CN110680803A - Selamectin ethosome preparation and preparation method and application thereof - Google Patents
Selamectin ethosome preparation and preparation method and application thereof Download PDFInfo
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Abstract
The invention discloses a selamectin ethosome preparation, a preparation method and application thereof, wherein the parasite expelling preparation comprises the following components: selamectin, egg yolk lecithin, alcohol (including ethanol and propylene glycol), tween-80 and phosphate buffer. Compared with a selamectin transdermal agent, the invention greatly reduces the toxicity, and has the advantages of good skin permeability, biological slow release, longer action time, good stability and high safety. Animal experiments prove that the ethosome preparation has the effect of resisting in-vivo and in-vitro parasitic infection of dogs and cats.
Description
Technical Field
The invention belongs to the field of insect control, and particularly relates to a selamectin ethosome preparation as well as a preparation method and application thereof.
Background
In recent years, with the rapid development of socioeconomic performance, the standard of living of people has been improved. Raising pets is increasingly favored by people. Parasitic diseases cause a series of problems for pets. The pet parasites are of various types, wherein the toxocara gondii is an important nematode parasitizing in dogs and cats, can cause the migration of animal internal organs and eye larvae, and is a zoonosis. The heartworm and lung failure and even death can be caused when the adult heartworm and lung are parasitized in the right ventricle and pulmonary artery of the dog. The heartworm transmission medium is a mosquito, a person is not a suitable host of the heartworm, but the person is bitten by the mosquito containing the larvae in the heartworm infection stage, and the infection can happen occasionally, which is shown as the formation of worm nodules by lung or subcutaneous tissue. Secondly, the infection rate of ectoparasites such as ticks, mites, fleas and lice of dogs and cats is still high and is distributed around the world, so that skin itch, depilation, red swelling, scabbing and the like of dogs and cats are caused, and the health of pets is seriously influenced. Brings certain influence to the health of pets and human beings, causes hidden health troubles,
the selamectin is a new generation of abamectin antiparasitic drug, the traditional transdermal agent is a traditional and main preparation form, and the slow-release, controlled-release and targeted drug delivery effects can be achieved by changing the selamectin preparation in order to improve the bioavailability of the drug.
The insect repellent preparation for pets mainly comprises 3 dosage forms: transdermal agents, oral agents and injections. When the composition is used for pets, the main preparation form is transdermal agent, and the parasite on the body surface of animals can be killed by simple operation. However, the drug effect of the selamectin is not long, and the penetration effect of the transdermal agent is not obvious. In view of the existing problems, the invention needs a medicament capable of effectively preventing or treating pet epizoonosis.
Disclosure of Invention
The invention aims at providing a selamectin ethosome preparation.
It is a further object of the present invention to provide a method for preparing the above-described ethosomes formulation.
It is yet another object of the present invention to provide a method for reducing parasites in animals.
It is a further object of the present invention to provide the use of the above-described ethosomes formulations.
The inventor finds that fipronil and methoprene are compounded in the existing scheme, but the effect of treating parasites is not obvious, the parasites cannot be completely killed, the drug action time is short, and a targeted, sustained-release and efficient transdermal drug delivery dosage form is lacked.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows:
in one aspect of the invention, a selamectin ethosome preparation is provided, which comprises the following components: selamectin, yolk lecithin, alcohol Tween-80 and phosphate buffer solution; the alcohol is ethanol and propylene glycol.
Further, the composition comprises the following components in parts by weight: 8.0-12.0 parts of selamectin; 2.0-2.5 parts of egg yolk lecithin; 30.0 parts of alcohol; and 55.0-65.0 parts of phosphate buffer solution by weight of 800.5 parts of tween-water.
Further, the composition comprises the following components in parts by weight: 8.0-10.5 parts of selamectin; 2.0-2.3 parts of egg yolk lecithin; 30.0 parts of alcohol; tween-800.5 parts and 57.0-65.0 parts of phosphate buffer solution.
Further, the composition comprises the following components in parts by weight: 10.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol; tween-80, 0.5 parts and 55.5 parts phosphate buffer.
