From bitter to sweet
The result of such an analysis by the electronic tongue is not an absolute judgment such as “bitter” or “sweet,” but rather a kind of “fingerprint.” It has the form of a star-shaped coordinate system in which the various individual values are represented. Färber shows a printout on which the measurement of pure metformin is compared to that of the finished medication. The plot for the active ingredient reveals high values on three of the arms of the star, in contrast to the even taste profile of the Glucophage® powder.
The comparison between a chewed classic tablet and the powder, which is dissolved in a glass of water to form a light opaque fluid, really does demonstrate a very clear difference. One has a strong, bitter taste that puckers the mucous membrane in the mouth, while the other is slightly sweet but with an otherwise almost imperceptible taste — research objective achieved!
The result of such an analysis by the electronic tongue is not an absolute judgment such as “bitter” or “sweet,” but rather a kind of “fingerprint.” It has the form of a star-shaped coordinate system in which the various individual values are represented. Färber shows a printout on which the measurement of pure metformin is compared to that of the finished medication. The plot for the active ingredient reveals high values on three of the arms of the star, in contrast to the even taste profile of the Glucophage® powder.
The comparison between a chewed classic tablet and the powder, which is dissolved in a glass of water to form a light opaque fluid, really does demonstrate a very clear difference. One has a strong, bitter taste that puckers the mucous membrane in the mouth, while the other is slightly sweet but with an otherwise almost imperceptible taste — research objective achieved!
Once a clinical trial had confirmed that the new dosage form as a dissolved powder behaved and acted in exactly the same way in the body as Glucophage® tablets, there were no further obstacles to approval by drug regulatory authorities. Glucophage® powder is manufactured and packaged in small foil sachets in Merck Serono’s plant in Mollet, near Barcelona, Spain.
Glucophage® powder isn’t the first innovation to be developed from the classic, film-coated tablet. “Merck Serono had already worked on further developing the medication” says Färber. The tablet variant XR was one result of these efforts. The abbreviation stands for Extended Release — in this form, the active ingredient is released more slowly than by the film-coated tablet. The aim with these tablets, which only had to be taken once a day, was also to ensure better therapeutic compliance. The alternative — Glucophage XR® — uses a matrix of a cellulose derivative which swells into a gel in the digestive tract and releases the metformin step by step in small doses.
Whether as powder or tablets, the metformin family of drugs from Merck Serono has potential for the future. This is true not least because there are currently no convincing alternatives to this active ingredient. The International Diabetes Federation (IDF), the American Diabetes Association (ADA), and the European Association for the Study of Diabetes (EASD), among others, recommend that the drug should be part of the first-line treatment for type 2 diabetes. The therapy should be combined with a change in lifestyle, including more exercise and a healthier diet.
© Merck
Type 2 diabetes: Insulin is produced by the beta cells of the pancreas. Its main function is to transport glucose into body cells. Like a key an lock, insulin fits into ist receptor and opens the way for glucose to enter the cell. Patients with type 2 diabetes have defective insulin receptors, so glucose is not absorbed by cells
Type 2 diabetes: Insulin is produced by the beta cells of the pancreas. Its main function is to transport glucose into body cells. Like a key an lock, insulin fits into ist receptor and opens the way for glucose to enter the cell. Patients with type 2 diabetes have defective insulin receptors, so glucose is not absorbed by cells
| Type 2 diabetes: How metformin helps |
| Type 2 diabetes is a glucose metabolism disorder. On the one hand, body tissue develops a partial resistance to insulin, one of the body’s own hormones, which is responsible for metabolizing the dissolved glucose in the blood. On the other hand, the limited function of the beta cells in the pancreas leads to an insufficient supply of insulin. The active ingredient metformin hydrochloride corrects the insulin resistance by making tissues, such as the liver and muscles, receptive to insulin uptake. This process reduces glucose production in the liver while simultaneously enhancing glucose uptake in the muscles, where the glucose is stored as glycogen or burned to produce energy. The result is a restoration of the normal glucose level — the most important objective in treatment of type 2 diabetes. The British UKPDS study has shown that metformin not only reduces the glucose content in the blood, but that it also significantly reduces the risk of long-term complications including heart attack or stroke. |
