1. Introduction of Benfotiamine
Benfotiamine powder is an organic compound with molecular formula C19H23N4O6PS, molecular weight 466.45, chemical name: benzoic acid sulf-2 - [[(4-amino-2-methyl-5-pyrimidinyl) methyl] formamido] - 1 - [2 - (phosphoroxyethyl) - 1-propenyl] ester, and its appearance is white crystalline powder.
Phenylphosphorothiamine is a fat soluble vitamin B1 derivative. In addition to its different physical and chemical properties from water-soluble vitamin B1, its structural difference is that it has an open thiazole ring, which forms physiologically active vitamin B1 through closed-loop action in the body.
After ingesting phenylphosphorothiamine, the maximum plasma concentration of thiamine is about 5 times higher than that of vitamin B1 and the maximum biological availability is about 3.6 times as much as vitamin B1, and is higher than other fat soluble vitamin B1 derivatives. Human and animal studies have shown that, compared with water-soluble vitamins, the bioavailability and biological activity of phenylphosphorothiamine are higher. Compared with vitamin B1, in plasma, whole blood, red blood cells and tissues, the peak and total concentration of vitamin B1 and its phosphate produced by phenylphosphorothiamine are higher, and its plasma half-life is longer. The relative bioavailability in muscle tissue (5 times) and brain (25 times) increased more significantly, and in other tissues, such as liver and kidney, it also increased by 10-40%.
Adults take Thiamine Phenylphosphates and Thiamine Hydrochloride orally, and measure the amount of total vitamin B1 in blood, the increase of coenzyme vitamin B1 (thiamine pyrophosphate) and free vitamin B1 in blood. The results show that, compared with Thiamine Hydrochloride, Thiamine Phenylphosphates has the highest absorption in digestive tubes, the total vitamin B1 in blood maintains a high concentration, and the conversion rate of coenzyme vitamin B1 is also high.
Benfotiamine can increase the activity of the normally low-active enzyme (transketolase) and reduce the pathological damage of diabetic microvascular damage caused by the accumulation of two metabolites in the hyperglycemic state, thus attenuating the hyperglycemia-induced Oxidative damage to endothelial cells.
Product name |
Benfotiamine |
Extract source |
Fat soluble vitamin B1 derivative |
Extraction Solvent |
Water/Ethyl alcohol |
Appearance |
White crystalline powder |
Solubility |
Slightly soluble in water and methanol, almost insoluble in ethanol, insoluble in ether and chloroform. Soluble in sodium hydroxide, sodium carbonate and dilute hydrochloric acid solution |
Identification |
TLC , HPLC |
Sulphated Ash |
NMT 0.5% |
Heavy metals |
NMT 20 PPM |
Loss On Drying |
NMT 5.0% |
Powder size |
80Mesh, NLT90% |
Assay of L-Carnosine(HPLC test, percent, Standard in House) |
Min. 98.0% |
Microbiological Quality (Total viable aerobic count) |
|
- Bacteria, CFU/g, not more than |
NMT 103 |
- Moulds and yeasts, CFU/g, not more than |
NMT 102 |
- E.coli, Salmonella, S. aureus, CFU/g |
Absence |
Shelf life |
This product should be sealed and shaded, and stored in a dry, cool, and well-ventilated place. The validity period is 2 years |
2. Physical and chemical properties
Solubility: insoluble in water and methanol, insoluble in ethanol, and insoluble in ether and chloroform. Soluble in sodium hydroxide, sodium carbonate, and slightly soluble in dilute hydrochloric acid solution. Aizomine ≤0.1%, heavy metals ≤20ppm, moisture ≤1.0%, melting point 200 ° C.
Phenylene is a fat -soluble vitamin B1 derivative. In addition to the different physical and chemical properties and water -soluble vitamin B1, the difference in structure is that there is an open azole ring. Vitamin B1.
After intake of phenylphomamine, the maximum blood concentration of vitamin B1 is about 5 times higher than ingesting vitamin B1, and the maximum biological utilization is about 3.6 times that of vitamin B1 Essence Human and animal studies have proved that compared with the form of water -soluble vitamin, the biological utilization and biological activity of benphomine is higher. Compared with vitamin B1, in plasma, whole blood, red blood cells, and tissue, vitamin B1 and its phosphate peak and total concentration of phosphates produced by phenyl phthysemaine are higher, and their plasma half -life is longer. In muscle tissue (5 times) and the brain (25 times), it has increased significantly compared to biological utilization. In other tissues such as liver and kidney, 10-40%are also improved.
Popularity of phenylhenyline and hydrochloride, determine the increase in total vitamin B1 in the blood, coenzyme -type vitamin B1 (coke phosphoric acid) and ionized vitamin B1 in the blood. The most absorbed by the digestive tube, the total vitamin B1 in the blood maintains a high concentration, and the conversion rate of coenzyme -type vitamin B1 is also very high.
