CN107823134A - A kind of long-acting veterinary ivermectin injection and preparation method thereof - Google Patents
A kind of long-acting veterinary ivermectin injection and preparation method thereof Download PDFInfo
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- CN107823134A CN107823134A CN201711446294.0A CN201711446294A CN107823134A CN 107823134 A CN107823134 A CN 107823134A CN 201711446294 A CN201711446294 A CN 201711446294A CN 107823134 A CN107823134 A CN 107823134A
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- ivermectin
- injection
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- acting veterinary
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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
- A61K9/10—Dispersions; Emulsions
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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
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Dispersion Chemistry (AREA)
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Abstract
The invention discloses a kind of long-acting veterinary ivermectin injection and preparation method thereof；The key component and its mass percent of the parenteral solution be：Ivermectin 0.5% ~ 2.5% is mass percent.The parenteral solution pest-resistant spectrum of the present invention is wide, and because employing novel ultrasonic dispersion technology, durative action preparation has been made, and can produce repelling and killing efficacy to the parasite inside and outside animal body for a long time；Easy to use, cure rate is high；Compared with similar products, there is more preferable therapeutic effect and lower cost.
Description
Technical field
The present invention relates to a kind of veterinary formulations technology, and in particular to a kind of long-acting veterinary ivermectin injection and its preparation
Method.
Background technology
Ivermectin is a kind of efficient, macrolides anti-parasite medicine of wide spectrum, hypotoxicity, to internal epizoa
Particularly nematode and arthropod, which have, good kills effect.Presently commercially available ivermectin medicine is mostly conventional formulation, mainly
There are parenteral solution, tablet etc., it has single-dose and maintains efficacy time short, needs repeat administration；The shortcomings of insufficient is absorbed, is this
Clinically repeated multiple times administration can be solved the problems, such as by developing a kind of long-acting veterinary ivermectin injection, reduce Animal stress, drop
Low aquaculture cost.
The content of the invention
It is an object of the invention to provide a kind of long-acting veterinary ivermectin injection and preparation method thereof.
The above-mentioned purpose of the present invention is achieved by the following technical programs:
A kind of long-acting veterinary ivermectin injection, it is characterised in that often the composition of 1000mL medicines is：
5 ~ 25g of ivermectin
20 ~ 40mL of oil phase
15 ~ 40mL of surfactant
Add water to 1000ml
Further, the oil phase is ethyl oleate, Ergol, ethyl acetate, soybean oil, isopropyl myristate（IPM）
With one or more of mixing in six kinds of oil of injection white oil.
Further, the surfactant is Tween-80, Arlacel-40, Arlacel-80, polyvinylpyrrolidone or polyoxy second
One or more of mixing in alkene fatty alcohol ether.
Further, invention additionally discloses described a kind of long-acting veterinary ivermectin injection and preparation method thereof：It is accurate to claim
Take qualified ivermectin raw material to be fed intake by 100.0%, be mutually stirred for dissolving with prescription gauging, after its dissolving, add surface and live
Property agent, and carried out with ultrasonic wave handling 5-10 minutes, after liquid is changed into clarification, add water for injection simultaneously stirred to full dose it is equal
It is even, packing, Zha Gai, labeling, vanning, inspection, storage after passed examination.
The present invention is relative to the advantages of existing product:
Employ ultrasonic disperse technology and novel injection agent has been made, it reduces production cost, subtracted simultaneously using water as decentralized medium
Stimulation during small injection to animal body, and be more easy to be absorbed, it is not easy locally causing inflammatory reaction.Simultaneously as effectively
The particle diameter of particle is controlled, can allow medicine after animal body is entered due to the different of particle diameter and so that being metabolized the time not
Together, long-acting slow-release effect is realized, reduces clinical application number, reduces aquaculture cost.
Embodiment
Some embodiments, comparative example and experimental example is listed below, present invention has been carried out further by these
Illustrate, it is not possible to be interpreted as the further limitation to invention, those skilled in the art utilize the professional knowledge of oneself
To make corresponding change and modify to complete the present invention, these will also fall into the scope of the present invention.
Inventive formulation is mainly：Using ivermectin 0.5 ~ 2.5%, oil phase 2 ~ 4%, surfactant 1.5 ~ 4%, remaining
For water.
Embodiment 1
Preparation method：Accurately weigh qualified ivermectin raw material 5g to feed intake by 100.0%, be stirred for ethyl acetate 20ml molten
Solution, after its dissolving, the 30ml of surface active agent tween -80 is added, and processing 8 minutes is carried out with ultrasonic wave, treat that liquid is changed into clear
After clear, add water for injection and to full dose 1000ml and stir, packing after passed examination, Zha Gai, labeling, vanning, examine, enter
Storehouse.
Embodiment 2
Preparation method：Accurately weigh qualified ivermectin raw material 10g to feed intake by 100.0%, with by 1:The Ergol of 1 mixing
It is stirred for dissolving with ethyl oleate 30ml, after its dissolving, adds the 40ml of surface active agent tween -80, be stirred, and
Processing 8 minutes is carried out with ultrasonic wave, after liquid is changed into clarification, water for injection is added and to full dose 1000ml and stirs, examine
Look into qualified rear packing, Zha Gai, labeling, vanning, inspection, storage.
Embodiment 3
Preparation method：Accurately weigh qualified ivermectin raw material 20g to feed intake by 100.0%, with by 1:The Ergol of 1 mixing
It is stirred for dissolving with injection soybean oil 40ml, after its dissolving, adds the 30ml of surface active agent tween -80, be stirred
After uniformly, polyvinylpyrrolidone 10ml is added, and processing 10 minutes is carried out with ultrasonic wave, after liquid is changed into clarification, is added
Enter water for injection to full dose and stir, packing, Zha Gai, labeling, vanning, inspection, storage after passed examination.
