CN106176617B - Amoxicillin soluble powder and preparation method thereof - Google Patents
Amoxicillin soluble powder and preparation method thereof Download PDFInfo
- Publication number
- CN106176617B CN106176617B CN201610790887.8A CN201610790887A CN106176617B CN 106176617 B CN106176617 B CN 106176617B CN 201610790887 A CN201610790887 A CN 201610790887A CN 106176617 B CN106176617 B CN 106176617B
- Authority
- CN
- China
- Prior art keywords
- soluble powder
- amoxicillin
- parts
- preparation
- amoxicillin soluble
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
Abstract
The present invention relates to amoxicillin soluble powder and preparation method thereof.Amoxicillin soluble powder is made up of in parts by weight following components：10~60 parts of Utimox, 3~20 parts of cosolvent, 3~30 parts of stabilizer, 0.4~85 part of filler, 0.05~1 part of glidant；Wherein, stabilizer is calgon.Preparation method includes：Raw material Utimox is micronized, and cosolvent, stabilizer, filler and glidant are pulverized and sieved respectively, and material is well mixed, and is dispensed, and is examined, is produced amoxicillin soluble powder finished product.Not only solubility is high for amoxicillin soluble powder of the present invention, and stability is good, can effectively suppress the hydrolysis of medicine, beneficial to practical application.
Description
Technical field
The present invention relates to a kind of amoxicillin soluble powder and preparation method thereof, suitable for field of veterinary.
Background technology
According to the inventors knowledge, Amoxicillin belongs to semi-synthetic penicillins beta-lactam antibiotic, has very strong kill
Bacterium acts on, and has a broad antifungal spectrum, has powerful inhibitory or killing effect to most of pathogenic gram-positive bacterias and Gram-negative bacteria.As
The general antibiotic of people and animals, Amoxicillin oral absorption is rapid, to the infection of the upper respiratory tract, urinary system infection contamination, enteric infection etc.
There is preferable preventive and therapeutic effect.
The water solubility of Amoxicillin at room temperature is about 1mg/ml, is microsolubility material.Due to containing in the molecule of Amoxicillin
There is carboxylic group, so alkaline environment is greatly improved the solubility of Amoxicillin.
However, the active group as antibacterial in the body of Amoxicillin, the beta-lactam nucleus in the molecule of Amoxicillin is in acidity
Under the conditions of it is stable, but in alkaline environment then easy open loop and cause Amoxicillin to be failed.
Soluble powder is veterinary drug common formulations, and due to storage transport and all very convenient with liquid, therefore cultivation industry is inclined to use
The formulation.
Prepare amoxicillin soluble powder, it is usually required mainly for solve two problems：(1) drug solubility is improved, (2) ensure dynamic
In the thing clinical drinking-water cycle, the non-degradable failure of pharmaceutical aqueous solution.
Found through retrieval, it is Application No. CN201410755886.0, application publication number CN105726487A, entitled
《A kind of high content amoxicillin soluble powder agent preparation method and application》Chinese invention patent application, the soluble powder by
Amoxicillin, cosolvent, stabilizer, flavouring and soluble filler composition, its cosolvent include sodium carbonate, and stabilizer includes
Sodium dihydrogen phosphate.
It is Application No. CN201410687658.4, application publication number CN104523687A, entitled《A kind of animal compound
Amoxicillin, probenecid salt soluble powder and its preparation technology》Chinese invention patent application, the soluble powder include Amoxicillin,
Probenecid salt, cosolvent, auxiliary material, its cosolvent include sodium carbonate.
It is Application No. CN200910054709.9, application publication number CN101601657A, entitled《A kind of Amoxicillin
Soluble powder and preparation method thereof》Chinese invention patent application, the soluble powder includes Amoxicillin and the anhydrous carbon of cosolvent
Sour sodium.
The content of the invention
The technical problems to be solved by the invention are：The problem of overcoming prior art to exist, there is provided a kind of Amoxicillin can
Dissolubility powder, solubility is high, and stability is good；There is provided its preparation method simultaneously.
