Amorphous stabilization of poorly soluble drugs – Upsalite
It is a well-known fact that the dissolution rate is higher for the amorphous form of a poorly soluble drug than from its various crystal forms. However, the amorphous state is inherently unstable and tends to recrystallise back into the poorly soluble form. As such, amorphous APIs are not feasible for the development of stable and high-quality oral drug products. Various approaches have thus been proposed for the stabilisation of amorphous drugs; for example, hot melt extrusion and spray-drying.
Upsalite has now entered that scene, and is featuring high drug loads, excellent stability and a low-temperature drug-loading procedure. It is an effective and scalable solution that can be already introduced in the preclinical phase, and then go the distance to market.
High drug loads
For many other solubilisation technologies such as cyclodextrins, liposomes and others, the drug/excipient ratio is rather low, compelling an unfortunate choice between dosage strength and dosage size. With drug loads up to 50% w/w for Upsalite, there is no contradiction between a high strength and convenient, normal-sized tablet or capsule. Scientists at Disruptive Materials are now pushing forward, studying Upsalite’s compression characteristics and other tablet-manufacturing properties.