Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy
Language English Country Netherlands Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
26861928
DOI
10.1016/j.ejpb.2016.02.001
PII: S0939-6411(16)30003-0
Knihovny.cz E-resources
- Keywords
- Aprepitant, Confocal Raman spectroscopy, Dissolution mechanisms, Polymer, Recrystallization, Solid dispersion,
- MeSH
- Aprepitant MeSH
- Hydrophobic and Hydrophilic Interactions MeSH
- Kinetics MeSH
- Microscopy, Confocal methods MeSH
- Crystallization MeSH
- Morpholines chemistry MeSH
- Drug Carriers chemistry MeSH
- Polyethylene Glycols chemistry MeSH
- Polymers chemistry MeSH
- Polyvinyls chemistry MeSH
- Povidone chemistry MeSH
- Spectrum Analysis, Raman methods MeSH
- Solubility MeSH
- Drug Stability MeSH
- Drug Liberation * MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Aprepitant MeSH
- Morpholines MeSH
- Drug Carriers MeSH
- Polyethylene Glycols MeSH
- Polymers MeSH
- polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer MeSH Browser
- Polyvinyls MeSH
- Povidone MeSH
In this study, we investigated the release mechanism of the poorly water soluble drug aprepitant from different amorphous solid dispersions using confocal Raman microscopy (CRM). Solid dispersions were fabricated based on either Soluplus®, as an amphiphilic copolymer and solubilizer, or on polyvinylpyrrolidone, as a hydrophilic polymer, in order to elucidate the influence of the polymer characteristics on the drug form and dissolution mechanisms. Aprepitant exhibited its amorphous form in both solid dispersions. However, the release differed depending on the polymer. The high complexation effect of Soluplus was shown to be a crucial factor for stabilization of the amorphous drug, resulting in continuous release without any recrystallization of aprepitant. In contrast, solid dispersions based on polyvinylpyrrolidone showed a different mechanism of dissolution; due to the good affinity of PVP and water, the polymer is dissolving fast, leading to phase separation and local recrystallization of the drug. The study highlights the complexity of release processes from solid dispersions and elucidates the influence of the polymer on drug release kinetics.
References provided by Crossref.org
The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions
