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Cephalosporin ester drug particle in non-gel state after meeting water, and preparation method and application of drug particle

A cephalosporin, non-gel technology, applied in the field of pharmaceutical preparations, can solve the problems of gelation, slow dissolution and the like

Active Publication Date: 2013-04-10
SUZHOU CHUNGHWA CHEM & PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is that in the prior art, when cephalosporin ester drugs are dissolved in water, the gelation phenomenon is serious, thereby causing the problem that the dissolution rate is relatively slow, thereby providing a cephalosporin that is in a non-gel state when it encounters water. Bactericin ester drug granules, preparation method and application thereof, good dispersibility and hydrophilicity during dissolution, no gelation phenomenon, and greatly improved dissolution rate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0026] Prepare the drug granules shown in Examples 1-3 with the following method and the formula shown in Table 1: sieve the cefuroxime axetil raw material, micropowder silica gel, anti-gelling auxiliary agent, and disintegrant respectively, and then sieve the above-mentioned The final raw and auxiliary materials are mixed evenly, pressed into large pieces, and then sieved and granulated. The details are shown in Table 1:

[0027] Table 1 Statistical Table of Formulation of Embodiment 1-3 (parts by weight)

[0028] .

Embodiment 4-6

[0030] Examples 4-6 adopt the following formula: in parts by weight, 100 parts of cefuroxime axetil, 3.2 parts of micropowdered silica gel, 3.2 parts of stearic acid as an anti-gelling agent, and 14 parts of croscarmellose sodium as a disintegrating agent.

[0031] The preparation method is as follows: mix part of cefuroxime axetil raw material (premixed cefuroxime axetil raw material) with part of micropowder silica gel (premixed micropowder silica gel), sieve, and then mix with other cefuroxime axetil raw materials that have passed through a 40-mesh sieve respectively , micropowder silica gel, anti-gelling agent stearic acid, and disintegrating agent are mixed, pressed into large tablets, and then granulated through a 24-mesh sieve. The details are shown in Table 2:

[0032] Table 2 Statistical table of premixed cefuroxime axetil raw materials and premixed micropowder silica gel in Examples 4-6 (parts by weight)

[0033] .

Embodiment 7-12

[0049] With reference to the preparation method of Example 2, the drug granules of Examples 7-12 were prepared, and the bulk density and dissolution rate of the granules were measured according to the methods shown in Table 5. The details are shown in Table 5:

[0050] Table 5 The formula of embodiment 7-12 and the statistical table of dissolution test situation (parts by weight)

[0051] .

[0052] Analysis of the above measurement data shows that the formula and preparation method of the present invention are applicable to other cephalosporin ester drugs such as cefpodoxime axetil, cefditoren axetil and cefditoren neopentyl axetil, and have a wide range of uses. At the same time, the bulk density of the obtained granules is also in the range of 0.4-0.6g / ml, and it disperses quickly in the dissolution medium without gelation phenomenon. The average dissolution rate in 15 minutes is over 93%, and the average dissolution rate in 45 minutes is over 97%.

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Abstract

The invention relates to a cephalosporin ester drug particle in a non-gel state after meeting water, and a preparation method and an application of the drug particle, and belongs to the technical field of pharmaceutical preparations. The drug particle comprises the following raw and auxiliary materials: a cephalosporin ester drug with the bulk density of 0.1-0.3g / ml, and the following auxiliary materials accounting for the mass percentage of the cephalosporin ester drug as follows: 2-4.5% of micropowder silica gel, 2-4.5% of anti-gel adjuvant, and 12-16% of disintegrating agent, wherein the anti-gel adjuvant is a glidant and / or a lubricant with the bulk density greater than 0.50g / ml. According to the cephalosporin ester drug particle in the non-gel state after meeting the water, and the preparation method and the application of the drug particle, the problem that the dissolution rate is relatively low due to the fact that gelatinization is severe when the cephalosporin ester drug is dissolved out in the water in the prior art is solved, the dispersity and the hydrophilicity in a dissolution-out process are good, no gelatinization exists, and the dissolution rate is increased greatly.

Description

technical field [0001] The invention relates to a drug granule, in particular to a cephalosporin ester drug granule in a non-gel state when exposed to water and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Cephalosporin ester drugs are a class of β-lactam antibiotics, which have the advantages of strong bactericidal activity, low toxicity, wide indications and good clinical efficacy, so they are widely used, such as cefditoren pivoxil and cefditoren neopentyl pivoxil , cefuroxime axetil and cefpodoxime axetil. From the perspective of physical and chemical properties, cephalosporin ester drugs have a low bulk density, generally 0.1-0.3g / ml, loose texture, poor fluidity, and are prone to gelation when encountering solvents such as water and ethanol. [0003] At present, the commonly used dosage forms of cephalosporin esters include tablets, capsules and granules, etc. The preparation methods inclu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/546A61K47/38A61K47/36A61K47/32A61K47/04A61P31/04
Inventor 李远福陈娟翟晶晶
Owner SUZHOU CHUNGHWA CHEM & PHARMA IND
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