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CN110638761A - Avermemycin soluble powder and preparation method thereof - Google Patents

Avermemycin soluble powder and preparation method thereof Download PDF

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Publication number
CN110638761A
CN110638761A CN201810585940.XA CN201810585940A CN110638761A CN 110638761 A CN110638761 A CN 110638761A CN 201810585940 A CN201810585940 A CN 201810585940A CN 110638761 A CN110638761 A CN 110638761A
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avilamycin
soluble powder
polyethylene glycol
parts
cosolvent
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CN110638761B (en
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马承国
王磊
万道喜
周志凤
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Shanghai Moxi Biotechnology Co Ltd
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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
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K9/145Intimate 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 compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention provides avilamycin soluble powder and a preparation method thereof. The preparation method of the avilamycin soluble powder comprises the following steps: (1) weighing the components of the avilamycin soluble powder composition, and (2) mixing the materials to prepare powder. The invention adopts one or more carrier components and adds the cosolvent simultaneously, so that the avilamycin can be uniformly dissolved in water, can be better absorbed and utilized, and improves the bioavailability. Meanwhile, the preparation method of the avilamycin soluble powder provided by the invention has the advantages of simple process, no wastewater generation, safety, environmental protection and easy mass production.

Description

Avermemycin soluble powder and preparation method thereof
Technical Field
The invention relates to a veterinary drug preparation and a preparation method thereof, in particular to avilamycin soluble powder and a preparation method thereof.
Background
Avilamycin, also known as throughout, is dichlorolichenin, which is fermented from streptomyces virididohrongenes strains, is an oligosaccharide antibiotic belonging to the family of the eumycin family, mainly inhibits gram-positive bacteria, has a slightly weaker effect on gram-negative bacteria, and is a novel digestion promoter and metabolic regulator. The avilamycin has the advantages of unique structure, high safety, low residue, low toxicity, no cross drug resistance, low environmental pollution and easy processing. The avilamycin can improve the utilization rate of protein in the feed for livestock and poultry, improves the feed conversion rate, and basically has no drug residue phenomenon, so the avilamycin serving as a veterinary drug additive is widely applied to the livestock breeding industry.
At present, only the dosage forms of the avilamycin premix are available in the international market, and the main problems of the products are that the products are difficult to mix uniformly when being mixed and used, and the bioavailability is low because the insoluble avilamycin is difficult to dissolve and absorb in the animal body. Along with the intensification and scale of livestock breeding, the soluble medicine is increasingly widely applied, and the advantages of convenience, timeliness, flexibility, high efficiency and the like of drinking water administration are gradually highlighted. The avilamycin is almost insoluble in water, and how to prepare the avilamycin into soluble powder is a technical problem to be solved urgently.
Disclosure of Invention
In order to solve the technical problems, the invention aims to provide avilamycin soluble powder and a preparation method thereof.
In one aspect of the invention, a preparation method of avilamycin soluble powder is provided, which comprises the following steps:
(1) weighing the components of the avilamycin soluble powder composition, wherein the avilamycin soluble powder composition comprises avilamycin, a carrier and a cosolvent;
(2) mixing the above materials, and making into powder.
Preferably, the avilamycin soluble powder composition may also include a stabilizer.
Preferably, the avilamycin soluble powder composition may also include a pH adjuster.
Preferably, the preparation step of the avilamycin soluble powder further comprises the following steps: micronization, sieving, and the like.
Preferably, after being weighed, the components of the avilamycin soluble powder composition can be respectively micronized and then sieved, or one or more of the components can be selected, mixed and then micronized and sieved, or can be respectively micronized and then mixed and sieved.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the avilamycin is 0.5% -5%, preferably 1% -2%.
In a preferred embodiment, the carrier may be one or more of hydroxypropyl- β -cyclodextrin, polylactic-co-glycolic acid (PLGA), polylactic acid (PLA), polylactide-caprolactone (PACA), poly n-Butyl Cyanoacrylate (BCA),. polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), polyamide-amine (PAMAM).
In a preferred embodiment, in the avilamycin soluble powder composition, the carrier mass proportion is 30-90%, preferably 50-70%.
