CN103610680A - Cefuroxime axetil composition and preparation method thereof - Google Patents
Cefuroxime axetil composition and preparation method thereof Download PDFInfo
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- CN103610680A CN103610680A CN201310554628.1A CN201310554628A CN103610680A CN 103610680 A CN103610680 A CN 103610680A CN 201310554628 A CN201310554628 A CN 201310554628A CN 103610680 A CN103610680 A CN 103610680A
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Abstract
The invention discloses a cefuroxime axetil composition which comprises the following components in parts by weight: 1 part of cefuroxime axetil, 1-15 parts of a low-melting-point wax material, 5-8 parts of filler, 0-0.6 part of a disintegrating agent, 0-0.15 part of a binder and 0-0.08 part of a corrigent. The invention further discloses a preparation method of the cefuroxime axetil composition. The cefuroxime axetil composition obtained can better cover bitter taste of the medicine and is good in dissolution rate, so that the medication compliance of patients is further improved.
Description
Technical field
The present invention relates to technical field of medicine, be specifically related to a kind of CEFUROXIME AXETIL composition and method of making the same.
Background technology
CEFUROXIME AXETIL is oral cephalosporin class antibiotic, has has a broad antifungal spectrum, antibacterial activity is strong, and gram-positive microorganism and gram-negative micro-organism are all had to good antibacterial activity, the advantage such as highly stable and side effect is little to beta-lactamase.But CEFUROXIME AXETIL to wet, heat is all unstable, poorly water-soluble, meet water agglomerate, and mouthfeel is extremely bitter, granulation agent, dry suspension, liquid preparation and dispersible tablet etc. need after preparation that water takes, very bitter while taking, and cause medication poor compliance, be unfavorable for clinical use, especially child, dysphagia etc. can not be used the patient of the medications of directly swallowing such as tablet, capsule.Prior art does not adopt enclose taste masking technology, but uses correctives and the conventional technology such as one-step palletizing such as common sweeting agent, essence, and the bitterness of CEFUROXIME AXETIL cannot be corrected at all, be covered to this method.
Summary of the invention
For addressing the above problem, by using low melt wax material hot melt spray congealing by CEFUROXIME AXETIL enclose, thoroughly solve CEFUROXIME AXETIL bitterness problem, improve the bitterness problem that CEFUROXIME AXETIL need be used the preparation of mixing in water for oral taking, improve clinical application compliance.The invention provides a kind of CEFUROXIME AXETIL composition and method of making the same.This cefuroxime ester composition has steady quality, and release is rapid, and dissolution is good, the advantage of comfortable taste.This CEFUROXIME AXETIL preparation method of composition can be covered the bitterness of cefuroxime ester formulation, can guarantee the dispersing uniformity of preparation in water and good dissolution simultaneously, and suitable especially child uses, and it is better that bitterness is covered effect.
First aspect, the invention provides a kind of cefuroxime ester composition, and by weight, this cefuroxime ester composition comprises following component:
Wherein, described low melt wax material comprises one or several in stearic acid, Glyceryl Behenate, hydrogenated vegetable oil, hexadecanol.
Preferably, described cefuroxime ester composition, by weight, this cefuroxime ester composition comprises following component:
Preferably, described cefuroxime ester composition is granule or dry suspension.
Preferably, consisting of of described cefuroxime axetil granule agent:
Active component in cefuroxime ester composition of the present invention be take CEFUROXIME AXETIL as existence form, changes in vivo the effect of cefuroxime performance curative effect of medication after patient takes.
The present invention also provides a kind of preparation method of cefuroxime ester composition, and described preparation method is that heat is melted granulation or heat is melted nebulization.
Preferably, described heat is melted granulation, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL is dispersed in the low melt wax material of melting and forms suspension;
3) be cooled to gradually and while just having started to solidify, add filler, disintegrating agent and binding agent, then shear granulation;
4) add correctives, mix homogeneously, obtains.
