A novel technique to predict a drug’s physical stability has piqued the interest of the biopharmaceutical industry, in-PharmaTechnologist.com reports. The method could help pharmaceutical companies de-risk early drug development.
The method concerns the developability of BCS Class II drugs, which are categorized by low solubility and high permeability. Alex Zeitler, Professor of Microstructure Engineering at the University of Cambridge, told in-PharmaTechnologist that “if solubility from any crystalline phases is too low, making the drug into an amorphous formulation is a great opportunity to keep the drug candidate in development.”1
Existing drug stability prediction method too slow, costly
Currently, it is nearly impossible for pharma companies to quickly test if such an amorphous form would have sufficient physical stability. This is not due to a lack of effort on the part of researchers to develop assays to test for the stability of amorphous drugs. The current method for testing physical stability involves storing an amorphous drug for up to two years before checking whether or not the drug is still amorphous, a process which is expensive and too time-intensive. However, Zeitler goes on to explain that “in our work, we show that it is not the glass transition temperature that matters but the temperature of a lower transition process, which we have shown represents the true onset of molecular mobility.”1
Early-detection of potential problem molecules
By using optical and mechanical measuring techniques, Zeitler and his team found that localized movement of molecules within a solid is responsible for crystallization. This development could enable companies to screen drug molecules to find out which ones will “happily stay amorphous for a really long time and which ones will rapidly crystalize… if the drug stays amorphous happily, it is very easy to make it into a better soluble drug product and the company can be confident that the drug remains amorphous over the shelf life of the product.”1
This process could allow drug developers to reduce risk by identifying potential problem molecules early in the development process. It could also breathe new life into previously discarded molecules. The technology has been licensed to a Cambridge spin-out company names TaraView, which is pursuing the method further for use in the pharmaceutical industry.1
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