Stable solid preparation containing amorphous cefditoren pivoxil and preparation method thereof

Abstract

The present invention relates to a stable drug compound of solid preparation containing amorphous cefditoren pivoxil, and its preparing method. The solid preparation can be prepared by drying method, and can be packaged with one or more layers water dispersoid which contains one or more kind film-forming agents. The drug compound can be used for antimicrobial.

Description

Technical field [0001] The present invention relates to a stable solid preparation, a dry method for preparing an amorphous solid preparation form of cefditoren pivoxil, and a solid preparation form coated with one or more water dispersions containing a film-forming agent. Background technique [0002] "Cefteren" is a cephalosporin compound: 7-[2-methoxyimino-2-(2-aminothiazol-4-yl)acetamido]-3-[2-(4-methylthiazole-5- Yl)vinyl]-3-cephem-4-carboxylic acid (cis isomer, trans isomer) common name. The synthesis of cefditoren is disclosed in U.S. Patent Nos. 4,839,350 and 4,918,068. A formulation of injectable cefditoren is disclosed in US Patent No. 5,595,986. Cefditoren pivoxil, synthesized by forming chloromethyl pivoxil on the carboxylic acid group of cefditoren, has improved oral absorption and is rapidly hydrolyzed by lipase into cefditoren when absorbed. [0003] Cefditoren has a broad antibacterial spectrum with relatively low toxicity and is beneficial for the treatment or pr...

AI Technical Summary

Problems solved by technology

[0012] Amorphous formulations with improved bioavailability have a disadvantage: amorphous materials are thermodynamically unstable and thus naturally show a tendency to crystallize

[0023] However, a method for preparing an acceptable dosage form containing cefditoren pivoxil with improved water solubility and stability using a simple, cost-optimized and time-saving method is not known