High Purity Bulk Rebeprazole sodium Powder

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Rebeprazole sodium Powder Usage and Synthesis.

Rabeprazole sodium is a proton pump inhibitor anti-ulcer disease drug, for the sodium salt form of rabeprazole, initially developed for the first time by the Japanese company Eisai, the trade name is Pollit, the role of proton pump inhibitors is to reduce the secretion of gastric acid to stabilise the site of the lesion, so as to achieve healing of gastric and duodenal ulcers and gastro-oesophageal reflux disease.

Clinically, it is mainly used for the treatment of acid-related diseases, such as gastric and duodenal ulcers ulcers, peptic ulcers, gastro-oesophageal reflux disease, and Drewe-Ayer's syndrome.

Rabeprazole is a benzimidazole substituent that inhibits gastric acid secretion by bonding to the proton pump of cells lining the stomach lumen.

It specifically inhibits the action of adenosine triphosphatase, a key enzyme in gastric acid production. It inhibits both basal gastric acid and gastric acid secretion induced by irritation.

Rabeprazole is a white-slightly yellowish-white powder, odourless, with a molecular weight of 381.43. It is extremely soluble in water or methanol, also in anhydrous ethanol or ethyl acetate, and practically insoluble in ether or ethane.

It does not show spin, has temperature absorption, its melting point is 225°C, and its partition coefficient in water/octane system at pH 7.0 is about 214.This product is a light yellow film-coated tablet (enteric-coated tablets).

Uses and functions of Rebeprazole sodium.

1、Active duodenal ulcer.

2, Benign active gastric ulcer.

3、Gastro-oesophageal reflux sign (GERD) with clinical symptoms of erosive or ulcerative nature.

4, Combined with appropriate antibiotics, it can eradicate Helicobacter pylori positive duodenal ulcer.

5, Maintenance therapy for erosive or ulcerative gastro-oesophageal reflux syndrome (GERD), the efficacy of which has not yet been evaluated for courses longer than 12 months.

Pharmacological Effects of  Rebeprazole sodium.

Rabeprazole sodium is converted to the active form (sulfinyl form) under acidic conditions in cells of the gastric lining, inhibiting the activity of H+,K+-ATPase and suppressing gastric acid secretion by modifying the sulfhydryl group of the proton pump (H+,K+-ATPase).The restoration of the activity of the H+,K+-ATPase is mainly due to the elimination of the drug from the site of action, and glutathione is probably also involved in the restoration of enzyme activity.

1, Human Pharmacology:

(1) Inhibition of gastric acid secretion: in healthy adult men, once daily oral administration of rabeprazole sodium tablets 10mg and 20mg significantly reduced gastric acid secretion induced by gastrin stimulation compared to the first day of administration. The average gastric acid secretion was reduced by 73% and 80% on the 1st and 7th day of oral intake of 10mg once a day, compared with that on the first day of intake; the average gastric acid secretion was reduced by 88-89% and 99% on the 2nd and 7th day of oral intake of 20mg once a day, respectively.

(2) Increase in intragastric pH: In healthy adult men, intragastric pH was significantly increased with oral administration of subdose of rabeprazole sodium tablets 10mg and 20mg daily. The proportions of pH values greater than 4 and 3 within 24 hours on day 4 of administration were 73% and 80%, respectively, at the administered dose of 10 mg, and 78% and 83%, respectively, at the administered dose of 20 mg.

2, Animal Pharmacology:

(1) Inhibition of H+,K+-ATPase in vitro: rabeprazole sodium inhibited H+,K+-ATPase prepared from porcine gastric mucosa.

(2) Inhibitory effect on gastric acid secretion: rabbit gastric gland gastric acid secretion induced by dibutyl cyclophosphate adenosine was inhibited by rabbit rabbit rabbit rabbit rabbit rabbit rabbit rabbit rabbit rabbit rabbit gastric gland gastric acid secretion by dibutyl cyclophosphate adenosine. In dogs with indwelling gastric fistula, rabeprazole sodium inhibited gastric acid secretion induced by histamine and pentagastrin; in rats, it inhibited basal gastric acid and gastric acid secretion induced by histamine.

(3) Anti-ulcer effect: For various experimental ulcers as well as experimental gastric mucosal lesions (induced by cold stimulation stress response, water immersion stress response, pylorus ligation, cysteamine or ethanol-hydrochloric acid) in rats, rabeprazole sodium showed significant therapeutic effects.

(4) Adjunctive use for eradication of H. pylori: In a gerbil animal model of H. pylori infection, rabeprazole sodium potentiated the synergistic effect of amoxicillin and clarithromycin by viable bacterial counts in gastric fluid. During the triple combination of rabeprazole sodium, amoxicillin and clarithromycin, rabeprazole sodium caused an increase in intragastric pH, which led to an increase in the antibacterial activity of amoxicillin and clarithromycin.

Formulation specifications of  Bulk Rebeprazole sodium Powder.

Tablet, 10mg, 20mg.This product is pure white powder, odourless. Easily soluble in water, methanol, can be dissolved in a small amount in pure alcohol and ether.

Peptic ulcer, gastro-oesophageal reflux disease, Droe-Ayer's syndrome, and so on.

H2 receptor antagonists and proton pump inhibitors are the 2 most commonly used drugs for the treatment of acid-related digestive diseases, they both elevate gastric pH, but proton pump inhibitors act on the H+/K+-ATPase, which strongly inhibits gastric acid secretion and produces a large and long-lasting elevation of gastric pH. Rebeprazole sodium is the newest proton pump inhibitor, and its anti-gastric acid secretion activity is greater than that of the original proton pump inhibitor, omeprazole. Compared with omeprazole, rabeprazole inhibits H+/K+-ATPase more strongly, and the inhibition can be recovered; it has a greater effect on plasma gastrin water than omeprazole.

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