In another aspect of the invention, a method for preparing an imidacloprid and moxidectin diol liposome preparation is provided, which comprises the following steps:
(1) weighing selamectin, yolk lecithin and tween-80 according to any one of the above formulas, and stirring under sealed condition until the selamectin, the yolk lecithin and the tween-80 are dissolved;
(2) dropping phosphate buffer solution while stirring, and cooling to room temperature;
(3) performing ultrasonic treatment to obtain a nano ethosome preparation;
(4) filtering to obtain the selamectin ethosome preparation with nano granularity and uniform distribution.
Further, the stirring temperature in the step (1) is 29.5-30.5 ℃, and the stirring speed is 600-800 rpm; the dropping speed in the step (2) is 3-6 mL/min; the pH value of the phosphate buffer solution is 6.5-7.0; the stirring time is 20-30 min.
Further, in the step (3), the ultrasonic power is 100-120W, and the frequency is 45-50 kHz; carrying out ultrasonic treatment for 3-4 s at intervals of 3-4 s for 30-40 cycles; filtering by a 50-100 nm microporous polycarbonate membrane for 10-15 times.
It is yet another object of the present invention to provide a method for reducing parasites in animals. The method for reducing parasites in animals is: applying any one of the above glycol plastid preparations to dry skin of an animal; the smearing mode is selected from pouring or dipping; the skin is back and neck skin.
The invention also aims to provide the application of the dialcohol plastid preparation in preparing medicaments. The use of the above-mentioned glycol plastid preparation in the preparation of a medicament for the control of animal parasites; the animal is a dog or a cat; the skin is back and neck skin; the parasites can be reduced in number by applying the formulation of glycol plastids to dry skin of the animal.
Further, the parasites include ectoparasites and endoparasites; the endoparasite comprises a roundworm or heartworm; the ectoparasites include ticks, scabies, fleas or lice.
The invention has the beneficial effects that:
the invention takes the selamectin as the main effective component, combines with other substances to prepare an ethosome preparation, takes ethosome as a percutaneous administration form of the selamectin, avoids the first pass effect of the medicament, maintains constant blood concentration and pharmacological effect, thereby enhancing the treatment effect of the medicament, reducing adverse reaction and achieving the slow release effect. The ethosome preparation of the selamectin is beneficial to improving the transdermal depth and the epidermal and dermal drug retention of the selamectin, so that the drug can reach longer effective action time, the insect expelling effect of the preparation is improved, the action time of the preparation is prolonged, the insect expelling number can be effectively reduced, and the treatment effect is improved.
Detailed Description
In one aspect of the invention, a selamectin ethosome preparation is provided, which comprises the following components: selamectin, yolk lecithin, alcohol Tween-80 and phosphate buffer solution; the alcohol is ethanol and propylene glycol.
Preferably, the composition comprises the following components in parts by weight: 8.0-12.0 parts of selamectin; 2.0-2.5 parts of egg yolk lecithin; 30.0 parts of alcohol; and 55.0-65.0 parts of phosphate buffer solution by weight of 800.5 parts of tween-water.
Preferably, the composition comprises the following components in parts by weight: 8.0-10.5 parts of selamectin; 2.0-2.3 parts of egg yolk lecithin; 30.0 parts of alcohol; tween-800.5 parts and 57.0-65.0 parts of phosphate buffer solution.
Preferably, the composition comprises the following components in parts by weight: 10.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol; tween-80, 0.5 parts and 55.5 parts phosphate buffer.
In another aspect of the invention, a method for preparing an imidacloprid and moxidectin diol liposome preparation is provided, which comprises the following steps:
(1) weighing selamectin, yolk lecithin and tween-80 according to any one of the above formulas, and stirring under sealed condition until the selamectin, the yolk lecithin and the tween-80 are dissolved;
(2) dropping phosphate buffer solution while stirring, and cooling to room temperature;
(3) performing ultrasonic treatment to obtain a nano ethosome preparation;
(4) filtering to obtain the selamectin ethosome preparation with nano granularity and uniform distribution.
