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Dispersible tablet of cefuroxime axetil

A technology of cefuroxime axetil and dispersible tablets, which can be used in pill delivery, pharmaceutical formulations, antibacterial drugs, etc. It can solve the problems of increasing the cost of excipients, increasing the amount of excipients, and discoloration of raw materials, so as to improve bioavailability and reduce dispersion. time, effect of improving compliance

Inactive Publication Date: 2012-10-03
GUANGZHOU NANXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This technology uses a lot of disintegrants and surfactants, and the production cost is high. At the same time, the risk of discoloration of raw materials and increase of related substances is prone to occur during the wet granulation process.
The publication number is CN101606914A Chinese patent application document discloses a preparation of cefuroxime axetil tablet suitable for direct powder compression, the preparation mainly achieves the powder direct compression effect of the preparation by increasing the fluidity of the auxiliary material, but The required excipients have a large bulk density and good fluidity, among which the bulk density of the disintegrant is greater than 0.35g / cm 3 , the bulk density of the filler is greater than 0.38g / cm 3 , the requirements for excipients are too high, which increases the cost of excipients. At the same time, this product needs to be dispersed within 10 minutes, which fails to meet the requirements of dispersible tablets
Publication number is that CN101703448A Chinese patent application document discloses a kind of direct compression process of cefuroxime axetil dispersible tablet, the proportion of crude drug cefuroxime axetil in the whole tablet is about 30% in this process prescription, increased The amount of auxiliary materials has increased the production cost, and no flavoring agent has been added at the same time, so the taste is poor
Patent WO9944614 discloses that in order to inhibit the gelation of cefuroxime axetil, the weight ratio of amorphous cefuroxime axetil to colloidal silicon dioxide must exceed 1:0.1. According to this prescription, the bulk density of the powder in production It will be relatively low, and the number of compactions in dry granulation will be relatively high, which will increase production costs

Method used

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  • Dispersible tablet of cefuroxime axetil
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Preparation:

[0025] Mix cefuroxime axetil, microcrystalline cellulose, crospovidone, sodium lauryl sulfate, colloidal silicon dioxide, orange powder flavor, aspartame, part of stearic acid, and dry granulation to make In the granulation process, 30 meshes are used for whole granulation. During the dry cycle granulation process, the proportion of particles between 30 mesh and 60 mesh sieve is more than 40% as the end point. After the tablet is compressed, the plain tablets are coated according to the conventional film coating operation. When the weight gain of the tablets reaches about 1.5%, the spraying is stopped, and the air is dried to make 1000 tablets.

[0026] The dissolution of cefuroxime axetil dispersible tablets was tested in accordance with the method under the "Chinese Pharmacopoeia" 2010 edition of cefuroxime axetil tablets. The test result reached 97.1% in 15 minutes, the content was 98.2%, and the uniformity of dispersion was dispersed in 1 minute. , Sweet...

Embodiment 2

[0029] Preparation method: same as Example 1, to prepare 1000 tablets.

[0030] The dissolution rate of cefuroxime axetil dispersible tablets was tested according to the method under "Chinese Pharmacopoeia" 2010 edition cefuroxime axetil tablets. The test result reached 98.1% in 15 minutes, and the content was 99.2%. The uniformity of dispersion has been dispersed in 1 minute. , Sweet. Placed for 6 months under the conditions of temperature 40℃±2℃ and humidity 75%±5%, the dissolution rate is 98.5% in 15 minutes, the content is 98.8%, and the uniformity of dispersion is 1 minute and 30 seconds. sweet.

Embodiment 3

5g

[0034] Preparation method: same as Example 1, to prepare 1000 tablets.

[0035] The dissolution of cefuroxime axetil dispersible tablets was tested in accordance with the method under the "Chinese Pharmacopoeia" 2010 edition of cefuroxime axetil tablets. The test result reached 99.1% in 15 minutes, and the content was 99.2%. The uniformity of dispersion was dispersed in 1 minute. , Sweet. Placed for 6 months under the temperature of 40℃±2℃ and humidity of 75%±5%, the dissolution rate is 97.2% for 15 minutes, the content is 99.2%, and the uniformity of dispersion is 1 minute and 30 seconds. sweet.

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Abstract

The invention provides a dispersible tablet of cefuroxime axetil, wherein the preparation formula includes cefuroxime axetil, loading agents, flow aid, disintegrating agents, surface-active agents, flavoring agents, lubricant, essence, and coating powder. According to the invention, specific disintegrating agents are adopted, meanwhile, the use amount of the disintegrating agents is not increased, the dispersion time of the dispersible tablet is shortened, and the dissolution rate of the dispersible tablet is improved; and meanwhile, flavoring agents and essence are added in the formula to mask bitter of the dispersible tablet of cefuroxime axetil, so that the mouth feel of a patient taking the dispersible tablet of cefuroxime axetil can be improved.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical preparation of cefuroxime axetil, in particular to a dispersible tablet of cefuroxime axetil. Background technique [0002] Cefuroxime axetil is a semi-synthetic second-generation cephalosporin with a broad antibacterial spectrum and strong antibacterial activity against Gram-positive and Gram-negative bacteria. It is a prodrug of cefuroxime. After oral administration, it is rapidly hydrolyzed by non-specific esterase in the mucosal cells of the gastrointestinal tract to release cefuroxime and exert its efficacy. Cefuroxime axetil is a lipophilic drug with bitter taste, poor water solubility, difficult to absorb, low bioavailability, and dissolution rate is the limiting factor for drug absorption. [0003] A Chinese patent application document with publication number CN101874791.A discloses a technical solution for improving the dissolution of cefurox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/36A61K31/546A61K47/38A61P31/04
Inventor 夏小军冯玉欢张世喜
Owner GUANGZHOU NANXIN PHARMA
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