With an increasing number of poorly soluble or difficult to crystallise drugs entering development, new formulation strategies are continually required to achieve sufficient bioavailability. Amorphous solid dispersions (ASDs) are an interesting option receiving increased attention in recent years and offer the advantages of improved dissolution rates and higher apparent solubility characteristics compared to the crystalline state. Therefore, if drug permeability is sufficient, the absorption rate and absolute bioavailability can be dramatically increased by enhancing solubility and dissolution kinetics.
How the ProRelease™ technology works;
Through Solvent Mediated Activation (SMA), ProRelease™ creates New Physical Entities (NPEs) of a drug by erasing the crystal lattice to produce an amorphous state, which is then stabilised with biologically inert GRAS carriers. The carriers used in the ProRelease™ system are biocompatible and readily dissolve in the body's GI fluids, releasing the drug in a molecularly dispered form to afford increased kinetics of dissolution and apparent solubility.
Benefits of the ProRelease™ technology:
Compared to current approaches to manufacture Amorphous Solid Dispersions (ASDs), the ProRelease™ technology requires only milligram quantities of material to effectively screen for suitable stabilising matrix systems. Once identified, our in-house designed process for manufacture allows for small scale production (typically < 200 mg) and subsequent analysis in vivo for preclinical testing.
Unlike many production methods (for example solvent evaporation or spray drying), using our process the final isolated product is a free-flowing, solvent free powder that can be incorporated into a variety of dosage forms to achieve the most effective delivery.
The ProRelease™ system offers additional advantages including:
- Produces molecularly dispersed and physically stable drug / excipient microparticulates
- Manufacturing process allows for quick and cost effective feasibility evaluation
- Ability to precisely control the particle size distrubition of amorphous microparticles to minimise batch-to-batch variability
- Careful selection of excipients allows production of immediate or modified release products
From concept to clinic in minimal time
In conjunction with our partner organisation (R5 Pharmaceuticals), we can rapidly transfer the manufacturing process for cGMP production of clinical Phase I and II material. Having already developed over 10 formulations for clinical trials manufacture, our scientific personel and in-house Qualified Person (QP) will manage the transfer process on behalf of the client, ensuring a smooth handover with minimal effort and delay.
For more information about the ProRelease™ amorphous microparticle technology, please contact us at enquiries@synectix-pharma.com