Preferably, the stirring temperature in the step (1) is 29.5-30.5 ℃, and the stirring speed is 600-800 rpm; the dropping speed in the step (2) is 3-6 mL/min; the pH value of the phosphate buffer solution is 6.5-7.0; the stirring time is 20-30 min.
Preferably, the ultrasonic power in the step (3) is 100-120W, and the frequency is 45-50 kHz; carrying out ultrasonic treatment for 3-4 s at intervals of 3-4 s for 30-40 cycles; filtering by a 50-100 nm microporous polycarbonate membrane for 10-15 times.
It is yet another object of the present invention to provide a method for reducing parasites in animals. The method for reducing parasites in animals is: applying any one of the above glycol plastid preparations to dry skin of an animal; the smearing mode is selected from pouring or dipping; the skin is back and neck skin.
The invention also aims to provide the application of the dialcohol plastid preparation in preparing medicaments. The use of the above-mentioned glycol plastid preparation in the preparation of a medicament for the control of animal parasites; the animal is a dog or a cat; the skin is back and neck skin; the parasites can be reduced in number by applying the formulation of glycol plastids to dry skin of the animal.
Further, the parasites include ectoparasites and endoparasites; the endoparasite comprises a roundworm or heartworm; the ectoparasites include ticks, scabies, fleas or lice.
The technical solution of the present invention is clearly and completely illustrated below with reference to the following examples, but is not limited thereto.
Example 1
The selamectin ethosome preparation comprises the following components in parts by weight: 8.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 30.0 parts of alcohol (ethanol: propylene glycol ═ 6.5: 3.5); tween-80, 0.5 parts and phosphate buffer (pH 6.5). (taking a total of 100ml as an example)
A preparation method of a selamectin ethosome preparation comprises the following steps:
(1) weighing selamectin, yolk lecithin, alcohol (ethanol: propylene glycol ═ 6.5:3.5) and tween-80 according to the proportion, adding into a reaction tank, stirring at the temperature of 30 ℃ and the stirring speed of 700rpm, and stirring until the selamectin, the yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) then adding phosphate buffer (pH 6.5) at a dropping rate of 1mL/min, stirring under sealed condition for 20min until complete dissolution, and cooling to room temperature;
(3) performing ultrasonic treatment for 3s at an ultrasonic power of 100W and an ultrasonic frequency of 45kHz at an interval of 3s for 30 cycles, and performing ultrasonic treatment by an ultrasonic pulverizer to obtain a nano ethosomes preparation;
(4) filtering with 100nm microporous polycarbonate membrane for 10 times to obtain nanometer eudragit ethosome preparation with uniform particle size distribution.
The selamectin ethosome preparation is characterized in that: the particle size is 46nm, the Zeta potential is-23.41 mV, the drug loading rate is 76.40 parts, the encapsulation rate is 97.05 parts, and the retention of the drug in the dermal layer of the epidermis is 27.11 mu g/cm2。
Example 2
The selamectin ethosome preparation comprises the following components in parts by weight: 10.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol (ethanol: propylene glycol ═ 6.5: 3.5); tween-80, 0.5 parts and phosphate buffer (pH 6.5). (taking a total of 100ml as an example)
A preparation method of a selamectin ethosome preparation comprises the following steps:
(1) weighing selamectin, yolk lecithin, alcohol (ethanol: propylene glycol ═ 6.5:3.5) and tween-80 according to the proportion, adding into a reaction tank, stirring at the temperature of 30 ℃ and the stirring speed of 700rpm, and stirring until the selamectin, the yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) then adding phosphate buffer (pH 6.5) at a dropping rate of 1mL/min, stirring under sealed condition for 20min until complete dissolution, and cooling to room temperature;
(3) performing ultrasonic treatment for 3s at an ultrasonic power of 100W and an ultrasonic frequency of 45kHz at an interval of 3s for 30 cycles, and performing ultrasonic treatment by an ultrasonic pulverizer to obtain a nano ethosomes preparation;
(4) filtering with 100nm microporous polycarbonate membrane for 10 times to obtain nanometer eudragit ethosome preparation with uniform particle size distribution.