The major technique design of the present invention is as follows：Inventor is by furtheing investigate Amoxicillin characteristic, from prescription and technique
Two aspects make targeted design respectively, have drawn finally better than the technical scheme using aforementioned patent as the prior art of representative,
Solubility and stability more preferably amoxicillin soluble powder, and meet pharmacopeia and Clinical practice requirement can be made.
The technical scheme that the present invention solves its technical problem is as follows：
A kind of amoxicillin soluble powder, it is characterized in that, it is made up of in parts by weight following components：
10~60 parts of Utimox, 3~20 parts of cosolvent, 3~30 parts of stabilizer, 0.4~85 part of filler,
0.05~1 part of glidant；Wherein, stabilizer is calgon.
Preferably, the cosolvent is strong base weak acid type salt, including at least one of natrium carbonicum calcinatum, anhydrous sodium phosphate.
Preferably, the filler comprises at least one of sucrose, lactose, PEG6000, PVPK30.
Preferably, the glidant is superfine silica gel powder.
Preferably, each component and its parts by weight are：
3~20 parts of 11.5~57.5 parts of Utimox, cosolvent natrium carbonicum calcinatum or anhydrous sodium phosphate, it is stable
3~30 parts of agent calgon, 0.45~82.45 part of filler sucrose, 0.05~1 part of glidant superfine silica gel powder.
The present invention also provides：
The preparation method of amoxicillin soluble powder described previously, it is characterized in that, comprise the following steps：
The first step, raw material Utimox is micronized, it is 50~100 microns to make its particle diameter；
Second step, cosolvent, stabilizer, filler and glidant pulverized and sieved respectively, sieve mesh number is 80~100
Mesh；
3rd step, the first step, second step resulting material be well mixed, incorporation time is 0.5~2 hour；Afterwards, will be mixed
Material dispenses after conjunction, examines, produces amoxicillin soluble powder finished product.
Preferably, mechanical lapping or air-flow crushing are used in the first step, during micronizing.
Compared with prior art, beneficial effects of the present invention are as follows：
(1) solubility property is good.Solubility (in terms of Amoxicillin) can reach 6mg/ml in finished product water at normal temperature of the present invention,
And can be thoroughly to be dissolved in the short time.This provides great convenience to aquaculture preparating liquid.
(2) stable storing.Finished product Acceleration study still meets quality criteria requirements after 6 months.
(3) stabilized aqueous solution of clinical concentration.At room temperature, within the drinking water for animals cycle (4~8 hours), with the present invention into
The aqueous solution medicament contg that product are prepared, which has no, to be decreased obviously, and can guarantee that drug effect is unaffected in the drinking-water cycle.
(4) formulation ingredients involved in the present invention are that field of medicaments is commonly used, cheap and easy to get, safe；This hair
The simple operation of process of bright design, it is adapted to extension production.
Embodiment
The present invention is described in further detail with reference to embodiment.But the invention is not restricted to given example.
Embodiment 1
The amoxicillin soluble powder of the present embodiment, its composition and preparation technology are as follows：
(1) raw material Utimox is micronized, by the way of air-flow crushing, obtain particle diameter 50~
100 microns of drug particle.
(2) anhydrous sodium phosphate, calgon, sucrose, superfine silica gel powder are pulverized and sieved, sieve mesh number be 80~
100 mesh.
(3) mix：(1), (2) resulting material are mixed, incorporation time is 40 minutes, is well mixed stand-by.
(4) dispense：(3) resulting material is dispensed, examines, obtains amoxicillin soluble powder finished product.
Embodiment 2
The amoxicillin soluble powder of the present embodiment, its composition and preparation technology are as follows：
(1) raw material Utimox is micronized, by the way of air-flow crushing, obtain particle diameter 50~
100 microns of drug particle.
(2) natrium carbonicum calcinatum, calgon, sucrose, superfine silica gel powder are pulverized and sieved, sieve mesh number be 80~
100 mesh.
