How to buy an expired patent
1. WHAT IS BENFOTIAMINE?
Benfotiamine is a lipid-soluble form of thiamine (vitamin B-1). It was developed in Japan in the early 1960's to treat alcoholic neuritis. It is the most effective metabolic precursor of active thiamine, or vitamin B1, available. One of the best description of benfotiamine I have found was assembled by AOR, a Canadian nutriceutical company: Abstracts & Summary Description of Benfotiamine. If you are interested in the benfotiamine molecule, you may view it here: Benfotiamine Molecule . You may also view the original U.S. patent for benfotiamine here: Adobe Version of Benfotiamine Patent .
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2. IS BENFOTIAMINE SAFE?
Though benfotiamine is lipid-soluble, it metabolizes quickly, producing high levels of thiamine pyrophosphate (TPP, the active form of thiamine), which then continues to metabolize in the body as usual. Benfotiamine itself does not accumulate in the body. The original patent filed in the United States on benfotiamine, Adobe Version of Benfotiamine Patent , included data from LD-50 tests on lab mice (Table III) indicating that benfotiamine is significantly less toxic than common vitamin B-1 (typically, thiamine hydrochloride). Thiamine hydrochloride has been the subject of much research. To quote from the European Commission Health and Consumer Protection Directorate General study on the tolerable upper intake level of vitamin B-1, paragraph 3. Hazard Identification:
"3.1. Evidence of adverse effects in humans. Orally ingested vitamin B1 has a long history of use as an oral supplement without reported adverse effects. Due to its therapeutic action in some frequently observed clinical syndromes, thiamine hydrochloride has been advised and used over a long period of time. There are no reports of adverse effects of oral thiamine, even at dosages of several hundred milligrams a day (SCOGS, 1978; DHEW, 1979; Marks, 1989).”
The entire EC study is available at: Tolerability of Thiamine (Vitamin B-1) . Again, vitamin-B-1 has proven safe after decades of public use and benfotiamine has been found to be significantly more tolerable than common vitamin B-1. Also, there are no known negative interactions between benfotiamine and other supplements or medications. However, there is information published by Ohio State University in 1996 and by the European Journal of Biochemistry in 2001 indicating thiamine supplementation should be carefully considered in patients undergoing therapy for tumorous forms of CANCER. These articles address thiamine in general (not specifically benfotiamine) but I find them relevant since benfotiamine is essentially a very effective form of thiamine. You may access that information here: OSU Article. EJB Abstract .
Otherwise, I believe there is minimal to nil downside in trying benfotiamine and the individual results have the potential to be quite significant. Still, it is wise and prudent to monitor your own reactions to any new supplement and adjust your dosage accordingly. In over 7 years I have had 2 or 3 reports of thiamine hypersensitivity and one report of excessive dosing. If you have a known sensitivity to thiamine, you should know that benfotiamine is a very potent metabolic precursor of active thiamine and dose it cautiously if at all. Symptoms of excessive dosing could include a feeling of warmth, weakness, sweating, nausea, restlessness, difficulty breathing, tightness of the throat or even bluish colored skin. If these symptoms occur you should immediately reduce your dosage or stop taking the product.
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3. HAVE THERE BEEN RECENT CLINICAL TRIALS USING BENFOTIAMINE?
Yes, in the past couple of years interest in this compound has grown significantly. You may link to some of the recent clinical trial abstracts here: Clinical Trials.
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4. HOW ABOUT INTERACTIONS WITH OTHER MEDICATIONS?
Benfotiamine has no known negative interactions with any medications. In fact, the use of some medications may cause a thiamine deficiency which benfotiamine would likely correct: Interactions.
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5. WHAT TYPE OF CONDITIONS MAY RESPOND WELL TO BENFOTIAMINE?
While the recent clinical trials have concentrated on conditions such as neuropathy, retinopathy and nephropathy, there is an expectation among those studying this compound that its beneficial effects may be far more wide-ranging, to include: sciatica, vascular health, general nerve health, improved blood pressure, general cellular protection, anti-aging, fibromyalgia, prevention of lactic acidosis, and treatment for Alzheimer’s disease. A most informative link on this topic is: Abstracts & Summary Description of Benfotiamine .