The selamectin ethosome preparation is characterized in that: the particle size is 44nm, the Zeta potential is-25.58 mV, the drug loading rate is 77.79 parts, the encapsulation rate is 98.01 parts, and the retention of the drug in the dermal layer of the epidermis is 28.35 mu g/cm2。
Example 3
The selamectin ethosome preparation comprises the following components in parts by weight: 12.0 parts of selamectin; 2.5 parts of egg yolk lecithin; 35.0 parts of alcohol (ethanol: propylene glycol ═ 6.5: 3.5); tween-80, 0.5 parts and phosphate buffer (pH 6.5). (taking a total of 100ml as an example)
A preparation method of a selamectin ethosome preparation comprises the following steps:
(1) weighing selamectin, yolk lecithin, alcohol (ethanol: propylene glycol ═ 6.5:3.5) and tween-80 according to the proportion, adding into a reaction tank, stirring at the temperature of 30 ℃ and the stirring speed of 700rpm, and stirring until the selamectin, the yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) then adding phosphate buffer (pH 6.5) at a dropping rate of 1mL/min, stirring under sealed condition for 20min until complete dissolution, and cooling to room temperature;
(3) performing ultrasonic treatment for 3s at an ultrasonic power of 100W and an ultrasonic frequency of 45kHz at an interval of 3s for 30 cycles, and performing ultrasonic treatment by an ultrasonic pulverizer to obtain a nano ethosomes preparation;
(4) filtering with 100nm microporous polycarbonate membrane for 10 times to obtain nanometer eudragit ethosome preparation with uniform particle size distribution.
The selamectin ethosome preparation is characterized in that: the particle size is 41nm, the Zeta potential is-23.94 mV, the drug loading rate is 78.14 parts, the encapsulation rate is 98.97 parts, and the retention of the drug in the dermal layer of the epidermis is 27.40 mu g/cm2。
Example 4
The selamectin ethosome preparation comprises the following components in parts by weight: 11.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol (ethanol: propylene glycol ═ 6.5: 3.5); tween-80, 0.5 parts and 54.5 parts of phosphate buffer (pH 6.5). (taking a total of 100ml as an example)
A preparation method of a selamectin ethosome preparation comprises the following steps:
(1) weighing selamectin, yolk lecithin, alcohol (ethanol: propylene glycol ═ 6.5:3.5) and tween-80 according to the proportion, adding into a reaction tank, stirring at the temperature of 30 ℃ and the stirring speed of 700rpm, and stirring until the selamectin, the yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) then adding phosphate buffer (pH 6.5) at a dropping rate of 1mL/min, stirring under sealed condition for 20min until complete dissolution, and cooling to room temperature;
(3) performing ultrasonic treatment for 4s at an ultrasonic power of 100W and an ultrasonic frequency of 45kHz at an interval of 4s for 40 cycles, and performing ultrasonic treatment by an ultrasonic pulverizer to obtain a nano ethosomes preparation;
(4) filtering with 100nm microporous polycarbonate membrane for 15 times to obtain nanometer eudragit ethosome preparation with uniform particle size distribution.
Example 5
The selamectin ethosome preparation comprises the following components in parts by weight: 10.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol (ethanol: propylene glycol ═ 6.5: 3.5); tween-80, 0.5 parts and 55.5 parts of phosphate buffer (pH 6.5). (taking a total of 100ml as an example)
A preparation method of a selamectin ethosome preparation comprises the following steps:
(1) weighing selamectin, yolk lecithin, alcohol (ethanol: propylene glycol ═ 6.5:3.5) and tween-80 according to the proportion, adding into a reaction tank, stirring at the temperature of 30 ℃ and the stirring speed of 700rpm, and stirring until the selamectin, the yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) then adding phosphate buffer (pH 6.5) at a dropping rate of 1mL/min, stirring under sealed condition for 20min until complete dissolution, and cooling to room temperature;
(3) performing ultrasonic treatment for 3s at an ultrasonic power of 100W and an ultrasonic frequency of 45kHz at an interval of 3s for 30 cycles, and performing ultrasonic treatment by an ultrasonic pulverizer to obtain a nano ethosomes preparation;
(4) filtering with 100nm microporous polycarbonate membrane for 12 times to obtain nanometer eudragit ethosome preparation with uniform particle size distribution.
