Mesalazine enteric-coated tablet composition with four-layer coating system and preparation method of mesalazine enteric-coated tablet composition

Abstract

The invention provides a mesalazine enteric-coated tablet composition with a four-layer coating system and a preparation method of the mesalazine enteric-coated tablet composition, and belongs to thefield of medicines. The composition is formed by combining a mesalazine tablet core and four layers of coatings, wherein the coatings sequentially comprise a first layer, a second layer, a third layerand a fourth layer from inside to outside, wherein the first layer is an isolation layer; the second layer is a slow-release casing layer; the third layer is a positioning acid-resistant layer; and the fourth layer is a moisture-proof layer. A second method for determining the dissolution rate by adopting the appendix of the Chinese pharmacopoeia is adopted, the release rate of the product is determined at 50rpm, and the release behavior should be as follows: the release rate is less than 10% in a dissolution medium with the pH value of 1.0 for 2h, then the product is transferred into a 7.4 medium, the release rate is 10-30% in 45min, the release rate is 50-75% in 75min and the release rate is 85% or above in 105min. The product is slowly released in intestines, most of the medicines canreach colons and act on inflammatory mucous membranes, prostaglandin synthesis causing inflammation and formation of inflammatory mediator leukotriene are inhibited, and the product has a remarkable anti-inflammatory effect on intestinal wall inflammation and particularly has a good effect on inflammatory intestinal wall connective tissues.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a composition of a four-layer coating system mesalazine enteric-coated tablet and a preparation method thereof. Background technique [0002] Inflammatory bowel disease is a persistent disease that has plagued doctors and scientists for many years, mainly including ulcerative colitis and Crohn's disease. Ulcerative colitis refers to chronic non-specific inflammation in the colon and rectum caused by a variety of reasons, which can cause ulcers and erosions on the inner wall of the intestine, and in severe cases, intestinal perforation and hemorrhage may occur, threatening the life safety of patients . The clinical manifestations are abdominal pain, blood in the stool, vomiting, body weight loss, with or without intestinal polyps, iritis, anal leakage and other symptoms. Relevant data show that the number of people suffering from ulcerative colitis in my country is as high a...

AI Technical Summary

Problems solved by technology

[0004] CN108159012A, discloses a kind of preparation method of mesalazine sustained-release tablet, and the dosage of this method single tablet is 1200mg, and the tablet prepared by this method, one, because dosage is bigger, can't meet clinical use of patients with mild disease Needed, there is a transition of treatment, and the second is that the design concept is different from this product, and the effect of the final product is different

The biggest problem with this method: 1) the preparation process uses an unconventional nano ball mill, which needs to be crushed to the nanometer level; The production conditions are not available yet, so the method is difficult, costly, poor in quality control, and the method is not feasible

[0007] The main problems of the mesalamine enteric-coated tablets in the market are as follows: one is that the release phenomenon of the tablet is disintegrating and non-erodible, and the resulting problem is the contact time between the active ingredient mesalamine and the lesion mucosa It is very short-lived and affects the curative effect; the second is that there is a large difference between the tablets, and patients often have the phenomenon of rowing the tablets, the drug cannot be absorbed by the mucous membrane, and it cannot play the role of treating inflammation; the third is that the stability is not good

Images