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Orlistat

A new type of lipid - lowering drugs Pharmacological effects Indications Adverse reactions Drug interactions Dosage and Usage Precautions

CAS No.96829-58-2
Chemical Name:Orlistat
Synonyms:XENICAL;oristat;Olistat;ORLISTAT;Orlistate;Orlipastat;RO-18-0647;ORLIPASTATUM;Ro 18-0647/002;Orlistat Powder
CBNumber:CB2431985
Molecular Formula:C29H53NO5
Formula Weight:495.73
MOL File:96829-58-2.mol
Orlistat Property
mp : <50 °C
storage temp. : 2-8°C
solubility : DMSO: 19 mg/mL
form : solid
color : white
CAS DataBase Reference: 96829-58-2(CAS DataBase Reference)
Safety
WGK Germany : 3
RTECS : OH3167600
Hazardous Substances Data: 96829-58-2(Hazardous Substances Data)

Orlistat Chemical Properties,Usage,Production

A new type of lipid - lowering drugs
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. 
 the orlistat tablets produced by the Zhejiang HiSun pharmaceutical Co.
Figure 1 the orlistat tablets produced by the Zhejiang HiSun pharmaceutical Co.
Pharmacological effects
Orlistat belongs to lipase inhibitor class weight-loss drugs, which is the hydration derivatives of lipstatin, being able to reduce the absorption of food fats so that the weight will get lost. This product has a potent and selective inhibitory effect on gastric lipase and pancreatic lipase with no influence on other kinds of digestive enzymes (amylase, trypsin, and chymotrypsin) and phospholipase without affecting the absorption of carbohydrates, protein and phospholipids. The drug is not absorbed by the gastrointestinal tract with its inhibition on lipase being reversible.
Orlistat 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, inhibiting the triglyceride hydrolysis so that the monoglyceride and free fatty acid intake will decrease, thereby controlling the body weight. The pharmacological activity of orlistat is dose-dependent with a therapeutic dose of orlistat (120 mg / day, taken at mealtime) in combination with a low-calorie balanced diet being capable of reducing 30% of fat absorption in the diet. Studies on normal-weight and obese volunteers have shown that orlistat is not substantially absorbed by the body and that the concentration of the drug in the plasma is very low. After oral administration of a single dose (maximal dose of 800 mg), the plasma concentration of orlistat within 8 hours is lower than 5 ng / ml.
Generally under the treatment dose, the body has a low systemic absorption of the orlistat without accumulation during short-term treatment. In vitro experiments, orlistat has an as high as over 99% binding rate to the plasma protein (lipoprotein, albumin as the major binding protein). Orlistat can rarely bind to red blood cells. Studies in obese patients show that orlistat, which is seldom absorbed, has two major metabolites in plasma, M1 (hydrolyzate of the 4-lactone ring) and M3 (M1 attached with a N-formyl-l Lysine lysis product) account for 42% of the total plasma concentration. M1 and M3 have extremely week inhibitory effect on lipase. The unabsorbed orlistat was mainly excreted from the feces, accounting for 97% of the dose taken, 83% of which were prototype drugs, and the cumulative renal excretion amount of orlistat and its metabolites was less than 2%. It needs 3 to 5 days for thorough excretion (feces and urine) of drugs. Both M1 and M3 can be excreted through bile.
This product also has an effect of regulating blood lipids: being able to reduce serum triglyceride (TG) and the low density lipoprotein cholesterol (LDL-C) and increase the proportion of high-density lipoprotein and low-density lipoprotein in the serum of obesity patients.
Indications
This combination of this product with mild low-calorie diet is applicable to obese and overweight patients, including for the long-term treatment of patients who have been associated with obesity-related risk factors. This product has long-term effects of weight control (weight loss, weight maintenance and prevention of rebound). Administration of orlistat can reduce the incidence of obesity-related risk factors and other obesity-related diseases, including hypercholesterolemia, type 2 diabetes, impaired glucose tolerance, hyperinsulinemia, hypertension, and can also reduce the fat content in the organ.
Adverse reactions
There have reports of rare increase in aminotransferase, elevated alkaline phosphatase, and severe hepatitis associated with orlistat administration, together with cases of liver failure of which some patients require a liver transplant or can lead directly to death. There are also cases that orlistat leads to rare allergic reactions. The main clinical manifestations include itching, rash, urticaria, angioedema, bronchospasm and allergic reactions while the emergence of large herpes is very rare. Post-marketing monitoring also noted pancreatitis reported.
Drug interactions
It can reduce the absorption of the vitamin A, D and E. The application of this product can be supplemented at the same time. If you are taking vitamins A, D and E preparations (such as some of the compound vitamin class preparations), we should take the goods after taking 2 hours or at bedtime.
Patients with type 2 diabetes may need to reduce the dose of oral hypoglycemic agents (such as sulfonylurea drugs).
Combination with cyclosporine can cause decreased plasma concentration of latter one.
Combination with amiodarone may lead to reduced absorption and reduce the efficacy of the latter.
Dosage and Usage
This combination of Xenical (orlistat) with mild low-calorie diet is applicable to obese and overweight patients, including for the long-term treatment of patients who have been associated with obesity-related risk factors. This product has long-term effects of weight control (weight loss, weight maintenance and prevention of rebound). Administration of orlistat can reduce the incidence of obesity-related risk factors and other obesity-related diseases, including hypercholesterolemia and type II diabetes
Adults: The recommended dose is taking a 120 mg capsule during meal or within one hour after meal. If a meal is not into the food or no fat, you can omit a medication. Long-term use of treatment (including weight control and risk factors for improvement) is sustainable.
The patient's diet should be nutritionally balanced with slightly low heat. There is about 30% of heat coming from fat. The food should be rich in fruits and vegetables. The intake of fats, carbohydrates and protein should be distributed in three meals a day. There is no evidence that over three times daily /120mg per time can enhance the efficacy. No dose adjustment is required for the elderly.
Precautions
Because of the reports regarding rare acute hepatocellular necrosis or acute liver failure after the marketing of orlistat, some of which require a liver transplant or can directly cause death, the prescribing physician should instruct the patient that if any liver symptoms and signs of dysfunction (such as loss of appetite, itching, jaundice, dark urine, fecal color, upper right quadrant pain) occur, the patients should immediately discontinued orlistat and other suspicious drugs, and test liver function.
Chemical Properties
Off-White Solid
Usage
An antiobesity agent. A pancreatic lipase inhibitor. Antiobesity agent.
Usage
antidiabetic
Usage
Orlistat is an antiobesity agent. Orlistat is an pancreatic lipase inhibitor.
Usage
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.
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 progastrokinetic, antiobesity and antihypercholesterolemic activity in vivo .
Orlistat Preparation Products And Raw materials
Raw materials
Preparation Products
Orlistat Suppliers      Global( 222)Suppliers     
SupplierTelFaxEmailCountryProdListAdvantage
Nanjing Sunlida Biological Technology Co., Ltd. 025-58378339 18913321387025-57019371sales@sunlidabio.comCHINA 4966 55
DONGGUAN AOME BIOTECHNOLOGY CO.,LTD 137901327470769-870537452784729268@qq.comCHINA 61 50
Guangzhou Isun Pharmaceutical Co., Ltd 020-39119399 18927568969020-39119999isunpharm@qq.com, isunpharm@hotmail.comCHINA 4852 55
XiaoGan ShenYuan ChemPharm co,ltd Tell:86-712-2580635 Mobile:15527768850 . 1552776883686-712-2580625 QQ:1623551145sales02@farchem.comCHINA 9490 52
Taizhou DongBang Fine Chemical Co. Ltd. +86-0523-86235448 15996000437+86-0523-862354482535251509@qq.comCHINA 46 55
Taizhou Hoyoo Chemical Co.,Ltd 0576-88666163 150576003390576-88666163hoyoochem@yahoo.comCHINA 279 58
Wuhan Runzeweiye Technology Co., Ltd. 027-50779735 15172337137 QQ:940329747027-50779735runzeweiye999@163.comCHINA 772 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833+86-10-82849933jkinfo@jkchemical.com;market6@jkchemical.comCHINA 96843 76
Meryer (Shanghai) Chemical Technology Co., Ltd. +86-(0)21-61259100(Shanghai) +86-(0)755-86170099(ShenZhen) +86-(0)10-59487313(Beijing)+86-(0)21-61259102(Shanghai) +86-(0)755-86170066(ShenZhen) +86-(0)10-88580358(Beijing)sh@meryer.comCHINA 40407 62
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:1893055203786-21-503281093bsc@sina.comCHINA 15972 69
 
