CN106074446B - Tilmicosin particle and preparation method thereof - Google Patents
Tilmicosin particle and preparation method thereof Download PDFInfo
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- CN106074446B CN106074446B CN201610538877.5A CN201610538877A CN106074446B CN 106074446 B CN106074446 B CN 106074446B CN 201610538877 A CN201610538877 A CN 201610538877A CN 106074446 B CN106074446 B CN 106074446B
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- tilmicosin
- particle
- polyacrylic resin
- saccharin
- starch
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- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract
The present invention provides a kind of Tilmicosin particle, its raw material is made of the phosphoric acid solution that major ingredient and pH value are 1.0~2.0, wherein, the major ingredient is made of the material of following mass percents: Tilmicosin 5%~30%, polyacrylic resin IV 5%~10%, saccharin 0.5%~3%, monosodium glutamate 0.5%~2%, starch 64%~80%.The present invention also provides a kind of preparation methods of above-mentioned Tilmicosin particle, it includes the steps that preparing mixture and is coated, dries to mixture.Tilmicosin grain fraction provided by the invention is simple, easily stored, stability is good, medication is convenient, palatability is good, and preparation step is simple, is suitable for industrialized production.
Description
Technical field
The present invention relates to a kind of antimicrobial DP finish for animals, specifically, relate to a kind of Tilmicosin particle and its preparation
Method.
Background technique
Tilmicosin (C46H80N2O13) it is white to light yellow crystalline powder, it is dissolved in water or methanol.Tilmicosin
A kind of semi-synthetic dedicated antibiotic of macrolides livestock and poultry, to all gram-positive bacterias and part Gram-negative bacteria,
Mycoplasma, conveyor screw etc. have inhibiting effect, especially to Actinobacillus pleuropneumoniae, pasteurella haemolytica, killing property Pasteur more
Bacillus and livestock and poultry Mycoplasma have antibacterial activity more stronger than " tylosin ".It is mainly used for prevention and treatment because of pleuropneumonia unwrapping wire bar
The mazoitis of poultry pneumonia, avian mycoplasmas disease and lactating mammal caused by the infection such as bacterium, Pasteurella, mycoplasma.It treats livestock and poultry
Infect curative for effect, significant effect, using safe.In addition, current research the result shows that Tilmicosin it is antiviral and improve machine
There is certain effect in terms of body immunity, also there is certain inhibiting effect to blue otopathy.Therefore, Tilmicosin is widely used in
The infectious diseases for treating the animals such as ox, goat, milk cow, pig, chicken.
Although Tilmicosin has the advantages that above, Tilmicosin itself has certain irritation, and allergy can be caused anti-
It answers, has very big toxicity to heart when serious, if may cause negativity mental and physical efforts when too fast excess dosage vein or intramuscular injection,
Lead to animal dead, therefore Tilmicosin is mainly using the administration of for oral administration or injected s.c..When through administration for oral administration, due to
Tilmicosin taste is extremely bitter, and odorous, and palatability is poor；On the other hand, meter Kao Xing is unstable under one's belt, degradable and to stomach lining
With irritation, it will cause the ill symptoms such as anorexia, the Nausea and vomiting of livestock and poultry during the administration or even some animals smell
The taste of Tilmicosin be unwilling to just be fed, and cause the failure of administration.Therefore, prepare it is a kind of it is good with palatability, without bitter taste
Tilmicosin oral granule will greatly improve the edible comfort of the drug.
Summary of the invention
So the purpose of the present invention is in view of the deficiencies of the prior art, thus provide a kind of tasteless, enteric, palatability it is good,
Simple Tilmicosin particle of preparation process and preparation method thereof
To achieve the goals above, the technical scheme adopted by the invention is that: a kind of Tilmicosin particle, its raw material by
The phosphoric acid solution that major ingredient and pH value are 1.0~2.0 forms, wherein the major ingredient is made of the material of following mass percents: being replaced
Meter Kao Xing 5%~30%, polyacrylic resin IV 5%~10%, saccharin 0.5%~3%, monosodium glutamate 0.5%~2%, starch 64%~80%.
