|Place of Origin:||China|
|Model Number:||orlistat for weight loss|
|Minimum Order Quantity:||1kg|
|Delivery Time:||1-3work days|
|Payment Terms:||T/T, Western Union, MoneyGram|
|Supply Ability:||5000kg per Month|
|Name:||Orlistat For Weight Loss||CAS:||96829-58-2|
|EINECS:||639-755-1||Solubility:||DMSO: 19 Mg/mL|
|Melting Point:||<50 °C||Specific Rotation:||D20 -32.0° (c = 1 In Chloroform)|
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Orlistat is globally recognized as a new type of weight-lowering lipid, the product name sold in the Saini market, first listed in New Zealand in 1998 for $ 146 million, sold for $ 538 million in 2007, and currently holds 80% market share in the world slimming market. China is the only Hong Kong Kong sales reach 80 million a year.
Orlistat is a long-lasting and gastrointestinal lipase inhibitor, white or white room temperature powder, insoluble in chloroform, soluble in ethanol, and inactivated by covalent bonds with active gastric lipase and pancreatic serine sites. The lumen of the abdomen and small intestine. Fats in the diet can not be broken down into free fatty acids and monoacylglycerol, so it can not be used to absorb fat, thereby reducing the body's calorie intake and controlling weight. The drug works without proper absorption.
This can prevent up to 30% fat absorption at regular doses. After oral administration, it is rarely absorbed and can be metabolized and deactivated in the intestine. The metabolic site is located in the gastrointestinal wall, and the elimination half-life is approximately 14 ~ 19 hours. Approximately 97% of the product is excreted in the feces, of which 83% is excreted in its original form. Arlistat can be used for obesity and hyperlipidemia. Typically, 120 mg can be taken orally three times a day or 1 hour after a meal. Weight loss can begin after 2 weeks of medication. It can be taken continuously for 6 - 12 months, if the dose is increased to more than 400 mg daily, the effect will no longer increase.
The lipase inhibitor, orlistat, is a hydration product of lipase that reduces fat intake in foods and leads to weight loss.
This product has strong selective effects on gastric lipase and pancreatic lipase, and has no effect on other digestive enzymes (amylase, trypsin, chymotrypsin) and phospholipase, and does not affect carbohydrates, proteins, and phospholipids. Absorbed.
The drug is not absorbed by the gastrointestinal tract and has the potential to inhibit lipase.
Orlistat covalently binds to serine residues in the active sites of gastric lipase and pancreatic lipase, inhibits the hydrolysis of triacylglycerols, and reduces the absorption of free glycerides and fatty acids, thus reducing controlling body weight, by which The enzyme in the gastrointestinal tract is inactive.
The medication activity of orlistat is dose dependent, and the therapeutic dose of orlistat (120 mg / d, tid, taken at meal time) combined with a balanced low-calorie diet decreased by 30%.
Studies of volunteers with normal weight and obesity have shown that orlistat is predominantly bodyless, and the plasma density of the drug is extremely low. Plasma orlistat density is <5 ng within 8 hours after oral administration. Ml dose (single dose) of 800 mg).
At the therapeutic dose, orlistat or short-term treatment usually have almost no systemic absorption.
In vitro, orlistat binds to plasma proteins in a ratio greater than 99% (lipoproteins and albumin are the major binding proteins), and orlistat rarely binds to red blood cells.
Studies in obese patients have shown that plasma contains two major metabolites, M1 (4-cyclo lactone hydrolyzate) and M3 (M1 (M1) linked to orthoyl leucine lysate). Lysates), making up 42% of the total plasma. Resolution.
M1 and M3 have very weak inhibitory effects on lipase.
Unchecked orlistat is mainly contraindicated in feces, accounting for about 97% of the dose used, and the main drug is 83%. The chronic renal excretion of orlistat and its metabolites is less than 2%, and total excretion (feces and urine) takes 3-5 days.
M1 and M3 can be banned throughout the bill.
This product also has the function of regulating blood lipids: it can reduce serum triglyceride (TG), low-density lipoprotein cholesterol ldl-c, and increase the ratio of high-density lipoprotein to low-density lipoprotein .
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 mass.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).
|Storage||In an airtight container, protected from light.|
|Items of analysis||Specification||Results|
|Appearance||while to off-while powder||White powder|
|Identification||HPLC retention time||Conforms|
|Melting Point||42 ºC -45°C||42°C-44°C|
|Specific optical rotation||-31.0°~-41.0°||-36.0°|
|Purity by HPLC||no less than 99.0%||99.8%|
|Total impurity||no more than 2.0%||1.4%|
|Max Individual impurity||no more than 0.5%||0.32%|
|Water content%(K&F)||no more than 0.5%||0.1%|
|Residual solvents||EtOH no more than 0.5%||N.D|
|EtAC no more than 0.5%||N.D|
|n-Heptane no more than 0.5%||less than 0.12%|
|Residue on ignition||less than 0.2%||0.10%|
|Assay (HPLC)||no less than 99.0%||99.80%|
|Conclusion||Conforms with Specification|