Comparative example 1
A selamectin transdermal agent comprising: 12.0 parts of selamectin, 5 parts of propylene glycol and 83 parts of ethanol.
The antiparasitic effect of the selamectin ethosome is illustrated below in connection with specific experiments.
Experimental materials:
control drugs: a selamectin transdermal agent.
Selamectin ethosome: the formulations are examples.
Experimental animals: 50 affected dogs veterinarily diagnosed with ectoparasites were provided by a canine farm.
50 diseased cats with ectoparasites diagnosed by a veterinarian were provided by the cat farm.
The experimental method comprises the following steps:
grouping: the 50 affected dogs were randomly divided into 7 groups, which were experimental group 1-5, drug control group and blank control group. The 50 diseased cats were randomly divided into 7 groups, which were experimental 8-12, drug control and blank control groups, respectively.
And (3) treatment: groups 1-6, administered at a dose of 0.1ml per 1Kg body weight, dropped between scapulae on the back of a dog, administered 1 time, and the healing condition was observed.
The control dogs were not dosed and observed for onset of disease.
Groups 8-13, administered 0.1ml per 1Kg body weight, dropped between scapulae on back of cat, administered 1 time, and the cure condition was observed. The cats in the control group were not treated with the drug and the onset of the disease was observed. The test lasted 1 month. The experimental groups are shown in Table 1.
TABLE 1 groups of tests
Scraping skin tissue at the junction of the diseased part and the healthy skin on days 1, 2, 7, 14, 21, 28, 35, 42, 49, 56 and 63 after administration, placing the skin tissue in a culture dish, and inspecting the conditions of worms, mites, fleas, lice and ova by a humidifying method;
collecting fecal samples on days 1, 2, 7, 14, 21, 28, 35, 42, 49, 56 and 63 after administration, and detecting ascarid and heartworm ovum condition.
The reduction rate was calculated according to the following formula. Evaluation of results, cure: clinical symptoms disappear, and the insect reduction rate is more than 80 parts; the method has the following advantages: the disease condition is obviously improved, and 80 parts of the pesticide composition is more than or equal to 60 parts of the pest reduction rate; and (4) invalidation: the disease condition is not obviously improved or aggravated, and the insect reduction rate is less than 60 parts.
Reduction rate (in parts) is (average number of adults detected in control group-average number of adults detected in experimental group)/(average number of adults detected in control group)
The experimental results are as follows:
the relevant clinical symptoms of the experimental animals were observed and recorded daily. 2 days after the administration, the symptoms of ectoparasite infection were reduced in groups 1 to 6 and 8 to 13 to which the preparations of examples were added, and the crust portion fell off. After 7 days of administration, the symptoms of ectoparasite infections completely disappeared from groups 1-6, and 8-13, and the presence of worms, fleas and eggs was not detected by microscopic examination. There was no improvement in symptoms in control group 7 and control group 14. The specific experimental results are shown in table 2.
TABLE 2 clinical efficacy of the groups on ectoparasites of the experimental animals
In summary, the alcoholic formulations of selamectin according to the invention can be used for controlling/combating (i.e. significantly reducing or even eliminating the number of parasites) ectoparasites. The parasites include ectoparasites and endoparasites; the endoparasites include roundworms, heartworms; the ectoparasites include ticks, scabies, fleas or lice.
The above embodiments are preferred embodiments of the present invention, but the present invention is not limited to the above embodiments, and any other changes, modifications, substitutions, combinations, and simplifications which do not depart from the spirit and principle of the present invention should be construed as equivalents thereof, and all such changes, modifications, substitutions, combinations, and simplifications are intended to be included in the scope of the present invention.
