CN104983685A - Amoxicillin soluble powder and preparation method - Google Patents
Amoxicillin soluble powder and preparation method Download PDFInfo
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- CN104983685A CN104983685A CN201510357400.2A CN201510357400A CN104983685A CN 104983685 A CN104983685 A CN 104983685A CN 201510357400 A CN201510357400 A CN 201510357400A CN 104983685 A CN104983685 A CN 104983685A
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- soluble powder
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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Abstract
The invention discloses a preparation method for amoxicillin soluble powder. The preparation method for the amoxicillin soluble powder comprises the following steps that amoxicillin is added after polysthylene glycol is heated and fused under the protection of protecting gas, cooling to the normal temperature is conducted after stirring and mixing are conducted, and micelle wrappage is obtained; smashing and filtering are conducted on the micelle wrappage, and finally the amoxicillin soluble powder is obtained. Compared with the prior art, the solubility of the amoxicillin soluble powder is higher, and the stability of the amoxicillin soluble powder is stronger.
Description
Technical field
The present invention relates to new drug research technical field, specifically refer to a kind of amoxicillin soluble powder and preparation method thereof.
Background technology
Amoxicillin belongs to beta-lactam antibiotic, is mainly used in the gram-positive cocci to ampicillin sensitive and gram positive bacterial infection, as Bacillus pasteurii disease, colibacillosis, Hakuri, salmonellosis, and staphylococcus, streptococcal infection; Laying rate decline and reproductive tract anaerobic infection, intestinal infection, intestinal toxicity syndrome auxiliary treatment.
Amoxicillin soluble powder includes kind for " Chinese veterinary pharmacopoeia " 2010 editions, and pharmacopeia prescription is that amoxicillin and anhydrous glucose are formulated.This prescription poor solubility, slightly soluble in water, dissolubility is only 4.0mg/ml.In addition, this prescription stability is also poor, degradation problem under the process of preserving exists moisture absorption, caking, flavescence, content reduction, curative effect.
In order to solve the problem of amoxicillin soluble powder stability and dissolubility, application number is 201010582327.6, publication number is the preparation method that application discloses a kind of amoxicillin soluble powder of CN102008445B, though the amoxicillin soluble powder using this kind of method to prepare can promote the dissolubility of amoxicillin and improve stability, but the dissolubility of this kind of amoxicillin soluble powder and stability are not also very good, can not meet reality need completely.
Summary of the invention
The object of the invention is to: overcome the above-mentioned defect of prior art, provide a kind of amoxicillin soluble powder and preparation method thereof, compared with prior art, the dissolubility of amoxicillin soluble powder prepared by this kind of method is better, stability is stronger.
The present invention is achieved through the following technical solutions:
The present invention adopts dispersion package technology, by by after Polyethylene Glycol melting, adds amoxicillin, after stirring and evenly mixing, is chilled to room temperature, obtains the micelle wrappage that amoxicillin and Polyethylene Glycol are formed after pulverizing and sieving.By solving the stability problem in amoxicillin with the form of micelle wrappage, and increase amoxicillin dissolubility.
A kind of amoxicillin soluble powder preparation method, comprises the following steps:
(1) mix: protection gas protection under by Polyethylene Glycol heating and melting after, add amoxicillin, after stirring and evenly mixing, be cooled to room temperature, obtain micelle wrappage;
(2) pulverize: the micelle wrappage obtained is carried out pulverizing and sieves obtain final products amoxicillin soluble powder.
As the preferred mode of one, in order to successful isolated extraneous air, and avoid protection gas and Polyethylene Glycol or amoxicillin to react, described protection gas can be one or several in rare gas, nitrogen and carbon dioxide.As preferably, the preferred argon of described rare gas.
As a kind of optimal way, micelle wrappage is formed for ensureing that amoxicillin fully can combine with Polyethylene Glycol, in the gross mass of amoxicillin and Polyethylene Glycol, the mass percentage content of amoxicillin is 1%-35%, and the mass percentage content of Polyethylene Glycol is 65%-99%.
