Low water-soluble compounds can exhibit bio-performance issues such as poor PK exposure or non-linear PK exposure. To improve the bio-performance, amorphous solid dispersions of amorphous drug stabilized in polymer excipients are commonly developed for solubility enhancement.
Amorphous solid dispersions have been shown to alter the properties of an API, including solubility, dissolution, and bioavailability. A variety of polymers or additives are available, and screening is needed to find possible miscible dispersions that will have the properties needed for development. It is helpful to start with common polymers or pharmaceutical excipients used in drug products since their toxicity is known. The chemical and physical stability of the amorphous solid dispersions are assessed as a function of relative humidity and temperature for a period of few weeks or month to identify the most stable amorphous dispersion. When the ideal candidate has been found, it will be scaled-up using spray-drying, melt extrusion, or other methods.
The amorphous solid dispersion will then be used in simple formulations for early development (such as suspensions, drug in capsules, or preliminary formulations) or formulated into a drug product (such as tablets or capsules) for late stage development and marketed products.
We perform comprehensive amorphous solid dispersion screening to identify ASD formulation that can provide sufficient solubility and drug release rate. Our capabilities include making mg quantity material for early development up to kilogram scale for late stage studies to support different needs.