Metformin Gum as Effective as Tablets With Less Side Effects

Generex, leader in the area of buccal drug delivery has announced the results of its metformin gum trial, a companion product to it’s oral insulin spray.

Generex Biotechnology Corporation a leader in the area of buccal drug delivery, announced the results of a clinical trial designed to compare pharmacokinetic profiles of metformin administered by both the traditional manner (tablets) and by an alternative presentation (the Generex Metformin Gum product) that can be chewed thereby delivering metformin into the human body by way of the buccal cavity (i.e., the mouth). Generex Metformin Gum is designed as a companion product to Oral-lyn(TM), the Company’s proprietary oral insulin spray product.

Metformin is used for the treatment of Type-2 diabetes mellitus in adults and children, particularly when incidental obesity and insulin resistance are present. Metformin is also used to prevent the development of diabetes in people at risk, to treat polycystic ovary syndrome (PCOS), and non-alcoholic steatohepatitis (liver disease). Metformin was approved by the FDA in December, 1994.

Diabetes results when there is a reduced production of insulin or when there is state of resistance to its action. Insulin is the hormone produced by the pancreas that lowers blood glucose levels by reducing the amount of glucose made by the liver and increasing glucose removal from the blood. Metformin increases the sensitivity of liver, muscle, fat, and other tissues to the uptake and effects of insulin, thereby lowering blood glucose levels. Unlike the sulfonylurea class glucose-lowering drugs (i.e. glyburide), metformin (a) does not increase the concentration of insulin in the blood and therefore does not cause hypoglycemia (i.e. excessively low blood glucose levels), and (b) does not cause weight gain. In fact, the weight loss observed with metformin use suggests, among others, an anoretic mechanism and a decrease in caloric expenditure. Scientific studies have indicated that metformin reduces complications associated with diabetes; nonetheless, in spite of its beneficial actions, a large number of metformin users (approximately 30%) develop significant adverse gastrointestinal (GI) effects, including diarrhea and nausea/vomiting.

The Generex study involved 10 healthy volunteers, six men with a mean age of 30 years and a mean Body Mass Index (BMI) of 23.9 and four women with a mean age of 29.8 years and a mean BMI of 21.49. The study utilized metformin tablets (Glucophage 850 mg per tablet) and Generex Metformin Gum pieces (214.5 mg per piece). Plasma metformin concentrations were sequentially measured (a) over a 12-hour period after administration of an 850 mg metformin tablet, (b) over a 24-hour period after administration of 429 mg Generex Metformin Gum (two pieces) and, (c) over a 24-hour period after administration of a 429 mg metformin tablet (a weighed fraction of the larger tablet). Plasma metformin concentrations were determined using High Performance Liquid Chromatography (HPLC) (chromatographic time was six minutes), with removal of proteins and lipids from the biological matrix by common methods prior to HPLC.

Retention time for metformin and internal standard atenolol (100 mg tablet) were 3.4 minutes and 2.9 minutes respectively.

The conclusion of the study is that the Generex Metformin Gum displays a pharmacokinetic profile similar to that of the metformin tablets and therefore shows promise as an alternative method of delivering metformin. The Generex Metformin Gum presentation should avoid the significant adverse gastrointestinal side-effects often accompanying the use of metformin tablets thereby improving patient compliance. In addition, Generex Metformin Gum is expected to be an ideal companion product for the Company’s oral insulin, Oral-lyn. Oral-lyn is designed to offer a safe, simple, fast, effective, flexible, and familiar alternative to subcutaneous injections of prandial insulin.

Generex Biotechnology