Topiramate is a moderately soluble CNS drug, with a market value of $500MM+/year. It is currently being evaluated for other indications, for which a controlled release system is being designed, or which might benefits from faster onset. Although the chemistry of the compound would not ordinarily suggest that it is “saltable,” we have identified several novel forms of Topiramate using our CrystalMax® technology, the most interesting of which is a crystalline salt whose solubility is >100X greater than that of the crystalline free acid. The salt has a good stability profile, is easily processed, and is an excellent candidate for development into a drug. We have also been able to demonstrate the ability to modulate the solubility of this compound, via the addition of solubility modifying agents, potentially making it a superior candidate for controlled release as compared to the original parent drug. Furthermore, in animal studies, TransForm’s salt form demonstrated significantly faster onset as compared to the original form.
