Department of Pharmacy, National and Kapodistrian University of Athens, Greece.
School of Life Sciences, University of Applied Sciences and Arts Northwestern Switzerland, Muttenz CH 4132, Switzerland.
Eur J Pharm Sci. 2023 Sep 1;188:106505. doi: 10.1016/j.ejps.2023.106505. Epub 2023 Jun 19.
Due to the strong tendency towards poorly soluble drugs in modern development pipelines, enabling drug formulations such as amorphous solid dispersions, cyclodextrins, co-crystals and lipid-based formulations are frequently applied to solubilize or generate supersaturation in gastrointestinal fluids, thus enhancing oral drug absorption. Although many innovative in vitro and in silico tools have been introduced in recent years to aid development of enabling formulations, significant knowledge gaps still exist with respect to how best to implement them. As a result, the development strategy for enabling formulations varies considerably within the industry and many elements of empiricism remain. The InPharma network aims to advance a mechanistic, animal-free approach to the assessment of drug developability. This commentary focuses current status and next steps that will be taken in InPharma to identify and fully utilize 'best practice' in vitro and in silico tools for use in physiologically based biopharmaceutic models.
由于现代开发管道中药物溶解度差的趋势较强，因此经常采用使药物制剂（如无定形固体分散体、环糊精、共晶和基于脂质的制剂）能够在胃肠道液中溶解或产生过饱和，从而增强口服药物吸收。尽管近年来引入了许多创新的体外和计算工具来辅助使能制剂的开发，但在如何最好地实施这些工具方面仍然存在很大的知识差距。因此，使能制剂的开发策略在行业内差异很大，并且许多经验主义元素仍然存在。InPharma 网络旨在推进一种机制性的、无动物的方法来评估药物的可开发性。本评论重点介绍了 InPharma 当前的状态和下一步计划，以确定和充分利用基于生理的生物药剂学模型中“最佳实践”的体外和计算工具。
