CN116196271A - Externally-applied siramectin drop for pets and preparation method thereof - Google Patents
Externally-applied siramectin drop for pets and preparation method thereof Download PDFInfo
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- CN116196271A CN116196271A CN202210796041.0A CN202210796041A CN116196271A CN 116196271 A CN116196271 A CN 116196271A CN 202210796041 A CN202210796041 A CN 202210796041A CN 116196271 A CN116196271 A CN 116196271A
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- siramectin
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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
- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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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
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
- A61K9/0017—Non-human animal skin, e.g. pour-on, spot-on
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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
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
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- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against 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)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Zoology (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Tropical Medicine & Parasitology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
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Abstract
The invention discloses a siramectin external drop for pets, and a preparation method and application thereof. The drop of the invention uses the sirametin as a core component, the dipropylene glycol methyl ether as a transdermal agent, and the components of the drop mutually promote and synergistically increase each other, thereby not only promoting transdermal penetration, but also covering peculiar smell in the drop, being more easily accepted by pets, and remarkably improving curative effect. The drops of the invention have the advantages of high stability, convenient use, simple preparation method, high efficiency and good insecticidal effect.
Description
Technical Field
The invention relates to the field of pet supplies, and relates to a siramectin external drop for pets and a preparation method thereof.
Background
With the improvement of life style, the more a human needs the companion of the pet. The breeding proportion of the pet dogs or the pet cats is larger. But pets are prone to skin disorders. There are several causes of dermatological diseases, parasitic dermatitis, bacterial dermatitis or allergic dermatitis. The parasites can be cysticercosis, ticks and the like, and are easy to cause symptoms such as pruritus of pets. Bacteria can destroy the immune system of the pet. Allergic dermatitis causes symptoms of redness, swelling and itching in pets.
The external medicine has high efficiency, good insecticidal effect and the like, and is popular with the vast users. However, the existing external medicines have the following problems, namely, the problem of drug resistance, and the excessive use of the existing external medicines for killing insects weakens the insecticidal effect and has to increase the use of the external medicines for killing insects. Secondly, excessive dosage of the insecticidal external medicine can cause uncomfortable symptoms of pets, such as vomiting, diarrhea and the like. And thirdly, excessive insecticidal external medicines are easy to cause environmental pollution and human body injury.
The siramectin is an avermectin antibiotic fermented by a new strain of genetically recombined streptomyces avermitilis (Streptomyces avermitilis), is a broad-spectrum efficient antiparasitic drug, has a certain peculiar smell, is generally sensitive to the smell of pets, and leads to lower acceptance of the siramectin preparation by the pets.
Disclosure of Invention
The invention aims to overcome at least one defect of the prior art and provides a siramectin external drop for pets and a preparation method thereof.
The technical scheme adopted by the invention is as follows:
in a first aspect of the present invention, there is provided a siramectin topical drop for pets, the siramectin drop for pets being made of, in weight percent:
5 to 15 percent of siramectin
Dipropylene glycol methyl ether 5-15%
Antioxidant 0.05-0.2%
Solvent, balance.
In some embodiments of the siramectin topical drops for pets, the antioxidant is selected from at least one of BHA, BHT.
In some embodiments of the siramectin topical drops for pets, the solvent is selected from at least one of ethanol, propylene glycol, and isopropanol.
In some embodiments of the siramectin topical drops for pets, the concentration of the siramectin is from 7 to 12%.
In some embodiments of the siramectin topical drops for pets, the concentration of the siramectin is 7 to 9%.
In some embodiments of the siramectin topical drops for pets, the concentration of dipropylene glycol methyl ether is from 7 to 12%.
In a second aspect of the present invention, there is provided a method of preparing a siramectin external drops for pets having a composition as defined in any of the above, comprising the steps of:
s1) dissolving siramectin in a part of solvent to obtain a siramectin solution;
s2) adding dipropylene glycol methyl ether into the siramectin solution, and continuously stirring and mixing;
s3) dissolving the antioxidant in the residual solvent, and then mixing with the solution obtained in the step S2) to obtain the siramectin external drops for pets.
In some embodiments of the method of preparing a siramectin for pets, S1) the solvent is selected from at least one of ethanol, propylene glycol, and isopropanol.
In some examples of methods of preparing a topical drop of siramectin for pets, S1) the concentration of siramectin is 8-12%.
In some embodiments of the method of preparing a siramectin topical drop for pets, S3) the antioxidant is selected from at least one of BHA, BHT.
The beneficial effects of the invention are as follows:
the invention uses the siramectin as the core component of the drop, and the dipropylene glycol methyl ether as the transdermal agent, so that the peculiar smell in the drop can be covered while the transdermal is promoted, the invention is more acceptable for pets, and the curative effect can be obviously improved.
The drop provided by the invention is convenient to use, simple in preparation method, high in efficiency and good in insecticidal effect.
Detailed Description
In a first aspect of the present invention, there is provided a siramectin topical drop for pets, the siramectin drop for pets being made of, in weight percent:
5 to 15 percent of siramectin
Dipropylene glycol methyl ether 5-15%
Antioxidant 0.05-0.2%
Solvent, balance.
Siramectin, a semisynthetic macrolide, is an antiparasitic and insect repellent. The siramectin can activate glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent infection of heartworm, filarial worms, nematodes and the like. The siramectin can improve the safety and has good effects of oral administration and injection.
The antioxidant BHT, also called dibutyl hydroxy toluene, is a common food additive, has the function of prolonging the shelf life and is particularly efficient in resisting fat oxidation and deterioration.
