Rebamipide Capsules

1. Pharmacological action According to foreign literature reports: This product is a gastric mucosal protective drug, which has the effect of protecting gastric mucosa and promoting ulcer healing. (1) Inhibitory effect on experimental gastric ulcer and the effect of promoting healing This product can inhibit the gastric mucosal damage caused by water immersion stimulation ulcer, aspirin ulcer, indomethacin ulcer, serum-based ulcer, pylorus ligation ulcer and ischemia-reperfusion related to active oxygen, platelet activating factor (PAF), diethyldithiocarbamate (DDC), stress response, indomethacin, etc. in rats. It can also promote the healing of acetic acid ulcer in rats and inhibit the recurrence of ulcer 120 to 140 days after formation. (2) Inhibitory effect on experimental gastritis and the effect of promoting healing This product not only inhibits the occurrence of experimental gastritis in rats induced by taurocholic acid, but also has the effect of promoting healing. (3) Effect of increasing gastric mucosal prostaglandins This product increases the content of prostaglandin E2 in the gastric mucosa of rats, and increases prostaglandin E2 and prostaglandin I2 in gastric juice. It also increases the metabolite of prostaglandin E2, 15-keto-13,14-dihydroprostaglandin E2. This product increases the content of prostaglandin E2 in the gastric mucosa of healthy adult men, and shows that it has an inhibitory effect on gastric mucosal damage caused by ethanol load. (4) Effect of protecting gastric mucosa This product can inhibit gastric mucosal damage in rats caused by ethanol, strong acid and strong alkali, and can also inhibit the damage of aspirin and taurocholic acid to gastric mucosal epithelial cells of rabbit fetuses, and inhibit the damage of aspirin, ethanol, and hydrochloric acid-ethanol load to gastric mucosal damage in healthy adult men. (5) Effect of increasing gastric mucosal fluid volume This product can increase the biosynthetic enzyme activity of rat mucus high molecular glycoprotein, and increase the surface viscosity of gastric mucosa and the amount of soluble mucus. The effect of increasing soluble mucus is related to endogenous prostaglandins. (6) Effect of increasing gastric mucosal blood flow This product increases the mucosal blood flow of rats and can improve blood circulation disorders caused by blood loss. (7) Effect on gastric mucosal barrier This product has almost no effect on the gastric mucosal potential difference of rats, but it can inhibit the decrease in gastric mucosal potential difference caused by ethanol. (8) Effect on hypersecretion of gastric alkaline substances This product hypersecretion of gastric alkaline substances in rats. (9) Effect of promoting gastric mucosal cell regeneration This product enhances the regeneration ability of gastric mucosal cells in rats and increases the number of surface epithelial cells. (10) Effect of repairing damaged gastric mucosa This product can normalize the repair process of rabbit cultured gastric mucosal epithelial cells in the trauma repair model that was delayed by bile acid and hydrogen peroxide. (11) Effect on gastric acid secretion This product has almost no effect on the basal gastric juice secretion of rats and does not show an inhibitory effect on the stimulation of gastric acid secretion. (12) Effect on reactive oxygen species This product has the effect of eliminating hydroxyl free radicals and inhibiting the production of peroxides by polymorphonuclear leukocytes. In vitro, it inhibits gastric mucosal damage caused by reactive oxygen species produced by neutrophils caused by Helicobacter pylori. While inhibiting the gastric mucosal damage of rabbits loaded with indomethacin in response to stress, this product reduces the content of lipid peroxides in the gastric mucosa. (13) Effect on gastric mucosal inflammatory cell infiltration Through studies on the taurocholic acid-induced gastritis model, NSAIDs gastric mucosal injury model, and ischemia-reperfusion model in rats, it was found that this product can inhibit inflammatory cell infiltration. (14) Effect on gastric mucosal inflammatory cytokine (interleukin-8) This product can inhibit the increase in interleukin-8 (IL-8) production in human gastric mucosal epithelial cells caused by Helicobacter pylori, and can inhibit the activation of NF-KB in epithelial cells and the appearance of IL-8 mmRNA (in vitro). II. Toxicological studies According to foreign literature reports: (1) Single-dose toxicity [LD50 (mg/kg)]: (2) Repeated-dose toxicity: No drug-induced changes were observed in 52-week oral administration studies in SD rats and Beagle dogs, and the estimated no-toxic dose was 1000 mg/kg/day. (3) Genotoxicity: The results of microbial DNA damage repair test, microbial or mouse cell gene mutation test were negative. The results of the Chinese hamster ovary cell chromosome aberration test were positive, and the rat micronucleus test was negative. (4) Reproductive toxicity: The results of the administration test before pregnancy and in early pregnancy (SD rats: 30-1000 mg/kg/day; NZW strain: 10-300 mg/kg/day) and the administration test during the perinatal and lactation period (SD rats: 10-1000 mg/kg/day) did not show obvious changes caused by the drug. (5) Carcinogenicity: The dosage of mice and rats was as high as 1500 mg/kg/day and 2000 mg/kg/day, respectively, and the mixed feed was administered for up to 2 years. No changes in carcinogenicity were observed in either animal. (6) Antigenicity: No antigenicity was observed in systemic anaphylaxis, Schultz-Dyer reaction, passive skin allergy test and agar gel immunodiffusion test.

Chemical name: (±)-2-(4-chlorobenzamido)-3-[2(1H)-quinolinone-4]-propionic acid Molecular weight: C19H15CLN2O4

This product is a cystic capsule, the contents are white granules or powder.

Improvement of gastric mucosal lesions (erosion, bleeding, congestion, edema) in gastric ulcer, acute gastritis, and acute exacerbation of chronic gastritis.

1. Improvement of gastric mucosal lesions (erosion, bleeding, congestion, edema) in acute gastritis and acute exacerbation of chronic gastritis: Usually, adults take 0.1g (1 tablet) at a time, 3 times a day, orally. 2. Gastric ulcer: Usually, adults take 0.1g (1 tablet) at a time, 3 times a day, orally in the morning, evening and before bedtime.

According to a Japanese study, adverse reactions including abnormal clinical test values occurred in 54 out of 10,047 cases (0.54%). Among them, 18 out of 3,035 elderly patients over 65 years old (0.59%) experienced adverse reactions. There was no difference in the types and incidence rates of adverse reactions between the elderly and non-elderly. Serious adverse reactions 1) Shock, allergic symptoms (incidence unknown*): Allergic shock may occur after taking this product. Careful observation should be made at this time. If any abnormality is found, the drug should be stopped and appropriate measures should be taken. 2) Leukopenia (less than 0.1%), thrombocytopenia (incidence unknown*): Leukopenia and thrombocytopenia may occur after taking this product. Careful observation should be made. If any abnormality is found, the drug should be stopped and appropriate measures should be taken.

Patients with a history of allergy to the ingredients of this product are prohibited from taking it.

Precautions for children: The safety of this product for children has not been confirmed (little experience in use). Precautions for pregnancy and lactation: (1) Since the safety of administration during pregnancy has not been confirmed, this product should only be used by pregnant women or women who may become pregnant when the benefits of treatment outweigh the risks. (2) According to animal experiments (rat studies), this product can be secreted in breast milk, so lactating women should avoid breastfeeding when using this product. Precautions for the elderly: Since the physiological functions of elderly patients are generally low, attention should be paid to adverse reactions of the digestive system.

This research has not yet been conducted and there are no reliable references.

Keep sealed.

0.1g

24 months