OTCQB: IGXT | TSX-V: IGX
OTCQB: IGXT | TSX-V: IG
Mucoadhesive Tablet

ADVERSA® MUCOADHESIVE TABLET

Pharmaceutical research and development services, regarding mucoadhesive pharmaceutical preparations, and scientific testing research and development for mucoadhesive pharmaceutical preparations.

Information Package
March 2017

Service Mark AdVersa®

IntelGenx’ AdVersa® technology consists in a thin mucoadhesive tablet which allows for buccal adhesion to the oral mucosa. Drug administration via the oral mucosa is convenient, ideal for treating chronic conditions and can improve patient compliance. In addition, therapeutically effective plasma concentrations can be achieved and maintained, side effects minimized, first pass metabolism avoided and dosing frequency reduced.

ORAL DRUG DELIVERY

Oral ingestion has traditionally been the preferred method of drug administration. However, these drug delivery systems have limited control over the release of the drug. The desired therapeutic levels are achieved by regular administration of doses which can undergo random rates of first pass metabolism. This can lead to high levels of unwanted metabolites and potentially variable plasma concentrations of active drug.

Oral Cavity

The oral cavity comprises the cheeks, hard and soft palates and the tongue. It is an entrance of the digestive system and plays many important functions including chewing, speaking and tasting.

oral cavity

Oral Cavity

The buccal mucosa refers to the inner lining of the lips and cheeks. The epithelium of the buccal mucosa is about 40-50 cells thick and the epithelial cells become flatter as they move from the basal layers to the superficial layers. Mucosal Membranes are moist membranes that line passageways and structures in the body that lead to the outside environment such as the mouth, respiratory tract, gastrointestinal tract, nose and vagina. They secrete a viscous fluid known as mucus, which acts as a protective barrier and also lubricates the mucosal membrane. The primary constituent of mucus is a glycoprotein known as mucin as well as water and inorganic salts.

AdVersa® IntelGenx’s Mucoadhesive Technology

AdVersa® consists of a unique technology blending hydrogel-forming polymers with mucoadhesive technology and solubility enhancers. The composition, size and thickness of AdVersa® promotes rapid hydrogel formation and maximum intimate physical contact with the mucosa. This allows optimal absorption of the drug. An example of a possible composition for AdVersa® is shown below.

ComponentDry Weight %
Active ingredient 2.84
Solubilizer and Stabilizer 12.24
Mucoadhesive polymer 36.85
Hydrogel forming polymer 35.82
Surfactant 9.44
Flavor 2.81
Total 100.00

Administration of drug using AdVersa® follows the following three steps.

Step 1. Wetting and swelling

AdVersa® is designed to undergo wetting and swelling as the dosage form spreads over the surface of the mucosal membrane to develop intimate contact with the substrate. It is able to bond with biological tissues using surface tension and forces that exist at the site of contact. Swelling of AdVersa® occurs due to its affinity for water.

Step 2. Mucoadhesion

The buccal mucosa is unable to retain oral dosage forms at the site of absorption. To overcome this shortcoming, IntelGenx uses bioadhesive polymers in AdVersa® for retention of the dosage form at the absorption site. Bioadhesive polymer chains present in AdVersa® and mucosal polymer chains, known as glycoproteins, bind to form semi-permeable adhesive bonds locking AdVersa® in place.

Step 3. Diffusion of the drug

AdVersa® technology can also control the absorption rate of the drug. The formulation can be designed to produce a range of delivery rates controlled by diffusion. Diffusion is the tendency of molecules to move into an available space. In the process of passive diffusion, the transport of molecules across cell membranes depends on the concentration of the molecule. Most drug molecules are transported across membranes by diffusion from a region of high concentration (e.g. inside AdVersa®) to one of a lower concentration such as blood.

Image 9

Diffusion through a membrane

AdVersa® has a simple manufacturing process which is illustrated below. This process will vary from active ingredient to active ingredient and depends upon drug solubility and dosage.

Image 9

Packaging Components

It can be packaged in bottles or blisters.

stability

AdVersa® can be formulated to address stability problems associated with many unstable and/or low solubility active ingredients. IntelGenx uses a special process to stabilize the formulations.

AdVersa®: A New Direction

AdVersa® is at the forefront of buccal mucoadhesive hydrogel technology combining maximum drug delivery efficiency and a patient oriented product. It is formulated with patients in mind. AdVersa® offers a unique alternative that focuses on patient comfort and compliance. It offers rapid or slow releasing alternatives, perfect for acute or chronic indications.

“With AdVersa® in place, patients can eat, drink and carry on normal daily activities.”

AdVersa® can be customized to your needs.

Intellectual Property Status:

AdVersa® is at the forefront of buccal mucoadhesive hydrogel technology combining maximum drug delivery efficiency and a patient oriented product. It is formulated with patients in mind. AdVersa® offers a unique alternative that focuses on patient comfort and compliance. It offers rapid or slow releasing alternatives, perfect for acute or chronic indications.

ComponentTitleFiling dateCurrent status as of Jan. 2017Subject matter
US Patent No. 7,592,328 Natural cyclodextrin complexes 2003/02/20 Issued Composition of Matter
US Patent No. 8,735,374 Oral mucoadhesive dosage form 2010/07/15 Issued Formulation > Composition
CA Patent No. 2,476,834 Natural cyclodextrin complexes of cannabinoids 2003/02/20 Issued Combination > Composition and Pharmacokinetic

IntelGenx also has the registered trademark ADVERSA®. The trademark is currently registered in the US.

Market Opportunity

AdVersa® can be a vehicle for many different drugs that can be negatively affected when delivered via traditional drug delivery methods. It is ideal for:

  • Avoiding a metabolic first pass effect
  • Maximum delivery efficiency of expensive active ingredients
  • Actives with poor water solubility
  • Immediate release of the active
  • Buccal or sublingual delivery
  • Slow release of the drug
  • Modular residential time
  • Release of the drug without mastication or water

Contact Information

DANA MATZEN

VP, Business and Corporate Development
6420 Abrams, Saint-Laurent, Quebec H4S 1Y2, Canada

This email address is being protected from spambots. You need JavaScript enabled to view it.

+1 514-331-7440 x220

IntelGenx Logo

6420 Abrams
Saint-Laurent, Quebec
Canada H4S 1Y2
www.IntelGenx.com