CN105796500A - Amoxicillin soluble powder and preparation method thereof - Google Patents

Amoxicillin soluble powder and preparation method thereof Download PDF

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Publication number
CN105796500A
CN105796500A CN201610166626.9A CN201610166626A CN105796500A CN 105796500 A CN105796500 A CN 105796500A CN 201610166626 A CN201610166626 A CN 201610166626A CN 105796500 A CN105796500 A CN 105796500A
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amoxicillin
soluble powder
beta
poloxamer
pvp
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张先碧
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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 organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • A61K31/43Compounds 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides amoxicillin soluble powder and a preparation method and application thereof. The amoxicillin soluble powder comprises 5%-30% of amoxicillin, 5%-15% of poloxamer F68, 5%-15% of PVPK30, 5%-30% of beta-cyclodextrin and the balance anhydrous glucose. According to the amoxicillin soluble powder and the preparation method and application thereof, the problems that in the prior art, amoxicillin is poor in stability in water, slightly soluble in water, low in dissolution rate and the like are solved.

Description

A kind of amoxicillin soluble powder and preparation method thereof
Technical field
The present invention relates to a kind of amoxicillin soluble powder and preparation method thereof.
Background technology
Amoxicillin is Penicillin antibiotics, to the Streptococcus such as streptococcus pneumoniae, Hemolytic streptococcus, do not produce the aerobic gram positive coccus such as penicillinase staphylococcus, enterococcus faecalis, the aerobic gram-negative bacteria such as escherichia coli, proteus mirabilis, Salmonella, hemophilus influenza, Diplococcus gonorrhoeae do not produce beta lactamase bacterial strain and helicobacter pylori has good antibacterial activity.Amoxicillin is synthesized by suppression bacteria cell wall and plays bactericidal action, antibacterial can be made to rapidly become spheroid and dissolve, rupture.
Amoxicillin is very poor at water stability, and degrade 1-5% per hour;Amoxicillin is slightly soluble in water, and in 100ml water, its dissolubility is only 0.1 gram, and its dissolution is less than 80%;Solve stability, dissolubility and the problem of dissolution, become Wymox and study the difficult problem faced.Having document announcement to add Tween 80, sodium lauryl sulphate, natrium carbonicum calcinatum etc. and increase the dissolubility of amoxicillin, it not only has a biggest toxic and side effects to animal, and lack of homogeneity, water stability is poor;Also having been reported that and amoxicillin is made nanoscale, microcapsule etc., this has delayed the drug action of amoxicillin significantly, reduces its intrinsic curative effect, and preparation technology is more complicated.Develop that a kind of water stability is good, good water solubility, dissolution rate high, the simple Wymox of preparation technology, be increasingly becoming the hot issue of research now.
Amoxicillin can oral administration absorb, but amoxicillin is the most insoluble in water, dissolution rate is low, and due to self structure, apt to deteriorate in water;How to improve this dissolubility in water of amoxicillin, dissolution rate, and to strengthen its stability in water be then problem to be solved by this invention.
Summary of the invention
The invention provides a kind of amoxicillin soluble powder and its preparation method and application, this dissolubility ratio in water of amoxicillin that can solve prior art existence is relatively low, and problem apt to deteriorate in water.
For solving above-mentioned technical problem, the present invention uses the following technical proposals to be: a kind of amoxicillin soluble powder, including amoxicillin 5-30%, poloxamer F68 5-15%, PVP K30 5-15%, beta-schardinger dextrin-5-30%, remaining anhydrous glucose polishing is to 100%.
Preferably, amoxicillin soluble powder includes amoxicillin 10%;Poloxamer F68 5%;PVP K30 10%;Beta-schardinger dextrin-20%;Remaining anhydrous glucose polishing is to 100%.
Another object of the present invention is to provide the preparation method of a kind of amoxicillin soluble powder, comprise the following steps:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number between 40-300 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: after total mixing, 40-300 mesh sieves.
The invention has the advantage that with good effect:
Amoxicillin soluble powder prepared by the present invention, not only increases amoxicillin dissolubility in water, and enhances the stability of amoxicillin.
Detailed description of the invention