Preferably, described heat is melted granulation, comprises the steps:
1), by low melt wax material, CEFUROXIME AXETIL, filler, disintegrating agent, binding agent and correctives, stir shear-mixed even;
2) heating and melting gradually stirs simultaneously, shear granulation;
3) add correctives, mix homogeneously, obtains.
Preferably, described heat is melted nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent and binding agent, carry out shear granulation;
5) add correctives, mix homogeneously, obtains.
Preferably, described heat is melted nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent and binding agent, carry out one-step palletizing;
5) add correctives, mix homogeneously, obtains.
Preferably, described heat is melted nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent, binding agent and correctives, mix homogeneously, obtains.
The present invention is by the melting of low melt wax material, then more bitter CEFUROXIME AXETIL is dispersed in the low melt wax material of melting and forms suspension, and CEFUROXIME AXETIL in suspension as nucleus, by wrapping one deck insoluble low melt wax material in water in CEFUROXIME AXETIL outside complete packet after spray congealing, thereby cover the bitterness of CEFUROXIME AXETIL.
The invention provides a kind of cefuroxime ester composition, its beneficial effect is as follows:
1. cefuroxime ester composition of the present invention has and well shelters bitterness effect, and has good result of extraction simultaneously;
2. cefuroxime ester composition of the present invention is particularly suitable for the crowd of child and dysphagia, and patient's medication compliance is better.
The present invention also provides a kind of preparation method of cefuroxime ester composition, and its beneficial effect is as follows:
In preparation method of the present invention by CEFUROXIME AXETIL together with low melt wax material enclose, to cover bitterness, promote mouthfeel and medication compliance, and there is good stripping simultaneously;
2. preparation method of the present invention is simple, is particularly suitable for suitability for industrialized production;
3. by mouthfeel, tasted with bitterness and detected, cefuroxime ester composition bitterness prepared by the present invention obviously alleviates.
The specific embodiment
Embodiment mono-
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 1. embodiment mono-component proportion
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 450 |
| Sucrose | 800 |
| Sucralose | 10 |
| Carboxymethylstach sodium | 50 |
| Polyvidone | 7.5 |
| Fructus Citri tangerinae essence | 4.5 |
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 1):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the stearic acid of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature of controlling condensing chamber is below 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, and solidifies formation clathrate;
4) polyvidone is made to 5%(w/w with 75% dissolve with ethanol) solution, as binding agent;
5) by CEFUROXIME AXETIL clathrate, sucrose, sucralose and carboxymethylstach sodium, put in efficient wet granulator and mix 5min, add suitable amount of adhesive soft material processed, with oscillating granulator, cross 18 mesh sieves, make wet granular;
6) wet granular is placed in to 45 ℃ of Fluidbedgranulatingdriers and is dried, cross respectively after 18 mesh sieves, 80 mesh sieves screenings, add Fructus Citri tangerinae essence, be placed in mixer mixing 5min, obtain cefuroxime axetil granule agent.
Embodiment bis-
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 2. embodiment bis-component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 150 |
| Sorbitol | 1000 |
| Aspartame | 15 |
| Carboxymethylstach sodium | 45 |
| Polyvidone | 10 |
| Fructus Fragariae Ananssae powdered flavor | 8 |
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 2):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add sorbitol, aspartame, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature and sieves by 16,80 mesh sieves, and 16 orders that screening obtains, the granule between 80 orders, add Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil granule agent.
Embodiment tri-
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 3. embodiment tri-component proportions
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 3):
1), by stearic acid, CEFUROXIME AXETIL, mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone, stir shear-mixed even;
2) open heating, stir on limit heating, limit, controls 70 ℃ of heating-up temperatures, and adjustment mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, shear granulation time 3min～15min;
3) granule is cooled to room temperature and sieves by 14,80 mesh sieves, and 14 orders that screening obtains, the granule between 80 orders, add Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil granule agent.
