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CAS NO.96829-58-2
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Product Name: Orlistat
Product Details:
ProductName
|
Orlistat |
Molecular Formula
|
C29H53NO5 |
Molecular Weight
|
495.7348 |
CAS Registry Number
|
96829-58-2 |
Density
|
0.976g/cm3 |
Boiling point
|
615.9°C at 760 mmHg |
Refractive index
|
1.469 |
Flash point
|
326.3°C |
Vapour Pressure
|
4.23E-15mmHg at 25°C |
Assay
|
99% |
Appearance |
White or white powder |
Description:
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.
The effectiveness of orlistat in promoting weight loss is definite, though modest. Pooled data from clinical trials suggest that people given orlistat in addition to lifestyle modifications, such as diet and exercise, lose about 2-3 kilograms (4.4-6.6 lb) more than those not taking the drug over the course of a year.Orlistat also modestly reduces blood pressure, and appears to prevent the onset of type 2 diabetes, whether due to weight loss itself or to other effects; in a large randomized controlled trial, orlistat was found to reduce the incidence of diabetes by nearly 40% in obese people.
Orlistat is a semi-synthetic derivative of lipstatin , a metabolite isolated from Streptomyces toxytricini . Orlistat acts as a potent , irreversible inhibitor of pancreatic lipase . In vivo , it blocks the absorption of triglycerides while allowing fatty acid absorption .
Orlistat is widely used for the treatment of obesity as weight loss steroids .Biological Activity Hypolipemic pancreatic , gastric and carboxylester lipase inhibitor . Exhibits no activity at phospholipase A 2 , liver esterase , trypsin and chymotrypsin . Inhibits the thioesterase domain of fatty acid synthase , leading to cell cycle arrest at the G 1 /S boundary in vitro . Prevents the absorption of approximately one third of fat from food and exhibits pro-gastrokinetic , antiobesity and antihypercholesterolemic activity in vivo .
Application:
Orlistat (also known as tetrahydrolipstatin) is a drug designed to treat obesity. The effectiveness of orlistat in promoting weight loss is definite, Orlistat also modestly reduces blood pressure, and appears to prevent the onset of type 2 diabetes. 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.
The effectiveness of orlistat in promoting weight loss is clear, albeit moderately. The pooled data from clinical trials show that people who give olivide have less than 2-3 kilograms (4.4-6.6 pounds) of medication than a year, except for changes in lifestyle such as diet and exercise. Is also a modest reduction in blood pressure, it seems to be able to prevent the onset of type 2 diabetes, whether due to weight loss itself or other effects; in a large randomized controlled trial, orlistat he was found in obese people will reduce the incidence of diabetes by nearly 40%
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).
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.
COA:
Items
|
Standard | Results |
Description
|
White to kind of white powder | kind of white powder |
Melting point
|
193.0-200 | 196.0-198.9 |
Water
|
5-6.5% | 5.6% |
Solubility
|
Soluble in methanol | Complies |
PH
|
4.0-6.0 | 5 |
Heavy Metals
|
<10ppm | Complies |
Assay
|
>96% | 99.2% |
Residue on ignition
|
<0.1% | 0.03% |
Single impurity
|
<0.2% | 0.19% |
Conclusion |
Up to the Standard USP 32. |
Dosage:
1) Usual Adult Dose for Obesity:
120 mg orally three times a day with each main meal containing fat. The dose may be taken during the meal or within 1 hour of completing the meal.
Your daily intake of fat, carbohydrate and protein should be distributed over three meals. This means you will usually take one capsule at breakfast, one at lunch and another at dinner. To gain optimal benefit, avoid the intake of food containing fat between meals, such as biscuits, chocolate and savory snacks.
2) Usual Pediatric Dose for Obesity:
12 years or older:120 mg orally three times a day with each main meal containing fat.
The dose may be taken during the meal or within 1 hour of completing the meal.
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