Benfotiamine (S-benzoylthiamine-O-monophosphate) is a synthetic derivative of thiamin, belonging to the family of compounds knows as "allithiamines." Benfotiamine is fat-soluble and more bioavailable and physiologically active than thiamin.* Benfotiamine raises the blood level of thiamin pyrophosphate (TPP), the biologically active co-enzyme of thiamin, and stimulates transketolase, a cellular enzyme essential for maintenance of normal glucose metabolic pathways.
Suggested Adult Use: Take 1 capsule twice daily, with or without food.
Serving Size: 1 capsule
Servings per container: 120 servings
Amount Per Serving %DV
Benfotiamine 80 mg †
† Daily Value not established
Other Ingredients: Modified cellulose (vegetarian capsule), cellulose, silicon dioxide.
Contains nothing other than listed ingredients.
Benfotiamine (S-benzoylthiamine O-monophosphate) is a synthetic derivative of thiamin (vitamin B1) that has been shown in studies to be far more bioavailable than actual thiamin.1-3 Benfotiamine taken orally is readily absorbed at higher doses, in sharp contrast to regular water-soluble forms of thiamin that exhibit a rapid decline in absorption when taken in doses above 5 mg.1, 4 Human and rodent studies indicate that benfotiamine can greatly improve thiamin status, especially in comparison with regular forms of thiamin.5 In a randomized, double-blind cross-over trial comparing bioavailability of benfotiamine to that of thiamin mononitrate (the most common supplemental form of vitamin B1) in 12 individuals, benfotiamine caused an average 5-fold greater increase in blood thiamin levels than thiamin mononitrate, with a concomitant greater thiamin concentration in red blood cells.3 Benfotiamine is converted to S-benzoylthiamin (through removal of the O-monophosphate by the digestive tract), which readily passes through intestinal cells and is converted into thiamin.6, 7
Support against oxidative stress*
Benfotiamine displays direct antioxidant action in vitro, and preliminary research with human subjects suggests that this activity can be advantageous in helping to safeguard the integrity of human DNA by increasing the antioxidant capacity of plasma.8 In the laboratory, when human, rat, and porcine kidney cells were exposed to toxins that assault the integrity of DNA, benfotiamine was able to reduce oxidative stress under these circumstances.9 Benfotiamine, like vitamins C and E, can deter the activation of NF-kB (a DNA-binding factor known to be activated by oxidative stress-generated reactive oxygen species) for more balanced immune responses. Furthermore, recent in vitro results suggest that the beneficial antioxidant properties of benfotiamine could work against some forms of lipid peroxidation.10 An animal model suggests that during oxidative stress generated by excess glucose, benfotiamine has the capacity to reduce levels of superoxide and hydroxyl radicals in the heart.11Similarly, an animal model of induced oxidative stress in the cerebral cortex (the outer most layer of the brain) suggests a beneficial antioxidant effect of benfotiamine.12
Supports blood levels of thiamin pyrophosphate (TTP), the biologically active co–enzyme form of thiamin*
Helps maintain healthy glucose metabolism*
Benfotiamine increases blood and tissue levels of thiamin pyrophosphate (TPP), the biologically active co-enzyme form of thiamin.1, 7, 13 TPP acts as a co-enzyme for three critical enzymes involved in glucose metabolism: 1) transketolase, 2) pyruvate dehydrogenase, and 3) a-ketoglutarate decarboxylase.14 The latter two enzymes are involved in utilizing glucose for fuel. Thus, TTP is vital to the cell’s energy supply.