Based on above-mentioned, the major ingredient in the Tilmicosin particulate material is made of the material of following mass percents:
Tilmicosin 23.5%, polyacrylic resin IV 6.4%, saccharin 2%, monosodium glutamate 1%, starch 67.1%.
Based on above-mentioned, the major ingredient in the Tilmicosin particulate material is made of the material of following mass percents:
Tilmicosin 5%, polyacrylic resin IV 10%, saccharin 3%, monosodium glutamate 2%, starch 80%.
Based on above-mentioned, the major ingredient in the Tilmicosin particulate material is made of the material of following mass percents: replacing rice
Examine star 30%, polyacrylic resin IV 5%, saccharin 0.5%, monosodium glutamate 0.5%, starch 64%.
The present invention also provides a kind of preparation method of Tilmicosin particle, it the following steps are included:
It is calculated according to the raw material of above-mentioned mass percent, it is 1.0~2.0 that polyacrylic resin IV, which is dissolved in pH value, first
Phosphoric acid solution in be made polyacrylic resin IV slurries；Then saccharin, monosodium glutamate, Tilmicosin are crushed, screening process
Boiling is carried out with starch afterwards and is mixed to get mixture；Finally the mixture is carried out using the polyacrylic resin IV slurries
Coated granule is made in Cotton seeds, the coated granule is dried so that the water content of the coated granule is less than
2%, so that the Tilmicosin particle be made.
Wherein, it should be understood that being coated place to the mixture using the polyacrylic resin IV slurries
In the step of reason, the duration of the Cotton seeds depends on the concentration of the polyacrylic resin IV slurries.Specifically
Ground, when the concentration of the polyacrylic resin IV slurries is larger, that is, the polyacrylic resin IV slurries total volume it is smaller when,
The duration of the Cotton seeds is shorter；When the concentration of the polyacrylic resin IV slurries is smaller, that is, polyacrylic acid
When resin IV slurries total volume is larger, the duration of the Cotton seeds is longer.
The present invention has substantive distinguishing features outstanding and significant progress compared with the prior art, and specifically, the present invention mentions
Each raw material of the Tilmicosin particle supplied also significantly improves while the bad smell for covering Tilmicosin host agent overflows
The sense of taste of product, improves the palatability of drug, makes livestock and poultry be easier to receive, in especially described Tilmicosin particulate material
Monosodium glutamate and saccharin, play key effect in the bad smell for covering the Tilmicosin host agent, can more cover and be replaced described
The bad smell that meter Kao Xing host agent is overflowed；Meanwhile polyacrylic resin slurries and starch are respectively adopted as film forming agent in the present invention
And embedding medium, to extend the action time of the Tilmicosin particle and reduce the stimulation of the Tilmicosin particle
Property, improve the edible comfort level of the drug.The preparation method simple process of offer of the present invention, low raw-material cost, side
Just industrialized production.
Specific embodiment
Below by specific embodiment, technical scheme of the present invention will be described in further detail.
Embodiment 1
The present embodiment provides a kind of Tilmicosin particle, its raw material is made of the phosphoric acid solution that major ingredient and pH value are 1.4,
Wherein the major ingredient is made of the material of following quality: 23.5 g of Tilmicosin, 6.4 g of polyacrylic resin IV, saccharin 2g,
Monosodium glutamate 10g, 67.1 g of starch.
The present embodiment also provides a kind of preparation method of above-mentioned Tilmicosin particle, and step includes:
It is molten to be dissolved in the phosphoric acid that pH value is 1.4 by the raw material for successively weighing above-mentioned quality by the polyacrylic resin IV of 6.4g
Polyacrylic resin IV slurries are made in liquid；Then 2g saccharin, 10g monosodium glutamate, 23.5 g Tilmicosins are crushed and through 100 purposes
It is added to after sieve screening with the starch of 67.1g and carries out boiling to mix 10 minutes in boiling seed-coating machine obtaining mixture；Finally will
The polyacrylic resin IV slurries are added to the boiling coating motor spindle, are carried out using bottom spray coating method to the mixture
Layering pelletization, and through dry obtained Tilmicosin particle of the moisture content less than 2%.