Benfotiamine is not just for diabetics. Any condition that is the result of a thiamine
deficiency will likely respond quite well to benfotiamine. Of course, any bodily function that is improved by a therapeutic level of thiamine would most likely be enhanced by benfotiamine, since benfotiamine is perhaps the most effective form of thiamine. Some interesting facts regarding thiamine can be found at this link: Thiamine Facts . More on thiamine can be found here: More Thiamine Facts.
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6. HOW MUCH BENFOTIAMINE SHOULD I USE DAILY?
Though the body cannot use more than about 10mg. of common, water-soluble vitamin B-1 per day, benfotiamine is lipid-soluble and can safely be used at much higher levels than common vitamin B-1.
Most people get excellent results in 14-21 days time using two 150mg. capsules twice per day (two in the morning and two in the evening). Benfotiamine need not be taken with meals. Some people get better results increasing the dosage to 900mg. or 1200mg. per day after the first two weeks. The point here is that benfotiamine is safe at any reasonable daily usage level. An individual should merely find the level that produces the maximum beneficial effect without reaching a point of diminishing return beyond which the excess amount is wasted.
Dr. Brownlee participated in a clinical trial using 600mg./day: Clinical Trial Using 600mg. Daily . As for me, I noted dramatic results after increasing daily usage to 600mg. My neuropathy symptoms ceased progression and began to reverse and I experienced a complete cessation of sciatica episodes. Also, my average blood pressure dropped from a persistent 145/90 to 120/80, without the use of other blood pressure medications. I now take four capsules in the morning and four in the evening, because I find that the higher dose further reduces my neuropathy symptoms without negative side effects. I would refer you to FAQ #2, above, for information on safety and upper daily limits.
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7. WHAT IS THE FDA POSITION ON BENFOTIAMINE?
At first I was curious as to whether benfotiamine is considered a drug or a supplement. I have established to my satisfaction (and based on the expert opinion of others in the industry) that benfotiamine, a synthetic derivative of vitamin B-1, is a dietary supplement under the Dietary Supplement Health and Education Act (DSHEA) of 1994. During 2003 I have successfully imported to the U.S. both bottled tablets as well as bulk benfotiamine, with full disclosure and full FDA and U.S. Customs review and approval at the respective U.S. ports of entry. Let me emphasize that. The FDA did a hands-on review and inspection of my imported benfotiamine, with full disclosure as to contents by both name and chemical formula, and approved all items for import. Benfotiamine may be imported under Tariff Number: 2936.22.00.00, (thiamine and its derivatives).
For those curious as to the current FDA stance on dietary supplements, I offer the following quote from their website:
“Under DSHEA, a firm is responsible for determining that the dietary supplements it manufactures or distributes are safe and that any representations or claims made about them are substantiated by adequate evidence to show that they are not false or misleading. This means that dietary supplements do not need approval from FDA before they are marketed .” See: http://www.cfsan.fda.gov/
dms/ds-oview.html . As to the safety of benfotiamine, please see the data provided above in this document.
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8. WHY HAVEN’T I HEARD OF BENFOTIAMINE BEFORE?
Though attempts were made by the Japanese pharmaceutical manufacturer Sankyo to market benfotiamine in the U.S. decades ago, there was little interest until the recent article published in the U.S. by Dr. Brownlee. Since that time, interest in benfotiamine has increased dramatically. I have heard some speculation that since the patent on benfotiamine expired years ago, no large company is interested in investing in its promotion. I personally remain mystified as to why this very beneficial compound has languished in obscurity in this country until now.
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9. WHAT DOES “PHARMACEUTICAL GRADE” MEAN?
“Pharmaceutical grade” means that the product has been manufactured under GMP conditions and is safe, pure and effective. Under GMP (Good Manufacturing Practices) every step of the process is documented by using established SOPs (Standard Operating Procedures). This includes training, equipment, raw materials, facilities, and final release criteria. Everything can be traced back to the date, time, person, lot number, and piece of equipment used.Source: www.benfotiamine.org