Benfotiamine is an organic compound, molecular formula C19H23N4O6PS, molecular weight 466.45, chemical name: Benzoate-sulfur-2 -[[(4-amino-2-methyl-5-pyrimidinyl) methyl] formamido -]-1-[2- (phosphacyloxyethyl) -1-propenyl] ester, appearance is a white crystalline powder.
Solubility: Insoluble in water and methanol, insoluble in ethanol, insoluble in ether and chloroform. Soluble in sodium hydroxide, sodium carbonate, slightly soluble in dilute hydrochloric acid solution. Thiamine ≤0.1%, heavy metal ≤20ppm, moisture ≤1.0%, melting point 200ºC.
Fenphothiamine is a fat-soluble vitamin B1 derivative, in addition to the physical and chemical properties and water-soluble vitamin B1 is different, the structural difference is that there is an open thiazole ring, in the body through closed-loop action to form physiologically active vitamin B1.
The maximum blood concentration of vitamin B1 is about 5 times higher and the maximum bioavailability is about 3.6 times higher than ingestion of vitamin B1 after ingestion of phenfothiamine, and is higher than other fat-soluble vitamin B1 derivatives. Human and animal studies have demonstrated a higher bioavailability and bioactivity of fenfothiamine compared to the water-soluble vitamin form. In plasma, whole blood, red blood cells, and tissues, fenphothiamine produces a higher peak and total concentration of vitamin B1 and its plasma half-life is longer than vitamin B1. Relative bioavailability increases were more significant in muscle tissue (5x) and brain (25x), and 10-40% in other tissues such as liver and kidney.
The increase of total vitamin B1 in blood, coenzyme vitamin B1 (thiamine pyrophosphate) and free vitamin B1 in blood was measured by oral administration of phenylphosphothiamine and thiamine hydrochloride in adults. The results showed that compared with thiamine hydrochloride, the absorption of phenylphosphothiamine in digestive tube was the highest, the concentration of total vitamin B1 in blood remained high, and the conversion rate of coenzyme vitamin B1 was also high.