Pharmaceutical Raw Materials Orlistat Powder CAS 96829-58-2 for Loss Weight and Fat Burner

Pharmaceutical Raw Materials Orlistat Powder CAS 96829-58-2 for Loss Weight and Fat Burner

Ollistat belongs to lipase inhibitor kind of slimming medicine, it is lipstatin (lipstatin) hydration derivative, can reduce the absorption of food fat, so as to reduce weight. This product has strong and selective inhibition of gastric lipase and pancreatic lipase, and has no effect on other digestive enzymes (amylase, trypsin, chymotrypsin) and phospholipase, and does not affect the absorption of carbohydrates, proteins and phospholipids. The drug was not absorbed by gastrointestinal tract and the inhibition of lipase was reversible.

Orlistat inactivates the enzyme primarily in the gastrointestinal tract by covalently binding to serine residues at the active sites of gastric lipase and pancreatic lipase, inhibits the hydrolysis of triacylglycerol, and reduces the intake of mono-glycerol and free fatty acids, thereby controlling body weight. The pharmacological activity of orlistat was dose-dependent. A therapeutic dose of orlistat (120 mg/ d, tid, taken with meals) combined with a slightly low-calorie balanced diet reduced dietary fat absorption by 30%. Studies in normal-weight and obese volunteers have shown that orlistat is largely unabsorbed by the body and the plasma concentration of the drug is low, with a plasma concentration of < 5ng/ml within 8h of a single dose (maximum dose 800mg) taken orally. Generally, systemic absorption of orlistat at therapeutic doses is minimal and short-term treatment does not accumulate. In vitro experiments, the binding rate of orlistat to plasma proteins was as high as 99% (lipoprotein and albumin were the main binding proteins), and orlistat rarely bound to red blood cells. Studies in obese patients have shown that minimally absorbed orlistat has two major metabolites in plasma, M1(4-cyclolactone ring hydrolysate) and M3(M1 with an n-formylleucine lysate attached), accounting for 42% of total plasma concentrations. The inhibition of LIPase by M1 and M3 was very weak. Unabsorbed orlistat is excreted mainly through the stool, accounting for approximately.

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