In a preferred embodiment, the cosolvent may be one or more of polyethylene glycol, sodium deoxycholate, poloxamer, polyvinylpyrrolidone (PVP), and polysorbate.
Preferably, the cosolvent comprises polyethylene glycol, and more preferably, the cosolvent comprises one or a combination of polyethylene glycol 4000, polyethylene glycol 6000 and polyethylene glycol 8000.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass ratio of the cosolvent is 10% -50%, preferably 20% -40%.
In a preferred embodiment, the cosolvent comprises polyethylene glycol and sodium deoxycholate; preferably, the mass ratio of the polyethylene glycol to the sodium deoxycholate is (05-2): (0.8-1.5), preferably 1: (0.8-1.5), more preferably 1: (1-1.2).
In a preferred embodiment, the stabilizer can be one or more of vitamin E, L-cystine, L-cysteine, and tea polyphenol.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the stabilizer is not higher than 8%, preferably 2% -5%.
In a preferred embodiment, the pH regulator may be one or more of sodium carbonate, sodium bicarbonate, sodium hydroxide, calcium bicarbonate, acetic acid, sodium acetate, and hydrochloric acid.
In a preferred embodiment, a pH adjuster is used to reduce acidity or increase alkalinity.
In a preferred embodiment, the pH adjusting agent is a single substance, and when the pH adjusting agent is a single substance, the alkaline substance is selected to be the pH adjusting agent.
In another preferred embodiment, the pH adjusting agent is a combination of substances, which is basic.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the pH value regulator is not higher than 8%, and is preferably 2% -5%.
In a preferred embodiment, the micronization is carried out under the condition of dry low-temperature mechanical dust-free pulverization, and the temperature of the material is controlled below 60 ℃.
In a preferred embodiment, the screening is performed with a screening mesh number of 100-.
In another aspect of the present invention, an avilamycin soluble powder is provided, which comprises: avilamycin, carrier and cosolvent.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the avilamycin is 0.5% -5%, preferably 1% -2%.
In a preferred embodiment, the carrier may be one or more of hydroxypropyl- β -cyclodextrin, polylactic-co-glycolic acid (PLGA), polylactic acid (PLA), polylactide-caprolactone (PACA), poly n-Butyl Cyanoacrylate (BCA),. polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), polyamide-amine (PAMAM).
In a preferred embodiment, in the avilamycin soluble powder composition, the carrier mass proportion is 30-90%, preferably 50-70%.
In a preferred embodiment, the cosolvent may be one or more of polyethylene glycol, sodium deoxycholate, poloxamer, polyvinylpyrrolidone (PVP), and polysorbate.
Preferably, the cosolvent comprises polyethylene glycol, and more preferably, the cosolvent comprises one or a combination of polyethylene glycol 4000, polyethylene glycol 6000 and polyethylene glycol 8000.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass ratio of the cosolvent is 10% -50%, preferably 20% -40%.
In a preferred embodiment, the cosolvent comprises polyethylene glycol and sodium deoxycholate; preferably, the mass ratio of the polyethylene glycol to the sodium deoxycholate is (05-2): (0.8-1.5), preferably 1: (0.8-1.5), more preferably 1: (1-1.2).
In a preferred embodiment, the stabilizer can be one or more of vitamin E, L-cystine, L-cysteine, and tea polyphenol.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the stabilizer is not higher than 8%, preferably 2% -5%.
In a preferred embodiment, the pH regulator may be one or more of sodium carbonate, sodium bicarbonate, sodium hydroxide, calcium bicarbonate, acetic acid, sodium acetate, and hydrochloric acid.
In a preferred embodiment, a pH adjuster is used to reduce acidity or increase alkalinity.
In a preferred embodiment, the pH adjusting agent is a single substance, and when the pH adjusting agent is a single substance, the alkaline substance is selected to be the pH adjusting agent.
In another preferred embodiment, the pH adjusting agent is a combination of substances, which is basic.
In a preferred embodiment, in the avilamycin soluble powder composition, the mass proportion of the pH value regulator is not higher than 8%, and is preferably 2% -5%.
