A kind of mesalazine colon-targeted controlled-release tablet and preparation method thereof

Abstract

The invention belongs to the technical field of mesalazine controlled-release preparations, and particularly relates to a mesalazine colon targeted controlled-release tablet and a preparation method thereof. The mesalazine colon targeted controlled-release tablet is composed of a splice core layer and a controlled-release layer located on the outer side of the splice core layer, the splice core layer is prepared from mesalazine and excipient pyrodextrin, the weight average molecular size Rh of the excipient pyrodextrin is 1.5-2.8 nm, and the solubility of the excipient pyrodextrin is of 80-98%; and the controlled-release layer is made of pyrodextrin with the weight average molecular size Rh of 8-12 nm and the solubility of 1.2-4.0%. According to the mesalazine colon targeted controlled-release tablet and the preparation method thereof, by taking the pyrodextrin with different characteristics as an excipient, the mesalazine colon targeted controlled-release tablet with a double-layer structure is prepared, compared with other controlled-release agents, starch-based pyrodextrin is simply taken as the excipient, and biological safety is high; and conventional tablet pressing processesare just used for preparing the mesalazine colon targeted controlled-release tablet, a processing technology is simple, and large-scale industrial production is easily conducted.

Description

technical field [0001] The invention belongs to the technical field of mesalazine controlled-release preparations, and in particular relates to a mesalazine colon-targeted controlled-release tablet and a preparation method thereof. Background technique [0002] Oral Colonic Drug Delivery System (OCDDS) refers to the use of certain pharmaceutical methods to prevent the release of drugs at the upper end of the gastrointestinal tract after oral administration, and begin to disintegrate or erode to release the drug at the colon, so as to improve the drug delivery at the target site. A drug delivery system that exerts a local or systemic therapeutic effect at a point concentration. The drug delivery system can obtain higher drug bioavailability and effective utilization rate, and can also reduce many adverse reactions after the drug is absorbed systemically. In recent years, based on the excellent properties of OCDDS such as targeting and sustained release, the colonic drug deli...

AI Technical Summary

Problems solved by technology

At present, enema administration can make the drug go directly to the lesion and achieve the best therapeutic effect of inflammatory bowel disease, but most patients are difficult to accept this method

Oral administration has the advantages of convenience, high patient compliance, and no infection. However, direct oral administration has its limitations: free 5-ASA can be absorbed into the blood through the small intestine, and the amount reaching the colon is small, resulting in drug loss. The effect is low, and long-term medication is required, resulting in large adverse reactions and poor patient compliance

However, whether it is resistant starch or chemically modified starch, it will be degraded by human digestive enzymes to varying degrees in the gastrointestinal tract, so the availability of drugs still needs to be improved

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