CAS Number | 22457-89-2 |
Density | 1.4±0.1 g/cm3 |
Boiling Point | 745.1±70.0 °C at 760 mmHg |
Melting Point | 165ºC |
Molecular Formula | C19H23N4O6PS |
Molecular Weight | 466.448 |
Flash Point | 404.4±35.7 °C |
Exact Mass | 466.107605 |
PSA | 191.05 |
LogP | 1.81 |
Vapour Pressure | 0.0±2.6 mmHg at 25°C |
Index of Refraction | 1.645 |
Storage condition | 2-8°C |
3. Benfotiamine Health Benefits
3.1 Benfotiamine May Help Improve Thiamine Deficiency
★Ataxia/poor motor control
★ confused
★edema/swelling
★irritability
★mood swings
★Nystagmus/uncontrolled eye movement
★Seizure
★Short-term memory loss
★ Tachycardia/rapid heart rate
3.2 Benfotiamine May Help Reduce Risk of Chronic Eye Disease
3.3. Benfotiamine May Help Improve Diabetes Symptoms
3.4. Benfotiamine May Help Alzheimer's Disease
3.5. Benfotiamine May Help With Kidney Disease
4. Indications of Benfotiamine powder
4.1 Benfluthiazine is a fat-soluble derivative of vitamin B1, which improves the bioavailability of water-soluble vitamin B1 and improves the healing effect by increasing the concentration of thiamine in blood and tissues.
Instructions are as follows:
(1) Prevent and treat vitamin B1 deficiency.
(2) When the demand for vitamin B1 increases and absorption of food is insufficient (fatigue, hyperthyroidism, pregnancy, lactation, intense physical labor, etc.), it is used for supplementation.
(3) use in the treatment of non-alcoholic Benick encephalopathy;
(4) used to treat athlete's foot;
(5) It is used to treat the following diseases known to be associated with vitamin B1 deficiency and metabolic disorders, such as neuralgia; myalgia, arthralgia; peripheral neuritis, peripheral nerve palsy; cardiometabolic disorders; constipation and other gastrointestinal power functions.
4.2 Application
Benfotiamine has been widely used in the field of medicine and health care, and its dosage form has been made into tablets/granules.
5.Vitamin B1 Derivative Benfotiamine Has Therapeutic Effect on Senile Dementia!
News from Shenzhen Special Zone, my country (Shenzhen Newspaper Group Shanghai correspondent Ma Xinfang) Alzheimer's disease is an age-related neurodegenerative disease with cognitive dysfunction such as learning and memory as the main clinical manifestations. A few days ago, Professor Zhong Chunjiu, deputy director of the Neurology Department of Zhongshan Hospital Affiliated to Fudan University, led the members of the scientific research team to discover for the first time that a vitamin B1 derivative, benfotiamine, has a therapeutic effect on senile dementia in the research on the treatment of senile dementia. The reporter learned from Fudan University yesterday that the research paper has been published in the international authoritative academic journal "Brain" and has obtained the national invention patent authorization.
According to reports, thiamine is an essential vitamin for the human body, and benfotiamine is a synthetic thiamine derivative with better bioavailability. In a related study, Zhong Chunjiu's research group injected thiamine derivatives, furathiamine and benfotiamine, into the stomachs of internationally accepted senile dementia model mice and treated them for 8 weeks. The results showed that benfotiamine had a good effect on improving spatial memory impairment in senile dementia model mice, and could reduce the number of senile plaques and neurofibrillary tangles in the brain, while furathiamine had no therapeutic effect. The researchers found through testing that thiamine itself has no effect on the treatment of Alzheimer's disease. Further studies have found that benfotiamine has a regulatory effect on the glucose metabolism signaling pathway (GSK-3) in the brain, that is, it plays a role by up-regulating the phosphorylation level of GSK-3 and reducing the activity of GSK-3.
6.A kind of production method of benfotiamine
The individual steps are:
1) When polyphosphoric acid reacts with vitamin B1, the reaction temperature is 80-130℃, the reaction time is 3-8 hours, and the weight ratio of vitamin B1 to polyphosphoric acid is 1:3-5;
2) After the above reaction, add water and hydrolysis at 80-120℃,the hydrolysis time is 2-10 hours,and the weight ratio of water to raw material vitamin B1 is 3-10;
3) After hydrolysis, reduce to room temperature, use the mixed solution of trioctylamine and organic solvent 1 as an extractant to extract the phosphoric acid in the system, remove the top phosphoric acid, and lower the concentration of phosphoric acid in the solution; The weight ratio of extractant to raw material 维生素 B1 is 3-5:1;
4) When the raw product of vitamin B1 phosphate monoester precipitates, organic solvent 2 is added, and its amount is 5-7 times the weight of vitamin B1 raw material;
5) The raw product is not cleaned and is directly beaten with water。After the PH value is adjusted to 8.0-14.0 with liquid alkali at 0-5℃, it reacted with benzoyl chloride for 2-3 hours. After the reaction, it is filtered,to obtain the filtrate。The filtrate is adjusted to 3.5-4.0 with concentrated hydrochloric acid to separate the solid, and then the solid is separated and dried to obtain a white solid, namely phenylthioamine; The dosage of benzoyl chloride is 1-2 times that of vitamin B1。
7. Why choose Kintai
8.Kintai manufacturing base
9.Our R&D center
10.Contact us
★If you want to get high quality Benfotiamine powder, please feel free to contact us at cheney@kintaibio.com or feedback in next page.
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