Canagliflozin Hemihydrate CAS 928672-86-0 Raw Materials Powder

CAS: 928672-86-0

MF: 2(C24H25FO5S).H2O

MW: 462.53

EINECS: 202-303-5

Specification​: 99% min Canagliflozin Hemihydrate

Sample: Canagliflozin Hemihydrate Powder

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Portal:https://henrikang.en.made-in-china.com/

Canagliflozin Hemihydrate Powder Usage and Synthesis.

Canagliflozin Hemihydrate Powder is a hydrate of canagliflozin. Canagliflozin Hemihydrate CAS 928672-86-0 is a selective type 2 sodium glucose Canagliflozin Hemihydrate CAS 928672-86-0 is a selective type 2 sodium glucose transporter (SGLT-2) inhibitor that specifically inhibits renal reabsorption of glucose, allowing excess glucose to be excreted from the urine. Canagliflozin Hemihydrate Raw Materials was approved by the FDA on March 29, 2013 for the treatment of Canagliflozin Hemihydrate Raw Materials was approved by the FDA on March 29, 2013 for the treatment of type II diabetes under the trade name Invokana.

Application/Function of Canagliflozin Hemihydrate Powder.

Cagliflozin hemihydrate is an oral C-glycoside sodium-dependent glucose type 2 cotransporter (SGLT2) inhibitor originally developed by MitsubishiTanabePharma, which can lower glucose by blocking the reabsorption of glucose from the proximal tubule so that the filtered glucose is excreted from the urine.

Canagliflozin has the formula C24H25FO5S and the molecular weight 444.52.

Canagliflozin is the first FDA-approved SGLT2 inhibitor for the treatment of diabetes mellitus in adult patients. The glucose in the renal tubules is not reabsorbed into the bloodstream and is excreted in the urine, thus reducing the blood glucose concentration. As glucose is excreted into the urine via the kidneys, it is accompanied by side effects such as renal impairment, symptomatic hypotension, and fungal infections.

Nine clinical trials involving 10,285 patients have demonstrated the safety and efficacy of Invokana, both alone and in combination with other hypoglycemic drugs. In a 26-week, double-breeding controlled trial, 584 patients with type 2 diabetes were divided into three groups, namely the 100 mg capagliflozin group, the 300 mg capagliflozin group and the placebo group. Compared to placebo, the mean additional reduction in HbA1c was 0.91% in the 100 mg capagliflozin group and 1.16% in the 300 mg capagliflozin group.

Canagliflozin is available as anhydrous and hemihydrate, which can be identified as hemihydrate based on the marketed formulation, where the hemihydrate is available in both amorphous and pharmaceutical crystal form.

Production Method of Canagliflozin Hemihydrate Powder

The present invention discloses a method for the preparation of Canagliflozin Hemihydrate in pharmaceutical crystalline form, the steps of which are as follows.

• Step 1, take the raw material of canagliflozin, add organic solvent, heat and dissolve, then add water Cool to 30~40°C.
• Step 2, adding organic solvent under stirring condition or adding crystal seeds after stirring for 30~60 minutes.
• Step 3, stirring for 4-10 hours at a temperature of 10-30°C, filtering, collecting the crystals and drying under vacuum at 40-60°C to obtain the crystalline form of Cagliflozin that meets the requirements of pharmaceutical preparations with a purity of up to 99.9%. The invention greatly improves the yield of Cagliflozin crystalline form by strictly controlling the crystallization temperature, time and the amount of solvent used in the process. It is suitable for the industrial production of Cagliflozin because of the low cost and high purity of the product.