28 July 2014

More than 80 per cent of all drug candidates in pharma research and development suffer from poor solubility and are therefore rejected early in the drug discovery process. Now Uppsala University researchers show that the new material Upsalite® has great potential for development of new formulations of these rejected drugs.

“These findings could allow the pharma companies to open up large libraries of potent drug candidates earlier discarded due to solubility problems and try them again together with Upsalite”, says Maria Strømme, Professor at the Division of Nanotechnology and Functional Materials at Uppsala University.

The new material was presented last year by her research group. The material has the highest surface area ever measured for an alkali earth metal carbonate; 800 square metres per gram.

In a new study, published in the International Journal of Pharmaceutics the researchers show that the extremely porous magnesium carbonate Upsalite may provide a great opportunity for the development of new drug formulations of active pharmaceutical ingredients with poor aqueous solubility.

About 40 per cent of newly marketed drugs have poor solubility and more than 80 per cent of drug candidates in the research and development pipeline fail because of solubility problems. These drugs subsequently have low bioavailability (i.e., they are difficult for the body to take up), which limits their therapeutic efficacy and hence seldom lead to new pharmaceuticals.

In the new study the pain killer Ibuprofen was used as a model substance for poorly soluble drugs and it was shown that crystallisation of the drug was completely suppressed in the formulation, resulting in both a higher solubility and a three times faster dissolution rate of the drug.

“We think that the narrow pores hinder the drug molecules from organizing in a poorly soluble crystalline form and are forced to maintain an amorphous structure that is easier for the body to absorb”, says Johan Gómez de la Torre.

The discovery will be commercialized though the University spin-out company Disruptive Materials AB (www.disruptivematerials.com) that has been formed by the researchers together with the holding company of Uppsala University.

More information about the research group can be found on Uppsala University website. The article can be found here: http://www.sciencedirect.com/science/article/pii/S0378517314004451