Embodiment tetra-
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 4. embodiment tetra-component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Glyceryl Behenate | 1500 |
| Mannitol | 1200 |
| Acesulfame potassium | 15 |
| Carboxymethylstach sodium | 80 |
| Polyvidone | 20 |
| Fructus Citri tangerinae essence | 12 |
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 4):
1) by Glyceryl Behenate heating and melting;
2) CEFUROXIME AXETIL is dispersed in the Glyceryl Behenate of melting and forms suspension;
3) be cooled to gradually and while just having started to solidify, add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone, then shear granulation;
4) granule is cooled to room temperature and sieves by 18,80 mesh sieves, and 18 orders that screening obtains, the granule between 80 orders, add Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil granule agent.
Embodiment five
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 5. embodiment five component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Hydrogenated vegetable oil | 1500 |
| Mannitol | 1200 |
| Acesulfame potassium | 15 |
| Carboxymethylstach sodium | 80 |
| Polyvidone | 20 |
| Fructus Citri tangerinae essence | 12 |
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 5):
1) by hydrogenated vegetable oil heating and melting;
2) CEFUROXIME AXETIL is dispersed in the hydrogenated vegetable oil of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature and sieves by 18,80 mesh sieves, and 18 orders that screening obtains, the granule between 80 orders, add Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil granule agent.
Embodiment six
A cefuroxime axetil granule agent, by weight, comprises following component:
Table 6. embodiment six component proportions
A preparation method for cefuroxime axetil granule agent, comprises the following steps (each amounts of components is by described in table 6):
1) by hexadecanol heating and melting;
2) CEFUROXIME AXETIL is dispersed in the hexadecanol of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature and sieves by 18,80 mesh sieves, and 18 orders that screening obtains, the granule between 80 orders, add Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil granule agent.
Embodiment seven
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 7. embodiment seven component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 450 |
| Sucrose | 800 |
| Sucralose | 10 |
| Xanthan gum | 12 |
| Carboxymethylstach sodium | 50 |
| Polyvidone | 7.5 |
| Fructus Citri tangerinae essence | 4.5 |
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 7):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the stearic acid of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature of controlling condensing chamber is below 30 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, and solidifies formation clathrate;
4) polyvidone is mixed with to 5%(w/w) aqueous solution, as binding agent;
5) CEFUROXIME AXETIL clathrate, sucrose, sucralose and carboxymethylstach sodium are crossed after 60 mesh sieves respectively, added in fluid bed, adopt top spray to granulate, control inlet temperature≤50 ℃;
6) dry granule is crossed after 18 mesh sieves respectively, adds Fructus Citri tangerinae essence and xanthan gum, is placed in mixer mixing 5min, obtains cefuroxime axetil for suspension.
