Benfotiamine Powder CAS 22457-89-2

Benfotiamine powder is an organic compound with the molecular formula C19H23N4O6PS, CAS 22457-89-2, The appearance is white crystalline powder. Insoluble in water and methanol, insoluble in ethanol, insoluble in ether and chloroform. Dissolved in sodium hydroxide and sodium carbonate, slightly soluble in dilute hydrochloric acid solution. Thiamine ≤ 0.1%, heavy metals ≤ 20ppm, moisture ≤ 1.0%, melting point 200 ℃. It is a lipid soluble derivative of vitamin B1. Apart from its physical and chemical properties being different from water-soluble vitamin B1, its structural difference lies in the presence of an open thiazole ring, which forms physiologically active vitamin B1 through closed-loop action in the body.
After ingestion of phenylphosphoramide, the maximum blood concentration of vitamin B1 is about 5 times higher than that of vitamin B1 intake, the maximum bioavailability is about 3.6 times that of vitamin B1 intake, and it is higher than other fat soluble vitamin B1 derivatives. Research on humans and animals has shown that compared to water-soluble vitamin forms, phenylphosphoramidite has higher bioavailability and biological activity. Compared with vitamin B1, phenylphosphoramide produces higher peak and total concentrations of vitamin B1 and its phosphate in plasma, whole blood, red blood cells, and tissues, and has a longer plasma half-life. The relative bioavailability increased more significantly in muscle tissue (5-fold) and brain (25-fold), and also increased by 10-40% in other tissues such as liver and kidney.

Synthesis method of Benfotiamine powder. The synthesis process of preparing anti diabetes drug phenylphosphamide from raw thiamine through several steps such as phosphorylation and thiazole ring opening. Phosphorus oxychloride is used as the phosphorylation reagent. Under the control of appropriate temperature and other conditions, the raw thiamine is phosphorylated in a short time to obtain phenylphosphamide. Finally, phenylphosphamide is obtained through ring opening, benzoylation and other steps. The synthetic process has the advantages of high raw material conversion, low cost, high product purity and greatly shortened production cycle, and is suitable for industrial production.

Benfotiamine powder is a fat soluble thiamine (vitamin B1) derivative, which can be converted into physiologically active vitamin B1 after entering the human body. Compared with water-soluble vitamin B1, phenylphosphamide has higher biological activity and its bioavailability is about 3.6 times. The increase of relative bioavailability in muscle tissue (about 5 times) and brain nerve (about 25 times) is more significant, and its plasma half-life is also longer. Therefore, it is helpful to overcome the defect of low absorption and utilization rate of thiamine and play a more therapeutic role.

The existing drugs for the treatment of diabetes can only control the plasma glucose level, while phenylphosphothiamine can decompose and convert the glucose molecules entering the cells and reduce the glycotoxicity (advanced glycation end products). This biochemical process is realized by the production of transketolase stimulated by thiamine diphosphate. Advancedglycation end products (ages) are the pathological basis of all complications of diabetes.

In Europe, thiamine diphosphate has been used as a prescription drug for decades. It can inhibit diabetes neuropathy and related complications such as retina and kidney, improve microvascular function, reduce numbness and nerve tingling in the end limbs such as feet and hands, and inhibit or relieve all organs involved in neuroregulation such as cardiovascular, gastrointestinal function, periodontal and reproductive system. In conclusion, thiamine diphosphate has become the key nutrition to control the complications of diabetes. In the United States, thiamine diphosphate was approved by FDA as a dietary supplement at the beginning of this century.

Benfotiamine has a wide range of applications in the pharmaceutical field. As a lipid soluble derivative of vitamin B1, it improves the low bioavailability of water-soluble vitamin B1, increases the concentration of vitamin B1 in blood and tissues, and enhances its therapeutic effect.

Treatment of diabetes and its complications

 

1. Overview of diabetes
Diabetes is a metabolic disease, mainly manifested as hyperglycemia. Long term hyperglycemia can lead to various complications, such as neuropathy, kidney disease, retinopathy, etc. These complications seriously affect the quality of life of patients and even endanger their lives.

2. Role in the treatment of diabetes and its complications
Research shows that it can reduce blood sugar and can be used for the treatment of diabetes. By increasing the concentration of vitamin B1 in the blood, it helps to improve insulin secretion and utilization, thereby reducing blood sugar levels. In addition, it can also alleviate diabetes patients' thirst, polyuria and other symptoms, and improve peripheral neuropathy and other diabetes complications. Although it is usually impossible to achieve the goal of radical cure of diabetes, it can be used as an auxiliary treatment to help patients better control their condition.

 

Treatment of neuropathic pain

1. Overview of neuropathic pain
Neuropathic pain is a type of pain caused by damage or dysfunction of the nervous system. This type of pain usually manifests as stabbing pain, burning sensation, numbness, etc., seriously affecting the patient's quality of life. There are various causes of neuralgia, including diabetes neuropathy, postherpetic neuralgia, etc.

2. The role in the treatment of neuropathic pain
As a derivative of vitamin B1, it has the effect of improving nervous system function. By increasing the concentration of vitamin B1 in the blood, it helps to repair damaged nerve tissue and alleviate nerve pain. Research shows that it has significant effect in the treatment of diabetes neuropathy, post herpetic neuralgia and other neuralgia.

Adjuvant therapy for multiple neuritis and peripheral neuropathy

1. Overview of Multiple Neuritis and Peripheral Neuritis
Polyneuropathy and peripheral neuropathy are common inflammatory diseases of the nervous system. These diseases usually manifest as numbness, stabbing pain, weakness, and even paralysis in the limbs. There are various causes of polyneuropathy and peripheral neuropathy, including infections, autoimmune diseases, etc.

2. The role of adjuvant therapy in multiple neuritis and peripheral neuropathy
As a derivative of vitamin B1, it has the effect of improving nervous system function. By increasing the concentration of vitamin B1 in the blood, it can help alleviate symptoms of polyneuropathy and peripheral neuropathy, promote the repair and regeneration of nerve tissue. Therefore, it can be used as one of the auxiliary treatment methods for these diseases.

Adjuvant therapy for myocarditis

1. Overview of myocarditis
Benfotiamine powder is a inflammatory disease caused by viral infection, autoimmune response, and other factors. Myocarditis usually presents with symptoms such as palpitations, chest tightness, and fatigue, and in severe cases can even lead to heart failure.

2. The role of adjuvant therapy in myocarditis
As a derivative of vitamin B1, it has the effect of improving the function of myocardial cells. By increasing the concentration of vitamin B1 in the blood, it can help alleviate the symptoms of myocarditis and promote the repair and regeneration of myocardial cells. Therefore, it can be used as one of the adjuvant treatments for myocarditis.

Benzathiamine is a fat soluble derivative of thiamine (vitamin B1). Because of its higher bioavailability and longer half-life in vivo, it is widely used as an auxiliary treatment for diabetes, neuropathy and other diseases. Although its safety has been recognized in most studies, there are still some populations that may experience adverse reactions.

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