As a kind of optimal way, described Polyethylene Glycol is one or more in Macrogol 4000, polyethylene glycol 6000 and PEG 8000.Those skilled in the art should know, Polyethylene Glycol should not be limited to these three kinds.
A kind of amoxicillin soluble powder, adopts said method to obtain.
The application of above-mentioned amoxicillin soluble powder in the medicine for the preparation for the treatment of gram-positive cocci and gram positive bacterial infection.As a kind of optimal way, described gram-positive cocci and gram negative bacteria are Bacillus pasteurii disease, colibacillosis, Hakuri, salmonellosis, one or more in staphylococcus, streptococcus.
The application of above-mentioned amoxicillin soluble powder declining for the preparation for the treatment of laying rate, in the medicine of reproductive tract anaerobic infection and intestinal infection.
The application of above-mentioned amoxicillin soluble powder in the medicine for the preparation of auxiliary treatment intestinal toxicity syndrome.
The present invention compared with prior art, has the following advantages and beneficial effect:
Adopt dispersion package technology, by by after Polyethylene Glycol melting, add amoxicillin, after stirring and evenly mixing, be chilled to room temperature, obtain the micelle wrappage that amoxicillin and Polyethylene Glycol are formed after pulverizing and sieving, this micelle wrappage effectively can solve stability and the solubility problem of amoxicillin, make amoxicillin dissolubility higher, stability is stronger.
Detailed description of the invention
All features disclosed in this description, or the step in disclosed all methods or process, except the speciality mutually repelled and/or step, all can combine by any way, unless specifically stated otherwise, all can be replaced by other equivalences or the alternative features with similar object, namely, unless specifically stated otherwise, each embodiment be characterized as in a series of equivalence or similar characteristics.
Below by three embodiments to prove compared with the patent application that the present invention and application number are 201010582327.6, its dissolubility is better, and stability is stronger.
All adopt nitrogen as protection gas in following three embodiments, those skilled in the art should know that protection gas also can adopt the noble gas such as carbon dioxide, rare gas, or the mixing of these noble gases.
Embodiment 1:
Experimental group one: get 88.5g Macrogol 4000, heating and melting under nitrogen protection, adds 11.5g Utimox after thawing, after stirring and evenly mixing, after being chilled to cold curing, pulverize, cross 80 mesh sieves, obtain content 10% amoxicillin soluble powder.
Contrast groups one: get 88.5g Macrogol 4000 and 11.5g Utimox pulverizes rear mixing respectively, crosses 80 mesh sieves, obtains content 10% amoxicillin soluble powder.
Dissolubility is tested: at normal temperatures, the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups one of getting experimental group one respectively carries out dissolubility test in water.
Dissolubility test result: the dissolubility recording experimental group one amoxicillin soluble powder is that 56g/ml(is in amoxicillin soluble powder), the dissolubility of contrast groups one amoxicillin soluble powder is that 12g/ml(is in amoxicillin soluble powder).
Dissolubility contrast conclusion: compared with contrast groups one, the amoxicillin soluble powder dissolubility of experimental group one is higher, and its dissolubility is better.
Stability test: the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups one of getting experimental group one respectively carries out Acceleration study, temperature 40 DEG C ± 2 DEG C, relative humidity 75% ± 5%, observes color and luster and measures content after 3 months.Assay adopts HPLC method, take octadecylsilane chemically bonded silica as filler, with 0.05mol/L potassium dihydrogen phosphate (by 2mol/L potassium hydroxide solution adjust ph to 5.0) and acetonitrile (volume ratio is for 97.5:2.5) for mobile phase, determined wavelength 254nm.
Stability test result: after 3 months, the amoxicillin soluble powder color and luster of experimental group one is white, and content is 99.96% of amoxicillin labelled amount; Amoxicillin soluble powder color and luster in contrast groups one turns yellow, and content is 80.36% of amoxicillin labelled amount.
Stability test conclusion: compared with contrast groups one, the stability of experimental group one is stronger, and in error allowed band, the amoxicillin soluble powder that can estimate experimental group one does not occur rotten or only has minute quantity to go bad.
