Omeprazole Raw Materials Powder

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Omeprazole Powder Usage and Synthesis.

Omeprazole is a proton pump inhibitor that can effectively inhibit the secretion of gastric acid, the market circulation of the trade names include an gastro-piprazole, omidrazole, subfonazole, Losec, methoxsulphonazole, wobbizole, Womeprazole, belongs to the class of acid-suppressing drugs, the common acid-suppressing drugs also include pantoprazole, rabeprazole, Esomeprazole, the mechanism of action is to selectively inhibit the secretory microtubules and tubular vesicles in the cytoplasm of the apical membrane of the gastric mucosal cells, H+,K+ ATPase.

The mechanism of action is to selectively act on the gastric mucosal wall cells, inhibit the activity of H+,K+-ATPase on the secretory microtubules and cytoplasmic tubular vesicles constituted by the apical membrane of the gastric wall cells, so as to effectively inhibit the secretion of gastric acid, with a rapid onset of action, and is suitable for the treatment of gastric ulcers, duodenal ulcers, reflux oesophagitis, and gastrinomas (Zuo - Ai syndrome).

However, it is important to note that overuse of acid-suppressing drugs such as omeprazole can lead to a decrease in the concentration of gastric acid, acidity is weakened, then the germs that enter the stomach may not be killed and enter the intestines, doubling the risk of intestinal infections with germs, and then diarrhoea may occur. Due to the lowering of stomach acid affects digestion, which in turn affects the intestinal absorption of calcium, iron and other trace elements and vitamins, leading to calcium deficiency in the body, prone to fractures.

Uses and functions of  Omeprazole.

1. For gastric and duodenal ulcers, stress ulcers, etc.

2. For reflux oesophagitis, gastrinoma.

3. This injection can also be used for:

① peptic bleeding, such as peptic ulcer bleeding, anastomotic ulcer bleeding, etc., as well as the prevention of upper gastrointestinal bleeding caused by severe diseases (such as cerebral haemorrhage, severe trauma, etc.) and after gastric surgery.

② Acute gastric mucosal injury complicated by stress or caused by non-steroidal anti-inflammatory drugs.

③ After general anaesthesia or major surgery and in comatose patients to prevent acid reflux and aspiration pneumonia.

4. Combined with amoxicillin and clarithromycin, or with metronidazole and clarithromycin, it can effectively kill Helicobacter pylori (Hp).

Proton pump inhibitors, i.e., inhibitors of intracellular H+-K+-ATPase in the wall cells. It has a strong and long-lasting effect of inhibiting gastric acid secretion caused by basal gastric acid and food, pentagastrin.

The effect is fast, reversible, and without H2 receptor antagonist-induced mental side effects. Used for gastric and duodenal ulcers, reflux or erosive oesophagitis, Zo-Edward's syndrome, etc. It is also effective in gastric and duodenal ulcers that are ineffective with H2 receptor antagonists.

Omeprazole is a proton pump inhibitor with a strong and prolonged inhibitory effect on gastric acid secretion in animals and humans.

It is used clinically for the treatment of peptic ulcer, reflux oesophagitis, Zollinger-Ellison syndrome, and eradication of Helicobacter pylori (HP) with satisfactory results.

Pharmacological Effects of Omeprazole.

omeprazole is a proton pump inhibitor used in the treatment of peptic ulcer and gastroesophageal reflux disease (GERD) and other diseases. It can specifically act on the site where the proton pump is located in the gastric mural cells and is converted to the active form of sulfenamide, which then irreversibly binds to the sulfhydryl group of the proton pump through the disulfide bond and generates the sulfenamide and proton pump (H+-K+-ATPase) complex, thus Inhibit the activity of this enzyme, so that the H+ in the wall cells can not be transported to the gastric cavity, blocking the final step of gastric acid secretion, which can make the amount of gastric acid in gastric juice greatly reduced.

Therefore, it has a strong and long-lasting inhibitory effect on gastric acid secretion caused by various reasons (e.g. basal gastric acid secretion and gastric acid secretion induced by histamine, pentagastrin and stimulation of vagus nerve, including gastric acid secretion caused by dibutyryl cyclic adenosine acid, which can not be inhibited by H2 receptor-blocking drugs). .

This is related to the irreversible nature of the inhibitory effect of the product on the proton pump, and the acid secretion can be restored only after the formation of a new proton pump.

Omeprazole was developed by AstraZeneca Pharmaceuticals of Sweden and first marketed in Sweden in 1988 under the trade name Losec, and by 1992 had been approved and used in 65 countries and regions, and was listed as the number one best-selling drug in the world for three consecutive years from 1998 to 2000, and its sales in 2002 were US$5.2 billion.

Production method of Omeprazole Powder.

3,5-Dimethyl-2-hydroxymethyl-4-methoxypyridine was chlorinated to produce 2-chloromethyl-3,5-dimethyl-4-methoxypyridine.4-Methoxy 1,2-phenylenediamine was reacted with potassium xanthate to produce 2-mercapto-5-methoxybenzimidazole, which in turn was reacted with pyridine derivatives obtained above to produce 2-[(3,5-dimethyl-4-methoxy-2-pyridinyl)methylthio ]-5-methoxy-1H-benzimidazole, and finally oxidised with m-chloroperbenzoic acid in chloroform at 5°C to give omeprazole. The crude omeprazole can be recrystallised with acetonitrile.

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