We supply Rebamipide API

We offer high- quality Rebamipide API that's used in the expression of colorful pharmaceutical products. Rebamipide hydrate is a gastroprotective agent that can treat gastric ulcers, gastric mucosal injuries, and gastritis. Our Rebamipide is manufactured under strict quality control measures, icing its chastity, stability, and effectiveness. It's available in different amounts and can be customized to suit individual conditions. With our rich experience and moxie in the API assiduity, we're committed to furnishing dependable and cost-effective results to our guests. communicate us moment for further information on our Rebamipide powder.

What's Rebamipide API?

Rebamipide is a new type ofanti-ulcer medicine. It was first retailed in Japan in 1990 as a medicine for gastric ulcers and acute and habitual gastritis. it is a gastric mucosal defensive agent that can increase gastric mucosal blood inflow, conflation of prostaglandin E2, stashing of gastric mucus, promote expression of epidermal growth factor and its receptors, help ulcer circumstance, and promote ulcer mending. Research has shown that it's effective for colorful experimental gastric ulcers, can promote the product of prostaglandins in the gastric mucosa, cover the gastric mucosa from colorful ulcer causing factors, and is suitable for the treatment of gastric ulcers, acute gastritis, acute exacerbation of habitual gastritis, and gastric mucosal lesions, with high clinical operation value. Background With the wide operation of proton pump impediments( PPIs) and the eradication of Helicobacter pylori infection as the main treatment for gastric ulcers, the clinical mending rate of peptic ulcers is as high as 80 to 90. still, the problem of ulcer rush still needs to be answered urgently. In recent times, the relationship between ulcer mending quality and ulcer rush has been decreasingly valued.

Basic Information

Product Name: Rebamipide

CAS:90098-04-7

MF:C19H15ClN2O4

MW:370.79

EINECS:1308068-626-2

MDL No.:MFCD00866895

Structural formula:

Purity: 99%+

Origin: China

Application: Anti-Ulcer

Technical Specification

Package: 1kg;25kg

Storage conditions: Preserve in tight,light-resistant containers in a cool place

What is the pharmacological action of Rebamipide API?

The chemical structure of Rebamipide API contains amide groups on the benzyl para position and double bonds at positions 3 and 4 with carbonyl groups at position 2. It can dose-dependently inhibit neutrophil activation and production of reactive oxygen species, and effectively eliminate free radicals, thereby preventing damage to the gastric mucosa caused by free radicals. This product can also promote the synthesis of prostaglandins in the gastric mucosa and enhance the gastric mucosal barrier. In addition, this product inhibits the damage of Helicobacter pylori (Hp) to the gastric mucosa by preventing its adhesion to gastric epithelial cells, reducing oxidative stress, and lowering the concentration of cytokines produced by H. pylori. Animal experiments have shown that rabapet can eliminate free radicals within mucosal epithelial cells, significantly inhibit the production of O2- by neutrophils, and also have a scavenging effect on hydroxyl radicals. It can inhibit the production of Hp and chemokines. It can increase the synthesis of prostaglandins by inhibiting the damaging effect of bile acids on the gastric mucosa.

What is Pharmacokinetics of Rebamipide API?

Absorption and metabolism: After oral administration of 0.6g, the peak time of blood drug reached (1.95 ± 0.73) hours, the peak concentration of blood drug was (510.3 ± 152.0) ng/ml, and the elimination half-life was (1.75 ± 0.63) hours. According to data reports, after oral administration of 0.1g of ribavirin, the peak blood concentration reached 210ng/ml after about 2 hours, with a half-life of about 2 hours. About 10% of the dosage was excreted by urine. Multiple administration studies have shown that this product does not accumulate in the human body.

What is purpose of Rebamipide API?

Rebamipide powder is used for gastric ulcers; New anti ulcer drugs.

Indications

(1) The prevention and treatment of gastric mucosal damage caused by NSAIDs: Ribapamide has a significant reversal effect on the side effects of NSAIDs induced reduction in prostaglandin production and increased mucosal permeability in the gastric mucosa. Moreover, research has found that patients who take NSAIDs have high expression of HIF-1 in the gastric mucosal epithelium, indicating that the patient's gastric mucosa is in a state of hypoxia and ischemia; However, patients who took rebamiphene showed a significant decrease in HIF-1, indicating that rebamiphene has a good protective effect on the gastric mucosa of NSAIDs users. From this, it can be seen that rabapet may have a preventive and therapeutic effect on gastric mucosal damage caused by NSAIDs (especially non selective NSAIDs) drugs.

