Bioavailability enhancement

Amorphous solid dispersions increase solubility by eliminating the impact of crystal lattice energy on the dissolution process. The conversion of the crystalline drug substance into an amorphous form, along with the physical stabilization of the amorphous state within a polymer matrix, is achieved through spray drying (a solvent-based method) or hot melt extrusion (a fusion-based method).

Polymers with sufficient solid-state miscibility with the drug substance are carefully identified to prevent recrystallization and ensure consistent performance over time. This is achieved using precise techniques conducted at a milligram scale.

Additional components that improve processability, bioavailability, or physical and chemical stability can be incorporated into amorphous solid dispersion formulations as needed. The selection and quantity of such additives are determined on a case-by-case basis, guided by robust scientific rationale.

Formulation concepts demonstrating adequate performance and physical stability are subsequently scaled up and GMP-manufactured for clinical supply.

Nanosuspensions show accelerated dissolution rates as a result of reducing the particle size, which leads to an increased surface area of these particles. The key to nanosuspension development is the identification of a suitable stabilizer system, such that crystal growth and agglomeration effects are suppressed during the lifetime of the formulation.

In addition to a broad range of milling systems, we have the technologies to convert (liquid) nanosuspensions into solid forms.