TIANFU-CHEM - Lansoprazole CAS NO.103577-45-3

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Product Details

Keywords

Lansoprazole
103577-45-3
C16H14F3N3O2S

Quick Details

ProName: TIANFU-CHEM - Lansoprazole
CasNo: 103577-45-3
Molecular Formula: C16H14F3N3O2S
Appearance: Solid
Application: Organic synthesis
DeliveryTime: PROMPT
PackAge: IN 25kg drums
Port: SHANGHAI
ProductionCapacity: 10 Metric Ton/Month
Purity: 99.0%
Storage: In Room Temperature
Transportation: As per MSDS
LimitNum: 1 Gram
Heavy metal: N/A
Grade: Industrial Grade,Food Grade,Pharma Gra...

Superiority

Henan Tianfu Chemical Co., Ltd. is located in Zhengzhou High-tech Development Zone with import and export license.

We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013.The objective of the company is to put quality first and put our customer’s needs first - the satisfaction of our customers is the company's ultimate goal.

Improving product quality and service level is our responsibility, and creating more value for our customer’s is our purpose. We are constantly striving to make Henan Tianfu a leading chemical supplier, and hope to create a better future with you.

Details

Lansoprazole Basic information

Brief Introduction Uses Gastric acid secretion inhibitor Pharmacokinetics Marketing internationally Clinical application Drug interactions Adverse reactions Cautions

Product Name: Lansoprazole

Synonyms: LANSOPRAZOLE, RELATED COMPOUND A2-[[[3-METHYL-4-(2,2,2-TRIFLOUROETHOXY)-2-PYRIDYL]METHYL]SULFONYL]BENZIMIDAZOLE USP STANDARD;LANSOPRAZOLE, MM(CRM STANDARD);LANSOPRAZOLE USP(CRM STANDARD);2-[3-METHYL-4-(2,2,2-TRIFLUORO-ETHOXY)-PYRIDIN-2-YLMETHANESULFINYL]-1H-BENZOIMIDAZOLE;Lansoprazole99.5%;A-65006, AG-1749, Agopton, Lansox, Lanzor, Limpidex, Ogast, Prevacid,;1H-Benzimidazole, 2-3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinylmethylsulfinyl-;LANSORAZOLE

CAS: 103577-45-3

MF: C16H14F3N3O2S

MW: 369.36

EINECS: 2017-001-1

Product Categories: Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;Ion Pump Inhibitors;Monovalent Ion Channels;Voltage-gated Ion Channels;ATPase;Pharmaceutical Intermediates;API Reference StandardFree Base API;Other APIs;pharmaceutical

Mol File: 103577-45-3.mol

Lansoprazole Structure

Lansoprazole Chemical Properties

Melting point 178-182°C dec.

storage temp. 2-8°C

form powder

color off-white

Merck 14,5362

CAS DataBase Reference 103577-45-3(CAS DataBase Reference)

Safety Information

Hazard Codes Xi

Risk Statements 36/37/38

Safety Statements 26-36

WGK Germany 2

RTECS DD9487500

Hazardous Substances Data 103577-45-3(Hazardous Substances Data)

MSDS Information

Provider Language

2-[[3-Methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-1H-benzoimidazole English

SigmaAldrich English

Lansoprazole Usage And Synthesis

Brief Introduction Lansoprazole is in a class of drugs called proton pump inhibitors (PPI) which prevent the stomach from producing gastric acid.The other drugs in PPI family include:

rabeprazole (Aciphex),

omeprazole (Prilosec),

pantoprazole (Protonix),

esomeprazole (Nexium).

Proton pump inhibitors are used for the treatment of conditions such as ulcers, gastroesophageal reflux disease (GERD) and Zollinger-Ellison syndrome that are caused by stomach acid. Lansoprazole, like other proton-pump inhibitors, blocks the enzyme in the

wall of the stomach that produces acid. By blocking the enzyme, the production of acid is decreased, and this allows the stomach and esophagus to heal.