In a preferred embodiment, the avilamycin soluble powder comprises, by mass, 1% -2% of avilamycin, 2% -5% of a pH value regulator, 2% -5% of a stabilizer, 10% -20% of polyethylene glycol, 10% -20% of sodium deoxycholate and 50% -70% of hydroxypropyl-beta-cyclodextrin.
In the above context of the present invention, a range of values may be given as one or more fixed values or ranges of values selected from the range.
The avilamycin soluble powder and the preparation method thereof provided by the invention have the following beneficial effects:
(1) the invention adopts one or more carrier components and adds the cosolvent simultaneously, so that the avilamycin can be uniformly dissolved in water, can be better absorbed and utilized, and improves the bioavailability.
(2) The invention increases the stability of the avilamycin soluble powder under the condition of containing the stabilizer, and the product is easier to store, so that the production, circulation and use of the product are more convenient.
(3) The preparation method of the avilamycin soluble powder provided by the invention has the advantages of simple process, no use of organic solvent, no generation of wastewater, safety, environmental protection and easy mass production.
Detailed Description
The invention provides avilamycin soluble powder, which comprises the following components: the sustained release preparation comprises avilamycin, a carrier, a cosolvent, or a stabilizer and/or a pH value regulator. Wherein: the carrier can be one or more of hydroxypropyl-beta-cyclodextrin, polylactic acid-glycolic acid copolymer (PLGA), polylactic acid (PLA), polylactide-caprolactone (PACA), poly n-Butyl Cyanoacrylate (BCA), polyvinylpyrrolidone (PVP), polyethylene glycol (PEG) and polyamide-amine (PAMAM); the cosolvent can be one or more of polyethylene glycol, sodium deoxycholate, poloxamer, polyvinylpyrrolidone (PVP) and polysorbate; the stabilizer can be one or more of vitamin E, L-cystine, L-cysteine, and tea polyphenols.
Example 1
The carrier is hydroxypropyl-beta-cyclodextrin, the cosolvent is polyethylene glycol-6000 and sodium deoxycholate, the stabilizer is L-cystine, and the pH value regulator is sodium bicarbonate.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
1.0 part of avilamycin, 3.0 parts of sodium bicarbonate, 3.0 parts of L-cystine, 600015.0 parts of polyethylene glycol, 15.0 parts of sodium deoxycholate and 63.0 parts of hydroxypropyl-beta-cyclodextrin are respectively weighed.
Step 2
Micronizing the six materials respectively, controlling the temperature of the micronized material at 45 + -2 deg.C, sieving, and sieving with 120 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 45 +/-2 ℃ during mixing, and the mixing time is 1.0 h; then sieving, sieving with a 120-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the embodiment has the solubility of 5% in water at normal temperature.
Example 2
The carrier is hydroxypropyl-beta-cyclodextrin, the cosolvent is polyethylene glycol-4000, polyethylene glycol-8000 and sodium deoxycholate, the stabilizer is vitamin E, and the pH regulator is sodium bicarbonate.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
1.5 parts of avilamycin, 3.5 parts of sodium bicarbonate, 3.5 parts of vitamin E, 40009.0 parts of polyethylene glycol, 80009.0 parts of polyethylene glycol, 18.0 parts of sodium deoxycholate and 55.5 parts of hydroxypropyl-beta-cyclodextrin are respectively weighed.
Step 2
Micronizing the above six materials respectively, controlling the temperature of the micronized material at 50 + -2 deg.C, sieving, and sieving with 160 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 50 +/-2 ℃ during mixing, and the mixing time is 1.5 h; then sieving, sieving with a 160-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the example has the solubility of 5.1% in water at normal temperature.
Example 3
The carrier is hydroxypropyl-beta-cyclodextrin, the cosolvent is polyethylene glycol-6000, polyethylene glycol-8000 and sodium deoxycholate, the stabilizer is vitamin E and L-cystine, and the pH value regulator is sodium bicarbonate.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
Respectively weighing 2.0 parts of avilamycin, 3.5 parts of sodium bicarbonate, 2 parts of vitamin E, 2.0 parts of L-cystine, 60009.0 parts of polyethylene glycol, 800010.0 parts of polyethylene glycol, 20.0.0 parts of sodium deoxycholate and 51.5 parts of hydroxypropyl-beta-cyclodextrin.
