Enema for treating ulcerative colitis and preparation method thereof

Abstract

The invention discloses an enema for treating ulcerative colitis and a preparation method of the enema. The enema comprises pyruvate-mesalazine-chitosan particles, and the pyruvate-mesalazine-chitosan particles are suspended in a liquid auxiliary material prepared for enema application; the preparation method comprises the following steps: dissolving water-soluble chitosan in an acetic acid solution to form a chitosan-acetic acid solution; continuously adding pyruvate into the chitosan-acetic acid solution, and uniformly stirring; dispersing mesalazine into the solution, uniformly stirring, then adding a cross-linking agent, centrifuging at a high speed, and freeze-drying a precipitate to obtain mesalazine-pyruvate-chitosan microspheres; and preparing a liquid auxiliary material, adding the pyruvate-mesalazine-chitosan particles into the liquid auxiliary material, uniformly stirring, and then carrying out homogenization treatment, thereby obtaining the mesalazine-pyruvate-chitosan emulsion. According to the enema, addition of sulfite compounds is avoided, nitrogen charging in the whole production process is not needed, and the enema has a quite long storage life.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to an enema for treating ulcerative colitis and a preparation method thereof. Background technique [0002] Ulcerative colitis is a chronic, nonspecific inflammatory disease of the colon and rectum of unknown etiology, with lesions confined to the mucosa and submucosa of the large intestine. The lesions are mostly located in the sigmoid colon and rectum, but can also extend to the descending colon or even the entire colon. The course of the disease is long and often recurring. The etiology of ulcerative colitis is still unknown, genetic factors may play a role, psychological factors play an important role in disease progression, and preexisting psychiatric disorders such as depression or social distancing improve significantly after colectomy. Ulcerative colitis is thought to be an autoimmune disease. [0003] Mesalazine is an aminosalicylate prescribed to treat infla...

AI Technical Summary

Problems solved by technology

[0005] At present, the commercially available mesalazine enema production companies mainly include Dr.Falk Pharma GmbH in Germany, Kyorin Pharmaceutical Co., Ltd. in Japan, Ferring Pharmaceuticals Ltd. in Switzerland, and the United States. Pharmaceutical LLC, the mesalazine enemas sold by these companies are packed with nitrogen. In addition, except for the United States sfROWASA of Pharmaceutical LLC TM In addition, the mesalazine enemas produced by several other companies all added sulfites as antioxidants, but sfROWASA TM In the production process, the substitution of oxygen is strictly controlled in the whole process of preparation, filling and packaging, and the residual oxygen is controlled below 0.2%, which greatly increases the production cost

Moreover, it is mentioned in the instructions that once the aluminum foil bag is opened, all 7 products must be used within 14 days. It can be seen that the mesalazine enema without sulfites is more sensitive to oxygen

This process of strictly controlling the oxygen substitution in the production process also has high requirements for production equipment and packaging materials. It requires special line production and customized equipment, resulting in extremely high production costs. As a result, the price of mesalazine enema sold is relatively high Expensive, bringing great financial burden to patients

However, if sulfite compounds (e.g., bisulfite, metabisulfite, etc.) are used to stabilize mesalamine enema compositions from oxidation of the 5-ASA active agent, resulting in decomposition, discoloration and reduced efficacy , so that the enema composition has a long shelf life after being stored for a long time, this way it is colon / intestinal irritating

In addition, this class of sulfites may cause allergic reactions, including anaphylaxis and life-threatening or non-severe asthma attacks, in certain susceptible individuals

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