因于比（极性）成分的增加，这是由于表面含有羧酸官能团的晶面的存在增多所致。比能成分的增加与布洛芬的黏附倾向相关。有人提出，利用本文所示技术研究该API及其他API黏附的化学因果关系将变得越来越重要。
