|Molecular Weight:||495.73||Molecular Formula:||C29H53NO5|
weight loss medication orlistat,
bitter orange extract synephrine
Top grade pure Orlistat powder CAS 96829-58-2 in raw material bulk
Orlistat is a potent and long-acting specific inhibitor of gastrointestinal lipase, by directly blocking the body's absorption of fat in the food intake of energy consumption and fat than once, natural reduction of body fat, so as to achieve the purpose of weight loss. It is safe to lose weight, the active ingredient does not enter the blood circulation, do not act on the central nervous system, with fewer side effects, no dizziness, palpitation, insomnia, dry mouth, and so on.
Orlistat, a lipase inhibitor, is a hydrated derivative of lipstatin, which reduces the absorption of fat from food and leads to weight loss.
This product has a strong and selective inhibition of gastric lipase and pancreatic lipase, no effect on other digestive enzymes (amylase, trypsin, chymotrypsin) and phospholipase, does not affect the absorption of carbohydrates, proteins and phospholipids.
The drug is not absorbed by the gastrointestinal tract and its inhibition of lipase is reversible.
Orlistat deactivates enzymes in the gastrointestinal tract by covalently binding to serine residues in the active sites of gastric lipase and pancreatic lipase, inhibits the hydrolysis of triacylglycerol, and reduces the intake of glycerides and free fatty acids, thereby controlling body weight.
The pharmacological activity of orlistat was dose-dependent, and the therapeutic dose of orlistat (120 mg/ d, tid, taken at mealtime) combined with a balanced diet with low calorie reduced dietary fat absorption by 30%.
Studies in normal weight and obese volunteers have shown that orlistat is largely not absorbed by the body and the plasma concentration of the drug is very low, with the plasma concentration of orlistat <5ng/ml within 8h after oral administration in a single dose (maximum dose 800mg).
There is usually little systemic absorption of orlistat at the treatment dose and no accumulation for short-term treatment.
In vitro, orlistat binds to plasma proteins at a rate of more than 99% (lipoprotein and albumin are the main binding proteins), and orlistat rarely binds to red blood cells.
Studies in obese patients have shown that the rarely absorbed orlistat has two major metabolites in plasma, M1(4-cyclolactone ring hydrolyzed product) and M3(M1 attached to an n-formyl leucine lysate lysate), accounting for 42% of the total plasma concentration.
The inhibition of lipase by M1 and M3 was very weak.
Orlistat, which is not absorbed, is excreted mainly through feces, accounting for about 97% of the dose taken, among which 83% is the primary drug. The cumulative renal excretion of orlistat and its metabolites is less than 2%, and complete excretion (feces and urine) requires 3-5d.
M1 and M3 can be excreted by bile.
This product also has the function of regulating blood lipid: it can reduce the serum triglyceride (TG), low-density lipoprotein cholesterol ldl-c and increase the ratio of high-density lipoprotein to low-density lipoprotein.
Orlistat in combination with a mildly low-calorie diet is recommended for long-term treatment of obese and overweight patients, including those who already have obesity-related risk factors.
This product has the long-term weight control effect (reduces the weight, maintains the weight and prevents the rebound).
Taking orlistat can lower the risk factors associated with obesity and the incidence of other diseases associated with obesity, including hypercholesterolemia, Ⅱ diabetes, reduce glucose tolerance, insulin hematic disease, high blood pressure, and can reduce the fat content of viscera.
|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%||99.5%|
|Total impurity||no more than 2.0%||1.6%|
|Max Individual impurity||no more than 0.5%||0.3%|
|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 0.1%|
|Residue on ignition||less than 0.2%||0.10%|
|Assay (HPLC)||no less than 99.0%||99.60%|
|Conclusion||Conforms with Specification|