Uses Lansoprazole is a proton pump inhibitor (PPI) similar to omeprazole that inactivates the hydrogen/potassium-stimulated ATPase pumps in parietal cells, thus inhibiting gastric acid secretion and increasing intragastric pH. It is a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. Dexlansoprazole is an isomer of lansoprazole that has a similar spectrum of activity and toxicities. Lansoprazole therapy is associated with a low rate of transient and asymptomatic serum aminotransferase elevations and is a reported, but very rare cause of clinically apparent liver injury.

Lansoprazole's plasma elimination half-life is not proportional to the duration of the drug's effects (i. e. gastric acid suppression). The plasma elimination half-life is 1. 5 hours or less, and the effects of the drug last for over 24 hours after it has been given for 5 days or more.

Lansoprazole is a prescription medicine used to treat:

gastroesophageal reflux disease (GERD)

erosive esophagitis

stomach ulcers

duodenal ulcers

H. Pylori infections

Zollinger-Ellison syndrome

Gastric acid secretion inhibitor R-(+)-Lansoprazole is the dextroisomer of lansoprazole and a kind of anti-ulcer drug. It is the substitution product of benzimidazole derivative byimporting the fluorine element in the molecular structure and the is the second proton pump inhibitor after omeprazole. R-(+)-Lansoprazole has a better inhibitory effect for gastric acid secretion than that of other drugs (omeprazole, pantoprazole, rabeprazole) and it can significantly inhibit ulcer. It has a better Curative effect for ethanol-induced gastric mucosa lesion and acid hypersecretion induced duodenal ulcer than that of famotidine and omeprazole. In addition, This product also has an anti-Helicobacter pylori effect similar to that of Bismuth preparations and can be used to treat reflux esophagitis and Zollinger-Ellison syndrome.

pharmacodynamics

R-(+)-Lansoprazole can transform into active sulfonamide derivatives. In the tubule acidic environment of parietal cells, which are connected to the sulfydryl of H+-K+-(ATP)adenosine triphosphatase(the last step of the enzyme catalyzed gastric acid secretion process),passivat H+-K+-ATP enzyme and Inhibit the gastric acid secretion regulated by central and peripheral nervous systems. The inhibition effect of gastric acid secretion of this product is at least as strong as omeprazole. In vivo studies of animal model have demonstrated that the inhibition effect for gastric acid secretion of R-(+)-Lansoprazole is inferior to H2 receptor antagonist ranitidine and famotidine, but just as effective as omeprazole. Unlike the H2 receptor antagonist, whether taken in the morning or evening, this product can inhibit gastric acid secretion during the day and night. It can also reduce the gastric acid secretion, inhibit the secretion of pepsin and its activity and clear pyloric campylobacter on gastric mucosa (A bacterium of causing recurrence. of peptic ulcer).

It can also be used to treat Helicobacter pylori infection, alongside antibiotics as adjunctive treatment, to kill H. pylori causing ulcers or other problems involves using two other drugs known as "triple therapy", and involves taking twice daily for 10 or 14 days lansoprazole, amoxicillin, and clarithromycin.

Pharmacokinetics When this product transform into active AG-1812 and AG-2000, R-(+)-Lansoprazole in serum is metabolized quickly and completely into two main faeces: Lansoprazole sulfone and hydroxy orchid sola. About 14%~23% of doses are excreted in the urine as conjugated and non-conjugated hydroxylation metabolites and no prototype of this product is found. The half-life of this product is 1.3~1.7 h, about 2 h for elderly people and as long as 7 h for patients with severe liver failure. The Peak blood concentration can reach 1038μg/L within 2 h after taking 30 mg enteric capsules of this product.

Marketing internationally The lansoprazole molecule is off-patent and so generic drugs are available under many brand names in many countries;there are patents covering some formulations in effect as of 2015.

Since 2009, lansoprazole has been sold over the counter (OTC) in the U.S. in a marketed by Novartis as Prevacid 24HR. In Australia, it is being marketed by Pfizer as Zoton.