(3) mix：(1), (2) resulting material are mixed, incorporation time is 40 minutes, is well mixed stand-by.
(4) dispense：(3) resulting material is dispensed, examines, obtains amoxicillin soluble powder finished product.
Embodiment 3
The amoxicillin soluble powder of the present embodiment, its composition and preparation technology are as follows：
(1) raw material Utimox is micronized, by the way of air-flow crushing, obtain particle diameter 50~
100 microns of drug particle.
(2) anhydrous sodium phosphate, calgon, sucrose, superfine silica gel powder are pulverized and sieved, sieve mesh number be 80~
100 mesh.
(3) mix：(1), (2) resulting material are mixed, incorporation time is 40 minutes, is well mixed stand-by.
(4) dispense：(3) resulting material is dispensed, examines, obtains amoxicillin soluble powder finished product.
The contrast test of embodiment 4：
Had the advantage that for the checking amoxicillin soluble powder of the invention prepared, particularly stabilizer calgon pair
The stabilization of medicament contg, choose following sample and carry out contrast test, including：Sample, the A Moxi of the preparation of embodiment 1~3
Woods raw material, comparative sample 1, comparative sample 2.The comparison project of progress includes：Sample dissolubility test, pharmaceutical aqueous solution at room temperature
Stability, medicine storage stability.
Above-mentioned comparative sample 1, its composition are：Utimox 11.5g, natrium carbonicum calcinatum 3g, sucrose
85.45g superfine silica gel powder 0.05g.Preparation technology is consistent with the present invention.
Above-mentioned comparative sample 2, its composition are：Utimox 11.5g, natrium carbonicum calcinatum 3g, di(2-ethylhexyl)phosphate
Hydrogen sodium 10g, sucrose 75.45g, superfine silica gel powder 0.05g.Preparation technology is consistent with the present invention.
(1) solubility experiment：
Experimental method and condition：A certain amount of test sample powder is weighed, is placed in 100ml, the water that temperature is 25 DEG C ± 2 DEG C
In, dissolving situation is observed after being shaken 30 seconds, 15 minutes every 5 minutes, and the apparent solubility of each sample is calculated with this.As a result such as
Shown in table 1.
The solubility experiment result of table 1
As can be seen from Table 1, compared to Amoxicillin raw material and comparative sample 1,2, dissolving of the embodiment 1 to 3 in water
Degree is greatly improved.
(2) aqueous stability
Experimental method and condition：Weigh a certain amount of test sample powder, with running water be configured to concentration be 0.5mg/ml (for
Clinic recommends the solution twice) of dosage, and opening is positioned in 25 DEG C ± 2 DEG C of environment, and 1,2,4,24 after preparation
Hour measure content, and compared with 0h contents are postponed, calculate degradation rate %.As a result it is as shown in table 2.
The each sample aqueous solution degradation rate of table 2 (%, compared with 0h contents after preparation)
It can be seen from the result of table 2 there is the shortcomings that content decline in the Amoxicillin aqueous solution at room temperature.Add cosolvent
(sodium carbonate) can accelerate content to decline (control sample 1).Calgon is only added as stabilizer, can effectively suppress Ah not
The hydrolysis failure process (embodiment 1~3) in XiLin, and medicine can not effectively be suppressed by adding other stabilizers (such as sodium dihydrogen phosphate)
Hydrolysis (control sample 2).
(3) accelerated stability is tested
Experimental method and condition：In order to predict stable case of each sample during storage, according to《Chinese veterinary pharmacopoeia》
Relevant regulations carry out accelerated stability experiment.Each sample is sealed with aluminium foil bag and packed, and experiment condition is 40 DEG C of temperature, relative humidity
75%, investigate character change and content decline degree that each sample is placed 1,2,3,6 month on this condition.As a result as table 3,
Shown in table 4.