Embodiment eight
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 8. embodiment eight component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 750 |
| Sorbitol | 1000 |
| Aspartame | 15 |
| Hypromellose | 20 |
| Carboxymethylstach sodium | 70 |
| Polyvidone | 10 |
| Fructus Citri tangerinae essence | 8 |
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 8):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add sorbitol, aspartame, hypromellose, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature by 20 mesh sieves, adds Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment nine
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 9. embodiment nine component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 2250 |
| Mannitol | 1200 |
| Acesulfame potassium | 15 |
| Hydroxypropyl cellulose | 20 |
| Carboxymethylstach sodium | 80 |
| Polyvidone | 20 |
| Fructus Citri tangerinae essence | 12 |
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 9):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature by 16 mesh sieves, adds Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment ten
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 10. embodiment ten component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 1500 |
| Mannitol | 1200 |
| Acesulfame potassium | 15 |
| Hydroxypropyl cellulose | 20 |
| Carboxymethylstach sodium | 80 |
| Polyvidone | 20 |
| Fructus Citri tangerinae essence | 12 |
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 10):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature by 18 mesh sieves, adds Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment 11
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 11. embodiment 11 component proportions
| Component | Weight (part) |
| CEFUROXIME AXETIL | 150 |
| Stearic acid | 1500 |
| Mannitol | 1200 |
| Acesulfame potassium | 15 |
| Hydroxypropyl cellulose | 20 |
| Carboxymethylstach sodium | 80 |
| Polyvidone | 20 |
| Fructus Citri tangerinae essence | 12 |
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 11):
1) by stearic acid heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and forms suspension;
3) be cooled to gradually while just having started to solidify and add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone, control mixing speed is 2rps～6rps, and shear rate is 2rps～30rps, then shear granulation;
4) granule is cooled to room temperature by 14 mesh sieves, adds Fructus Citri tangerinae essence, and mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment 12
A cefuroxime axetil for suspension, by weight, comprises following component:
Table 12. embodiment 12 component proportions
A preparation method for cefuroxime axetil for suspension, comprises the following steps (each amounts of components is by described in table 12):
1) by stearic acid and Glyceryl Behenate heating and melting;
2) CEFUROXIME AXETIL is dispersed in the stearic acid of melting and Glyceryl Behenate and forms suspendible
Liquid;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature of controlling condensing chamber is below 30 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, and solidifies formation clathrate;
4) add sucrose, mix homogeneously, obtains cefuroxime axetil for suspension.
comparative example
For clearly setting forth beneficial effect of the present invention, provide the contrast test of cefuroxime ester composition embodiment of the present invention and prior art cefuroxime ester composition as follows.
CEFUROXIME AXETIL composition component in prior art:
The preparation method of said components, comprises the following steps:
1) take CEFUROXIME AXETIL, sucrose, sucralose, the carboxymethyl starch sodium mix homogeneously of group component, with PVP K30 solution, as binding agent, granulate;
2) compositions that will wet is placed in Fluidbedgranulatingdrier and is dried, and obtains dry composition;
3) by after dry composition granulate, add the Fructus Citri tangerinae powdered flavor of group component, mix homogeneously, obtains.
One, mouthfeel taste test
The prepared cefuroxime ester composition of embodiment mono-to 12 and prior art adds respectively appropriate warm water and is suspension; In 24Wei health adult, carry out taste test, in table 13, provided the accepted number in various degree of experimenter to its mouthfeel.
Table 13 sensory test table
| Sample title | Mouthfeel is fine | Can accept | Partially bitter | Extremely bitter |
| Embodiment mono- | 18 | 6 | 0 | 0 |
| Embodiment bis- | 15 | 9 | 0 | 0 |
| Embodiment tri- | 13 | 11 | 0 | 0 |
| Embodiment tetra- | 16 | 8 | 0 | 0 |
| Embodiment five | 14 | 8 | 2 | 0 |
| Embodiment six | 15 | 9 | 0 | 0 |
| Embodiment seven | 20 | 4 | 0 | 0 |
| Embodiment eight | 15 | 8 | 1 | 0 |
| Embodiment nine | 13 | 10 | 1 | 0 |
| Embodiment ten | 15 | 6 | 3 | 0 |
| Embodiment 11 | 16 | 6 | 2 | 0 |
| Embodiment 12 | 21 | 2 | 1 | 0 |
| Prior art | 0 | 0 | 5 | 19 |
Table 13 result clearly illustrates that: respectively compared with prior art, taste is greatly improved the embodiment of the present invention one to 12.
