Mesalazine slow-release granules and preparation method thereof

Abstract

The invention relates to mesalazine slow-release granules and a preparation method thereof. The slow-release granules are composed of the following active compositions and auxiliary agent in percent by weight: 40-60% of mesalazine, 18-36% of pill-preparing mother nucleuses, 3-7% of a bonding agent, 0.5-1% of a plasticizer, 15-35% of a coating material, 0.5-1% of a lubricant and 0.5-2% of a flow aid. The slow-release granules are characterized in that the mesalazine slow-release granules are prepared by performing medicine-charging pill preparation for two times and performing coating for two times, and the preparation technology successively comprises the following medicine-charging pill preparation and coating steps: (1) performing first medicine-charging pill preparation on the pill-preparing mother nucleuses, so as to obtain first medicine-charged pills; (2) performing first coating on the first medicine-charged pills, so as to prepare first-coated medicine pills; (3) performing secondary medicine-charging pill preparation on the first medicine-charged pills, so as to prepare secondary medicine-charged pills; and (4) performing secondary coating on the secondary medicine-charged pills. According to the slow-release granules prepared through the specific technology, the coating efficiency and the release behavior of mesalazine are improved.

Description

[technical field] [0001] The application relates to a new drug preparation, in particular to a mesalazine sustained-release granule, and the application also provides a preparation method of the sustained-release granule. It belongs to the field of pharmaceutical preparations. [Background technique] [0002] Inflammatory bowel disease (Inflammatory bowel disease, IBD) includes ulcerative colitis (Ulcerative colitis, UC) and Crohn's disease (Crohn's disease, CD), ulcerative colitis is the most common rectum, colon inflammatory disease, The local intestinal tract shows continuous and diffuse mucosal and submucosal inflammatory changes, which can form visible erosions and ulcers, and the clinical manifestations are mucus, pus and blood in the stool. Its etiology and exact pathogenesis are still unclear. It is generally believed that it is a chronic disease mainly manifested by intestinal inflammation caused by the interaction of various environmental factors on the basis of g...

AI Technical Summary

Problems solved by technology

5-Aminosalicylic acid is the active ingredient that plays a therapeutic role. Most of the adverse reactions are caused by sulfapyridine, such as sulfa allergy, gastrointestinal reactions, liver and kidney dysfunction, pancreatitis and abnormal sperm motility. Patients cannot tolerate it. Due to SASP, its clinical application is limited

[0007] Currently on the market, mesalazine enteric-coated tablets and mesalazine enteric-coated preparations prepared by the prior art have solved the above problems, but both have high release in acid and low release in buffer, and cannot reach the lesion site, insufficient curative effect, poor product quality stability, complicated process, etc.

Invention CN200480010790 is a high-loaded mesalazine sachet, although it solves the problem of insufficient drug load, it cannot be effectively released in the colon, and the prepared sachet does not have the effect of targeted release

Especially for drugs with local effects like mesalazine; CN201080063271 was invented as a suppository, although the first-pass effect is avoided, but the action site is mainly in the rectum, the coverage is small, and the patient's compliance is not as good as oral preparations; mesalazine enteric coating Tablets (CN201180040925 and CN201210072493) can achieve higher drug loading and release behavior, but compared with the same dose of granules, the specific surface area is much smaller, which also limits the drug release and absorption interval, so the bioavailability is worse than that of granules agent

Existing mesalazine and sustained-release technology tend to cause unstable drug release curves and large fluctuations in blood drug concentration

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