Resources

Unlocking the softgel formulation option for FEXO using our deep eutectic solvent technology

 

FEXO is a widely used over-the-counter therapeutic to treat hay fever, seasonal allergies and urticaria. It is commercially available in a variety of presentations, including tablets, powder-filled capsules and suspensions. However, there is no FEXO softgel formulation on the market, in spite of a strong preference for this type of dosage form by the consumer healthcare market. This is related to the low solubility of FEXO in liquid excipients, combined with a high dose requirement (180 mg). Using our deep eutectic solvent technology, we have developed a physically and chemically stable liquid fill, containing 350 mg/ml of FEXO. This enabled us to fill the 180 mg dose in a single size 10 softgel, which conventional solubilisation technologies have been unable to do. The ability of our deep eutectic solvent based formulation platform to create highly solubilising formulations for the most physicochemically diverse drugs opens up myriad new product development opportunities in both the prescription drug as well as the consumer healthcare market.

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Designing a high-payload liquid formulation for a lipophilic weak base using our deep eutectic solvent technology

 

The antimycotic compound ITZ is extremely poorly water-soluble, which is mainly driven by its high lipophilicity. The oral solution as developed by the originator contains hydroxypropyl-β-cyclodextrin (40%), propylene glycol and hydrochloric acid (pH 2) as solubilising excipients. In spite of the cocktail of solubilisation strategies employed in this product (cyclodextrin complexation, cosolvency and pH-adjustment), the total ITZ concentration is only 10 mg/ml. In general, developing a high-payload solubilised formulation is difficult, given ITZ's low solubility in excipients. Harnessing the potential of our our deep eutectic solvent platform, we have designed a formulation that has equivalent biopharmaceutical performance but 14-fold higher ITZ loading than the marketed oral solution. These findings illustrate the potential of our technology for the formulation of lipophilic, poorly soluble weak bases.

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Overcoming poor solubility using our deep eutectic solvent technology - Answers to the 10 questions we get asked the most

 

What are the key benefits of your technology?

What is the maximum API loading achievable using your technology?

How are your formulations manufactured?

Do your formulations show side effects?

What is the regulatory status of your technology?

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We have taken some time to write answers to 10 questions your are likely to have when considering working with us.

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