CN103610680B - A kind of CEFUROXIME AXETIL composition and method of making the same - Google Patents
A kind of CEFUROXIME AXETIL composition and method of making the same Download PDFInfo
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- CN103610680B CN103610680B CN201310554628.1A CN201310554628A CN103610680B CN 103610680 B CN103610680 B CN 103610680B CN 201310554628 A CN201310554628 A CN 201310554628A CN 103610680 B CN103610680 B CN 103610680B
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Abstract
The invention discloses a kind of cefuroxime ester composition, by weight, this cefuroxime ester composition comprises following component: CEFUROXIME AXETIL 1 part; Low melt wax material 1 part ~ 15 parts; Filler 5 parts ~ 8 parts; Disintegrating agent 0 part ~ 0.6 part; Binding agent 0 part ~ 0.15 part; Correctives 0 part ~ 0.08 part; The invention also discloses a kind of preparation method of cefuroxime ester composition, the cefuroxime ester composition obtained can cover bitter taste of drug well, and dissolution is good, further increases the compliance of patient medication.
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
The advantages such as CEFUROXIME AXETIL is oral cephalosporin class antibiotic, has has a broad antifungal spectrum, antibacterial activity is strong, all have good antibacterial activity to gram-positive microorganism and gram-negative micro-organism, and highly stable and side effect is little to beta-lactamase.But CEFUROXIME AXETIL is to wet, heat all instability, poorly water-soluble, meet water agglomerate, and mouthfeel is extremely bitter, make after granule, dry suspension, liquid preparation and dispersible tablet etc. need the preparation taken with water, very bitter when taking, cause medication poor compliance, be unfavorable for clinical use, especially child, dysphagia etc. can not use tablet, capsule etc. directly to swallow the patient of medication.Prior art does not adopt enclose taste masking technology, but uses the technology such as the correctivess such as common sweeting agent, essence and conventional one-step palletizing, and the bitterness of CEFUROXIME AXETIL cannot be corrected at all, be covered to this method.
CEFUROXIME AXETIL composition component in prior art:
The preparation method of said components, comprises the following steps:
1) take the CEFUROXIME AXETIL of group component, sucrose, sucralose, carboxymethyl starch sodium mix homogeneously, granulate as binding agent with PVP K30 solution;
2) wet compositions is placed in Fluidbedgranulatingdrier and carries out drying, obtain dry composition;
3) by after dry composition granulate, add the Fructus Citri tangerinae powdered flavor of group component, mix homogeneously, to obtain final product.
One, mouthfeel taste test
Summary of the invention
For solving the problem, by using low melt wax material hot melt spray congealing by CEFUROXIME AXETIL enclose, thoroughly solving CEFUROXIME AXETIL bitterness problem, improving CEFUROXIME AXETIL and with the bitterness problem of the preparation of mixing in water for oral taking, clinical application compliance need be improved.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 cover the bitterness of cefuroxime ester formulation, and can ensure the dispersing uniformity of preparation in water and good dissolution, suitable especially child uses, and it is better that bitterness covers effect simultaneously.
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, the consisting of of described cefuroxime axetil granule agent:
Active component in cefuroxime ester composition of the present invention take CEFUROXIME AXETIL as existence form, changes into cefuroxime in vivo and play curative effect of medication effect after patient takes.
Present invention also offers a kind of preparation method of cefuroxime ester composition, described preparation method is that heat melts granulation or heat melts nebulization.
Preferably, described heat melts 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 just started to add filler, disintegrating agent and binding agent when solidifying, then shear granulation;
4) add correctives, mix homogeneously, to obtain final product.
Preferably, described heat melts granulation, comprises the steps:
1) by low melt wax material, CEFUROXIME AXETIL, filler, disintegrating agent, binding agent and correctives, shear-mixed is stirred even;
2) heating and melting gradually, stirs simultaneously, shear granulation;
3) add correctives, mix homogeneously, to obtain final product.
Preferably, described heat melts nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL after dispersion of sieving be dispersed in the low melt wax material of melting, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, CEFUROXIME AXETIL, lower than 10 DEG C, wraps, solidifies formation clathrate by the temperature controlling condensing chamber in condensing chamber;
4) add filler, disintegrating agent and binding agent, carry out shear granulation;
5) add correctives, mix homogeneously, to obtain final product.
Preferably, described heat melts nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL after dispersion of sieving be dispersed in the low melt wax material of melting, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, CEFUROXIME AXETIL, lower than 10 DEG C, wraps, solidifies formation clathrate by the temperature controlling condensing chamber in condensing chamber;
4) add filler, disintegrating agent and binding agent, carry out one-step palletizing;
5) add correctives, mix homogeneously, to obtain final product.
Preferably, described heat melts nebulization, comprises the steps:
1) by low melt wax material heating and melting;
2) CEFUROXIME AXETIL after dispersion of sieving be dispersed in the low melt wax material of melting, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, CEFUROXIME AXETIL, lower than 10 DEG C, wraps, solidifies formation clathrate by the temperature controlling condensing chamber in condensing chamber;
4) add filler, disintegrating agent, binding agent and correctives, mix homogeneously, to obtain final product.
