Amorphous cefditoren pivoxil composition and process for producing the same

A composition and amorphous technology, applied in the field of pharmaceutical compositions for oral administration, can solve the problems of unsatisfactory production efficiency, process management and long time, and achieve high therapeutic effectiveness, good dissolution and stability excellent effect

Inactive Publication Date: 2004-10-13
MEIJI SEIKA KAISHA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, this method requires process management and a long time due to many processes, so it is not satisfactory in terms of production efficiency.

Method used

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  • Amorphous cefditoren pivoxil composition and process for producing the same
  • Amorphous cefditoren pivoxil composition and process for producing the same
  • Amorphous cefditoren pivoxil composition and process for producing the same

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manufacture example

[0063] Amorphous cefditoren and pivoxil compositions 1 to 7 of the present invention were prepared as follows.

[0064] Amorphous Composition 1

[0065] With 0.3g crystalline cefditoren pivoxil (manufactured by Meiji Seika Co., Ltd.), 2.7g sodium caseinate (manufactured by New Zealand Dairy Board) (the weight ratio of cefditoren pivoxil / casein sodium is 10 / 90) was put into a pulverizing container made of alumina, and pulverized for 30 minutes using a vibrating rod mill (manufactured by CMT, model TI-200) to obtain an amorphous composition 1.

[0066] Amorphous Composition 2

[0067] Mix 0.3 g of crystalline cefditoren pivoxil (manufactured by Meiji Seika Co., Ltd.), 2.7 g of crystalline cellulose (manufactured by Asahi Kasei Co., Ltd.) (the weight ratio of cefditoren pivoxil / crystalline cellulose is 10 / 90) was placed in a pulverizing container made of alumina, and pulverized for 30 minutes using a vibrating rod mill (manufactured by CMT: TI-200) to obtain an amorphous c...

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Abstract

A composition of an amorphous cefditoren pivoxil excellent in stability and releasability; and a process for producing the amorphous composition. The composition comprises cefditoren pivoxil and a pharmaceutically acceptable organic polymer, and is characterized by being obtained by pulverizing crystalline cefditoren pivoxil in the presence of a pharmaceutically acceptable organic polymer and making the cefditoren pivoxil amorphous.

Description

[Background of the invention] [0001] field of invention [0002] The present invention relates to an amorphous cefditoren pivoxil composition with excellent stability and improved dissolution properties, a pharmaceutical composition for oral administration containing the amorphous composition, and a method for preparing the composition. [0003] Background technique [0004] Cefditoren pivoxil (Cefditoren pivoxil) is, in order to endow the antibiotic cefditoren (that is, (+)-(6R,7R)-7-[(Z)-2-( 2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[(Z)-2-(4-methylthiazol-5-yl)ethylenyl]-8-oxo -5-thio-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, its alias is [6R-[3(Z), 6α, 7β(Z)]]-7 -[[(2-amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[2-(4-methyl-5-thiazolyl)ethenyl]-8-oxo-5-thia-1-azabicyclo[4.2 .0] oct-2-ene-2-carboxylic acid) excellent oral absorbability, and make trimethyl acetoxymethyl and its 4-position carboxylic acid carry out the ester binding of the new prodrug o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/16A61K9/48A61K31/546A61P31/00A61P31/04
CPCA61K9/1617A61K9/4858A61K9/146A61K9/1652A61K9/4866A61K31/546A61K9/1623A61P31/00A61P31/04
Inventor 太田真人
Owner MEIJI SEIKA KAISHA LTD
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