Solubility: insoluble in water and methanol, insoluble in ethanol, insoluble in ether and chloroform. Soluble in sodium hydroxide and sodium carbonate, slightly soluble in dilute hydrochloric acid solution. Thiamine ≤0.1%, heavy metal ≤20ppm, water ≤1.0%, melting point 200℃.
Benfotiamine is a fat-soluble vitamin B1 derivative. In addition to the physical and chemical properties that are different from water-soluble vitamin B1, the structural difference is that it has an open thiazole ring, which forms physiologically active vitamin B1 through ring closure in the body.
After ingestion of benfotiamine, the maximum blood concentration of vitamin B1 is about 5 times higher than that of ingested vitamin B1, and the maximum bioavailability is about 3.6 times that of ingested vitamin B1, and is higher than other fat-soluble vitamin B1 derivatives. Human and animal studies have shown that benfotiamine has higher bioavailability and biological activity than water-soluble vitamin forms. Compared with vitamin B1, benfotiamine produces higher peak and total concentrations of vitamin B1 and its phosphate in plasma, whole blood, red blood cells and tissues, and its plasma half-life is also longer. The relative bioavailability increases more significantly in muscle tissue (5 times) and brain (25 times), and in other tissues such as liver and kidney, there is also a 10~40% increase.
Adults took benfotiamine and thiamine hydrochloride orally, and the total vitamin B1 level in the blood, the increase in coenzyme vitamin B1 (thiamine pyrophosphate) and free vitamin B1 in the blood were measured. The results showed that compared with thiamine hydrochloride, benfotiamine was most highly absorbed in the digestive tract, the total vitamin B1 in the blood was maintained at a very high concentration, and the conversion rate of coenzyme vitamin B1 was also very high.
Benfotiamine is a fat-soluble derivative of vitamin B1. It improves the low bioavailability of water-soluble vitamin B1 and increases the concentration of thiamine in the blood and tissues, thereby improving the efficacy.
Benfotiamine has been widely marketed in the United States, Japan, Europe and other parts of the world. Its marketed dosage forms include tablets, granules and other dosage forms. The indications are:
(1) For the prevention and treatment of vitamin B1 deficiency;
(2) For the supplementation of vitamin B1 when the demand for vitamin B1 increases and the intake from food is insufficient (fatigue, hyperthyroidism, pregnancy, lactation, strenuous physical labor, etc.);
(3) For the treatment of non-alcoholic Wernicke's encephalopathy;
(4) For the treatment of beriberi;
(5) For the treatment of the following diseases that are presumed to be related to vitamin B1 deficiency and metabolic disorders, such as: neuralgia; muscle pain, joint pain; peripheral neuritis, peripheral nerve paralysis; myocardial metabolic disorders; constipation and other gastrointestinal motility disorders.
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