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Weight Loss Orlistat Powder For the Treatment of Obesity and Hyperlipidemia CAS 96829-58-2
|Melting point||<50 °C|
Orlistat blocks some of the fat which you eat, keeping it from being absorbed because of your body. Orlistat is used to aid in weight reduction, or to lessen the risk of regaining weight lost.
This medicine is employed together with a reduced-calorie diet. Orlistat is good for use only in grown-ups. Orlistat (prescription and nonprescription) is utilized with an individualized low-calorie, low-fat eating and working out program to help lose weight. Prescription orlistat is used in overweight people who can also have high blood pressure, diabetes, high-cholesterol, or coronary disease.
Orlistat is also used after weight-loss to help keep from gaining back that weight. Orlistat is within a class of medications called lipase inhibitors. It functions by preventing a number of the fat in foods eaten from being absorbed from the intestines. This unabsorbed fat will be removed from our bodies in the stool.
Orlistat is currently internationally recognized as a new type of weight loss lipid-lowering drugs with the marketed product being under the name of Xenical. It was first listed in New Zealand in 1998 with annual sale of $ 146 million at that time. In 2007, the sale reaches $ 538 million, Orlistat occupy 80% of the market share of the global weight-loss market with the annual sale of only China Hong Kong year reaching 80 million US dollars.
Orlistat is a long-acting and potent specific inhibitor of gastrointestinal tract lipase, appearing as white or white-like powder at room temperature and being insoluble in water, soluble in chloroform and easily soluble in ethanol. It can form covalent bonds with the active serine sites of the gastric lipase and the pancreatic lipase in the stomach and small intestine cavity, resulting in inactivation of the enzymes. Fat in food can’t be broken down into free fatty acids and monoacylglycerols so that the fat can’t be absorbed and utilized, thereby having reduced the body's calorie intake to control the body weight.
The drug does not need to be absorbed through the body. At normal doses, the absorption of fat can be inhibited by 30%. There is little absorption after oral administration. It can be subject to metabolic inactivation in the intestine with the metabolic sites located in the gastrointestinal wall. The elimination half-life is about 14 to 19 hours. About 97% of the goods are excreted with the feces, of which 83% are in the prototype.
Clinically orlistat can be applied to the treatment of obesity and hyperlipidemia. Under normal circumstances, it can be subject to oral administration at a dose of 120 mg for three times per day. Take it during the meal or 1 hour after a meal. After 2 weeks of administration, the body weight can begin to decline. It can be taken continuously for 6 to 12 months. If the dose is increased to above 400 mg daily, the effect will no longer be further enhanced.
Fat Loss Mechanism:
Orlistat is a drug that promotes loss of weight by preventing the digestion and absorption of fat in food. In the intestine, an enzyme called lipase (produced primarily by the pancreas) breaks apart fat in food so that it can be absorbed into the body. Orlistat blocks the action of lipase and thereby prevents the breakup and absorption of fat. Orlistat blocks absorption of about 25% of the fat in a meal. The unabsorbed fat is excreted in the stool.
This medication is used along with a doctor-approved reduced-calorie diet, exercise, and behavior modification program to help significantly overweight (obese) persons lose weight. Taking orlistat can also help prevent you from regaining the weight you have lost. Losing weight and keeping it off can reduce the many health risks that obesity causes, including heart disease, diabetes, high blood pressure, some forms of cancer, certain breathing problems, and a shorter life span.
Dietary fats need to be broken down into smaller pieces before the body can absorb them. Orlistat works by blocking the enzyme that breaks down fats in your diet. This undigested fat then passes out of your body in your bowel movement. Orlistat does not block the absorption of calories from sugar and other non-fat foods, so you still need to restrict your total intake of calories.
|Covalently-Bonded Unit Count||1|
|Isotope Atom Count||0|
|Undefined Bond Stereocenter Count||0|
|Defined Bond Stereocenter Count||0|
|Undefined Atom Stereocenter Count||0|
|Defined Atom Stereocenter Count||4|
|Heavy Atom Count||35|
|Compound Is Canonicalized||True|
|Exact Mass||495.392 g/mol|
|Monoisotopic Mass||495.392 g/mol|
|Topological Polar Surface Area||81.7 A^2|
|Rotatable Bond Count||23|
|Hydrogen Bond Acceptor Count||5|
|Hydrogen Bond Donor Count||1|
|Molecular Weight||495.745 g/mol|
Uses of Orlistat:
1) An antiobesity agent. A pancreatic lipase inhibitor. Antiobesity agent.
3) Orlistat is an antiobesity agent. Orlistat is an pancreatic lipase inhibitor.
4) Tetrahydrolipstatin (orlistat) is a semi-synthetic derivative of lipstatin, a metabolite isolated from Streptomyces toxytricini. Tetrahydrolipstatin acts as a potent, irreversible inhibitor of pancreatic lipase. In vivo, it blocks the absorption of triglycerides while allowing fatty acid absorption. Tetrahydrolipstatin is widely used for the treatment of obesity.
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