Step 2
Micronizing the above six materials respectively, controlling the temperature of the micronized material at 55 + -2 deg.C, sieving, and sieving with 160 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 55 +/-2 ℃ during mixing, and the mixing time is 1.5 h; then sieving, sieving with a 160-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the embodiment has the solubility of 5% in water at normal temperature.
Example 4
The carrier is polylactic acid-glycolic acid copolymer, the cosolvent is polyethylene glycol-4000, polyethylene glycol-8000 and sodium deoxycholate, the stabilizer is tea polyphenol, and the pH value regulator is sodium hydroxide.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
Respectively weighing 2.0 parts of avilamycin, 3.5 parts of sodium hydroxide, 4 parts of tea polyphenol, 400010.0 parts of polyethylene glycol-80009.0 parts of sodium deoxycholate, 20.0.0 parts of polylactic acid-glycolic acid copolymer and 51.5 parts of the polylactic acid-glycolic acid copolymer.
Step 2
Micronizing the above six materials respectively, controlling the temperature of the micronized material at 55 + -2 deg.C, sieving, and sieving with 160 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 55 +/-2 ℃ during mixing, and the mixing time is 1.5 h; then sieving, sieving with a 160-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the embodiment has 4.9% of solubility in water at normal temperature.
Example 5
The carrier is polylactic acid-glycolic acid copolymer, the cosolvent is polyethylene glycol-4000, polyethylene glycol-8000 and sodium deoxycholate, the stabilizer is calcium bicarbonate, and the pH value regulator is calcium bicarbonate.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
Respectively weighing 2.0 parts of avilamycin, 3.5 parts of calcium bicarbonate, 4 parts of tea polyphenol, 400010.0 parts of polyethylene glycol-80009.0 parts of sodium deoxycholate, 20.0.0 parts of polylactic acid-glycolic acid copolymer and 51.5 parts of the polylactic acid-glycolic acid copolymer.
Step 2
Micronizing the above six materials respectively, controlling the temperature of the micronized material at 55 + -2 deg.C, sieving, and sieving with 160 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 55 +/-2 ℃ during mixing, and the mixing time is 1.5 h; then sieving, sieving with a 160-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the embodiment has the solubility of 5.2% in water at normal temperature.
Example 6
The carrier is polyamide-amine, the cosolvent is polyethylene glycol-6000 and sodium deoxycholate, the stabilizer is L-cysteine, and the pH value regulator is sodium bicarbonate.
The preparation method of the avilamycin soluble powder comprises the following steps:
step 1
2.0 parts of avilamycin, 3 parts of sodium bicarbonate, 3.5 parts of L-cysteine, 600020 parts of polyethylene glycol, 20.0.0 parts of sodium deoxycholate and 51.5 parts of polyamide-amine are respectively weighed.
Step 2
Micronizing the above six materials respectively, controlling the temperature of the micronized material at 60 + -2 deg.C, sieving, and sieving with 160 mesh sieve; fully mixing the sieved materials, wherein the temperature of the materials is controlled to be 60 +/-2 ℃ during mixing, and the mixing time is 1.5 h; then sieving, sieving with a 160-mesh sieve, detecting, and subpackaging to obtain the product.
The avilamycin soluble powder obtained in the example has the solubility of 5.1% in water at normal temperature.
The avilamycin soluble powder obtained by the invention is tested and evaluated in appearance by adopting the following method:
weighing a certain amount of avilamycin soluble powder, putting 100ml of water into a 500ml beaker, putting the product obtained in the six embodiments at room temperature, putting the product into a water bath shaking table, shaking for 30min, observing the dissolution condition, and testing the solubility.
The test results were as follows:
TABLE 1 evaluation and examination results of solubility and appearance of solution of avilamycin obtained in examples 1 to 6
Figure RE-GDA0001854841640000081
As can be seen from Table 1, the water-soluble avilamycin powder has a good water-soluble effect, and the solubility of avilamycin in water can reach more than 5%.
