Production of mesalazine colon-specific drug administration sustained-release tablet

Abstract

The invention discloses a production of a mesalazine colon-specific drug administration sustained-release tablet. The mesalazine (5-ASA) is widely applied clinically, and becomes a priority drug for treating inflammatory bowel diseases. The mesalazine is ineffective when being orally taken, because the mesalazine is quickly absorbed in the small intestine, then acetylated and discharged along with urine, thus being not able to reach the colon part. 5-ASA can only play the treatment function when reaches the colon lesion part in a prototype, and is produced into a pH-dependent colon-specific drug administration sustained-release tablet, so that the 5-ASA drug which reaches the colon has enough concentration to have an anti-inflammatory effect. Eudragit L100 and Eudragit S100 can be used to produce a film coating which meets the colon-specific release requirement according to a certain proportion. The mesalazine is produced into a coating sustained-release tablet, so that the 5-ASA drug which reaches the colon has enough concentration to achieve the anti-inflammatory effect.

Description

1. Technical Field [0001] The invention relates to the field of medicine, in particular to a preparation method of mesalazine colon-positioned administration sustained-release tablets. 2. Background technology [0002] Ulcerative colitis is a type of inflammatory bowel disease. It is a chronic non-specific inflammatory disease of the rectum and colon whose etiology is not yet clear. The treatment of this disease is mainly through drug therapy to improve symptoms and reduce recurrence. The traditional drug sulfasalazine for the treatment of ulcerative colitis is clinically proven to have serious side effects. As its alternative, mesalazine (5-ASA) is widely used in clinical practice and has become the first choice for the treatment of inflammatory bowel disease. The anti-inflammatory effect is mainly achieved by inhibiting the secretion of prostaglandins and the production of leukotrienes and free radicals. Oral mesalazine is ineffective because it is quickly absorbed in the sma...

AI Technical Summary

Problems solved by technology

Eudragit has the advantages of excellent film-forming performance and good compatibility among various models, but the coating film has a high glass transition temperature and high brittleness. Therefore, plasticizers such as triethyl citrate are added in the coating process to increase the flexibility of the membrane