McDonagh Alan F, Duff Bronagh, Brennan Lorna, Tajber Lidia
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland; Synthesis and Solid State Pharmaceutical Centre, Ireland.
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Dublin 2, Ireland.
Eur J Pharm Sci. 2020 Nov 1;154:105505. doi: 10.1016/j.ejps.2020.105505. Epub 2020 Aug 7.
Direct compression remains one of the most favourable methods available to produce tablet compacts due to its simplicity, efficiency and cost effectiveness however, the technique still remains unsuitable for the majority of formulations due to materials exhibiting poor physical properties such as inadequate compressibility and deformation mechanisms. Whereas crystallo-co-spray drying of various blends has shown to improve the tabletting properties of poorly processable materials, the role of the solvent feed composition in altering the soluble fraction ratio of the excipient to the drug in a crystallo-co-spray dried agglomerate is not well understood. The aim of this work was to investigate the role of the soluble fraction of a drug (paracetamol) and an excipient (α-lactose monohydrate) on the tabletting properties of their crystallo-co-spray dried agglomerates produced via co-spray drying using various inlet feed solvent compositions in order to vary the soluble fraction of the excipient in the feed. It was found that an increase in excipient soluble fraction in the inlet feed resulted in a greater degree of intimate mixing in the final spray dried powder blend, which in turn led to an improvement in tabletting properties of the poorly processable drug.
由于直接压片法简单、高效且具有成本效益,它仍然是制备片剂的最有利方法之一。然而,由于材料表现出较差的物理性质,如压缩性不足和变形机制不佳,该技术仍然不适用于大多数制剂。虽然各种混合物的结晶共喷雾干燥已显示出可改善难加工材料的压片性能,但溶剂进料组成在改变结晶共喷雾干燥团聚物中辅料与药物的可溶部分比例方面的作用尚未得到充分理解。这项工作的目的是研究药物(对乙酰氨基酚)和辅料(一水合α-乳糖)的可溶部分对通过使用各种进料溶剂组成进行共喷雾干燥生产的结晶共喷雾干燥团聚物的压片性能的作用,以便改变进料中辅料的可溶部分。结果发现,进料中辅料可溶部分的增加导致最终喷雾干燥粉末混合物中更紧密的混合程度,这反过来又改善了难加工药物的压片性能。