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A pharmaceutical composition of microencapsulated cefuroxime axetil

A cefuroxime axetil and microencapsulation technology, which is applied in microcapsules, capsule delivery, antibacterial drugs, etc., can solve the problems that cefuroxime axetil cannot be encapsulated and mask bitterness, etc., and achieve stable raw material configuration and in vitro high dissolution effect

Active Publication Date: 2008-07-16
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solid dispersion improves the bioavailability and stability of cefuroxime axetil, but the water-insoluble inorganic carrier cannot encapsulate cefuroxime axetil to achieve the purpose of masking its bitter taste

Method used

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  • A pharmaceutical composition of microencapsulated cefuroxime axetil
  • A pharmaceutical composition of microencapsulated cefuroxime axetil
  • A pharmaceutical composition of microencapsulated cefuroxime axetil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment one, preparation microencapsulated cefuroxime axetil

[0029] After weighing ethyl cellulose 50g, povidone 25g and adding 95% ethanol to dissolve, cefuroxime axetil 100g was added to the above solution to dissolve or be in a good state of suspension, and the mixed liquid was placed in a spray dryer (QP3 type , Beijing Research Institute of Chemical Industry, Ministry of Chemical Industry) spray-dried at an inlet temperature of 80°C and an outlet temperature of 50°C to obtain microencapsulated cefuroxime axetil in powder form.

Embodiment 2

[0030] Embodiment two, preparation microencapsulated cefuroxime axetil

[0031] Repeat the operation steps of Example 1, but the ethyl cellulose used is 100g, and the povidone is 50g.

Embodiment 3

[0032] Embodiment three, preparation microencapsulated cefuroxime axetil

[0033] Weigh 200g of ethyl cellulose, 50g of polyethylene glycol 1500 and add it into 95% ethanol to dissolve, then add 100g of cefuroxime axetil into the above solution to dissolve or be in a good suspension state, stir and mix the liquid in a spray dryer (QP3 type, Beijing Research Institute of Chemical Industry, Ministry of Chemical Industry) is spray-dried, with an inlet temperature of 70° C. and an outlet temperature of 40° C. to obtain microencapsulated cefuroxime axetil in powder form.

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Abstract

The present invention relates to one kind of medicine composition of cefuroxime ester microcapsule and its preparation process. The cefuroxime ester microcapsule consists of cefuroxime ester and filming material, selected from ethyl cellulose and acrylic resin type L or S, in the weight ratio of 1 to 0.5-5, as well as additive, selected from polyvidone, polyethylene glycol and hydroxypropyl ethyl cellulose, in the amount of 10-50 wt% of the filming material. The prepared granule and dry suspension have excellent effects of masking bitter taste, raising excorporeal leaching rate, etc.

Description

technical field [0001] The invention relates to a pharmaceutical composition of microencapsulated cefuroxime axetil and a preparation method thereof. technical background [0002] Cefuroxime axetil (Ceftin) chemical name: (6R,7R)-7-[2-furyl(methoxyimino)acetamido]-3-carbamoyloxymethyl-8-oxo- 5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 1-acetoxyethyl ester. [0003] Chemical Structure: [0004] [0005] Molecular formula: C 20 h 22 N 4 o 10 S; molecular weight: 510.48. [0006] Cefuroxime axetil is a second-generation semi-synthetic cephalosporin with broad antibacterial spectrum and strong antibacterial activity. It is highly stable to β-lactamase and has a high blood concentration. The advantages of low toxicity. It is currently one of the best-selling oral antibiotics in the world. [0007] Cefuroxime axetil exists in three polymorphic forms: crystalline form with a melting point of 180°C, amorphous form with a melting point of 135°C, and amorphous f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/546A61K9/50A61K9/16A61K9/10A61P31/04
Inventor 张宏武周桂荣李云立李鹏坤孟程军孙建华
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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