Abstract:
: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 (70-218 degrees C), 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.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Shibata Y,Fujii M,Kokudai M,Noda S,Okada H,Kondoh M,Watanabe Ydoi
10.1002/jps.20794subject
Has Abstractpub_date
2007-06-01 00:00:00pages
1537-47issue
6eissn
0022-3549issn
1520-6017pii
S0022-3549(16)32274-2journal_volume
96pub_type
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