BACKGROUND

Retention in the upper gastrointestinal tract is critical for some active pharmaceutical ingredients (API).

Gastric retentive dosage systems (GRDS) are available (high & low density, expendable, superporous hydrogel, mucoadhesive, magnetic). However, there is constant need for innovative GRDS that improve API uptake and efficiency.

HOW IT WORKS

Our oral GRDS are characterized by intrinsic low density and high porosity; researchers produce them by state of the art wet granulation manufacturing process.

The formulation incorporates highly hydrophobic dusty powder that allows immediate and continuous buoyancy in the stomach and sustained release of API up to 18h, even on a gastric emptying.

Final form: tablets and hard capsules.

KEY BENEFITS vs. STATE OF THE ART

• “Once a day” administration of drugs improves bioavailability and drug efficiency by reducing both frequency of administration and fluctuations in drug plasma levels.
• As opposed to others GRDS, our formulation floats immediately within the gastric juice: avoids the “all or nothing effect” during the gastric “housekeeper wave” 
• Pills contain up to 85% of API vs. 50% for current GRD forms.
• Allows the delivery of all types of API (hydrophobic or hydrophilic) and especially suitable for API with very narrow absorption window.

DEVELOPMENT STATUS

• In vitro evaluation of dissolution profiles and buoyancy in drastic conditions (150 rpm, pH:1,2)
• APIs studied include: theophylline, doxycycline, paracetamol, carbamazepine, metformin…
• In vivo evaluation on pigs showed sustained release of doxycycline with a retention time ≧6h

APPLICATIONS

Controlled release drug delivery in human and veterinary medicine:

• Improved formulation and life-cycle management of drugs
• Generics or new API requiring sustained release by improved gastric residence time

Food processing industry, nutraceuticals