Cefuroxime axetil granule and process for the preparation thereof

A technology for cefuroxime axetil and granules, applied in the field of cefuroxime axetil granules and preparation thereof, can solve the problems of poor dispersion, bitter aftertaste of preparations and the like

Inactive Publication Date: 2007-02-07
HANMI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the granules obtained by the above method are poorly dispersed in water during the preparation process due to the presence of stearic acid, and the preparation still has a bitter aftertaste, causing problems when oral administration to humans, especially infants

Method used

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  • Cefuroxime axetil granule and process for the preparation thereof
  • Cefuroxime axetil granule and process for the preparation thereof
  • Cefuroxime axetil granule and process for the preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Preparation of CA particles

[0059] 1-1) Preparation of non-crystalline CA solid dispersion

[0060] 100 parts by weight of crystalline cefuroxime axetil (HANMI Fine Chemical Co., Ltd., South Korea) and 16.63 parts by weight of Twin 80  (ICI Inc., USA) was dissolved in acetone, and 16.63 parts by weight of silica were dispersed therein. The dispersion was spray-dried using a spray dryer (Minispray dryer B-191, Buchi, Switzerland) set at an inlet temperature of 45°C and an outlet temperature of 37°C to obtain a solid dispersion. The solid dispersion was further dried at 30-40°C for about 3 hours to remove residual solvent.

[0061] 1-2) Preparation of CA particles

[0062] 227 g of fatty acid sucrose ester (fatty acid sucrose ester 37318-31-3, Dai-ichi Kogyo Seiyaku Inc., Japan) and 318 g of Eudragit  L100-55 (Röhm Inc., USA) were mixed together, and the resulting mixture was melted at a temperature of about 75°C. Subsequently, 31.8 g of triacetin was ...

Embodiment 2

[0063] Example 2: Preparation of CA particles

[0064] The procedure in Example 1-2) was repeated, except that substantially amorphous cefuroxime axetil (Orchid Chemicals & Pharmaceuticals Inc., India) was used instead of the non-crystalline cefuroxime axetil solid dispersion to prepare cefuroxime axetil granules.

Embodiment 3

[0065] Example 3: Preparation of CA particles

[0066] The procedure in Example 1-2) was repeated except that croscarmellose sodium (AVEBE Inc., USA) was used instead of alginic acid as a disintegrant to prepare cefuroxime axetil granules.

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Abstract

A cefuroxime axetil granule composition, comprising non-crystalline cefuroxime axetil solid dispersion or substantially amorphous cefuroxime axetil, fatty acid sucrose ester, methacrylic acid-ethyl acrylate copolymer and a disintegrant, which is used in masking Cefuroxime axetil has desirable performance characteristics in terms of bitter taste, and has high bioavailability and stability of cefuroxime axetil, so it can be advantageously used for oral administration of cefuroxime axetil.

Description

field of invention [0001] The invention relates to oral cefuroxime axetil granules and a preparation method thereof. The granules can well mask the bitter taste of cefuroxime axetil and exhibit high bioavailability of cefuroxime axetil. Background technique [0002] Cefuroxime axetil (CA) is an oral cephalosporin antibiotic with high activity against a broad spectrum of Gram-positive and Gram-negative bacteria. It exhibits three forms of polymorphism: a crystalline state with a melting point of about 180°C, an essentially amorphous form with a melting point of about 135°C, and an essentially amorphous form with a low melting point of about 70-95°C. The crystalline form of cefuroxime axetil has excellent antibacterial activity, but is only slightly soluble in water and is not easily absorbed in the intestinal tract. [0003] Accordingly, the present inventors have prepared an amorphous cefuroxime axetil solid dispersion having enhanced water solubility and high cefuroxime ax...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
CPCA61K9/1623A61K9/0095A61K9/1635A61K9/1652A61K9/5026A61K9/5042A61K9/5047A61K31/545A61K31/546A61P31/00A61P31/04
Inventor 禹钟守张熙喆李鸿基
Owner HANMI PHARMA
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