The antioxidant BHA, also known as butyl hydroxy anisole, is a mixture of two components (3-BHA and 2-BHA). The resistance of BHA blocks the autoxidation of the grease by the released hydrogen atoms.
Dipropylene glycol methyl ether is a colorless viscous liquid having a pleasant smell and being miscible with water and various organic solvents.
In some embodiments of the siramectin topical drops for pets, the antioxidant is selected from at least one of BHA, BHT.
In some embodiments of the siramectin topical drops for pets, the solvent is selected from at least one of ethanol, propylene glycol, and isopropanol.
In some embodiments of the siramectin topical drops for pets, the concentration of the siramectin is from 7 to 12%.
In some embodiments of the siramectin topical drops for pets, the concentration of the siramectin is 7 to 9%.
In some embodiments of the siramectin topical drops for pets, the concentration of dipropylene glycol methyl ether is from 7 to 12%.
In a second aspect of the present invention, there is provided a method of preparing a siramectin external drops for pets having a composition as defined in any of the above, comprising the steps of:
s1) dissolving siramectin in a part of solvent to obtain a siramectin solution;
s2) adding dipropylene glycol methyl ether into the siramectin solution, and continuously stirring and mixing;
s3) dissolving the antioxidant in the residual solvent, and then mixing with the solution obtained in the step S2) to obtain the siramectin external drops for pets.
In some embodiments of the method of preparing a siramectin for pets, S1) the solvent is selected from at least one of ethanol, propylene glycol, and isopropanol.
In some examples of methods of preparing a topical drop of siramectin for pets, S1) the concentration of siramectin is 8-12%.
In some embodiments of the method of preparing a siramectin topical drop for pets, S3) the antioxidant is selected from at least one of BHA, BHT.
The technical scheme of the invention is further described below by combining examples. In the following examples, the raw materials were all commercially available unless otherwise specified.
Example 1
The siramectin drops are prepared from the following components in percentage by weight
Cypramycin 7.24%
Dipropylene glycol methyl ether 7.24%
BHT 0.1％
85.42 percent of isopropanol.
Example 2
The siramectin drops are prepared from the following components in percentage by weight
Cypramycin 13.5%
Dipropylene glycol methyl ether 7.5%
BHA 0.1％
78.9% of isopropanol.
Example 3
The siramectin drops are prepared from the following components in percentage by weight
Cypramycin 12.21%
Dipropylene glycol methyl ether 1.75%
BHT 0.3％
85.74% of propylene glycol.
The stability of the test results at a high temperature of 60℃for 10 days was examined by using examples 1 to 3, and the test results are shown in Table 1.
TABLE 1 stability test of the invention
The results of examining the data for 10 days according to the stability of the influencing factors at a high temperature of 60 ℃ show that the sirolimus content in the prescription of the example 1 is the most stable, the increase range of related substances is the lowest compared with the other two prescriptions (the examples 2 and 3), and the antioxidant is the most stable in the prescriptions, so the example 1 is the better prescription. The components are mutually promoted and synergistically enhanced, and the maximum efficacy of the drops can be exerted.
The above description of the present invention is further illustrated in detail and should not be taken as limiting the practice of the present invention. It is within the scope of the present invention for those skilled in the art to make simple deductions or substitutions without departing from the concept of the present invention.
Claims (10)
1. The siramectin external drops for pets are characterized by comprising the following components in percentage by weight:
5 to 15 percent of siramectin
Dipropylene glycol methyl ether 5-15%
Antioxidant 0.05-0.2%
Solvent, balance.
2. The siramectin topical drop for pets according to claim 1, characterized in that said antioxidant is selected from at least one of BHA, BHT.
3. The siramectin external drops for pets according to claim 1, characterized in that said solvent is selected from at least one of ethanol, propylene glycol and isopropanol.
4. The external drops of siramectin for pets according to claim 1, characterized in that the concentration of said siramectin is 7-12%.
5. The external drops of siramectin for pets according to claim 1, characterized in that the concentration of said siramectin is 7-9%.
6. The siramectin topical drop for pets according to claim 1, characterized in that said dipropylene glycol methyl ether concentration is 7-12%.
7. A process for the preparation of a siramectin topical drop for pets having a composition according to any of claims 1 to 6, comprising the steps of:
s1) dissolving siramectin in a part of solvent to obtain a siramectin solution;
s2) adding dipropylene glycol methyl ether into the siramectin solution, and continuously stirring and mixing;
s3) dissolving the antioxidant in the residual solvent, and then mixing with the solution obtained in the step S2) to obtain the siramectin external drops for pets.
8. The method according to claim 7, wherein S1) the solvent is at least one selected from the group consisting of ethanol, propylene glycol and isopropanol.
9. The method of claim 7, wherein S1) the concentration of sirolimus is 8-12%.
10. The method according to claim 7, wherein S3) the antioxidant is at least one selected from the group consisting of BHA and BHT.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210796041.0A CN116196271A (en) | 2022-07-07 | 2022-07-07 | Externally-applied siramectin drop for pets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202210796041.0A CN116196271A (en) | 2022-07-07 | 2022-07-07 | Externally-applied siramectin drop for pets and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN116196271A true CN116196271A (en) | 2023-06-02 |
Family
ID=86515216
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202210796041.0A Pending CN116196271A (en) | 2022-07-07 | 2022-07-07 | Externally-applied siramectin drop for pets and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN116196271A (en) |
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2022
- 2022-07-07 CN CN202210796041.0A patent/CN116196271A/en active Pending
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