Pharmaceutical raw materials Powder Omeprazole

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Omeprazole Usage and Synthesis.

Omeprazole is a proton pump inhibitor, which has a strong and long-term inhibitory effect on gastric acid secretion in animals and humans. It is used in the treatment of peptic ulcer, reflux esophagitis, Zollinger-Ellison syndrome, and eradication of Helicobacter pylori (HP), and has achieved satisfactory curative effect.

Omeprazole is a proton pump inhibitor, which has a strong and long-term inhibitory effect on gastric acid secretion in animals and humans. It is used in the treatment of peptic ulcer, reflux esophagitis, Zollinger-Ellison syndrome, and eradication of Helicobacter pylori (HP), and has achieved satisfactory curative effect. Suitable for peptic ulcer, reflux esophagitis and so on.

Proton pump inhibitors, or intramural H+-K+ -ATPase inhibitors. It has a strong and lasting inhibitory effect on the secretion of gastric acid caused by basic gastric acid, food and pentapeptide gastrin. The effect is rapid, reversible, and there are no psychogenic side effects induced by H2 receptor antagonists. It is used for gastric and duodenal ulcers, reflux or erosive esophagitis, and Zauberg-Ehlberg syndrome. It is also effective for gastric and duodenal ulcers that do not respond to H2 receptor antagonists.

Uses of Omeprazole.

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

2. For reflux esophagitis and gastrinoma.

3. This injection can also be used for: ① gastrointestinal bleeding, such as peptic ulcer bleeding, anastomotic ulcer bleeding, etc., and to prevent severe diseases (such as cerebral hemorrhage, serious trauma, etc.) and upper gastrointestinal bleeding caused by gastric surgery. ② Acute gastric mucosal injury caused by non-steroidal anti-inflammatory drugs or concurrent stress. ③ After general anesthesia or major surgery and coma patients to prevent acid reflux and aspiration pneumonia.

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

Pharmacological action of Omeprazole.

omeprazole (omeprazole) is a proton pump inhibitor used to treat diseases such as peptic ulcer and gastroesophageal reflux disease (GERD). It can act specifically on the site of the proton pump in gastric parietial cells, and is converted into the active form of sulfamide, and then irreversely binds to the sulfhydryl group of the proton pump through disulfide bonds. The formation of a complex of sulfamide and proton pump (H+-K+ -ATPase), thereby inhibiting the activity of this enzyme, so that H+ in parietal cells cannot be transported to the stomach cavity, blocking the last step of gastric acid secretion, which can greatly reduce the amount of gastric acid in gastric juice. Therefore, this product has a strong and lasting inhibitory effect on gastric acid secretion caused by various causes (such as basal gastric acid secretion and gastric acid secretion caused by histamine, pentagastrin and vagus stimulation, including the gastric acid secretion caused by dibutyl cyclic adenylate that cannot be inhibited by H2 receptor blocking drugs). This is related to the irreversibility of the inhibition effect of this product on the proton pump, and the effect of acid secretion can be restored only after the formation of a new proton pump.

Product method of Omeprazole.

3, 5-dimethyl-2-hydroxymethyl-4-methoxypyridine is chlorinated to form 2-chloromethyl-3, 5-dimethyl-4-methoxypyridine.

4-methoxy-1, 2-benzimidazole reacts with potassium xanthate to form 2-mercapto-5-methoxybenzimidazole, which reacts with the pyridine derivative obtained above to form 2-[(3, 5-dimethyl-4-methoxy-2-pyridyl) methylthioyl] -5-methoxy-1h-benzimidazole, which is finally oxidized in chloroform at 5℃ with m-chloroperbenzoic acid. You get omeprazole. Crude omeprazole can be recrystallized with acetonitrile.

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