Stimulates transketolase, a cellular enzyme essential for maintenance of normal glucose metabolic pathways*
Superoxide, a type of free radical known as a reactive oxygen species (ROS), is a highly toxic molecule produced by our immune system as part of our defense network; in this capacity, it is carefully controlled and works in our favor. However, superoxide is also a byproduct of cellular energy production and other vital processes such as the breakdown of nucleic acids (DNA & RNA) and ATP. It can be produced in quantities beyond our immediate capacity to neutralize, hindering another enzyme involved in the metabolism of glucose, GAPDH. This can lead to a build up of upstream glucose metabolites15; in other words, the pathway can get “backed up.” Biological metabolic pathways can be thought of as similar to assembly (or disassembly) lines, where enzymes in the pathway are analogous to steps in the assembly or disassembly of a product. Blocking GAPDH essentially slows the metabolism of glucose, causing a build up of the metabolites being produced up to that point in the process. These glucose metabolites can be safely metabolized by transketolase. However, if transketolase activity is not optimal, some of these metabolites may be diverted to other biochemical pathways, including the production of advanced glycation end-products (AGEs). Benfotiamine can enhance transketolase activity by promoting tissue levels of TPP.16
Supports healthy aging*
Disrupts formation of Advanced Glycation End-Products (AGEs)*
Helps maintain healthy circulation*
This benfotiamine enhanced transketolase activity leads to metabolic pathways favoring less production of AGEs.16 AGEs are formed by a complex series of reactions between reducing sugars and amino acids on proteins, lipids, and nucleic acids. Diet is a major external source of AGEs, with about 10% of AGEs from food remaining in the body after ingestion.17 Bodily AGE levels are higher in smokers and individuals consuming AGE-rich diets.18 In food, AGEs are created by a non-enzymatic browning process called the Maillard reaction, which can contribute to desired colors, odors, and tastes (caramelized onions is one example of the reaction’s results). However, this reaction is not restricted to food; in 1981, researchers discovered that the Maillard reaction also takes place within the body,19 and that it accelerates as we age (hence the term “AGE”).20 AGEs are especially a concern among long–lived proteins, such as serum albumin, lens crystalline, and collagen in the extracelluar matrix. Internal AGEs may also be formed within cells due to accumulation of super–reactive glucose metabolic intermediates, such as triosephosphates, affecting nearby proteins, lipids, and DNA.5
In a crossover study of 13 participants, a test meal with high AGE content was provided before and after 3 days of oral benfotiamine administration at a dose of 1,050 mg.17 Measurements of endothelial function (behavior of cells lining the blood vessel walls) and oxidative stress were taken on both occasions. The high AGE meal significantly increased TBARS (an indicator of oxidative stress) and impaired circulation—yet these effects of the meal were negated by supplemental benfotiamine when compared to the baseline meal as measured prior to supplementation. Although this study was small and more research is needed, it implies that benfotiamine may help to maintain healthy post-meal circulation. In laboratory animals, benfotiamine has been demonstrated to decrease AGE production in the nerves, kidneys, and retina of the eyes.16, 21, 22 While these studies are suggestive of an ability of benfotiamine to reduce production of AGEs in humans, this has yet to be strongly demonstrated clinically.
Helps maintain nervous system health*
Benfotiamine also has a history of nerve-related research, including a 3-week randomized, double-blinded, placebo-controlled pilot trial of 40 participants. In this short study, the group taking 400 mg benfotiamine daily had superior sensory function and other statistically significant outcome measures pertaining to nerve health.23 These findings are supported by results from other placebo-controlled trials in which benfotiamine was administered as tablets or capsules in doses ranging from 120 to 600 mg daily (higher doses showed the greatest benefit).24-26 In a mouse model, benfotiamine has been shown to support cognitive function.27
Benfotiamine has an excellent tolerability and safety profile and can be taken for long periods without adverse effects.2, 23, 24, 26, 28-33 There have been no reports of toxicity from benfotiamine in the scientific literature over the five decades that have past since it was first synthesized.34
* These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.
1. Bitsch R, Wolf M, et al. Ann Nutr Metab. 1991; 35: 292-6.
2. Loew D. Int J Clin Pharmacol Ther. 1996; 34: 47-50.
3. Schreeb KH, Freudenthaler S, et al. Eur J Clin Pharmacol. 1997; 52: 319-20.
4. European Commission. Opinion of the Scientific Committee on Food on the tolerable upper intake level of Vitamin B1. European Commission Health & Consumer Protection Directorate-General Scientific Committee on Food. 2001. 1-8.
