Pharmaceutical solid form screening and selection : which form emerges?

Chappa, Praveen (avtor), Jenjeti, Ramesh Naidu (avtor), Kljun, Jakob (avtor), Mittapalli, Sudhir (avtor), Pichler, Arthur (avtor), Desiraju, Gautam R. (avtor)

Solid form screening is an essential step in drug discovery and development because different solid forms of a drug substance may significantly affect the stability, dissolution, and/or manufacturing of the corresponding drug products. This paper takes up these issues, aiming to provide practical guidance on how to obtain and identify stable solid forms as well as validating proposed crystallization conditions in a set of representative active pharmaceutical ingredients (APIs). Techniques for solid form identification and characterization are discussed from the viewpoint of obtaining forms that are suitable for pharmaceutical development (e.g., physically/chemically stable, easily produced and manipulated on a large scale). Ten representative APIs are taken up for detailed study of their crystallization conditions. The forms are identified definitively using single-crystal X-ray diffraction methods. It is found that for all the APIs in this study, the proposed crystallization methods consistently yield the stable form, as previously identified in the literature.

• Jezik: Angleški jezik
• Ključne besede: polymorph, active pharmaceutical ingredients, crystallization, hydrogen bond
• Vrsta gradiva: Članek v reviji
• Tipologija: 1.01 - Izvirni znanstveni članek
• Organizacija: FKKT - Fakulteta za kemijo in kemijsko tehnologijo
• Status publikacije: Objavljeno
• Različica publikacije: Objavljena publikacija
• Leto izida: 2025
• Št. strani: Str. 4783-4794
• Številčenje: Vol. 25, iss. 13
• PID: 20.500.12556/RUL-173659
• UDK: 548.33:615
• ISSN pri članku: 1528-7483
• DOI: 10.1021/acs.cgd.5c00252
• COBISS.SI-ID: 246153987
• Datum objave v RUL: 19.09.2025

Gradivo je del revije

• Naslov: Crystal growth & design
• Skrajšan naslov: Cryst. growth des.
• Založnik: American Chemical Society
• ISSN: 1528-7483
• COBISS.SI-ID: 512176921

Licence

• Licenca: CC BY-NC-ND 4.0, Creative Commons Priznanje avtorstva-Nekomercialno-Brez predelav 4.0 Mednarodna
• Povezava: http://creativecommons.org/licenses/by-nc-nd/4.0/deed.sl
• Opis: Najbolj omejujoča licenca Creative Commons. Uporabniki lahko prenesejo in delijo delo v nekomercialne namene in ga ne smejo uporabiti za nobene druge namene.

Sekundarni jezik

• Jezik: Slovenski jezik
• Ključne besede: polimorf, aktivne farmacevtske učinkovine, kristalizacija, vodikova vez

Projekti

• Financer: ARIS - Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije
• Številka projekta: I0-0022
• Naslov: Mreža raziskovalnih infrastrukturnih centrov Univerze v Ljubljani (MRIC UL)

• Financer: ARIS - Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije
• Številka projekta: P1-0175
• Naslov: Napredna anorganska kemija