O-1080Enantia / Spain
Cocrystals to enhance solubility in solids
cocrystallisation, drug development, bioavailability, Cocrystals, API, APIs, active ingredients, pharmaceutical products, drug products, solubility enhancement, pharmaceutical, pharmaceutics, pharma, bioavailability
Organization type : SMEs
Type of tech offer : Services
Current Development Status : Commercially available technologies
|Posted on: 06/03/2013||Deadline : 05/10/2013||Active users : 884||Tech Offer ID : O-1080|
Description of the technology offer
Solubility is one of the determining parameters for the bioavailability of a compound. Therefore, it is a major concern in drug development taking into account that a large percentage of drug candidates never reach the market due to solubility problems and that recent trends in discovery pipelines tend to more lipophilic compounds. In this context, preformulation solutions to enhance aqueous solubility have a key role to play.
COCRYSTALLISATION offers an alternative to salt screening when the salt approach is ineffective or the molecule has no ionisable points. A cocrystal might enhance the solubility effect by:
- Thermodynamic improvement
- Kinetic improvement:”spring and parachute effect”
New and innovative aspects
The application of cocrystallization technologies has only recently been recognised as a way to improve physico-chemical properties of APIs and their synthetic intermediates. Better profiles may include enhanced solubility, better stability and the extension or widening of IP position with respect to the development of active pharmaceutical ingredients (APIs).
Unlike salt formation, cocrystallization does not rely on ionisation of the API and the counterion to make a cryst... Read more
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