Two, bitterness testing result comparison
The bitterness of the oral solid formulations such as cefuroxime axetil granule agent, dry suspension is all from CEFUROXIME AXETIL, therefore according to patient's oral medication process, measure CEFUROXIME AXETIL stripping quantity, bitterness in the time of can reflecting product and take, according to patient's medication, be accustomed to, each serving consumption, according to 0.25g specification, calculate, the about 100ml of water, takes within 5min; Conventional dose 0.25g specification one bag of product of preparing with prior art is poured in 100ml purified water, places 5min, and the CEFUROXIME AXETIL of stripping is as base value (measuring 6 duplicate samples averages).Each embodiment prepares sample and uses 100ml water by the identical CEFUROXIME AXETIL amount of conversion, the CEFUROXIME AXETIL of 5min stripping obtains sample bitterness coefficient (measuring 6 duplicate samples) divided by base value, coefficient equals 1 and shows to be equal to prior art, be less than 1 and show that bitterness decreases, coefficient is less, bitterness is lighter, and taste masking effect is better.
Table 14 bitterness testing result
From the comparative result of table 14, can find out, the bitterness coefficient of prior art is 1.00, and bitterness coefficient is all no more than 0.24 in embodiment mono-to 12, the bitterness that the embodiment of the present invention one to 12 is described alleviates than prior art is obvious, uses component proportion of the present invention and preparation method sedan-chair taste effect better.
Three, dissolution
With reference to cefuroxime axetil for suspension dissolution detection method in American Pharmacopeia, leaching condition is: dissolution medium is 0.07M pH7.0 phosphate 900ml, slurry method, rotating speed 50rpm, 30min sampling, 280nm wavelength detects, and standard limit regulation 30min dissolution is not less than 60%.
Table 15 dissolution testing result
From the dissolution testing result of table 15, can find out, the average dissolution of embodiment mono-is 88.63%, the average dissolution of embodiment bis-is 86.56%, the average dissolution of embodiment tri-is 90.72%, the average dissolution of embodiment tetra-is 88.11%, the average dissolution of embodiment five is 89.90%, the average dissolution of embodiment six is 83.62%, the average dissolution of embodiment seven is 87.13%, the average dissolution of embodiment eight is 91.39%, the average dissolution of embodiment nine is 87.86%, the average dissolution of embodiment ten is 86.60%, the average dissolution of embodiment 11 is 89.92%, the average dissolution of embodiment 12 is 88.04%, the average dissolution of embodiment mono-to 12 is all far longer than 60% of standard code, illustrates that cefuroxime ester composition prepared by the present invention all has good result of extraction.
CEFUROXIME AXETIL of the present invention is granulated after adopting low melt wax candlewood material enclose, not stripping substantially in oral cavity during drug administration, so existence of the imperceptible bitterness of patient, good mouthfeel, but it is good according to dissolution method, to detect dissolution, in body, also can normally discharge, not affect curative effect of medication.
Above combination embodiment is detailed description of the invention; be only explanation technical conceive of the present invention and feature; its object is to allow person skilled in the art understand content of the present invention and implemented; can not limit protection scope of the present invention with this; all equivalences that spirit is done according to the present invention change or modify, and all should be encompassed in protection scope of the present invention.
Claims (10)
1. a cefuroxime ester composition, is characterized in that: by weight, this cefuroxime ester composition comprises following component:
Wherein, described low melt wax material comprises one or several in stearic acid, Glyceryl Behenate, hydrogenated vegetable oil, hexadecanol.
2. cefuroxime ester composition according to claim 1, is characterized in that: by weight, this cefuroxime ester composition comprises following component:
3. cefuroxime ester composition according to claim 1, is characterized in that: described cefuroxime ester composition is granule or dry suspension.
4. cefuroxime axetil granule agent according to claim 3, is characterized in that: the consisting of of described cefuroxime axetil granule agent:
5. according to the preparation method of the cefuroxime ester composition described in any one in claim 1 to 5, it is characterized in that: described preparation method is that heat is melted granulation or heat is melted nebulization.
6. heat according to claim 5 is melted granulation, it is characterized in that, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL is dispersed in the low melt wax material of melting and forms suspension;
3) be cooled to gradually and while just having started to solidify, add filler, disintegrating agent and binding agent, then shear granulation;
4) add correctives, mix homogeneously, obtains.
