Cryomilling-induced solid dispersion of poor glass forming/poorly water-soluble mefenamic acid with polyvinylpyrrolidone K12
- Authors
- Kang, Naewon; Lee, Jangmi; Choi, Ji Na; Mao, Chen; Lee, Eun Hee
- Issue Date
- 6월-2015
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Ball-milling; cryomilling; mefenamic acid; PVP K12; solid dispersion
- Citation
- DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, v.41, no.6, pp.978 - 988
- Indexed
- SCIE
SCOPUS
- Journal Title
- DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
- Volume
- 41
- Number
- 6
- Start Page
- 978
- End Page
- 988
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/93432
- DOI
- 10.3109/03639045.2014.920024
- ISSN
- 0363-9045
- Abstract
- The effect of mechanical impact on the polymorphic transformation of mefenamic acid (MFA) and the formation of a solid dispersion of mefenamic acid, a poor glass forming/poorly-water soluble compound, with polyvinylpyrrolidone (PVP) K12 was investigated. The implication of solid dispersion formation on solubility enhancement of MFA, prepared by cryomilling, was investigated. Solid state characterization was conducted using powder X-ray diffraction (PXRD) and Fourier-transform infrared (FTIR) spectroscopy combined with crystal structure analysis. Apparent solubility of the mixtures in pH 7.4 buffer was measured. A calculation to compare the powder patterns and FTIR spectra of solid dispersions with the corresponding physical mixtures was conducted. Solid state characterization showed that (1) MFA I transformed to MFA II when pure MFA I was cryogenically milled (CM); and (2) MFA forms a solid dispersion when MFA was cryogenically milled with PVP K12. FTIR spectral analysis showed that hydrogen bonding facilitated by mechanical impact played a major role in forming solid dispersions. The apparent solubility of MFA was significantly improved by making a solid dispersion with PVP K12 via cryomilling. This study highlights the importance of cryomilling with a good hydrogen bond forming excipient as a technique to prepare solid dispersion, especially when a compound shows a poor glass forming ability and therefore, is not easy to form amorphous forms by conventional method.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - College of Pharmacy > Department of Pharmaceutical Science > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.