Embodiment 2
The present embodiment provides a kind of Tilmicosin particle, specific material composition and the material composition substantially phase in embodiment 1
Together, the difference is that, major ingredient described in the present embodiment is made of the raw material of following quality: 5 g of Tilmicosin, polyacrylic resin
10 g of IV, 3 g of saccharin, 2 g of monosodium glutamate, 80 g of starch.
Preparation method of the Tilmicosin particle provided in this embodiment during the preparation method is the same as that of Example 1.
Embodiment 3
The present embodiment provides a kind of Tilmicosin particle, specific material composition and the material composition substantially phase in embodiment 1
Together, the difference is that, the embodiment of the present invention major ingredient is made of the raw material of following quality: Tilmicosin 30g, polyacrylic acid tree
5 g of rouge IV, 0.5 g of saccharin, monosodium glutamate 0.5g, 64 g of starch.
Preparation method of the Tilmicosin particle provided in this embodiment during the preparation method is the same as that of Example 1.
Verification experimental verification
Animal experiment verifying, test are carried out to the administering effect of Tilmicosin particle made from Examples 1 to 3 respectively
Process is as follows:
Subjects: the different illness pig of 40 breeding cycles of selection Zhengzhou farm, 40 pigs all suffer from because of branch
Pathogen infection causes pneumonia.
Test grouping and processing: being divided into 4 groups for 40 illness pigs, three groups of test groups and one group of control group, and every group 10.Its
In, test group 1~3 is successively treated using the Tilmicosin particle of Examples 1 to 3 preparation, and administration mode is spice administration,
Drug additive amount is the Tilmicosin particle that every kilogram of feed adds 2g-~4.5g, continuous treatment 7 days；And 10 of control group
Illness pig is not cooked any treatment processing.After the test, 4 groups of test results are counted, test result is as shown in table 1.
The clinical treatment outcome of 1 zoopery of table
| Experimental group 1 | Experimental group 2 | Experimental group 3 | Control group | |
| Drug eats success rate | 100% | 100% | 100% | -- |
| Cough head number | 2 | 1 | 2 | 9 |
| Every cough number | 10 times | 6 times | 9 times | 60 times |
As can be seen from the table, Tilmicosin particle prepared by the present invention makes the bitter taste and its irritation quilt of drug itself
Coverage is got up, and takes Tilmicosin particle provided by the invention to 30 illness pigs of experimental group, all experimental subjects are not
There is anorexia, nausea or vomiting phenomenon, drug eats success rate and reaches 100%, to solve the problems, such as that administration is difficult.It throws simultaneously
After feeding seven days, Tilmicosin particle is significant to the therapeutic effect of pig pneumonia, hence it is evident that the quantity and number for reducing cough are conducive to disease
The control and purification of disease, are also beneficial to the raising of production performance, reduce aquaculture cost on the whole, be worth of widely use.
Finally it should be noted that: the above embodiments are merely illustrative of the technical scheme of the present invention and are not intended to be limiting thereof；To the greatest extent
The present invention is described in detail with reference to preferred embodiments for pipe, it should be understood by those ordinary skilled in the art that: still
It can modify to a specific embodiment of the invention or some technical features can be equivalently replaced；Without departing from this hair
The spirit of bright technical solution should all cover within the scope of the technical scheme claimed by the invention.
