Rebeprazole sodium enteric-coated tablet and preparation process thereof

Abstract

A rebeprazole sodium enteric-coated tablet comprises, by weight, 65-125 parts of tablet core, 10-40 parts of isolation layer and 80-170 parts of enteric-coated layer, wherein filler is one or more of microcrystalline cellulose, lactose and mannitol, stabilizer is one or more of magnesium oxide and anhydrous sodium carbonate, disintegrating agent is one or more of polyvinyl pyrrolidone, cross-linking sodium carboxymethyl cellulose and lauryl sodium sulfate, lubricating agent is one or two of talcum powder and magnesium stearate, binder is the anhydrous ethanol solution of crospovidone or the aqueous solution of hydroxypropyl methylcellulose, the isolation layer is one or two of magnesium oxide and ethyl cellulose, and the enteric-coated layer is one or more of hydroxypropyl methylcellulose phthalic acid ester, enteric-coated acrylic resin, cellulose acetate phthalic ester, talcum powder and 93F19255 type coating agent. A preparation process of the rebeprazole sodium enteric-coated tablet is simple, low in equipment requirement, high in yield, and controllable in product quality. The dissolution rate of the rebeprazole sodium enteric-coated tablet is highly consistent with the release behavior of originally-developed drugs, and the rebeprazole sodium enteric-coated tablet is good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a proton pump inhibitor rabeprazole sodium enteric-coated tablet and a preparation process thereof. Background technique [0002] Rabeprazole sodium is a new generation of proton pump inhibitors jointly developed by Japan's Eisai and Janssen for the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis and Zoe-Eck syndrome. Rabeprazole sodium specifically acts on the activity of hydrogen ion-potassium ion-adenosinyl triphosphatase, thereby inhibiting basal gastric acid and stimulation-induced gastric acid secretion. [0003] The chemical structural formula of rabeprazole sodium is: [0004] [0005] Chemical name: 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}methylsulfinyl]-1H-sodium benzimidazole, molecular formula is C 18 h 20 NaO 3 S. [0006] Rabeprazole sodium is a new generation of benzimidazole substitute after omeprazole and lansoprazole. It...

AI Technical Summary

Problems solved by technology

Proton pump inhibitors are unstable in an acidic environment and will be destroyed by gastric acid when they enter the stomach. Rabeprazole sodium is prone to degradation and oxidation reactions under acidic, humid, heat and light conditions, resulting in inactive impurities. As a result, the content of the main drug decreases, so the long-term stability and efficacy of rabeprazole sodium preparations are key issues that all drug manufacturers need to solve urgently

[0007] Although the enteric-coated tablet disclosed by the patent No. WO2008129517A can prevent the degradation of the drug, the disintegration is relatively slow and the bioavailability is low, which is not conducive to timely relief of the pain of the patient

[0008] The patent No. CN104873471A disclosed rabeprazole sodium enteric-coated tablets, although the problem of poor dissolution rate of the tablet core of rabeprazole sodium coated tablets or enteric-coated tablets is solved, the dissolution rate of rabeprazole sodium element tablets is high , does not mean that the bioavailability of rabeprazole sodium enteric-coated tablets is good, and it does not mean that the faster the dissolution, the better

[0009] The patent No. CN104337789A discloses Rabeprazole Sodium Enteric-coated Tablets, although it solves the degradation and discoloration problems of Rabeprazole Sodium, but does not mention bioavailability, and does not solve the drug efficacy problem of Rabeprazole Sodium Enteric-coated Tablets

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