Nejvíce citovaný článek - PubMed ID 26861928
Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy
PURPOSE: Imaging methods were used as tools to provide an understanding of phenomena that occur during dissolution experiments, and ultimately to select the best ratio of two polymers in a matrix in terms of enhancement of the dissolution rate and prevention of crystallization during dissolution. METHODS: Magnetic resonance imaging, ATR-FTIR spectroscopic imaging and Raman mapping have been used to study the release mechanism of a poorly water soluble drug, aprepitant, from multicomponent amorphous solid dispersions. Solid dispersions were prepared based on the combination of two selected polymers - Soluplus, as a solubilizer, and PVP, as a dissolution enhancer. Formulations were prepared in a ratio of Soluplus:PVP 1:10, 1:5, 1:3, and 1:1, in order to obtain favorable properties of the polymer carrier. RESULTS: The crystallization of aprepitant during dissolution has occurred to a varying degree in the polymer ratios 1:10, 1:5, and 1:3, but the increasing presence of Soluplus in the formulation delayed the onset of crystallization. The Soluplus:PVP 1:1 solid dispersion proved to be the best matrix studied, combining the abilities of both polymers in a synergistic manner. CONCLUSIONS: Aprepitant dissolution rate has been significantly enhanced. This study highlights the benefits of combining imaging methods in order to understand the release process.
- Klíčová slova
- FT-IR spectroscopic imaging, amorphous solid dispersion, confocal Raman spectroscopy, crystallisation, magnetic resonance imaging,
- MeSH
- aprepitant MeSH
- farmaceutická chemie metody MeSH
- krystalizace MeSH
- magnetická rezonanční tomografie metody MeSH
- morfoliny chemie MeSH
- nosiče léků chemie MeSH
- polyethylenglykoly chemie MeSH
- polymery chemie MeSH
- polyvinyly chemie MeSH
- pyrrolidiny chemie MeSH
- rozpustnost MeSH
- spektroskopie infračervená s Fourierovou transformací metody MeSH
- uvolňování léčiv MeSH
- voda chemie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- aprepitant MeSH
- morfoliny MeSH
- nosiče léků MeSH
- poly(N-vinylpyrrolidine) MeSH Prohlížeč
- polyethylenglykoly MeSH
- polymery MeSH
- polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer MeSH Prohlížeč
- polyvinyly MeSH
- pyrrolidiny MeSH
- voda MeSH
