Cas:96829-58-2 Orlistat powder
| product name |
Orlistat |
| cas number |
96829-58-2 |
| apperance |
White powder |
| Density |
1.0±0.1 g/cm3 |
| MF |
C29H53NO5 |
| MW |
495.735 |
Orlistat is a lipase inhibitor used to control obesity, which works by inhibiting the absorption of dietary fat.
Orlistat belongs to the lipase inhibitor class of weight-loss drugs. It is a hydration derivative of lipostatin (lipstatin), which can reduce the absorption of food fat, thereby reducing weight. This product has a strong and selective inhibitory effect on gastric lipase and pancreatic lipase, and has no effect on other digestive enzymes (amylase, trypsin, chymotrypsin) and phospholipase, and does not affect the performance of carbohydrates, proteins and phospholipids. absorb. The drug is not absorbed by the gastrointestinal tract, and its inhibitory effect on lipase is reversible.
Orlistat is mainly in the gastrointestinal tract by covalently binding to serine residues of gastric lipase and pancreatic lipase to inactivate enzymes, inhibit triacylglycerol hydrolysis, and reduce the intake of monoglycerides and free fatty acids. , So as to control weight. The pharmacological activity of orlistat is dose-dependent. A therapeutic dose of orlistat (120 mg/d, tid, taken with meals) combined with a low-calorie balanced diet can reduce 30% of the fat absorption in the diet. Studies in normal-weight and obese volunteers have shown that orlistat is basically not absorbed by the body, and the concentration of the drug in plasma is very low. After a single dose (maximum dose 800mg) is taken orally, the plasma concentration of orlistat within 8 hours is < 5ng/ml. The body's systemic absorption of orlistat is usually low at therapeutic doses, and short-term treatment does not accumulate. In in vitro experiments, the binding rate of orlistat to plasma proteins is as high as 99% (lipoprotein and albumin are the main binding proteins), and orlistat rarely binds to red blood cells. Studies conducted in obese patients have shown that orlistat, which is rarely absorbed, has 2 main metabolites in plasma, M1 (4-ring lactone ring hydrolysate) and M3 (M1 attached to an N-formyl bright Acid cleavage products) accounted for 42% of the total plasma concentration. M1 and M3 inhibited lipase very weakly. The unabsorbed orlistat is mainly excreted through feces, accounting for about 97% of the dose taken, of which 83% is the original drug, and the cumulative renal excretion of orlistat and its metabolites is less than 2%. The drug is completely It takes 3 to 5 days for excretion (feces and urine). Both M1 and M3 can be excreted via bile.
This product also has the effect of regulating blood lipids: it can reduce the serum triglycerides (TG) and low-density lipoprotein cholesterol LDL-C in obese patients and increase the ratio of high-density lipoprotein to low-density lipoprotein.
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