Dexketoprofen Tromethamine Sustained Release Tablets for Gastric Retention

Abstract

The invention provides a dexketoprofen trometamol gastroretentive sustained-release tablet and a preparation method thereof, and belongs to the field of medicines. Dexketoprofen trometamol is a non-steroidal analgesic and anti-inflammatory drug. Ordinary tablets of dexketoprofen trometamol need to be administered frequently, and taking of 1-2 tablets of the ordinary tablets 3-4 times a day is inconvenient for patients. The dexketoprofen trometamol gastroretentive sustained-release tablet can fully absorb gastric juice after being orally taken, and expands to form a hydrogel, so the drug release rate is controlled, the water absorbing expanded hydrogel preparation generates a gastroretentive effect by the comprehensive action of floatation, mucous membrane adherence and the expansion volume, and has a continuous sustained release effect for 24 h in vivo and in vitro; the dexketoprofen trometamol gastroretentive sustained-release tablet can be well absorbed in beagle dogs, reduces the plasma concentration change, achieves one dose per day, and increases the administration compliance of patient; and the gastroretentive sustained-release tablet is prepared by a direct powder tabletingprocess, so the method has the advantages of simple technology, and facilitation of industrial production.

Description

technical field [0001] The invention relates to a dexketoprofen trometamol gastric retention sustained-release tablet and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Gastro-retentive drug delivery systems (Gastro-retentive drug delivery systems) is a sustained and controlled release system for oral drugs, as well as a site-specific release system for the gastrointestinal tract. Compared with ordinary tablets, it has the ability to prolong the residence time of the drug release system (DDS) in the stomach, release the drug to the stomach, duodenum and small intestine and other gastrointestinal absorption sites in a continuous and controlled release manner, and reduce the blood drug Concentration fluctuations, reduce the frequency of medication, reduce mucosal irritation, improve bioavailability and other advantages. Drug delivery systems for gastric retention include (a) gastric buoyant DDS, which has a low density and floa...

AI Technical Summary

Problems solved by technology

Dexketoprofen is the dextromorph of ketoprofen, which is the active ingredient in the racemate of ketoprofen, and its effect is equivalent to twice that of ketoprofen in the same dose. The advantage is to reduce the toxic and side effects of the L-body (ineffective component) in ketoprofen, but the solubility of dexketoprofen is small and the absorption is poor, so it is usually used as tromethamine salt

Dexketoprofen tromethamine tablets were first launched in Spain in 1996. The original research company is The Menarini Group. Currently, the formulations of dexketoprofen tromethamine listed in China include ordinary tablets, capsules and injections , ordinary tablets and capsules need to be administered frequently, 3 to 4 times a day, 1 to 2 tablets / grain each time, which brings inconvenience to patients, and the side effects of ordinary preparations are still relatively large, and long-term oral administration can cause gastrointestinal symptoms. ulcer or bleeding symptoms

[0006] At present, there is still a blank in the dexketoprofen tromethamine sustained-release preparation product market, and the patent of China relating to dexketoprofen tromethamine sustained-release preparation has CN2012102642579 (dexketoprofen tromethamine sustained-release Microparticles and their preparation methods and sustained-release preparations), CN201210362299.6 (dexketoprofen trometamol quick-release sustained-release double-layer tablet and its preparation process) and CN2015101856042 (a kind of dexketoprofen tromethamine Sustained-release tablets and preparation methods thereof), but these patents only measure the in vitro release, and do not investigate the in vivo release and absorption of beagle dogs and larger animals, and cannot objectively reflect whether these preparations have good sustained release and absorption in vivo; in addition, these The preparation process of the sustained-release microparticles, double-layer tablets and sustained-release tablets reported in the patent is relatively complicated, and the sustained-release tablets need to be fully mixed with Eudragit EPO and part of the precrossified starch PC-10 before the total blending

[0007] Dexketoprofen Tromethamine Gastric Retention Sustained-Release Tablets There is currently no research report

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