Clinical application Applied to reflux esophagitis, gastric ulcer, duodenal ulcer. Patients with duodenal ulcer take this product 30 mg a day for a period of 2～4 weeks. An cure efficiency rate of 75%～100% can be achieved.It cures faster than famotidine and omeprazole and reduces ulcers-induced pain faster thanranitidine. Taking this product 30 mg a day can effectively treat reflux esophagitis and the cure rates after 4 weeks and 8 weeks can reach 63%～84% and 85%～92% respectively. The cure effect for reflux esophagitis of this product is better than ranitidine and comparative to omeprazole. After 4 weeks treatment, the alleviation effect for heartburn symptoms of this product is much better than that of ranitidine and omeprazole. R-(+)-Lansoprazole can effectively treat patients with Peptic ulcer and reflux esophagitis whom cannot be cured by H2 receptor antagonist. A cure rate of 69%～100% can be achieved by taking this product 30 mg a day for a period of 8 weeks. A higher cure rate can be achieved if the dosage is increased to 30mg a day.

Drug interactions 1. Take R-(+)-Lansoprazole in conjunction with acetaminophen can increase the Peak blood concentration and shorten the time to peak.

2. Take R-(+)-Lansoprazole in conjunction with Roxithromycin can increase the local concentration of the latter and has a synergistic effect when treating Hp infection.

3. Take R-(+)-Lansoprazole in conjunction with antacids can reduce the bioavailability of this product. If necessary, this product should be taken after 1 hour use of antacids.

4. Take R-(+)-Lansoprazole in conjunction with theophylline can slightly reduce the blood concentrations of theophylline.

5. R-(+)-Lansoprazole can inhibit gastric acid secretion significantly and persistently, thereby reduce the absorption of itraconazole and ketoconazole. So they should not be used at the same time.

6. Sucralfate may interfere the absorption of this product and reduce its bioavailability. So this product should be taken at least 30 minutes before taking sucralfate.

7. Take R-(+)-Lansoprazole in conjunction with clarithromycin may cause Glossitis, stomatitis and black tongue. Patients should pay attention to the change of oral mucosa , stop using clarithromycin and reduce the dose of this product if necessary.

Adverse reactions This product can cause constipation, diarrhea, dry mouth, abdominal distention, anemia, increased white blood cells and eosinophils, thrombocytopenia, elevated liver enzymes, headache, drowsiness, insomnia, skin rashes, itching, etc., and occasionally cause fever, increased total cholesterol and uric acid value, etc.

Cautions 1.This drug is forbidden for those who are allergic to this product, pregnant and lactant women. Patients with a history of drug allergy

and hepatic insufficiency should use this product with caution.

2.Elderly patients with medication must be closely observed

3.This product may mask the stomach cancer symptoms. Therefore, this product should be taken before excluding stomach cancer.

Chemical Properties White Crystalline Powder

Uses A H+,K+-ATPase inhibitor that displays antisecretory activity

Uses Treatment of gastroesophageal reflux disease (GERD), erosive esophagitis, duodenal ulcers, Helicobacter pylori (H. pylori) infections,stomach ulcers, prevention of stomach ulcers in those people taking non-steroidal anti-inflammatory drugs (NSAIDs), such

Uses For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.

Uses Used as a gastric proton pump inhibitor. An antiulcerative

Biological Activity H + ,K + -ATPase inhibitor (IC 50 = 6.3 μ M) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC 50 = 0.09 μ M for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacterial against Helicobacter pylori in vitro . Also blocks swelling-dependent chloride channel (ICIswell) in NIH3T3 fibroblasts. More potent than omeprazole (5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole ).

Lansoprazole Preparation Products And Raw materials

Raw materials Acetic acid glacial-->Thionyl chloride-->Acetic anhydride-->tert-Butanol-->Vanadium pentoxide -->2,3-Lutidine-->2-Mercaptobenzimidazole

Henan Tianfu Chemical Co., Ltd.