Effect of characteristics of compounds on maintenance of an amorphous state in solid dispersion with crospovidone

✍ Scribed by Yusuke Shibata; Makiko Fujii; Makiko Kokudai; Shinobu Noda; Hideko Okada; Masuo Kondoh; Yoshiteru Watanabe

• Publisher: John Wiley and Sons
• Year: 2007
• Tongue: English
• Weight: 192 KB
• Volume: 96
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.20794

✦ Synopsis

Solid dispersion (SD) of indomethacin with crospovidone (CrosPVP) shows useful characteristics for preparation of dosage forms. This study aimed to determine the types of drugs that could adopt a stable amorphous form in SD. Twenty compounds with various melting points (70-2188C), molecular weights (135-504) and functional groups (amide, amino, carbonyl, hydroxyl, ketone etc.) were prepared in SD with CrosPVP. The CrosPVP SDs were prepared using a mechanical mixing and heating method. Melting point and molecular weight were found to have no influence on the ability of a compound to maintain an amorphous state in SD. All compounds containing hydrogen-bond-donor functional groups existed in an amorphous state in SD for at least 6 months. Infrared spectra suggested an interaction between the functional groups of these compounds and amide carbonyl group of CrosPVP. Compounds without hydrogen-bond-donor groups could not maintain an amorphous state and underwent recrystallization within 1 month. It was suggested that the presence of a hydrogen-bond-donor functional group in a compound is an important factor affecting the stable formation of SD with CrosPVP, which contains a hydrogen-bond acceptor.