Building a better particle: Leveraging physicochemical understanding of amorphous solid dispersions and a hierarchical particle approach for improved delivery at high drug loadings.

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