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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.
Use of Benfotiamine.
Fenphothiamine, a fat-soluble derivative of vitamin B1, improves the low bioavailability of water-soluble vitamin B1 and increases the concentration of thiamine in the blood and tissues, thereby improving the efficacy.
Phenylphosphothiamine has been widely listed in the United States, Japan, Europe and other parts of the world, its listed dosage forms are tablets, granules and other dosage forms, indications are:
(1) For the prevention and treatment of vitamin B1 deficiency;
(2) It is used to supplement when the demand for vitamin B1 is increased and the intake from food is insufficient (fatigue, hyperthyroidism, pregnancy, lactation, strenuous physical labor, etc.);
(3) For the treatment of non-alcoholic Wernicke encephalopathy;
(4) for the treatment of beriberi;
(5) for the treatment of the following diseases, presumably 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 motor dysfunction.
Pharmacological action of Benfotiamine.
Fenphothiamine is a fat-soluble derivative of thiamine and has higher bioavailability than thiamine, but it must be dephosphorylated by alkaline phosphatase to become a fat-soluble precursor before it can cross the cell membrane to exert its biological effect. Clinically, it is mainly used for the treatment of diabetic complications, especially for the treatment and prevention of diabetic retinopathy. Compared with other thiamine derivatives, this product is absorbed more quickly and completely after oral administration. Phenfothiamine is absorbed into the systemic circulation and is rapidly metabolized into thiamine without increasing the concentration of the drug in the brain, while hippuric acid is produced and excreted in the urine.
Product Method of Bulk Benfotiamine Powder.
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