Cefoxitin esterified prodrug compound and oral preparations

Abstract

The invention discloses an esterified prodrug compound and salt forming compounds and oral preparations thereof. The prodrug compound is shown in the structural formula (IV) in the specification, takes cefoxitin as an active ingredient and can exist in the form of salts. The prodrug compound has the following advantages that a lipophilic group acetoxy-1-halothane is introduced on the basis of cefoxitin to esterify carboxyl to become the esterified prodrug, thus providing an active pharmaceutical ingredient changing the original dosage forms; orally taken, the esterified prodrug not only relieves pains suffered by the patients during injection but also is not only used in professional organizations, thus saving time and widening the application range of the drug; and the esterified prodrug has a confirmed curative effect.

Description

technical field The invention relates to a class of esterified prodrug compounds with the second-generation cephalosporin antibiotic cefoxitin as an active ingredient, a salt-forming compound and oral preparations thereof, belonging to the field of pharmaceutical compounds. Background technique Cefoxitin Sodium is the second-generation semi-synthetic cephalosporin (cephamycin antibiotic), developed by Merck & Co. of the United States. It was launched in 1974, and then listed in more than 20 countries around the world. In 1992, the injection was launched in China, and in 2002 The API was launched in China in 2009. The trade name of cefoxitin sodium for injection listed in the United States is "MEFXOIN". ? " (or "Meifuxian ? ”), FDA-approved specifications are 1.0, 2.0g. It is mainly used clinically for sensitive bacteria (such as: Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus, Morganella morganii, Providencia , Peptostreptococcus, Bacteroides, etc...

AI Technical Summary

Problems solved by technology

The present invention aims to overcome the shortcomings of single usage of cefoxitin sodium for injection, inconvenient use, and inability to meet the needs of different groups of people, and provides a cefoxitin esterified prodrug compound and its salt-forming compound and oral preparations