96829-58-2(Orlistat)Related Search:
Sibutramine hydrochloride Sibutramine N-FORMYL-L-LEUCINE (2S,3S,5S)-5-[(N-Formyl-L-leucyl)oxy]-2-hexyl-3-hydroxyhexadecanoic Acid (Orlistat Impurity) Orlistat-d3 Orlistat Impurity,(2S,3R,5S)-5-[(N-Formyl-L-leucyl)oxy]-2-hexyl-3-hydroxyhexadecanoic Acid (Orlistat Impurity) BETA-BUTYROLACTONE Orlistat Methyl Methanol 1,2-EPOXYTETRADECANE Basic Violet 1 L-tert-Leucine Methyl acrylate Acetonitrile Dodecyl alcohol Kresoxim-methyl Methylparaben
(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 Enzyme Inhibitors by Enzyme Enzymes, Inhibitors, and Substrates Enzyme Inhibitors XENICAL L to O Lipase, Pancreatic BioChemical Biochemicals and Reagents 96829-58-2 (-)-Tetrahydrolipstatin(EquivalentToOrlistat) C29H53NO5 Orlipastat Xenical, (-)-Tetrahydrolipstatin, N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl Ester, Orlistate Pharmaceutical Raw Materials Orlistat, Tetrahydolipstat ORLIPASTATUM Miscellaneous Biochemicals (-)-Tetrahydrolipstatin API Antiobesity Agent C25H53NO3 Ro 18-0647/002 Chiral Reagents Intermediates & Fine Chemicals Pharmaceuticals (-)-Tetrahydrolipstatin, Ro-18-0647, N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester L-Leucine, N-formyl-, (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester N-Formyl-L-leucine (1S)-1-[[(2S)-3α-hexyl-4-oxooxetan-2β-yl]methyl]dodecyl ester N-Formyl-L-leucine (S)-1-[[(2S)-3α-hexyl-4-oxooxetane-2β-yl]methyl]dodecyl ester Orlistat,()-Tetrahydrolipstatin, N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester, Ro-18-0647 Orlistat (200 mg) ORLISTAT (BULK MATERIAL) ORLISTAT PELLETS 50% Amino Acids & Derivatives Heterocycles Orlistat(synthesis) Orlistat(FerMentation) (S)-2-FORMYLAMINO-4-METHYL-PENTANOIC ACID (S)-1-[[(2S,3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]-DODECYL ESTER S,S,S,S-Orlistat (2S)-1-[(2S,3S)-3-hexyl-4-oxooxetan-2-yl]tridecan-2-yl (2S)-2-forMaMido-4-Methylpentanoate oristat ACTOS Orlipastat, Orlistat Other APIs N-formyl-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester L-Leucine Orlistat N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester Lipid-lowering medicine reducing weight Orlistat Powder Orlistat, >=98% Olistat Lipase Inhibitor, THL
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