期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 559, 期 -, 页码 147-155出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2019.01.009
关键词
Amorphous solid dispersion; Precipitation; Spray drying; Dissolution; Bioavailability; Thin film evaporation
Amorphous solid dispersions are a promising option for managing compounds with poor aqueous solubility. However, for compounds with high melting points, thermal stability limitations, or poor solubility in volatile solvents, conventional routes of hot melt extrusion or spray drying may not be viable. Co-precipitated amorphous dispersions (cPAD) can provide a solution. For the material studied in this paper, the cPAD material that was seemingly identical to spray dried material in terms of being single phase amorphous (as measured by DSC and XRD ) but showed slower dissolution behavior. It was identified that physical properties of the cPAD material could be improved to enhance wettability and improve dissolution performance. This was achieved by incorporating the cPAD material into a matrix of water soluble excipients generated via evaporative isolation routes. Importantly, this approach appears to offer another route to further increase the drug load in final dosage units and is significant as increased drug loading generally results in slower or incomplete release. Results showed successful proof of concept via in vitro biorelevant dissolution and confirmatory canine pharmacokinetic studies yielding comparable exposure for capsules comprised of conventional spray dried material as well as capsules with elevated drug load comprised of cPAD hierarchical particles.
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