7. heat according to claim 5 is melted granulation, it is characterized in that, comprises the steps:
1), by low melt wax material, CEFUROXIME AXETIL, filler, disintegrating agent, binding agent, stir shear-mixed even;
2) heating and melting gradually stirs simultaneously, shear granulation;
3) add correctives, mix homogeneously, obtains.
8. heat according to claim 5 is melted nebulization, it is characterized in that, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent and binding agent, carry out shear granulation;
5) add correctives, mix homogeneously, obtains.
9. heat according to claim 5 is melted nebulization, it is characterized in that, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent and binding agent, carry out one-step palletizing;
5) add correctives, mix homogeneously, obtains.
10. heat according to claim 5 is melted nebulization, it is characterized in that, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL of sieving after disperseing is dispersed in the low melt wax material of melting, dispersed with stirring is evenly made suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, control the temperature of condensing chamber lower than 10 ℃, in condensing chamber, CEFUROXIME AXETIL is wrapped, solidify formation clathrate;
4) add filler, disintegrating agent, binding agent and correctives, mix homogeneously, obtains.
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| CN103816123A (en) * | 2014-03-17 | 2014-05-28 | 广东药学院 | Cefuroxime axetil composition and preparation method thereof |
| CN103877027A (en) * | 2014-03-17 | 2014-06-25 | 广东药学院 | Cefuroxime axetil hot-melt coating composition and preparation method of composition |
| CN104586854A (en) * | 2014-12-24 | 2015-05-06 | 石家庄四药有限公司 | Cefuroxime axetil pharmaceutical composition and preparation method thereof |
| CN106692085A (en) * | 2016-11-24 | 2017-05-24 | 杭州新诺华医药有限公司 | Donepezil oral disintegrating tablet and preparation method thereof |
| CN107050023A (en) * | 2017-01-13 | 2017-08-18 | 北京顺慈医药科技有限公司 | A kind of preparation of Berberine hydrochloride and the formulation method for covering adverse drug taste |
| CN107148267A (en) * | 2014-10-31 | 2017-09-08 | 埃迪制药公司 | Active material particle with dual taste masking technology, its production method and dispersible of the oral cavity comprising it |
| CN109432014A (en) * | 2018-12-08 | 2019-03-08 | 海南医学院 | A kind of masking methods of CEFUROXIME AXETIL drug |
| CN110038013A (en) * | 2018-01-15 | 2019-07-23 | 成都倍特药业有限公司 | A kind of cefuroxime axetil solid preparation and its preparation process |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103816123A (en) * | 2014-03-17 | 2014-05-28 | 广东药学院 | Cefuroxime axetil composition and preparation method thereof |
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| CN103816123B (en) * | 2014-03-17 | 2016-03-02 | 广东药学院 | A kind of CEFUROXIME AXETIL composition and method of making the same |
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| CN106692085A (en) * | 2016-11-24 | 2017-05-24 | 杭州新诺华医药有限公司 | Donepezil oral disintegrating tablet and preparation method thereof |
| CN107050023A (en) * | 2017-01-13 | 2017-08-18 | 北京顺慈医药科技有限公司 | A kind of preparation of Berberine hydrochloride and the formulation method for covering adverse drug taste |
| CN110038013A (en) * | 2018-01-15 | 2019-07-23 | 成都倍特药业有限公司 | A kind of cefuroxime axetil solid preparation and its preparation process |
| CN109432014A (en) * | 2018-12-08 | 2019-03-08 | 海南医学院 | A kind of masking methods of CEFUROXIME AXETIL drug |
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Address after: 518110, No. 16, Lan Qing Road, Guanlan new high tech Zone, Longhua New District, Guangdong, Shenzhen Applicant after: Sinopharm (Shenzhen) Pharmaceutical Co., Ltd. Address before: 518110 Guanlan high tech Industrial Park, Shenzhen, Guangdong, Baoan Applicant before: Zhijun Pharmaceutical Co., Ltd., Shenzhen |
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