CAS 96829-58-2 Weight Loss Raw Materials API Orlistat Tetrahydrolipstatin

Weight Loss Raw Materials powder Orlistat

The Introductction of Orlistat

(S)-2-FORMYLAMINO-4-METHYL-PENTANOIC ACID (S)-1-[[(2S,3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]-DODECYL ESTER;RO-18-0647;(-)-TETRAHYDROLIPSTATIN;ORLISTAT;N-FORMYL-L-LEUCINE (1S)-1-[[(2S,3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]DODECYL ESTER;XENICAL;(-)-Tetrahydrolipstatin(EquivalentToOrlistat);Orlipastat

Orlistat belongs to the lipase inhibitor class of weight loss drugs, which are hydrated derivatives of lipostatin that reduce the absorption of food fat, resulting in weight loss. This product has potent and selective inhibition of gastric lipase and pancreatic lipase, has no effect on other digestive enzymes (amylase, trypsin, chymase) and phospholipase, and does not affect carbohydrate, protein and phospholipid absorption. The drug is not absorbed by the gastrointestinal tract, and the inhibition of lipase is reversible.

Orlistat inactivates the enzyme mainly in the gastrointestinal tract by covalently binding to serine residues in the active sites of gastric lipase and pancreatic lipase, inhibiting triacylglycerol hydrolysis and decreasing the intake of monoglycerides and free fatty acids, thereby controlling body weight. Orlistat pharmacological activity was dose-dependent, and therapeutic doses of orlistat (120 mg / D, TID, taken at meals) combined with a slightly hypocaloric balanced meal reduced fat absorption by 30% of the meal. Studies in normal weight and obese volunteers have shown that orlistat is not essentially absorbed by the body and that drug concentrations in plasma are low, with plasma concentrations < 5 ng / ml within 8 h after a single dose (maximum dose 800 mg) administered orally. There is little systemic absorption of orlistat by the body at usual therapeutic doses and no accumulation with short-term treatment. Orlistat was found to bind more than 99% of plasma proteins in in vitro assays (lipoproteins, albumin being the major binding protein) and was rarely bound to erythrocytes. Studies performed in obese patients revealed that orlistat, which is minimally absorbed, has 2 major metabolites in plasma, M1 (product of 4-ring lactone ring hydrolysis) and M3 (product of one n-formylleucine cleavage attached to M1) accounting for 42% of total plasma concentrations. M1 and M3 showed extremely weak inhibition of lipase. Unabsorbed orlistat is mainly excreted in the feces, accounting for approximately 97% of the dose administered, 83% of which is the original drug, the cumulative renal excretion of orlistat and its metabolites is less than 2%, and complete excretion of the drug (feces and urine) takes 3-5 D. Both M1 and M3 can undergo biliary excretion.

The Function of Orlistat

Combined with micro low-calorie diet for obese and overweight participants including those already obesity-related risk factors of patients with long-term treatment. With long-term weight control (weight loss, maintain weight rebound and prevention) curative effect.

Orlistat (also known as tetrahydrolipstatin) is a drug designed to treat obesity. It is marketed as a prescription drug under the trade name by Roche in most countries, and is sold over-the-counter as by GlaxoSmithKline in the United Kingdom and the United States.Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. It is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

Orlistat is used for the treatment of obesity. The amount of weight loss achieved with orlistat varies. In one-year clinical trials, between 35.5% and 54.8% of subjects achieved a 5% or greater decrease in body mass, although not all of this mass was necessarily fat. Between 16.4% and 24.8% achieved at least a 10% decrease in body fat.After orlistat was stopped, a significant number of subjects regained weight-up to 35% of the weight they had lost.

The incidence of type 2 diabetes in an obese population over four years is decreased with orlistat (6.2%) compared to placebo (9.0%).Long-term use of orlistat also leads to a modest reduction in blood pressure (mean reductions of 2.5 and 1.9 mmHg in systolic and diastolic blood pressure respectively).

The COA of Orlistat