Clinical test：
The present embodiment has been carried out to the 1% long-acting ivermectin injection of the present invention and common 1% ivermectin injection
Pharmacokinetic in goat body, its research are as follows：
Choose healthy black goat 12, male and female half and half, the kg of body weight 24 ± 2, normal feeding management.Based on dark green herbage, fine fodder
Not add the complete feed of anti-parasite medicine and antibiotic, free water, clinical observation 3 days before experiment.It is random before experiment
Packet, blood sampling check, as a result show that experiment is used in goat body and are free of ivermectin.12 goats are divided into two groups of A, B at random,
A is long-acting injection group, and B is normal injection group.By 0.2mg/kg single dose subcutaneous administration, 1h, 12h after administration,
24h, 48h, 72h, 96h, 144h, 240h, 336h, 432h, 528h jugular vein blood collection, detect ivermectin concentrations in blood plasma, inspection
Survey result such as table 1.
Main pharmacokinetic parameters compare after the goat single subcutaneous injection ivermectin of table 1（n=6）
Note：* represent notable with common group comparing difference（P ＜ 0.05）；* expressions are notable with commonly organizing poor heteropole（P ＜
0.01）；Represent not notable with common group comparing difference without shoulder mark（P ＞ 0.05）；
Testing result shows that long-acting ivermectin injects its area under the drug-time curve（AUC）It is significantly higher than common ivermectin note
Liquid is penetrated, and eliminates half-life period（T1/2(α)）Considerably longer than common ivermectin injection, absorb Cmax（Cmax）Also it is significantly high
In common ivermectin injection, show that its absorption of long-acting ivermectin is more abundant, half-life period is longer, can remain longer effective
Time.
Finally illustrate, preferred embodiment above is merely illustrative of the technical solution of the present invention and unrestricted, although logical
Cross above preferred embodiment the present invention is described in detail, it is to be understood by those skilled in the art that can be
Various changes are made to it in form and in details, without departing from claims of the present invention limited range.
Claims (3)
1. a kind of long-acting veterinary ivermectin injection, it is characterised in that often the composition of 1000mL medicines is：
5 ~ 25g of ivermectin
20 ~ 40mL of oil phase
15 ~ 40mL of surfactant
Add water to 1000ml
According to a kind of above-mentioned long-acting veterinary ivermectin injection, it is characterised in that：The oil phase is ethyl oleate, benzoic acid
Benzyl ester, ethyl acetate, soybean oil, isopropyl myristate（IPM）With it is one or more of mixed in six kinds of oil of injection white oil
Close.
A kind of 2. long-acting veterinary ivermectin injection according to claim 1, it is characterised in that：The surfactant
To be one or more of mixed in Tween-80, Arlacel-40, Arlacel-80, polyvinylpyrrolidone or polyoxyethylene aliphatic alcohol ether
Close.
3. a kind of long-acting veterinary ivermectin injection as claimed in claim 1, it is characterised in that comprise the following steps：Accurately
Weigh qualified ivermectin raw material to feed intake by 100.0%, be mutually stirred for dissolving with prescription gauging, after its dissolving, add surface
Activating agent, and processing 5-10 minutes are carried out with ultrasonic wave, after liquid is changed into clarification, adds water for injection and simultaneously stirred to full dose
It is even, packing, Zha Gai, labeling, vanning, inspection, storage after passed examination.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017111250466 | 2017-11-14 | ||
| CN201711125046 | 2017-11-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107823134A true CN107823134A (en) | 2018-03-23 |
Family
ID=61645500
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711446294.0A Withdrawn CN107823134A (en) | 2017-11-14 | 2017-12-27 | A kind of long-acting veterinary ivermectin injection and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108992403A (en) * | 2018-08-31 | 2018-12-14 | 田红卫 | A kind of long-acting slow-release ivermectin injection and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1241404A (en) * | 1999-07-16 | 2000-01-19 | 王玉万 | Avermectin-or ivermectin-containing slow releasing injecta |
| CN101590016A (en) * | 2008-05-26 | 2009-12-02 | 烟台绿叶动物保健品有限公司 | A kind of ivermectin emulsion for injection and preparation method thereof |
| CN101862294A (en) * | 2010-06-22 | 2010-10-20 | 华南农业大学 | Ivermectin suspending agent, preparation method and application thereof |
| CN106974887A (en) * | 2017-04-18 | 2017-07-25 | 哈尔滨生物制品二厂有限责任公司 | A kind of ivermectin slow-release injection |
-
2017
- 2017-12-27 CN CN201711446294.0A patent/CN107823134A/en not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1241404A (en) * | 1999-07-16 | 2000-01-19 | 王玉万 | Avermectin-or ivermectin-containing slow releasing injecta |
| CN101590016A (en) * | 2008-05-26 | 2009-12-02 | 烟台绿叶动物保健品有限公司 | A kind of ivermectin emulsion for injection and preparation method thereof |
| CN101862294A (en) * | 2010-06-22 | 2010-10-20 | 华南农业大学 | Ivermectin suspending agent, preparation method and application thereof |
| CN106974887A (en) * | 2017-04-18 | 2017-07-25 | 哈尔滨生物制品二厂有限责任公司 | A kind of ivermectin slow-release injection |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108992403A (en) * | 2018-08-31 | 2018-12-14 | 田红卫 | A kind of long-acting slow-release ivermectin injection and preparation method thereof |
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Application publication date: 20180323 |
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