High Quality Repaglinide Raw Powder

CAS:135062-02-1

MF:C27H36N2O4

MW:452.59

EINECS:629-921-1

Specification: 99% min Repaglinide Powder

Sample: Repaglinide Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Repaglinide Powder Usage and Synthesis.

Repaglinide is usually taken within 15 minutes before a meal and the dose should depend on the individual's blood glucose profile, with a recommended starting dose of 0.5mg and a maximum recommended single dose of 4mg taken with a meal. However, the maximum daily dose should not exceed 16mg.

It is used in type 2 diabetes mellitus where dietary control, weight reduction and exercise are not effective in controlling hyperglycaemia. Combination with metformin has a synergistic effect on glycaemic control.

Uses and functions of Repaglinide.

The mechanism of action of Repaglinide is mainly through the closure of potassium channels on the β-cell membrane, resulting in the inward flow of calcium ions and an increase in the intracellular concentration of calcium ions, thereby stimulating insulin secretion.

However, the receptor site of action with sulfonylureas is different, and the drug does not enter the β-cells, does not inhibit protein synthesis or does not directly cause the cytotoxic effect of insulin.

Its absorption and metabolism is rapid, the peak and half-life of the drug is about 1 hour, after taking the drug, plasma insulin concentration rises rapidly and significantly and leads to a significant drop in blood glucose. Therefore, this drug is taken with meals, not without meals, and is the so-called "meal-time blood glucose regulator". The dosage is 0.25g and 2g per dose.

Flexible dosing reduces hypoglycaemia caused by missed and delayed meals. After taking the drug for six months can reduce postprandial blood glucose 6mmol/L, reduce fasting blood glucose 4mmol/L, reduce HbAlc2%; compared with placebo can significantly improve blood glucose control.

Repaglinide is as effective as metformin on blood glucose in obese patients with type 2 diabetes, and is more effective in combination with metformin than alone. Safety studies have shown no severe hypoglycaemia or liver damage, few drug interactions and good patient tolerance.

Pharmacological Effects of Fenofibrate.

Monoamine oxidase inhibitors, non-selective beta-blockers, ACE inhibitors, non-steroidal anti-inflammatory drugs, salicylates, octreotide, alcohol and anabolic-promoting hormones may potentiate the hypoglycaemic effect of this product. beta-blockers may mask symptoms of hypoglycaemia.

Production method of Repaglinide Powder.

After converting compound (I) to its N-acetyl derivative, the (S)-type rotamer isomer was obtained by salt splitting with L-glutamic acid, and then reacted with compound (II) to form amide (III), which was then hydrolysed to give the product.