Glibenclamide Chemical Raw Materials CAS 10238-21-8 For Hypoglycemic Drugs

CAS 10238-21-8 Glibenclamide Raw Materials For Hypoglycemic Drugs

Description

Glibenclamide (INN), a sulfonylurea hypoglycemic drug. It is also commercially available in combination with metformin called Glucovance [1]. Glibenclamide inhibits hepatic glycogenolysis and gluconeogenesis by increasing portal vein insulin levels or acting directly on the liver, reducing liver production and output of glucose; oral absorption is fast, and the protein binding rate is very high, which is 95%. The plasma concentration reaches the peak within 2 to 5 hours, and the effect lasts for 24 hours. T1/2 is 10 hours. Metabolized in the liver, about 50% are excreted by the liver and kidney.

Glibenclamide releases insulin by stimulating islet β cells, and its action strength is 200 times that of tolbutamide, so the dose used is significantly reduced. Same as tolbutamide, but with stronger hypoglycemic effect.

① Promoting the secretion of insulin by pancreatic islet B cells, the prerequisite is that the pancreatic islet B cells still have a certain function of synthesizing and secreting insulin;

② By increasing the level of portal vein insulin or directly acting on the liver, inhibiting hepatic glycogenolysis and gluconeogenesis, The production and output of glucose by the liver is reduced;

③ it may also increase the sensitivity of extrapancreatic tissue to insulin and the utilization of sugar (maybe mainly through the post-receptor effect), so the overall effect is to reduce fasting blood sugar and postprandial blood sugar.

The product is mainly metabolized by the liver, 50% is excreted from the urine within 24 hours, and the effect can last for 15 to 24 hours.

Glibenclamide is rapidly and completely absorbed after oral administration, and the time to peak plasma drug concentration is 2 to 6 hours. The absorption is not affected by food. Take 1 hour earlier than meal. The action time is maintained for more than 16 hours, the plasma protein binding rate is about 99%, the apparent volume of distribution is 0.3L/kg, and the plasma half-life is 6-12 hours. Glibenclamide is completely metabolized in the liver into two hydroxy derivatives and another unidentified metabolite, of which 4-trans-hydroxyglibenclamide has 15% activity. 40% of the administered dose can be recovered in the feces within 48 hours, and then the excretion slows down, and the excretion can reach 95% after 5 days

Application

Glibenclamide is suitable for mild to moderate non-insulin-dependent diabetes mellitus whose curative effect is unsatisfactory with diet alone. Patients with pancreatic islet B cells have a certain function of secreting insulin and have no serious complications. Glibenclamide is used in non-insulin-dependent (adult, obese) diabetic patients. Due to the long clearance rate of glibenclamide, hypoglycemic reactions are most likely to occur, so it should be used with caution in clinical use, and it can be used for some patients whose hypoglycemic effect of gliclazide and glipizide is not obvious.