https://pubmed.ncbi.nlm.nih.gov/37343604/
Reppas C, Kuentz M, Bauer-Brandl A, Carlert S, Dallmann A, Dietrich S, Dressman J, Ejskjaer L, Frechen S, Guidetti M, Holm R, Holzem FL, Karlsson Ε, Kostewicz E, Panbachi S, Paulus F, Senniksen MB, Stillhart C, Turner DB, Vertzoni M, Vrenken P, Zöller L, Griffin BT, O'Dwyer PJ. Leveraging the use of in vitro and computational methods to support the development of enabling oral drug products: An InPharma commentary. Eur J Pharm Sci. 2023 Jun 19:106505. doi: 10.1016/j.ejps.2023.106505. Epub ahead of print. PMID: 37343604.
Abstract
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 assessment of drug developability. This commentary focuses on current 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.
Keywords: Amorphous Solid Dispersions; Co-crystals; Computational; Cyclodextrins; Enabling formulations; Lipid-Based Formulations; PBBM; Salts; in silico; in vitro; rDCS.
https://pubmed.ncbi.nlm.nih.gov/37343604/ Reppas C, Kuentz M, Bauer-Brandl A, Carlert S, Dallmann A, Dietrich S, Dressman J, Ejskjaer L, Frechen S, Guidetti M, Holm R, Holzem FL, Karlsson Ε, Kostewicz E, Panbachi S, Paulus F, Senniksen MB, Stillhart C, Turner DB, Vertzoni M, Vrenken P, Zöller L, Griffin BT, O'Dwyer PJ. Leveraging the use of in vitro and computational methods to support the development of enabling oral drug products: An InPharma commentary. Eur J Pharm Sci. 2023 Jun 19:106505. doi: 10.1016/j.ejps.2023.106505. Epub ahead of print. PMID: 37343604.
Abstract 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 assessment of drug developability. This commentary focuses on current 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.
Keywords: Amorphous Solid Dispersions; Co-crystals; Computational; Cyclodextrins; Enabling formulations; Lipid-Based Formulations; PBBM; Salts; in silico; in vitro; rDCS.
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