Claims (10)
1. An ethosome preparation, which is characterized by comprising selamectin, yolk lecithin, alcohol, Tween-80 and phosphate buffer; the alcohol is ethanol and propylene glycol.
2. The ethosome formulation according to claim 1, characterized by comprising the following ingredients in parts by weight: 8.0-12.0 parts of selamectin; 2.0-2.5 parts of egg yolk lecithin; 30.0 parts of alcohol; tween-800.5 parts and 55.0-65.0 parts of phosphate buffer solution.
3. The ethosome formulation according to claim 2, characterized by comprising the following ingredients in parts by weight: 8.0-10.5 parts of selamectin; 2.0-2.3 parts of egg yolk lecithin; 30.0 parts of alcohol; tween-800.5 parts and 57.0-65.0 parts of phosphate buffer solution.
4. The ethosome formulation according to claim 3, characterized by comprising the following ingredients in parts by weight: 10.0 parts of selamectin; 2.0 parts of egg yolk lecithin; 32.0 parts of alcohol; tween-80, 0.5 parts and 55.5 parts of phosphate buffer.
5. The method for preparing a liposome preparation according to any one of claims 1 to 4, comprising the steps of:
(1) weighing selamectin, egg yolk lecithin, alcohol and tween-80 according to the formula of any one of claims 1 to 4, and stirring in a closed state until the selamectin, the egg yolk lecithin, the alcohol and the tween-80 are dissolved;
(2) dropping phosphate buffer solution while stirring, and cooling to room temperature;
(3) obtaining a nanometer ethosome by ultrasonic;
(4) filtering to obtain the selamectin ethosome.
6. The preparation method according to claim 5, wherein the stirring temperature in the step (1) is 29.5 to 30.5 ℃, and the stirring speed is 600 to 800 rpm; the dropping speed in the step (2) is 3-6 mL/min; the pH value of the phosphate buffer solution is 6.5-7.0; the stirring time is 20-30 min.
7. The preparation method according to claim 5, wherein the ultrasonic power in the step (3) is 100-120W, and the frequency is 45-50 kHz; carrying out ultrasonic treatment for 3-4 s at intervals of 3-4 s for 30-40 cycles; filtering by a 50-100 nm microporous polycarbonate membrane for 10-15 times.
8. A method for reducing parasites on animals, comprising applying an ethosome formulation according to any one of claims 1 to 4 to the dry skin of an animal; the smearing mode is selected from pouring or dipping; the skin is back and neck skin.
9. Use of an ethosome formulation according to any one of claims 1 to 4 for the preparation of a medicament for the control of animal parasites; the animal is a dog and/or a cat; the skin is back and neck skin; the parasites can be reduced in number by applying the formulation of glycol plastids to dry skin of the animal.
10. The use according to claim 9, wherein the parasites comprise ectoparasites and endoparasites; the endoparasite comprises a roundworm or heartworm; the ectoparasites include ticks, scabies, fleas or lice.
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| WO2015123750A1 (en) * | 2014-02-20 | 2015-08-27 | Cura Health Inc. | Transdermal composition for treating pain |
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2019
- 2019-10-17 CN CN201910986012.9A patent/CN110680803A/en active Pending
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| WO2008052263A1 (en) * | 2006-11-01 | 2008-05-08 | Veterinary Encapsulation Biosciences Pty Ltd | Delivery system for remote treatment of an animal |
| CN101273971A (en) * | 2008-05-09 | 2008-10-01 | 绍兴文理学院 | Etosome preparation of antifungal drug and preparation method thereof |
| CN102949340A (en) * | 2011-08-24 | 2013-03-06 | 中国农业科学院兰州畜牧与兽药研究所 | Sarah rhzomorph nano emulsion medicine composition and preparation method thereof |
| WO2015123750A1 (en) * | 2014-02-20 | 2015-08-27 | Cura Health Inc. | Transdermal composition for treating pain |
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