Taste Masking

Technologies

OXP zero™ is a technology platform that allows acidic and anionic drugs to be administered orally without bad taste or irritation in non-tablet form and without affecting the release properties of the drug in the body.

The OXP zero™ platform includes intellectual property and know-how on the design and use of novel salts of the specific drug, the low cost manufacture of the novel salts and on the formulation and manufacturing of finished products using these. OXP zero™ is ideally suitable for the development of non tablet forms such as liquids, gels, chewables, ODT's (orally disintegrating tablets) where taste, irritation or stability of the drug active or finished product have previously hindered successful results.

OXP zero™ is based on a novel salt system for acidic and anionic APIs where the API is surrounded in a layered structure which protects the API. The salt is insoluble in the mouth but it readily dissolves in the acidic environment of the stomach releasing the API in the anionic form without affecting its release profile.

OXP zero™ salts have the following properties:

• They are not soluble in the mouth, therefore leading to:
  • ZERO taste of the API
  • ZERO irritation or 'burn' from the API in the mouth
• They are hydrophilic and can be more easily dispersed in liquids or gels
• They rapidly dissolve at stomach pH, thereby immediately releasing the API and not affect the release profile of the API.

OXP zero™ is an ideal system to aide reformulation of bitter or irritating APIs into non-tablet formats.

• It is NOT a coating system, which are primarily limited to tableting
• It is NOT a microencapsulation technique, which is typically very expensive and alters the release profile of the API.

The synthesis of OXP zero™ is a simple crystallisation step. This step can be added to the existing API synthesis or can be applied as a standalone process to a purchased API, thereby giving great flexibility to the product formulator.

We have established proof of concept for OXP zero™ ibuprofen, which has totally removed the typical burning sensation on the throat of this active. The “burn” of ibuprofen has prevented ibuprofen from being successfully formulated in doses over 100mg per 5ml in suspension or other non-tablet forms. In addition, OXP zero™ ibuprofen showed in vitro bioequivalent release profiles to those of standard ibuprofen tablets, surpassing the USP monograph requirements.

We are now expanding our range to develop proof of concept OXP zero™ products (including in vitro bioequivalence studies) for a range of NSAIDS including Diclofenac, Mefenamic acid and Naproxen, all of which have taste or burning issues to overcome in developing non-tablet formulations, especially at higher doses.

Suitable APIs for OXP zero™

OXP zero™ has the potential to be applied to a wide range of acidic drugs, this is drugs having at least one anionic group, ideally a carboxylic acid group but also other anionic forms. It is applicable to a range of drug categories including the following. Note, this is not an exhaustive list.

NSAIDs: ibuprofen, naproxen, diclofenac, mefenamic acid, aspirin.

Statins: atorvastatin, rosuvastatin. simvastatin, pravastatin, losuvastatin.

Antibiotics: fluoroquinolones and cephalosporins.

Gaba-analogues: gabapentin and pregabalin.

ACE inhibitors: enalapril, lisinopril, peridopril, ramipril, quinapril.

OXP zero™ can also be applied to many other important acidic drugs such as valproic acid, methotrexate, fexofenadine and levodopa. There may be many drugs in the development pipeline for which the technology could be applicable as well.

Technology Evaluation

The partner companies who adopt our technology pay an up-front license fee followed by development milestone payments and then royalties on finished products sold using the technology. OXP invests the upfront licence fee to optimise product development and to ensure seamless technology transfer to the pharmaceutical partner. To enable our customers to validate our technology and products we provide the following prior to the signing of the upfront licence:

• Product specification sheet
• MSDS
• In vitro demonstration of bioequivalence
• 250g of material. Larger quantities or GMP batches can be made available.
• Stability data on the material.

Once the licence is signed, know-how and process documentation are provided to facilitate scale up, product formulation and dossier development.