The each sample accelerated stability Apparent character result of table 3 (0 month sample is off-white powder)
The each sample accelerated stability assay result of table 4, is represented (%, each month is compared with 0 month) with degradation rate
Cosolvent can influence the storage stability of Amoxicillin it can be seen from table 3 and table 4, and it is inclined only to the addition of six
Sodium phosphate is not affected by and significantly affected as sample (embodiment 1~3) medicament contg under the conditions of Acceleration study of stabilizer, content
As a result still it is maintained at as defined in quality standard in scope.
Three contrast and experiments show that amoxicillin soluble powder prepared by the present invention has good water solubility, storage steady
The not degradable advantage of fixed, Clinical practice preparation solution, convenient and quality assurance is provided for animal clinical medication.
Claims (3)
1. a kind of amoxicillin soluble powder, it is characterized in that, it is made up of in parts by weight following components：
3~20 parts of 11.5~57.5 parts of Utimox, natrium carbonicum calcinatum or anhydrous sodium phosphate, calgon 3~
30 parts, 0.45~82.45 part of sucrose, 0.05~1 part of superfine silica gel powder.
2. the preparation method of amoxicillin soluble powder described in claim 1, it is characterized in that, comprise the following steps：
The first step, raw material Utimox is micronized, it is 50~100 microns to make its particle diameter；
Second step, cosolvent, stabilizer, filler and glidant pulverized and sieved respectively, sieve mesh number is 80~100 mesh；
3rd step, the first step, second step resulting material be well mixed, incorporation time is 0.5~2 hour；Afterwards, by after mixing
Material dispenses, and examines, produces amoxicillin soluble powder finished product.
3. preparation method according to claim 2, it is characterized in that, use mechanical lapping or gas in the first step, during micronizing
Stream crushes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610790887.8A CN106176617B (en) | 2016-08-31 | 2016-08-31 | Amoxicillin soluble powder and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610790887.8A CN106176617B (en) | 2016-08-31 | 2016-08-31 | Amoxicillin soluble powder and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106176617A CN106176617A (en) | 2016-12-07 |
| CN106176617B true CN106176617B (en) | 2018-02-13 |
Family
ID=58085969
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610790887.8A Active CN106176617B (en) | 2016-08-31 | 2016-08-31 | Amoxicillin soluble powder and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106176617B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107582539A (en) * | 2017-06-01 | 2018-01-16 | 合肥远志医药科技开发有限公司 | Amoxil capsule and preparation method thereof |
| CN107308116A (en) * | 2017-07-06 | 2017-11-03 | 山东中牧兽药有限公司 | A kind of amoxicillin soluble powder for animals and preparation method thereof |
| CN108261397B (en) * | 2018-02-09 | 2020-09-22 | 山东华辰制药有限公司 | High-content amoxicillin soluble powder and preparation method thereof |
| CN110522730B (en) * | 2019-07-31 | 2021-10-01 | 洛阳惠中兽药有限公司 | Amoxicillin soluble powder and preparation method thereof |
| CN110711193A (en) * | 2019-12-03 | 2020-01-21 | 成都新亨药业有限公司 | Compound amoxicillin soluble powder and preparation method thereof |
| CN111529493A (en) * | 2020-05-30 | 2020-08-14 | 潍坊中科力邦生物工程研究院 | Amoxicillin soluble powder easy to dissolve in water and high in stability and preparation method thereof |
| CN112587481B (en) * | 2020-12-28 | 2022-03-15 | 成都中牧生物药业有限公司 | Alkalescent amoxicillin soluble powder and preparation method thereof |
| CN113304112B (en) * | 2021-05-26 | 2022-09-30 | 浙江耐司康药业有限公司 | Amoxicillin soluble powder and preparation method thereof |