(2) According to Haruma et al.'s report on the treatment of HP related gastritis, in a clinical medication observation of 86 HP positive patients, 53 patients who took rebamiphene showed a significant reduction in infiltration of monocytes and neutrophils in the gastric antrum and body, and a significant reduction in gastric inflammation compared to those who did not take the medication, indicating that it has a good quality effect on HP related gastritis.

(3) Other studies have reported that gastric cancer patients who took rebamiphene before surgery had significantly lower body temperature and serum IL-6 levels than the control group three days after surgery, indicating that rebamiphene has a certain improvement effect on postoperative systemic inflammatory response syndrome in gastric cancer patients undergoing surgery; Rebapatite may become a new method for treating ulcerative colitis; It may become a new and effective therapeutic drug for Meniere's disease.

Production methods of Rebamipide API

1. Preparation of racemic ribavirin. Using 2 (1H) quinoline-4-carboxylate methyl ester (I) as raw material, it was reduced by lithium hydroborate to 2 (1H) quinoline-4-yl methanol (II), and then brominated with hydrobromic acid to form 4-bromomethyl-2 (1H) quinolinone (III). Dissolve diethyl acetaminomalonate (12.0g, 55mmo1) and metallic sodium (1.5g, 65mmo1) in 150ml anhydrous ethanol, heat to boiling, add (III) (12.0g, 50mmo1) with stirring, and reflux for 2 hours. Concentrate under reduced pressure and pour the remaining material into water. Filter and collect the precipitate, recrystallize with ethanol to obtain 13.0g of colorless prismatic crystalline compound (IV) with a yield of 69% and a melting point of 224-226 ℃ (decomposition). Compound (IV) (5.0g, 13mmo1) was suspended in 150ml of 20% hydrochloric acid and refluxed for 9 hours. Concentrate under reduced pressure until dry, and the remaining material is recrystallized with ethanol water to obtain 3.2g of colorless prismatic crystalline compound (V) with a yield of 89% and a melting point of 220-225 ℃ (decomposition). Compound (V) (2.7g, 10mmo1) and potassium carbonate (4.2g, 30mmo1) were dissolved in a mixed solution of 100rnl acetone and 20ml water. After cooling and stirring in an ice bath, p-chlorobenzoyl chloride (2.1g, 12mmo1) was dropped and stirred for another 2 hours. Evaporate acetone under reduced pressure, and acidify the remaining liquid with dilute hydrochloric acid. Filter and collect the precipitate, and recrystallize with methanol water to obtain 1.8g of white powdery Rebar Pat, with a yield of 49% and a melting point of 288-290 ℃ (decomposition).

2. Preparation of (-) - configuration. Derived from the separation of racemates. 21.6g of racemic ribavirin was suspended in 1100ml of methanol, and 23g of (-) - dimethylbrucine was added to form a clear solution. The solution was stirred at room temperature for 4 hours and then cooled overnight. Filter and collect precipitates, wash with cold methanol. Recrystallization 4 times yields 7.6g of pure salt[ α] D20+60.4 ° (C=1.0, chloroform). Add 10% hydrochloric acid to the methanol suspension of the salt, filter the precipitate, and wash with water. Then, the mixture was recrystallized three times with dimethylformamide water to obtain 1.6g of colorless needle shaped (-) - configuration ribavirin with a yield of 14.8% and a melting point of 305-306 ℃[ α] D20-116.7 ° (C=1.0, dimethylformamide).

3. Preparation of (+) - configuration. Dissolve the solid obtained from the first preparation of the (-) - configuration in methanol and add 10% hydrochloric acid. Filter the precipitate, wash it with water, suspend it in methanol, then add (-) - dimethylbrucine and stir at room temperature for 1 hour. Filter to remove insoluble substances and add concentrated hydrochloric acid to the filtrate. Filter and collect precipitates, wash with water. Recrystallize 4 times with dimethylformamide water to obtain 3g of colorless needle shaped crystalline (+) one configuration ribavirin with a yield of 27.8% and a melting point of 305-306 ℃ (decomposition)[ α] D20+116.9 ° (C=1.0, dimethylformamide).

Our Advantage

Rich experience: we have 13 Years of professional experience;

Customers all over the world: sell to more than 100 countries;

Provide diversified products: the products have been applied to all major international brands in the fields of drugs, dietary supplements, cosmetics, animal nutrition and functional food.

Price advance: low MOQ with competitive price;

Quality certification: ISO; Halal; Kosher certified

After-sales service: Professional team 7*24 hours customer service.

Contact Us

Yihui takes pride in being a trusted Rebamipide API manufacturer and supplier. To acquire this groundbreaking product or discuss your specific requirements, contact us immediately at sales@yihuipharm.com. Rest assured, with Yihui, you're accessing a product of unparalleled quality, backed by certifications that underscore our commitment to excellence in the global market.