The present invention is by low melting point waxy materials melt, 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 after spray congealing outside CEFUROXIME AXETIL complete packet wrap one deck low melt wax material insoluble in water, thus 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 bitter effects, 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 medication compliance is better.
Present invention also offers a kind of preparation method of cefuroxime ester composition, its beneficial effect is as follows:
1. 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. tasted by mouthfeel and bitterness detection, cefuroxime ester composition bitterness prepared by the present invention obviously alleviates.
Detailed description of the invention
Embodiment one
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 1. embodiment one 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) be dispersed in the stearic acid of melting by the CEFUROXIME AXETIL after dispersion of sieving, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature controlling condensing chamber is less than 10 DEG C, CEFUROXIME AXETIL is wrapped, solidify formation clathrate in condensing chamber;
4) polyvidone 75% dissolve with ethanol is made 5%(w/w) 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, cross 18 mesh sieves with oscillating granulator, obtained wet granular;
6) wet granular is placed in Fluidbedgranulatingdrier 45 DEG C of dryings, after crossing 18 mesh sieves, 80 mesh sieve screenings respectively, adds Fructus Citri tangerinae essence, be placed in mixer mixing 5min, obtain cefuroxime axetil granule agent.
Embodiment two
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 2. embodiment two component proportion
| 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 and just started to add sorbitol, aspartame, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule sieves through 16,80 mesh sieves after being cooled to room temperature, and the granule between 16 orders that screening obtains, 80 orders, adds Fructus Citri tangerinae essence, mix homogeneously, obtain cefuroxime axetil granule agent.
Embodiment three
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 3. embodiment three components proportioning
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, shear-mixed is stirred even;
2) open heating, limit heating, limit are stirred, and control heating-up temperature 70 DEG C, adjustment mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, shear granulation time 3min ~ 15min;
3) granule sieves through 14,80 mesh sieves after being cooled to room temperature, and the granule between 14 orders that screening obtains, 80 orders, adds Fructus Citri tangerinae essence, mix homogeneously, obtain cefuroxime axetil granule agent.
Embodiment four
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 4. embodiment Four composition proportioning
| 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 just started to add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone when solidifying, then shear granulation;
4) granule sieves through 18,80 mesh sieves after being cooled to room temperature, and the granule between 18 orders that screening obtains, 80 orders, adds Fructus Citri tangerinae essence, mix homogeneously, obtain cefuroxime axetil granule agent.
Embodiment five
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 5. embodiment five component proportion
| 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 and just started to add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule sieves through 18,80 mesh sieves after being cooled to room temperature, and the granule between 18 orders that screening obtains, 80 orders, adds Fructus Citri tangerinae essence, mix homogeneously, obtain cefuroxime axetil granule agent.
Embodiment six
A kind of cefuroxime axetil granule agent, by weight, comprises following component:
Table 6. embodiment six component proportion
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 and just started to add mannitol, acesulfame potassium, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule sieves through 18,80 mesh sieves after being cooled to room temperature, and the granule between 18 orders that screening obtains, 80 orders, adds Fructus Citri tangerinae essence, mix homogeneously, obtain cefuroxime axetil granule agent.
Embodiment seven
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 7. embodiment seven component proportion
| 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) be dispersed in the stearic acid of melting by the CEFUROXIME AXETIL after dispersion of sieving, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature controlling condensing chamber is less than 30 DEG C, CEFUROXIME AXETIL is wrapped, solidify formation clathrate in condensing chamber;
4) polyvidone is mixed with 5%(w/w) aqueous solution, as binding agent;
5) after CEFUROXIME AXETIL clathrate, sucrose, sucralose and carboxymethylstach sodium being crossed 60 mesh sieves respectively, add in fluid bed, adopt top spray to granulate, control inlet temperature≤50 DEG C;
6), after dry granule crosses 18 mesh sieves respectively, add Fructus Citri tangerinae essence and xanthan gum, be placed in mixer mixing 5min, obtain cefuroxime axetil for suspension.
Embodiment eight
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 8. embodiment eight component proportion
| 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 and just started to add sorbitol, aspartame, hypromellose, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule to be cooled to after room temperature through 20 mesh sieves, adds Fructus Citri tangerinae essence, mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment nine
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 9. embodiment nine component proportion
| 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 and just started to add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule to be cooled to after room temperature through 16 mesh sieves, adds Fructus Citri tangerinae essence, mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment ten
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 10. embodiment ten component proportion
| 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 and just started to add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule to be cooled to after room temperature through 18 mesh sieves, adds Fructus Citri tangerinae essence, mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment 11
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 11. embodiment 11 component proportion
| 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 and just started to add mannitol, acesulfame potassium, hydroxypropyl cellulose, carboxymethylstach sodium and polyvidone when solidifying, control mixing speed is 2rps ~ 6rps, and shear rate is 2rps ~ 30rps, then shear granulation;
4) granule to be cooled to after room temperature through 14 mesh sieves, adds Fructus Citri tangerinae essence, mix homogeneously, obtains cefuroxime axetil for suspension.
