EGP-1214 – INTRAORAL (SUBLINGUAL) INSULIN TABLET BY EASTGATE BIOTECH
The Intraoral Insulin Tablet:
EGP-1214, the EastGate Biotech’s flagship product in the field of diabetes and metabolic syndrome. It is a compressed tablet containing human recombinant insulin and designed for sublingual administration. The tablet contains relatively small amount of insulin (1 mg per tablet). The tablet is administered sublingually (under the tongue) where it dissolves and provides transmucosal delivery of the peptide for blood glucose management. The tablet should not be swallowed to avoid degradation of insulin in the stomach.
The intraoral insulin tablet designed for the treatment of early stages of Type 2 diabetes as well as for pre-diabetes. Providing additional exogenic insulin to Type 2 diabetes patients should slow down the rate of pancreas deterioration and improve glycemic control. The gland can respite and the disease progress may decelerate. The tablet can be used as an add-on medicine in a combination treatment with other oral antidiabetic drugs, commonly prescribed for treatment of Type 2 diabetes.
The tablet can also be employed to treat pre-diabetes; due to exaggerating pandemic growth of diabetes amongst young and aging adult age groups, patients are looking for a non-invasive means to treat and counteract the disease early enough.
Current research has shown that the administration of insulin at earlier stages of Type 2 diabetes mellitus has positive effects and is now beginning to be included in the standard treatment regimens. While the benefits can be significant, some patients are hesitant to introduce injections into their daily routine. The addition of an effective non-injectable insulin dosage form to the anti-diabetes treatment regimen will have significant benefits in terms of compliance among patients.
Drug delivery via the buccal and sublingual mucosa:
BENEFITS AND ADVANTAGES OF SUBLINGUAL DELIVERY
-Pre-systemic metabolism of the peptide in the GI and liver is avoided
-Good accessibility; the drug is in direct contact with the mucosa, avoiding significant dilution;
-Formation of a high gradient across the mucosa allowing drug diffusion into the underlying tissue
-High level of vascularization in sublingual area
-Small variations of pH (not as in gastrointestinal tract)
-Buccal and Sublingual enzymatic activity is mainly intracellular and less pronounced than in other parts of GI tract; practically no protease activity in saliva
-Non-invasive blood sugar maintenance
-Low probability of hypoglycemic events
INITIAL EXPERIMENTS
Initial experiments of EGP-1214 demonstrated that the developed sublingual insulin tablet is easy and convenient to use; does not irritate the sublingual mucosa and has a fast and reproducible onset of glucose lowering action (within 30 minutes). The transmucosal penetration of EGP-1214 was clearly confirmed by the decrease of C-peptide concentration in blood.
From 2010 to 2020, the number of people with diabetes is expected to rise by another 1.2 million, bringing the total to about 3.7 million. These increases escalate the proportion of the total population with diabetes from 4.2% in 2000 to 7.3% in 2010 and to 9.9% by 2020
DIABETES CAN LEAD TO SERIOUS COMPLICATIONS AND PREMATURE DEATH:
• 80% of patients with diabetes die from a heart attack or a stroke
• 42% of new kidney dialysis patients in 2004 had diabetes
• Diabetes is the single leading cause of blindness
• 7 of 10 non-traumatic limb amputations are the result of diabetes complications
• 25% of people with diabetes suffer from depression
• The life expectancy for people with type 1 diabetes may be shortened by ~15 years
• The life expectancy for people with type 2 diabetes may be shortened by 5-10 years
HUMAN INSULIN IS THE MOST SAFE (as long as hypoglycemia avoided) AND EFFECTIVE MEDICINE FOR DIABETES TREATMENT
LACK OF CONVENIENT NON-INJECTABLE DOSAGE FORMS PRECLUDES WIDE USE OF INSULIN FOR EARLY STAGES OF DIABETES