5. Balakumar P, Rohilla A, et al. Pharmacol Res. 2010; 61: 482-8.
6. Shindo H, Okamoto K, et al. Vitamins (Japan). 1968; 38: 30-37.
7. Volvert ML, Seyen S, et al. BMC Pharmacol. 2008; 8: 10.
8. Schupp N, Dette EM, et al. Naunyn Schmiedebergs Arch Pharmacol. 2008; 378: 283-91.
9. Schmid U, Stopper H, et al. Diabetes Metab Res Rev. 2008; 24: 371-7.
10. Shoeb M and Ramana KV. Free Radic Biol Med. 2012; 52: 182-90.
11. Katare RG, Caporali A, et al. Circ Heart Fail. 2010; 3: 294-305.
12. Wu S and Ren J. Neurosci Lett. 2006; 394: 158-62.
13. Frank T, Bitsch R, et al. Eur J Clin Pharmacol. 2000; 56: 251-7.
14. Beltramo E, Berrone E, et al. Diabetes Metab Res Rev. 2004; 20: 330-6.
15. Du XL, Edelstein D, et al. Proc Natl Acad Sci U S A. 2000; 97: 12222-6.
16. Hammes HP, Du X, et al. Nat Med. 2003; 9: 294-9.
17. Stirban A, Negrean M, et al. Diabetes Care. 2006; 29: 2064-71.
18. Goh SY and Cooper ME. J Clin Endocrinol Metab. 2008; 93: 1143-52.
19. Sakurai S, Yonekura H, et al. J Am Soc Nephrol. 2003; 14: S259-63.
20. Monnier VM, Kohn RR, et al. Proc Natl Acad Sci U S A. 1984; 81: 583-7.
21. Babaei-Jadidi R, Karachalias N, et al. Diabetes. 2003; 52: 2110-20.
22. Stracke H, Hammes HP, et al. Exp Clin Endocrinol Diabetes. 2001; 109: 330-6.
23. Haupt E, Ledermann H, et al. Int J Clin Pharmacol Ther. 2005; 43: 71-7.
24. Woelk H, Lehrl S, et al. Alcohol Alcohol. 1998; 33: 631-8.
25. Winkler G, Pal B, et al. Arzneimittelforschung. 1999; 49: 220-4.
26. Stracke H, Gaus W, et al. Exp Clin Endocrinol Diabetes. 2008; 116: 600-5.
27. Pan X, Gong N, et al. Brain. 2010; 133: 1342-51.
28. Alkhalaf A, Klooster A, et al. Diabetes Care. 2010; 33: 1598-601.
29. Araki M, Hama T, et al. Vitamins (Japan). 1963; 28: 132-143.
30. Geyer J, Netzel M, et al. Int J Vitam Nutr Res. 2000; 70: 311-6.
31. NIH. Benfotiamine [INN:DCF:JAN], RN: 22457-89-2. [(2012; Retrieved April 25, 2012, 2012.
32. Stirban A, Negrean M, et al. Diabetes Care. 2007; 30: 2514-6.
33. Stracke H, Lindemann A, et al. Exp Clin Endocrinol Diabetes. 1996; 104: 311-6.
34. Anon. Altern Med Rev. 2006; 11: 238-42.
What is Silicon Dioxide and how is it produced?
Silicon dioxide is the most abundant mineral in the Earth’s crust, and it is found across the world in various forms. Silicon dioxide (SiO2) in its pure form is colorless to white. Precipitated synthetic amorphous silicas are obtained from a process essentially using sand.
Precipitated silica is a safe (non-crystalline) mineral. According to the relevant United States and European Union standards, precipitated silica is non-hazardous with regard to manufacture, transportation and handling. Precipitated silica is an inert powder and a certified food and feed additive.
Do you test your products for heavy metals and pesticides, etc.?
We receive Certificates of Analysis from all our ingredient suppliers. These certificates specify the maximum allowable amounts for any impurities and report the precise amounts of impurities present. We always strive to use the purest ingredients available.
Is Benfotiamine derived from garlic?
No, Benfotiamine is a fat-soluble derivative of Vitamin B1, produced through synthesis.
Is Benfotiamine a co-enzyme?
Benfotiamine is converted into a coenzyme (TDP) once in the body.
What is HPLC?
HPLC stands for "High Performance Liquid Chromatography." This is an analytical lab testing method that is used to quantify the active ingredients. It is considered to be a very sensitive and accurate test. HPLC testing is a tool recognized as a quality benchmark for herbal extracts.