Embodiment 12
A kind of cefuroxime axetil for suspension, by weight, comprises following component:
Table 12. embodiment 12 component proportion
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 suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, the temperature controlling condensing chamber is less than 30 DEG C, CEFUROXIME AXETIL is wrapped, solidify formation clathrate in condensing chamber;
4) add sucrose, mix homogeneously, obtain 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.
It is suspension that embodiment one to ten two adds appropriate warm water respectively with the cefuroxime ester composition prepared by prior art; In 24 health adults, carry out taste test, in table 13, give experimenter the accepted number in various degree to its mouthfeel.
Table 13 sensory test table
| Sample ID | Mouthfeel is fine | Can accept | Partially bitter | Extremely bitter |
| Embodiment one | 18 | 6 | 0 | 0 |
| Embodiment two | 15 | 9 | 0 | 0 |
| Embodiment three | 13 | 11 | 0 | 0 |
| Embodiment four | 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 ten two.
Two, bitterness testing result compares
The bitterness of the oral solid formulations such as cefuroxime axetil granule agent, dry suspension is all from CEFUROXIME AXETIL, therefore CEFUROXIME AXETIL stripping quantity is measured according to patient's oral medication process, bitterness when product is taken can be reflected, be accustomed to according to patient medication, calculate according to 0.25g specification each serving consumption, be about 100ml with water, take within 5min; The product prepared with prior art is commonly used dose 0.25g specification one bag and is poured in 100ml purified water, and place 5min, the CEFUROXIME AXETIL of stripping is as base value (the 6 increment product that measure are averaged).Each embodiment is prepared sample and is used 100ml water by the CEFUROXIME AXETIL amount that conversion is identical, the CEFUROXIME AXETIL of 5min stripping obtains sample bitterness coefficient (measuring 6 increment product) 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
As can be seen from the comparative result of table 14, the bitterness coefficient of prior art is 1.00, and bitterness coefficient is all no more than 0.24 in embodiment one to ten two, illustrate that the bitterness of the embodiment of the present invention one to ten two is more obvious than prior art to alleviate, use 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 0.07MpH7.0 phosphate 900ml, slurry processes, rotating speed 50rpm, 30min samples, and 280nm wavelength detecting, standard limits regulation 30min dissolution is not less than 60%.
Table 15 dissolution testing result
As can be seen from the dissolution testing result of table 15, the average dissolution of embodiment one is 88.63%, the average dissolution of embodiment two is 86.56%, the average dissolution of embodiment three is 90.72%, the average dissolution of embodiment four 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 one to ten two is all far longer than 60% of standard regulation, 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 melting point candle materials enclose, substantially not stripping in the oral cavity during drug administration, so the existence of the imperceptible bitterness of patient, good mouthfeel, but it is good to detect dissolution according to dissolution method, also normally can discharge in body, not affect curative effect of medication.
More than detailed description of the invention in conjunction with embodiment; only for technical conceive of the present invention and feature are described; its object is to allow person skilled in the art understand content of the present invention and to be implemented; protection scope of the present invention can not be limited with this; all equivalences done according to spirit of the present invention change or modify, and all should be encompassed in protection scope of the present invention.
Claims (2)
1. a cefuroxime axetil granule agent, is characterized in that: by weight, consisting of of described cefuroxime axetil granule agent:
The preparation method of described cefuroxime axetil granule agent is that heat melts nebulization, and described heat melts nebulization, comprises the steps:
1) by stearic acid heating and melting;
2) be dispersed in the stearic acid of melting by the CEFUROXIME AXETIL after dispersion of sieving, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, CEFUROXIME AXETIL, lower than 10 DEG C, wraps, solidifies formation clathrate by the temperature controlling condensing chamber in condensing chamber;
4) add sucrose, sucralose, carboxymethylstach sodium and polyvidone, carry out shear granulation or one-step palletizing; Add Fructus Citri tangerinae essence, mix homogeneously, to obtain final product; Or adding sucrose, sucralose, carboxymethylstach sodium, polyvidone and Fructus Citri tangerinae essence, mix homogeneously, to obtain final product.
2. the preparation method of cefuroxime axetil granule agent according to claim 1, is characterized in that: described preparation method is that heat melts nebulization, comprises the steps:
1) by stearic acid heating and melting;
2) be dispersed in the stearic acid of melting by the CEFUROXIME AXETIL after dispersion of sieving, dispersed with stirring evenly makes suspension;
3) by compressed air, suspension atomization is sprayed into condensing chamber, CEFUROXIME AXETIL, lower than 10 DEG C, wraps, solidifies formation clathrate by the temperature controlling condensing chamber in condensing chamber;
4) add sucrose, sucralose, carboxymethylstach sodium and polyvidone, carry out shear granulation or one-step palletizing; Add Fructus Citri tangerinae essence, mix homogeneously, to obtain final product; Or adding sucrose, sucralose, carboxymethylstach sodium, polyvidone and Fructus Citri tangerinae essence, mix homogeneously, to obtain final product.
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| CN110038013B (en) * | 2018-01-15 | 2022-02-11 | 成都倍特药业股份有限公司 | Cefuroxime axetil solid preparation and preparation process thereof |
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