Embodiment 2:
Experimental group two: get 77g polyethylene glycol 6000, heating and melting under nitrogen protection, adds 23g Utimox after thawing, after stirring and evenly mixing, after being chilled to cold curing, pulverize, cross 80 mesh sieves, obtain content 20% amoxicillin soluble powder.
Contrast groups two: get 77g polyethylene glycol 6000 and 23g Utimox pulverizes rear mixing respectively, crosses 80 mesh sieves, obtains content 20% amoxicillin soluble powder.
Dissolubility is tested: at normal temperatures, the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups two of getting experimental group two respectively carries out dissolubility test in water.
Dissolubility test result: the dissolubility recording experimental group two amoxicillin soluble powder is that 29g/ml(is in amoxicillin soluble powder), the dissolubility of contrast groups two amoxicillin soluble powder is that 10.8g/ml(is in amoxicillin soluble powder).
Dissolubility contrast conclusion: compared with contrast groups two, the amoxicillin soluble powder dissolubility of experimental group two is higher, and its dissolubility is better.
Stability test: the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups two of getting experimental group two respectively carries out Acceleration study, temperature 40 DEG C ± 2 DEG C, relative humidity 75% ± 5%, observes color and luster and measures content after 3 months.Assay adopts HPLC method, take octadecylsilane chemically bonded silica as filler, with 0.05mol/L potassium dihydrogen phosphate (by 2mol/L potassium hydroxide solution adjust ph to 5.0) and acetonitrile (volume ratio is for 97.5:2.5) for mobile phase, determined wavelength 254nm.
Stability test result: after 3 months, the amoxicillin soluble powder color and luster of experimental group two is white, and content is 100.02% of amoxicillin labelled amount; Amoxicillin soluble powder color and luster in contrast groups two turns yellow, and content is 82.76% of amoxicillin labelled amount.
Stability test conclusion: compared with contrast groups two, the stability of experimental group two is stronger, and in error allowed band, the amoxicillin soluble powder that can estimate experimental group two does not occur rotten or only has minute quantity to go bad.
Embodiment 3:
Experimental group three: get 65.5g PEG 8000, heating and melting under nitrogen protection, adds 34.5g Utimox after thawing, after stirring and evenly mixing, after being chilled to cold curing, pulverize, cross 80 mesh sieves, obtain content 30% amoxicillin soluble powder.
Contrast groups three: get 65.5g PEG 8000 and 34.5g Utimox pulverizes rear mixing respectively, crosses 80 mesh sieves, obtains content 30% amoxicillin soluble powder.
Dissolubility is tested: at normal temperatures, the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups three of getting experimental group three respectively carries out dissolubility test in water.
Dissolubility test result: the dissolubility recording experimental group three amoxicillin soluble powder is that 18g/ml(is in amoxicillin soluble powder), the dissolubility of contrast groups three amoxicillin soluble powder is that 9.5g/ml(is in amoxicillin soluble powder).
Dissolubility contrast conclusion: compared with contrast groups three, the amoxicillin soluble powder dissolubility of experimental group three is higher, and its dissolubility is better.
Stability test: the amoxicillin soluble powder of the amoxicillin soluble powder and contrast groups three of getting experimental group three respectively carries out Acceleration study, temperature 40 DEG C ± 2 DEG C, relative humidity 75% ± 5%, observes color and luster and measures content after 3 months.Assay adopts HPLC method, take octadecylsilane chemically bonded silica as filler, with 0.05mol/L potassium dihydrogen phosphate (by 2mol/L potassium hydroxide solution adjust ph to 5.0) and acetonitrile (volume ratio is for 97.5:2.5) for mobile phase, determined wavelength 254nm.
Stability test result: after 3 months, the amoxicillin soluble powder color and luster of experimental group three is white, and content is 101.88% of amoxicillin labelled amount; Amoxicillin soluble powder color and luster in contrast groups three turns yellow, and content is 68.96% of amoxicillin labelled amount.
Stability test conclusion: compared with contrast groups three, the stability of experimental group three is stronger, and in error allowed band, the amoxicillin soluble powder that can estimate experimental group three does not occur rotten or only has minute quantity to go bad.
The above is only preferred embodiment of the present invention, and not do any pro forma restriction to the present invention, every any simple modification, equivalent variations done above embodiment according to technical spirit of the present invention, all falls into protection scope of the present invention.