The avilamycin soluble powder obtained by the invention adopts the following method to test the stability of the aqueous solution:
weighing a certain amount of avilamycin soluble powder, preparing an aqueous solution with the concentration of 2mg/ml by using tap water, standing for 1, 4, 8, 12 and 24 hours at the open room temperature, detecting the content, comparing with the prepared solution, and calculating the degradation rate.
The test results were as follows:
TABLE 2 results of stability (% degradation) measurement of aqueous solutions of the avilamycin soluble powders obtained in examples 1 to 6
Figure RE-GDA0001854841640000082
As can be seen from Table 2, the Avermectin has excellent stability, and the degradation of the Avermectin in the dissolved state is not more than 0.2% in 24 hours.
The avilamycin soluble powder obtained by the invention is subjected to accelerated stability test by adopting the following method:
and (3) sealing and packaging each avilamycin soluble powder sample by using an aluminum foil bag, wherein the experimental conditions are 40 ℃, the relative humidity is 75%, and the current change and degradation rate of each sample after the sample is placed for 1, 2, 4 or 6 months are inspected. The results are shown in tables 3 and 4.
TABLE 3 evaluation of the present Change in the soluble powder of Avermectin obtained in examples 1 to 6
Figure RE-GDA0001854841640000091
TABLE 4 degradation ratio (%) of the avilamycin soluble powder aqueous solution obtained in examples 1 to 6 of this example
Figure RE-GDA0001854841640000092
As can be seen from tables 3 and 4, the avilamycin soluble powder has stable product shape and high stability in a general storage state, and the degradation rate of the avilamycin is obviously lower than the quality standard requirement of veterinary drugs.
The embodiments of the present invention have been described in detail, but the embodiments are merely examples, and the present invention is not limited to the embodiments described above. Any equivalent modifications and substitutions to those skilled in the art are also within the scope of the present invention. Accordingly, equivalent changes and modifications made without departing from the spirit and scope of the present invention should be covered by the present invention.

Claims (10)

1. An avilamycin soluble powder, characterized in that, the avilamycin soluble powder is a composition, comprising: avilamycin, carrier and cosolvent.
2. An avilamycin soluble powder as claimed in claim 1, wherein the mass proportion of avilamycin in the composition is 0.5% -5%.
3. An avilamycin soluble powder as claimed in claim 1, wherein the cosolvent is one or more of polyethylene glycol, sodium deoxycholate, poloxamer, polyvinylpyrrolidone (PVP) and polysorbate.
4. An avilamycin soluble powder as claimed in claim 1, wherein the mass proportion of the cosolvent in the composition is 10-50%.
5. An avilamycin soluble powder as claimed in claim 1, wherein the cosolvent comprises polyethylene glycol and sodium deoxycholate.
6. An avilamycin soluble powder as in claim 5, wherein the mass ratio of the polyethylene glycol to the sodium deoxycholate is (05-2) to (0.8-1.5).
7. An avilamycin soluble powder as claimed in claim 1, characterized in that the carrier is present in the composition in a proportion of 30% to 90% by mass.
8. An avilamycin soluble powder as claimed in claim 1, wherein the composition comprises a stabilizer, and/or a pH modifier.
9. The avilamycin soluble powder as claimed in claim 1, which comprises, by mass, 1-2% of avilamycin, 2-5% of a pH regulator, 2-5% of a stabilizer, 10-20% of polyethylene glycol, 10-20% of sodium deoxycholate and 50-70% of hydroxypropyl-beta-cyclodextrin.
10. A process for preparing the avilamycin soluble powder of claim 1, comprising:
(1) weighing the components of the avilamycin soluble powder composition, wherein the avilamycin soluble powder composition comprises avilamycin, a carrier and a cosolvent;
(2) mixing the above materials, and making into powder.
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CN103070827A (en) * 2011-10-26 2013-05-01 青岛康地恩药业股份有限公司 Method for preparing tulathromycin soluble powder
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Publication number Priority date Publication date Assignee Title
CN1382445A (en) * 2001-04-23 2002-12-04 许晓全 Veterinary licking antihelmintic
CN1439263A (en) * 2003-03-06 2003-09-03 喻少帆 Avilamycin granules and their preparing method
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