The detailed description of the invention of the present invention will be described in detail below.In order to avoid the most unnecessary details, in the examples below to belonging to known structure or function will not be described in detail.
In addition to being defined, technology used in following example and scientific terminology have the identical meanings being commonly understood by with those skilled in the art of the invention.
All of Digital ID, is all approximation.It is to be understood that, although all add term " about " before all of Digital ID of the clearest and the most definite narration.Simultaneously it will also be understood that, although the clearest and the most definite narration, composition described herein is only example, and its equivalent is known in the art.
Test reagent consumptive material used in following example, if no special instructions, is routine biochemistry reagent;Described experimental technique, if no special instructions, is conventional method;Quantitative test in following example, is respectively provided with three times and repeats experiment, results averaged.
Embodiment 1
A kind of amoxicillin soluble powder, it is made up of amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, wherein containing amoxicillin 10g, poloxamer F68 5g, PVP K30 10g, beta-schardinger dextrin-20g, anhydrous glucose polishing to 100g in every 100g.
Its preparation method is:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number at 40 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: grit number excessively, at 40 mesh, obtains high stability amoxicillin soluble powder.
Embodiment 2
A kind of amoxicillin soluble powder, it is made up of amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, wherein containing amoxicillin 15g, poloxamer F68 7.5g, PVP K30 10g, beta-schardinger dextrin-25g, anhydrous glucose polishing to 100g in every 100g.
Its preparation method is:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number at 200 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: grit number excessively, at 200 mesh, obtains high stability amoxicillin soluble powder.
Embodiment 3
A kind of amoxicillin soluble powder, it is made up of amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, wherein containing amoxicillin 20g, poloxamer F68 10g, PVP K30 10g, beta-schardinger dextrin-15g, anhydrous glucose polishing to 100g in every 100g.
Its preparation method is:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number at 300 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: grit number excessively, at 300 mesh, obtains high stability amoxicillin soluble powder.
Embodiment 4
A kind of amoxicillin soluble powder, it is made up of amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, wherein containing amoxicillin 25g, poloxamer F68 5g, PVP K30 10g, beta-schardinger dextrin-10g, anhydrous glucose polishing to 100g in every 100g.
Its preparation method is:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number at 100 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: grit number excessively, at 100 mesh, obtains high stability amoxicillin soluble powder.
Embodiment 5
A kind of amoxicillin soluble powder, it is made up of amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, wherein containing amoxicillin 30g, poloxamer F68 15g, PVP K30 15g, beta-schardinger dextrin-30g, anhydrous glucose polishing to 100g in every 100g.
Its preparation method is:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number at 80 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: grit number excessively, at 80 mesh, obtains high stability amoxicillin soluble powder.
Test example Amoxicillin soluble powder stability test in water
Test method: take amoxicillin soluble powder appropriate, accurately weighed, adding flowing and making dissolving dilution make in every 1ml the solution containing about 0.5mg (amoxicillin meter) mutually, shaking up.Measure 20ul in 0h, 4h, 8h, 12h, 16h, 20h, 24h different time precision respectively and inject chromatograph of liquid, record chromatogram.
Result of the test: measuring the effective content of amoxicillin in different time amoxicillin soluble powder, result is 0h (0.502mg), 4h (0.501mg), 8h (0.499mg), 12h (0.498mg), 16h (0.498mg), 20h (0.497mg), 24h (0.497mg).
Result shows: amoxicillin soluble powder of the present invention effective content of 24h amoxicillin in water does not reduces, and illustrates that amoxicillin soluble powder is stablized in water.
Above the embodiment of the invention is described in detail, but described content has been only the preferred embodiment of the invention, it is impossible to be considered the practical range for limiting the present invention.All impartial changes made according to the invention scope and improvement etc., all should still belong to this patent covering scope.