Claims (10)
1. an amoxicillin soluble powder preparation method, is characterized in that: comprise the following steps:
(1) mix: protection gas protection under by Polyethylene Glycol heating and melting after, add amoxicillin, after stirring and evenly mixing, be cooled to room temperature, obtain micelle wrappage;
(2) pulverize: the micelle wrappage obtained is carried out pulverizing and sieves obtain final products amoxicillin soluble powder.
2. a kind of amoxicillin soluble powder preparation method according to claim 1, is characterized in that: described protection gas is one or several in rare gas, nitrogen and carbon dioxide.
3. a kind of amoxicillin soluble powder preparation method according to claim 2, is characterized in that: described rare gas is argon.
4. a kind of amoxicillin soluble powder preparation method according to claim 1, it is characterized in that: in the gross mass of amoxicillin and Polyethylene Glycol, the mass percentage content of amoxicillin is 1%-35%, and the mass percentage content of Polyethylene Glycol is 65%-99%.
5. a kind of amoxicillin soluble powder preparation method according to claim 1, is characterized in that: described Polyethylene Glycol is one or more in Macrogol 4000, polyethylene glycol 6000 and PEG 8000.
6. an amoxicillin soluble powder, is characterized in that: adopt the method described in any one of claim 1 ~ 5 to obtain.
7. the application of a kind of amoxicillin soluble powder according to claim 6 in the medicine for the preparation for the treatment of gram-positive cocci and gram positive bacterial infection.
8. application according to claim 7, is characterized in that: described gram-positive cocci and gram negative bacteria are Bacillus pasteurii disease, colibacillosis, Hakuri, salmonellosis, one or more in staphylococcus, streptococcus.
9. the application of a kind of amoxicillin soluble powder according to claim 6 declining for the preparation for the treatment of laying rate, in the medicine of reproductive tract anaerobic infection and intestinal infection.
10. the application of a kind of amoxicillin soluble powder according to claim 6 in the medicine for the preparation of auxiliary treatment intestinal toxicity syndrome.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105168145A (en) * | 2015-10-29 | 2015-12-23 | 林州中农生物肽科技有限公司 | Compound amoxycillin soluble powder and preparation method thereof |
| CN105287389A (en) * | 2015-10-29 | 2016-02-03 | 林州中农生物肽科技有限公司 | Amoxicillin soluble powder and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001045667A2 (en) * | 1999-12-22 | 2001-06-28 | LEK, tovarna farmacevtskih in kemičnih izdelkov, d.d. | Water-soluble powders for oral solution and use thereof |
| CN101023917A (en) * | 2006-02-22 | 2007-08-29 | 刘凤鸣 | Technology for preparing medicine and relative oral preparations |
| CN102008445A (en) * | 2010-12-10 | 2011-04-13 | 青岛康地恩药业有限公司 | Amoxicillin soluble powder as well as preparation method and application thereof |
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2015
- 2015-06-25 CN CN201510357400.2A patent/CN104983685A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001045667A2 (en) * | 1999-12-22 | 2001-06-28 | LEK, tovarna farmacevtskih in kemičnih izdelkov, d.d. | Water-soluble powders for oral solution and use thereof |
| CN101023917A (en) * | 2006-02-22 | 2007-08-29 | 刘凤鸣 | Technology for preparing medicine and relative oral preparations |
| CN102008445A (en) * | 2010-12-10 | 2011-04-13 | 青岛康地恩药业有限公司 | Amoxicillin soluble powder as well as preparation method and application thereof |
Non-Patent Citations (1)
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| 叶兵，等: "阿莫西林缓释片的制备及体外释放度的研究", 《中国抗生素杂志》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105168145A (en) * | 2015-10-29 | 2015-12-23 | 林州中农生物肽科技有限公司 | Compound amoxycillin soluble powder and preparation method thereof |
| CN105287389A (en) * | 2015-10-29 | 2016-02-03 | 林州中农生物肽科技有限公司 | Amoxicillin soluble powder and preparation method thereof |
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Application publication date: 20151021 |