Benfotiamine (S-benzoylthiamine monophosphate) is a compound that is an analog vitamin B1 (thiamine). Because it is lipid-soluble, the body metabolizes benfotiamine more quickly than vitamin B1. Upon dephosphorylation of benfotiamine in the intestinal tract, a lipophilic molecule is produced which readily diffuses across cell membranes and is absorbed much better than water soluble thiamine salts. This attribute allows for more absorption in the intestines and in target tissues as compared with thiamine itself. Higher plasma thiamine levels are achieved with oral benfotiamine intake, and blood and tissue concentrations are maintained long time. Oral benfotiamine dosages in these experiments ranged from 40-250 mg daily.
1954, Fujiwara discovered a group of lipid-soluble thiamine derivatives, subsequently called allithiamines because they occur naturally in Allium family vegetable: roasted crushed garlic, onions, leeks. Benfotiamine has been existing in Japan since 1961 and is sold under the trade name “Biotamin“. Has been marketed in Germany since 1978 as under the trade name “Milgamma Mono“. Used for decades in Europe as a prescription drug, benfotiamine reduces the progression of diabetic nerve, retinal, and kidney, damage, and relieves the painful symptoms of diabetic neuropathy. Various clinical trials have demonstrated a reversal in diabetic neuropathy, with improved nerve function and alleviation of pain.
Benfotiamine activates transketolase efficiency, therefore facilitating conversion of harmful glucose metabolites and affecting Advanced Glycation End product (AGE) formation. Advanced glycation end products are caused by hyperglycemia, a trouble that diabetics often have. Different researchs have shown that benfotiamine inhibits 3 important pathways that lead to the formation of toxic substances such as advanced glycation end products. In a clinical trial with 6 patients, benfotiamine lowered Advanced Glycation End Product (AGE) by 40 percent.
Lab experiments and controlled trials have confirmed that benfotiamine alleviates and may even reverse diabetic neuropathy, kidney disease, endothelial dysfunction, peripheral vascular disease, and diabetic retinopathy.
Benfotiamine is remarkably active at inhibiting the formation of AGE (Advanced Glycation End products). It increases threefold the concentration of the endogenous enzyme transketolase which breaks down AGE and converts them into inoffensive compounds. AGE’s main targets are the nerves, eyes, blood vessels and kidneys, and since diabetics produce AGE in excess. In a study, benfotiamine effectively increased transketolase activity in cell cultures by an dramatically 300 percent, compared to a mere 20 percent for thiamine.
In an in vitro study of human endothelial progenitor cells, scientists demonstrated that benfotiamine can help correct hyperglycemic impairment of EPC differentiation into mature, healthy endothelial cells. In 2006, experts at the ‘American Diabetes Association‘ found benfotiamine to be useful in preventing blood vessel degeneration in people with type 2 diabetes.
A double-blind study in Germany found that diabetes patients with polyneuropathy who supplemented with 100 mg of benfotiamine four times daily for 3 weeks demonstrated statistically remarkable development in nerve function scores. A study reported in Experimental and Clinical Endocrinology and Diabetes in November 2008 examined the feature of benfotiamine on individuals with diabetic-neuropathy. 2 groups received the benfotiamine, first group taking 300 mg per day, while the other group took 600 mg. Found those individuals in the 600 mg group the most development in they neuropathy. 13 patients with type 2 diabetes were given a three-day trial of benfotiamine and challenged with a hyperglycemic diet. The researchers concluded that benfotiamine had important prevented both macrovascular and microvascular endothelial dysfunction and oxidative stress in these subjects challenged with a meal rich in advanced glycation end products ages.
Foods Contain Benfotiamine
Benfotiamine is found naturally in onions, garlic, shallots, leeks, and other members of the allium family of vegetables.
Benfotiamine is well tolerated at doses up to 600 mg daily or higher. Based on clinical trials to date, daily doses of benfotiamine range from 300-450 milligrams daily in divided doses. Animal-based studies in which high doses of up to 100 milligrams benfotiamine/kg bw for six months were administered, reported no negative effects.