Claims (4)

1. an amoxicillin soluble powder, it is characterised in that: described amoxicillin soluble powder includes amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose.
Amoxicillin soluble powder the most according to claim 1 is characterized in that, being made up of the component of following weight percentage: amoxicillin 5-30%, poloxamer F68 5-15%, PVP K30 5-15%, beta-schardinger dextrin-5-30%, remaining anhydrous glucose polishing is to 100%.
Amoxicillin soluble powder the most according to claim 1 is characterized in that being made up of the component of following weight percentage: amoxicillin 10%, poloxamer F68 5%, PVP K30 10%, beta-schardinger dextrin-20%, and remaining anhydrous glucose polishing is to 100%.
4. the preparation method of amoxicillin soluble powder described in a claim 1 comprises the following steps:
(1) pulverize, sieve: take amoxicillin, poloxamer F68, PVP K30, beta-schardinger dextrin-, anhydrous glucose, pulverize respectively, cross grit number and exist Between 40-300 mesh;
(2) mixing: amoxicillin and poloxamer F68, PVP K30 after pulverizing premix, and then, always mix with beta-schardinger dextrin-, anhydrous glucose, pulverize after mixing;
(3) sieve: after total mixing, 40-300 mesh sieves.
CN201610166626.9A 2016-03-23 2016-03-23 Amoxicillin soluble powder and preparation method thereof Pending CN105796500A (en)

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106309374A (en) * 2016-09-21 2017-01-11 西安乐道生物科技有限公司 Amoxicillin superfine powder water-soluble preparation and preparation method thereof
CN107157936A (en) * 2017-07-19 2017-09-15 山东福美乐动物药业有限公司 A kind of amoxicillin soluble powder 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
CN107789321A (en) * 2016-08-31 2018-03-13 瑞普(天津)生物药业有限公司 A kind of amoxicillin soluble powder for improving solubization
CN108606954A (en) * 2016-12-13 2018-10-02 河南后羿实业集团有限公司 A kind of lincomycin hydrochloride soluble powder and preparation method thereof
CN108670956A (en) * 2018-07-04 2018-10-19 河南牧翔动物药业有限公司 A kind of amoxicillin soluble powder and preparation method thereof

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CN104548122A (en) * 2013-10-23 2015-04-29 洛阳惠中兽药有限公司 Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application 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
CN105168143A (en) * 2015-10-08 2015-12-23 青岛康地恩动物药业有限公司 Amoxicillin preparation and preparation method thereof

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CN104548122A (en) * 2013-10-23 2015-04-29 洛阳惠中兽药有限公司 Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application 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
CN105168143A (en) * 2015-10-08 2015-12-23 青岛康地恩动物药业有限公司 Amoxicillin preparation and preparation method thereof

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Title
凌沛学主编: "《药物制剂技术》", 31 May 2007 *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107789321A (en) * 2016-08-31 2018-03-13 瑞普(天津)生物药业有限公司 A kind of amoxicillin soluble powder for improving solubization
CN106309374A (en) * 2016-09-21 2017-01-11 西安乐道生物科技有限公司 Amoxicillin superfine powder water-soluble preparation and preparation method thereof
CN108606954A (en) * 2016-12-13 2018-10-02 河南后羿实业集团有限公司 A kind of lincomycin hydrochloride soluble powder 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
CN107157936A (en) * 2017-07-19 2017-09-15 山东福美乐动物药业有限公司 A kind of amoxicillin soluble powder and preparation method thereof
CN107157936B (en) * 2017-07-19 2020-09-01 山东福美乐动物药业有限公司 Amoxicillin soluble powder and preparation method thereof
CN108670956A (en) * 2018-07-04 2018-10-19 河南牧翔动物药业有限公司 A kind of amoxicillin soluble powder and preparation method thereof

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Application publication date: 20160727