Cefixime sustained-release double-layer tablet

Abstract

The invention relates to cefixime sustained release double layer tablet, which comprises tocefixime quick-release layer and cefixime slow release layer. Cefixime disperses in quick-release layer and slow release layer according to proper ratio, wherein cefixime or its medicinal salt or hydrate in sustained release layer has a release time over 12h.The inventive sustained release double layer tablet provides higher initial blood concentration and more ideal concentration versus curve, improves bactericidal action and reduces drug tolerance.

Description

field of invention [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cefixime sustained-release double-layer tablet composed of an immediate-release layer and a slow-release layer and its application for treating infection. Background technique [0002] The chemical name of cefixime is (6R, 7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(carboxymethoxyimine)-acetamido ]-3-vinyl-8-oxo-5-thia-1-azabicyclo[4.2.0]-2-octene-2-carboxylic acid is a commonly used oral third-generation cephalosporin The drug was successfully developed by Fujisawa Pharmaceutical Co., Ltd., Japan, and was first listed in Japan in 1987. It was launched in the United States in 1989, and 7 years later it was sold in 44 countries around the world. In 1999, cefixime was clinically used in more than 80 countries around the world. In 1998, among five developed countries in Europe, cefixime surpassed cefuroxime axetil to become the oral cephalosporin with the largest market s...

AI Technical Summary

Problems solved by technology

For example, the inventors of WO2005030178 and WO2004066910 have overlooked a problem, that is, only by controlling the type and dosage of sustained-release materials, it is impossible to simultaneously meet the requirements of releasing part of the drug in a short time and maintaining the release of the rest of the drug for a long time

At the same time, these two patents did not mention the release situation and blood drug concentration of the preparation; although the inventor of US20040005361 realized the importance of rapid drug release, he divided cefixime into two parts, immediate release and sustained release, but he used The mixed sustained and rapid release preparation process, that is, mixing the sustained release granules and the immediate release granules and then compressing the tablets, will lead to slow drug release in the early stage of the sustained release preparation, and rapid drug release in the later stage, which is contrary to the clinical drug requirements of antibiotics ; Although WO9822091 discloses a controlled-release β-lactam antibiotic, at least 50% is released within 3-4 hours after oral administration, and the rest is released at a controlled agent rate, but its technical scheme has no cefixime controlled-release preparation embodiment support, and No initial drug release (in vitro release within 1 hour) and blood concentration requirements, more than 50% release within 3-4 hours

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