Claims (5)
1. a kind of Tilmicosin particle, which is characterized in that the phosphoric acid solution group that its raw material is 1.0~2.0 by major ingredient and pH value
At, wherein the major ingredient is made of the material of following mass percents: Tilmicosin 5%~30%, polyacrylic resin IV 5%
~10%, saccharin 0.5%~3%, monosodium glutamate 0.5%~2%, starch 64%~80%；The Tilmicosin particle is through the following steps that be made
: the polyacrylic resin IV is dissolved in the phosphoric acid solution that pH value is 1.0~2.0 polyacrylic resin IV is made first
Slurries；Then the saccharin, the monosodium glutamate, the Tilmicosin crushed, boil with starch after screening process and mixes
Conjunction obtains mixture；Processing finally is coated to the mixture using the polyacrylic resin IV slurries, coating is made
Grain is dried the coated granule so that the water content of the coated granule is less than 2%, so that being made described replaces rice
Examine star particle.
2. Tilmicosin particle according to claim 1, which is characterized in that the major ingredient by following mass percents object
Material composition: Tilmicosin 23.5%, polyacrylic resin IV6.4%, saccharin 2%, monosodium glutamate 1%, starch 67.1%.
3. Tilmicosin particle according to claim 1, which is characterized in that the major ingredient it by following mass percents
Material composition: Tilmicosin 5%, polyacrylic resin IV 10%, saccharin 3%, monosodium glutamate 2%, starch 80%.
4. Tilmicosin particle according to claim 1, which is characterized in that the major ingredient by following mass percents object
Material composition: Tilmicosin 30%, polyacrylic resin IV 5%, saccharin 0.5%, monosodium glutamate 0.5%, starch 64%.
5. a kind of preparation method of Tilmicosin particle, it the following steps are included:
It calculates according to the raw material of any one of Claims 1 to 4 mass percent, is first dissolved in polyacrylic resin IV
Polyacrylic resin IV slurries are made in the phosphoric acid solution that pH value is 1.0~2.0；Then saccharin, monosodium glutamate, Tilmicosin are carried out
It crushes, boil with starch after screening process is mixed to get mixture；Finally use the polyacrylic resin IV slurries pair
The mixture is coated processing and coated granule is made, and the coated granule is dried so that the coated granule
Water content less than 2%, so that the Tilmicosin particle be made.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610538877.5A CN106074446B (en) | 2016-07-11 | 2016-07-11 | Tilmicosin particle and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610538877.5A CN106074446B (en) | 2016-07-11 | 2016-07-11 | Tilmicosin particle and preparation method thereof |
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| Publication Number | Publication Date |
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| CN106074446A CN106074446A (en) | 2016-11-09 |
| CN106074446B true CN106074446B (en) | 2019-03-22 |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101879141A (en) * | 2009-05-05 | 2010-11-10 | 烟台绿叶动物保健品有限公司 | Taste-masking tilmicosin gastric-soluble particle preparation |
| CN103990132A (en) * | 2014-05-07 | 2014-08-20 | 北京化工大学 | Method for preparing medicine taste-masking preparation from acrylic resin mixed aqueous dispersion |
| CN104586774A (en) * | 2015-01-26 | 2015-05-06 | 成都乾坤动物药业有限公司 | Process for preparing tilmicosin pellets |
| CN104958764A (en) * | 2015-06-05 | 2015-10-07 | 广西大学 | Tilmicosin smell masking preparation and preparing method thereof |
-
2016
- 2016-07-11 CN CN201610538877.5A patent/CN106074446B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101879141A (en) * | 2009-05-05 | 2010-11-10 | 烟台绿叶动物保健品有限公司 | Taste-masking tilmicosin gastric-soluble particle preparation |
| CN103990132A (en) * | 2014-05-07 | 2014-08-20 | 北京化工大学 | Method for preparing medicine taste-masking preparation from acrylic resin mixed aqueous dispersion |
| CN104586774A (en) * | 2015-01-26 | 2015-05-06 | 成都乾坤动物药业有限公司 | Process for preparing tilmicosin pellets |
| CN104958764A (en) * | 2015-06-05 | 2015-10-07 | 广西大学 | Tilmicosin smell masking preparation and preparing method thereof |
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