Since Doctor's Best does not manufacture its supplements, how are the purity and integrity of supplements verified? In addition, how are your prices lower than other brands? Does this mean that quality is being compromised?
Doctor's Best supplements are manufactured in the US at cGMP (current Good Manufacturing Practice) certified facilities. All of our manufacturers and suppliers go through our vendor qualification program, which includes inspections and testing, before we agree to work with them. Our finished products have also been tested at the raw material level, in process, and as a finished product to ensure safety and quality. We place the highest importance on safety and quality and do not compromise for the sake of a better price point. The price points are lower because of production size and the overall business structure. We also place great importance on making our supplements available and affordable to those who need them most.
What is the source of the cellulose found in the some of the Doctor’s Best products?
The cellulose is made from alpha cellulose from softwood pulp. This softwood pulp may be derived from hemlock, Spruce or other soft woods.
What is cellulose and modified cellulose produced from?
Vegetarian capsules are made from cellulose, a non-animal product, which complies with cultural and/or vegetarian requirements. The capsules are certified with Kosher and Halal. Cellulose is derived from high quality wood pulp.
Why is silicon dioxide used as an excipient in DRB products?
Silicon Dioxide is commonly used as a flow agent in supplements. It also works as an anti-caking agent, and is added as an ingredient in foods, many multivitamins and mineral supplements because silicon is necessary for good health and is a necessary nutrient for the health of skin, hair, nails and bones.
Should I be concerned when I see that Silicon Dioxide has been used as an excipient in DRB products?
According to numerous studies reviewed to date on this long-term Generally Recognized As Safe (GRAS) listed food additive, the following was found:
The oral toxicity in mice is greater than (>) 5 grams/kilogram of body weight (Kimmerle 1968), or greater than 350 grams in one dose in humans based on allometric comparisons between mice and humans.
A single dose of 2.5 grams of amorphous polymeric silicon dioxide to human volunteers did not significantly raise the SiO2 excretion in the urine thus suggesting poor absorption of the compound (silicon dioxide)--(Langendorf 1966). Less than one one-hundredth (1000th) of the dose was found in urine, suggesting extremely poor absorption--(Langendorf 1966).
This would suggest that there is no scientific reason to eliminate silicon dioxide as an excipient at the very low levels found in dietary supplements.
For further information re: Silicon dioxide, see "Minerals, Trace Elements and Human Health, 4th Edition."
What are the other ingredients and why are they used?
These are used as flow agents and aid in the production to keep the machinery running smoothly and the capsules filling correctly. Similarly for the croscarmellose sodium, which is cellulose (sourced from the cell walls of green plants), and is used to help the tablet to dissolve in the stomach.
Is there a limit to how many vitamins can be taken safely in one day?
While our bodies need vitamins and minerals, like other things, if taken in large amounts they may adversely affect health. Large amounts of anything can be toxic. It is important to follow all label directions and discuss any concerns with your physician.
I am somewhat confused on how to take the DRB products. On many of the labels the Suggested Adult Use will list something along the lines of: Take 2 capsules daily, but it does not state whether they should be taken together or separately. What is the correct usage?
Unless otherwise specified on the label, the product may be taken together or separately.
What is modified cellulose and is it safe?
The cellulose is derived from alpha cellulose from softwood pulp. This softwood pulp may be derived from hemlock, spruce or other soft woods. It is made by cooking raw plant fiber in an aqueous solution to separate the cellulose, and then purified. It then goes through extra processing to further break down the fiber. The finished product contains no residual solvents. Excipients are needed to make the materials flow into the capsule and are extremely minute in amounts and are safe.
Are there any safety concerns for Benfotiamine?
Benfotiamine has an excellent tolerability profile and adverse events attributed to long-term use are extremely rare. Benfotiamine is fat-soluble and more bioavailable and physiologically active than thiamin. Persons allergic to thiamin should not take.
What’s the difference between Benfotiamine and plain old Vitamin B1?
Benfotiamine is an analog of thiamin (Vitamin B1). However, when we take supplemental thiamin, the absorption and metabolism is limited. By increasing the relative levels of thiamin in the body, Benfotiamine enhances enzyme activity that inhibits the production of advanced glycation end products (AGEs). Studies suggest an ability of benfotiamine to help maintain normal blood vessel and nerve structure.