| CN115531321A (en) * | 2022-10-27 | 2022-12-30 | 广东温氏大华农生物科技有限公司 | Amoxicillin composition, preparation method and application thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101601657A (en) * | 2009-07-13 | 2009-12-16 | 上海恒丰强动物药业有限公司 | A kind of amoxicillin soluble powder and preparation method thereof |
| CN101836950A (en) * | 2010-03-12 | 2010-09-22 | 陕西合成药业有限公司 | Moxifloxacin hydrochloride glucose injection and preparation method and use thereof |
| CN104840426A (en) * | 2015-06-03 | 2015-08-19 | 上海富朗特动物保健有限公司 | Amoxicillin soluble powder as well as preparation method and application of amoxicillin soluble powder |
| CN105726487A (en) * | 2014-12-10 | 2016-07-06 | 瑞普（天津）生物药业有限公司 | Preparation method and application of high-amoxicillin-content soluble powder |
-
2016
- 2016-08-31 CN CN201610790887.8A patent/CN106176617B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101601657A (en) * | 2009-07-13 | 2009-12-16 | 上海恒丰强动物药业有限公司 | A kind of amoxicillin soluble powder and preparation method thereof |
| CN101836950A (en) * | 2010-03-12 | 2010-09-22 | 陕西合成药业有限公司 | Moxifloxacin hydrochloride glucose injection and preparation method and use thereof |
| CN105726487A (en) * | 2014-12-10 | 2016-07-06 | 瑞普（天津）生物药业有限公司 | Preparation method and application of high-amoxicillin-content soluble powder |
| CN104840426A (en) * | 2015-06-03 | 2015-08-19 | 上海富朗特动物保健有限公司 | Amoxicillin soluble powder as well as preparation method and application of amoxicillin soluble powder |
Also Published As
| Publication number | Publication date |
|---|---|
| CN106176617A (en) | 2016-12-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN106176617B (en) | Amoxicillin soluble powder and preparation method thereof | |
| US20050277634A1 (en) | Liquid composition for veterinary medicine and process for the preparation and use thereof | |
| CA2777225C (en) | Granulated anthelmintic preparations and delivery systems | |
| CN106074543B (en) | A kind of water-soluble synergistic composition and its application containing Amoxicillin | |
| CN102525963B (en) | Netilmicin sulfate lyophiled powder injection and preparation method thereof | |
| CN101496811B (en) | Soluble and stable tilmicosin composition | |
| CN115337292A (en) | Inhalation solution pharmaceutical composition and preparation method thereof | |
| CN102860980A (en) | Method for preparing rocuronium bromide injection | |
| CN104013629B (en) | The compound medicament composition of cefoperazone sodium and tazobactam sodium and preparation technology thereof | |
| CN117379378A (en) | Compound amoxicillin soluble powder for livestock and preparation process thereof | |
| AU2014249529B2 (en) | Micronized pharmaceutical compositions | |
| EP4000628A1 (en) | Composition and method for vancomycin oral liquid | |
| CN108670956A (en) | A kind of amoxicillin soluble powder and preparation method thereof | |
| CN108853025A (en) | A kind of Tilmicosin solid dispersions and preparation method thereof | |
| NZ552293A (en) | Tablet formulation comprising a macrocyclic lactone and a levamisole compound having anthelmintic activity | |
| CN113197850A (en) | Oral suspension of iron glucoheptonate and ponazuril and preparation method thereof | |
| CN108272756A (en) | A kind of amoxicillin soluble powder and preparation method thereof | |
| CN114306218B (en) | Transmucosal administration R-ketamine pharmaceutical composition meeting pharmaceutical bacteriostasis requirements | |
| AU2008360070B2 (en) | Tablet manufacturing method | |
| AU752266B2 (en) | Micronised pharmaceutical compositions | |
| CN102335136A (en) | Meropenem medicinal composition for injection and preparation method thereof | |
| CN105769756A (en) | Sitafloxacin fumarate injection and preparation method thereof | |
| CN110522730B (en) | Amoxicillin soluble powder and preparation method thereof | |
| CN106937944A (en) | A kind of injection metronidazole freeze-dried powder and preparation method thereof | |
| AU2014201152B2 (en) | Tablet Formulation |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |