CN116808033A - Moxidectin compound preparation and preparation method and application thereof - Google Patents

Moxidectin compound preparation and preparation method and application thereof Download PDF

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Publication number
CN116808033A
CN116808033A CN202310794009.3A CN202310794009A CN116808033A CN 116808033 A CN116808033 A CN 116808033A CN 202310794009 A CN202310794009 A CN 202310794009A CN 116808033 A CN116808033 A CN 116808033A
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moxidectin
compound preparation
imidacloprid
solution
prednisone
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周淑贞
伍洁燕
元晓琪
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Foshan Nanhai Eastern Along Pharmaceutical Co ltd
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Foshan Nanhai Eastern Along Pharmaceutical Co ltd
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Abstract

The invention discloses a moxidectin compound preparation and a preparation method and application thereof, wherein the moxidectin compound preparation comprises the following components in percentage by mass: 0.4% -2.5% moxidectin, 0.4% -3.5% imidacloprid, 0.3% -1% non-prednisone, 10% -40% oil phase solvent, 20% -60% emulsifying agent, 10% -30% co-emulsifying agent and 0.05% -0.2% antioxidant. The moxidectin compound preparation provided by the invention is formed by compounding three medicinal components of moxidectin, imidacloprid and non-prednisone, and can be used for simultaneously expelling and killing various internal and external parasites such as fleas, mites, lice, ticks, nematodes, tapeworms and heartworms, and has the advantages of broad insect expelling spectrum, low toxicity and high efficiency; the moxidectin compound preparation is microemulsion, which can increase the drug permeation and improve the permeation speed; the moxidectin compound preparation adopts lower alcohol as an auxiliary emulsifier, can promote the whole transdermal transport of a drug carrying system, plays a role of a reservoir, enables the drug to be slowly released, and plays a long-acting role.

Description

Moxidectin compound preparation and preparation method and application thereof
Technical Field
The invention relates to the technical field of veterinary medicines, in particular to a moxidectin compound preparation and a preparation method and application thereof.
Background
With the increasing number of pets, parasitic diseases show a high tendency. And the parasitic infection not only can influence the health of pets, including host nutrition, toxin effect, tissue injury and the like, but also can cause hidden danger to the health of a feeding owner. Thus, the control of parasites is very important.
Moxidectin has a very high lipophilicity and therefore its concentration of distribution in fat is very high. Active against many internal and external parasites, especially the larval stage heartworms, is a rare anthelmintic against heartworms. The imidacloprid has the contact killing effect and is particularly suitable for being used as an external drop to expel insects to dogs. Imidacloprid inhibits cholinergic transmission of insects resulting in paralysis and death. Meanwhile, since imidacloprid has weak interaction property with the nicotinic receptor of mammal and is difficult to penetrate the blood brain barrier of mammal, it has little influence on the central nervous system of mammal and has high safety. Non-prednisone Luo Nineng compensates the short board for the expelling and killing of ticks well, so that the compound preparation has wider expelling spectrum.
While considering the efficacy of anthelmintics, we should pay more attention to the acceptability of pets. The oral insect repellent is not easy to feed; the externally applied insect repellent is convenient to use, but due to the problem of solution permeability, the skin is slow to permeate, the solution stays on the surface of the skin or hair for a long time, and pets are easier to scratch, lick, scratch, dehairing and even poisoning.
Therefore, it is necessary to develop an antiparasitic compound preparation for pets, which has wide spectrum of insect resistance, stable thermodynamics, good skin permeability and slow release.
Disclosure of Invention
In view of the defects of the prior art, the invention aims to provide a moxidectin compound preparation, a preparation method and application thereof, and aims to solve the problems of poor skin permeability, unstable thermodynamics and over-fast release of the existing antiparasitic compound preparation.
The technical scheme of the invention is as follows:
the moxidectin compound preparation comprises the following components in percentage by mass: 0.4% -2.5% moxidectin, 0.4% -3.5% imidacloprid, 0.3% -1% non-prednisone, 10% -40% oil phase solvent, 20% -60% emulsifying agent, 10% -30% co-emulsifying agent and 0.05% -0.2% antioxidant.
The moxidectin compound preparation comprises the following components in percentage by mass: 0.4% -1.4% moxidectin, 0.8% -3.5% imidacloprid, 0.3% -0.7% non-prednisone, 10% -28% oil phase solvent, 18% -52% emulsifying agent, 11% -21% co-emulsifying agent and 0.05% -0.1% antioxidant.
The moxidectin compound preparation is characterized in that the emulsifier is one or two of tween-80 and castor oil polyoxyethylene ether-40.
The moxidectin compound preparation is characterized in that the auxiliary emulsifier is one or two of 1, 2-propylene glycol and isopropanol.
The moxidectin compound preparation is characterized in that the antioxidant is one or two of dibutyl hydroxy toluene and butyl hydroxy anisole.
A method for preparing a compound preparation of moxidectin, which comprises the following steps:
sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in an oil phase solvent, and magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
mixing an emulsifying agent and a coemulsifier, and magnetically stirring to obtain a solution B;
mixing the solution A and the solution B, and canning to obtain the moxidectin compound preparation.
A method for preparing a compound preparation of moxidectin, which comprises the following steps:
mixing an oil phase solvent, an emulsifier and a co-emulsifier, and magnetically stirring to obtain a solution C;
and sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in the solution C, magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution D, and filling to obtain the moxidectin compound preparation.
The preparation method of the moxidectin preparation further comprises the step of adding purified water before canning.
The moxidectin compound preparation is used for preparing an insect repellent for animals.
The use wherein the animal is a canine or a feline.
The beneficial effects are that: the moxidectin compound preparation provided by the invention is formed by compounding three medicinal components of moxidectin, imidacloprid and non-prednisone, and can be used for simultaneously expelling and killing various internal and external parasites such as fleas, mites, lice, ticks, nematodes, tapeworms and heartworms, and has the advantages of broad insect expelling spectrum, low toxicity and high efficiency; the moxidectin compound preparation is microemulsion, and the lipophilic region can interact with the horny layer, so that the lipophilic medicament such as moxidectin can be directly distributed into the lipid of the horny layer to increase the medicament permeation, and the hydrophilic region can hydrate the horny layer to obviously improve the permeation rate; the moxidectin compound preparation adopts lower alcohol as an auxiliary emulsifier, can promote the whole transdermal transport of a drug carrying system, plays a role of a reservoir, enables the drug to be slowly released, and plays a long-acting role. Furthermore, the moxidectin compound preparation provided by the invention has the advantages of simple preparation process, easiness in preparation at room temperature, no special requirement on equipment and suitability for industrial production.
Drawings
Fig. 1 is a flow chart of a preparation method of a compound preparation of moxidectin.
Fig. 2 is a comparison graph of skin irritation after the moxidectin compound preparation and physiological saline are applied to guinea pigs in example 1 for 4 hours, wherein the left graph is the moxidectin compound preparation applied and the right graph is the physiological saline applied.
Fig. 3 is a graph showing the comparative results of the cumulative permeation amounts of moxidectin of the moxidectin compound formulations of example 1 and comparative example 3.
Fig. 4 is a graph showing the comparative results of the cumulative permeation amounts of moxidectin of the moxidectin compound formulations of example 2 and comparative example 4.
Fig. 5 is a graph showing the comparative results of the cumulative permeation amounts of moxidectin in the moxidectin compound formulations of example 3 and comparative example 5.
Detailed Description
The invention provides a moxidectin compound preparation, a preparation method and application thereof, and aims to make the purposes, the technical scheme and the effects of the invention clearer and more definite, and the invention is further described in detail below. It should be understood that the specific embodiments described herein are for purposes of illustration only and are not intended to limit the scope of the invention.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The terminology used herein in the description of the invention is for the purpose of describing particular embodiments only and is not intended to be limiting of the invention.
The invention provides a moxidectin compound preparation, which comprises the following components in percentage by mass: 0.4% -2.5% moxidectin, 0.4% -3.5% imidacloprid, 0.3% -1% non-prednisone, 10% -40% oil phase solvent, 20% -60% emulsifying agent, 10% -30% co-emulsifying agent and 0.05% -0.2% antioxidant.
In the invention, the moxidectin compound preparation is formed by compounding three medicinal components of moxidectin, imidacloprid and non-prednisone, can simultaneously kill various internal and external parasites such as fleas, mites, lice, ticks, nematodes, tapeworms, heartworms and the like, and has wide insect repelling spectrum, low toxicity and high efficiency; the moxidectin compound preparation is prepared into microemulsion by adding the emulsifier and the auxiliary emulsifier, and the lipophilic region can interact with the horny layer, so that the lipophilic medicament such as moxidectin can be directly distributed into the lipid of the horny layer, the medicament permeation is increased, and the hydrophilic region can be hydrated with the horny layer, so that the permeation speed is obviously improved; the moxidectin compound preparation adopts lower alcohol as a co-emulsifier and combines with an oil phase solvent, so that the moxidectin compound preparation can promote the whole transdermal transport of a drug carrying system, plays a role of a reservoir, enables a drug to be slowly released and plays a long-acting role.
In some embodiments, the moxidectin compound preparation comprises, in mass percent: 0.4% -1.4% moxidectin, 0.8% -3.5% imidacloprid, 0.3% -0.7% non-prednisone, 10% -28% oil phase solvent, 18% -52% emulsifying agent, 11% -21% co-emulsifying agent and 0.05% -0.1% antioxidant. In the embodiment, the moxidectin compound preparation prepared by optimizing the components has better insect repellent effect, better drug permeation and more stable thermodynamics.
In some embodiments, the emulsifier is one or two of tween-80 and castor oil polyoxyethylene ether-40, but is not limited thereto; the auxiliary emulsifier is one or two of 1, 2-propylene glycol and isopropanol, but is not limited to the above.
In some embodiments, the antioxidant is one or both of dibutyl hydroxy toluene (BHT), butyl Hydroxy Anisole (BHA), but is not limited thereto.
In some embodiments, there is also provided a method for preparing a compound moxidectin preparation, as shown in fig. 1, comprising the steps of:
s10, sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in an oil phase solvent, and magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
s20, mixing an emulsifying agent and a coemulsifier, and magnetically stirring to obtain a solution B;
s30, mixing the solution A with the solution B, and canning to obtain the moxidectin compound preparation.
The moxidectin compound preparation provided by the invention has the advantages of simple preparation process, easiness in preparation at room temperature, no special requirement on equipment and suitability for industrial production.
In another embodiment, there is also provided another method for preparing a compound preparation of moxidectin, comprising the steps of: mixing an oil phase solvent, an emulsifier and a co-emulsifier, and magnetically stirring to obtain a solution C; and sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in the solution C, magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution D, and filling to obtain the moxidectin compound preparation.
In some embodiments, the method further comprises the step of adding purified water before canning, wherein the concentration and physical state of the moxidectin compound preparation are adjusted by adding purified water.
In some embodiments, the invention also provides an application of the moxidectin compound preparation, wherein the moxidectin compound preparation is used for preparing an insect repellent for animals. In this embodiment, the animal is a canine or a feline.
The invention is further illustrated by the following examples:
example 1
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 1%, imidacloprid 2%, non-prednisone 0.5%, benzyl alcohol 22%, EL-40 41.6%,1, 2-propanediol 20.35%, BHT 0.05% and purified water 12.5%.
In yet another aspect of the present embodiment, a method for preparing a compound preparation of corresponding moxidectin is provided, including the following steps:
a. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in benzyl alcohol, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
b. mixing an emulsifier and a coemulsifier according to a certain proportion, magnetically stirring for 10min at a rotating speed of 500r/min to obtain a solution B;
c. mixing the solution A and the solution B, adding purified water, changing the solution from turbidity to clarification, and filling to finish.
The using method comprises the following steps: based on the product, the external use is as follows: the dosage is 0.2mL/kg once, and the administration is once a month; the product can be dropped onto skin between two scapula on animal back to buttock to prevent animal licking. Animals other than and not only dogs and cats below their age of february are forbidden, and are carefully used for dogs and cats during pregnancy and lactation.
Example 2
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 1.4%, imidacloprid 2.85%, non-prednisone 0.6%, benzyl alcohol 28%, EL-40%, isopropanol 17.1%, BHT 0.05% and purified water 0.
In still another aspect of the present invention, a method for preparing a compound moxidectin preparation is provided, comprising the following steps:
a. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in benzyl alcohol, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
b. mixing an emulsifier and a coemulsifier according to a certain proportion, magnetically stirring for 10min at a rotating speed of 500r/min to obtain a solution B;
c. mixing the solution A and the solution B, and filling to finish.
The using method comprises the following steps: based on the product, the external use is as follows: the dosage is 0.15mL/kg once, and the administration is once a month. The product can be dropped on the skin between the two scapula of the back of the animal to the buttock to prevent the animal from licking; animals other than and not only dogs and cats below their age of february are forbidden, and are carefully used for dogs and cats during pregnancy and lactation.
Example 3
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 0.4%, imidacloprid 0.8%, non-prednisone 0.3%, benzyl alcohol 10.9%, tween-80 25%,1, 2-propanediol 12.5%, BHT 0.1% and purified water 50%.
In still another aspect of the present invention, a method for preparing a compound moxidectin preparation is provided, comprising the following steps:
a. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in benzyl alcohol, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
b. mixing an emulsifier and a coemulsifier according to a certain proportion, magnetically stirring for 10min at a rotating speed of 500r/min to obtain a solution B;
c. mixing the solution A with the solution B, and filling to obtain a solution C.
d. The solution C was then added with an appropriate amount of water and shaken to obtain a clear solution D from cloudiness.
The using method comprises the following steps: based on the product, the medicine is prepared for external use at present: the amount is 0.4mL/kg once, and 1-2 times per week when severe. The product can be sprayed on the parts with more ectoparasites to prevent animals from licking; animals other than and not only dogs and cats below their age of february are forbidden, and are carefully used for dogs and cats during pregnancy and lactation.
Example 4
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 1.3%, imidacloprid 3.5%, non-prednisone 0.7%, benzyl alcohol 25%, EL-40% 52%, isopropanol 17.35%, BHT 0.05% and purified water 0.
In still another aspect of the present invention, a method for preparing a compound moxidectin preparation is provided, comprising the following steps:
a. mixing benzyl alcohol, an emulsifying agent and a coemulsifier according to a certain proportion, magnetically stirring for 10min at 40 ℃ and rotating at 500r/min to obtain a solution A;
b. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in the solution A, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution B;
the using method comprises the following steps: based on the product, the external use is as follows: the dosage is 0.1mL/kg once, and the administration is once a month. The product can be dropped on the skin between the two scapula of the back of the animal to the buttock to prevent the animal from licking; animals other than and not only dogs and cats below their age of february are forbidden, and are carefully used for dogs and cats during pregnancy and lactation.
Comparative example 1
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 0.4%, imidacloprid 0.8%, non-prednisone 0.3%, benzyl alcohol 23.45%, tween-80 25%,1, 2-propanediol 25%, BHT 0.05% and purified water 25%.
In still another aspect of the present invention, a method for preparing a compound moxidectin preparation is provided, comprising the following steps:
a. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in benzyl alcohol, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
b. mixing an emulsifier and a coemulsifier according to a certain proportion, magnetically stirring for 10min at a rotating speed of 500r/min to obtain a solution B;
c. mixing the solution A with the solution B, and filling to obtain a solution C;
d. purified water was added to solution C and shaken to give solution D.
Comparative example 2
The invention provides a moxidectin compound preparation, which comprises the following raw materials in percentage by mass (g): moxidectin 0.7%, imidacloprid 1.8%, non-prednisone 0.3%, benzyl alcohol 10%, EL-40.65%, isopropanol 8%, BHT 0.05%
And (3) 62.5% of purified water.
In still another aspect of the present invention, a method for preparing a compound moxidectin preparation is provided, comprising the following steps:
a. sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in benzyl alcohol, magnetically stirring at a rotating speed of 500r/min until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
b. mixing an emulsifier and a coemulsifier according to a certain proportion, magnetically stirring for 10min at a rotating speed of 500r/min to obtain a solution B;
c. mixing the solution A and the solution B, adding purified water, changing the solution from turbidity to clarification, and filling to finish.
Specific components and contents of the moxidectin compound preparation in the above examples 1 to 4 and comparative examples 1 to 2 are shown in table 1.
Table 1 specific ingredients and contents of moxidectin compound formulation
The moxidectin compound preparation prepared in examples 1 to 4 and comparative examples 1 and 2 is used for carrying out stability test, and the preparation with better stability is initially screened out for carrying out skin local irritation test, in-vitro skin permeability test and in-vitro insect repellent effect test of dogs and cats.
Test example 1
Stability test:
the samples of examples 1 to 4 and the samples of comparative examples 1 and 2 were centrifuged at 3000r/min for 5min, and the liquid layer and the sedimentation were observed, and the results are shown in Table 2.
Table 2 sample centrifugation results
Samples of examples 1 to 4 and samples of comparative examples 1 and 2 were stored at 25℃and 60℃respectively, taken out at 0d, 5d and 10d, left standing at room temperature for 3 hours, and then observed for turbidity, delamination and precipitation, and the results are shown in Table 3.
TABLE 3 results of sample standing
As can be seen from the results in tables 2-3, the moxidectin compound preparations prepared in examples 1-4 are relatively stable, and a small amount of imidacloprid is easy to separate out after long-term setting in example 3, so that the moxidectin compound preparation is suitable for being prepared at present; in the compound preparation of moxidectin in comparative example 1, microemulsion cannot be formed due to improper proportion of oil phase, water phase, emulsifier and co-emulsifier; the moxidectin compound preparation in comparative example 2 can form microemulsion, but the high-proportion imidacloprid and the aqueous phase solvent have poor compatibility and separate out a large amount of crystals, so the compound preparation is eliminated.
Test example 2
Skin irritation experiments:
skin irritation tests were performed on the samples of examples 1 to 4 with reference to the pharmaceutical non-clinical study quality control Specification and the guidelines for the study of chemical drug irritation, allergy and hemolysis.
And selecting guinea pigs with the weight of more than or equal to 200g, wherein the number of animals in each group is 4, and the female animals and the male animals are half. Physiological saline is used for comparison, and a self-comparison method of the left side and the right side of the homozygote is adopted. Dehairing was performed on both sides of the back 24 hours prior to the test. The dehairing range is 3cm multiplied by 3cm on the left and right. Damaged skin is eliminated.
0.5mL of the test object is directly coated on the skin with one side dehaired, then covered by two layers of gauze (2.5 cm multiplied by 2.5 cm) and a layer of preservative film, and then fixed by gauze and bandage; the other side was coated with 0.5mL of physiological saline as a control. The application time is 1h. After the application, the test substance was removed and the administration site was cleaned with warm water. The skin reaction was observed under natural light. The skin erythema and edema were scored according to the scoring criteria given in tables 4 to 5, and the results are shown in table 6 and fig. 2, and fig. 2 is a graph showing the comparison of skin irritation after the moxidectin compound preparation and physiological saline for 4 hours in example 1 were applied to guinea pigs, wherein the left graph is the moxidectin compound preparation, and the right graph is the physiological saline.
TABLE 4 skin irritation response scoring criteria
TABLE 5 skin irritation intensity evaluation criteria
Evaluation Score value
No irritation 0-0.49
Mild irritation 0.5-2.99
Moderate irritation 3.0-5.99
Strong irritation 6.0-8.0
TABLE 6 skin irritation response scoring results
As can be seen from the results of Table 6 and FIG. 2, the moxidectin compound formulations prepared in examples 1 to 4 were not irritating to the skin of guinea pigs.
Test example 3
In vitro skin penetration test:
collecting Kunming mice, killing the mice by neck breakage, peeling the skin of chest and abdomen, cleaning the hair and subcutaneous tissue by a shaver and a surgical blade, and eliminating skin damage. Then normal temperature normal saline is cleaned, and the mixture is placed in normal saline for preservation at 4 ℃ and used up within 4 days. The skin should be warmed to room temperature before use.
Examples 1-3 were selected for testing, and a comparative recipe having a moxidec Ding Zhiliang fraction identical to that of examples 1-3, respectively, was additionally prepared as comparative examples 3-5, as shown in Table 7.
Table 7 moxidectin Compound formulation of comparative examples 3-5
The test was performed using a transdermal diffusion device. The skin is pre-immobilized, the skin contacts the receiving pool subcutaneously, and the epidermis contacts the supply pool. The instrument is rotated and adjusted to 200r/min, the temperature is 37+/-0.2 ℃, 1mL of each of 6 prescriptions is respectively taken in a supply tank, and the upper end of the administration is sealed by a preservative film. After starting the apparatus, 4mL of the receiving pool liquid was withdrawn every 1, 3, 6, 9, 12, 16, 21, 28h, and 4mL of the receiving liquid (30% ethanol-physiological saline solution) was supplemented. After the extracted receiving solution was filtered with a 0.2nm filter, the moxidectin concentration was measured by HPLC, and the results are shown in Table 8 and FIGS. 3 to 5.
TABLE 8 cumulative osmotic amount of moxidectin
As can be seen from the data in table 8 and fig. 3-5, the self-microemulsions of examples 1-3 had a cumulative moxidectin permeation greater than the corresponding comparative example group over 28 hours at the same mass fraction moxidectin content, and the permeation rate was relatively gentle.
Test example 4
In vitro insect repellent test for dogs and cats
The anti-lice and flea effects of the moxidectin formulated self-microemulsions prepared in accordance with the present invention are described below in connection with specific experiments.
Condition of selection: adult breeds are not limited, the weight of dogs is more than or equal to 5kg, the weight of cats is more than or equal to 2.5kg, and the number of on-body lice and fleas is not less than 5.
The experimental method comprises the following steps: the 40 sick dogs were randomly divided into 4 groups, and moxidectin compound preparations in examples 1 to 4 were used, respectively; the 40 diseased cats were randomly divided into 4 groups and moxidectin compound preparations of examples 1 to 4 were used, respectively.
The experimental method comprises the following steps: the teeth comb is used to comb along the longest muscles of the back and waist (i.e. two sides of the spine), the head and abdomen, and count the total number of lice and fleas. Lice and flea counts were observed at 0d (pre-dose), 1d, 3d, 7d and 28d, and the results are shown in Table 9.
Evaluation of results: and (3) curing: the clinical symptoms disappear, and the insect reduction rate is more than or equal to 90%; the effective rate is more than or equal to 90 percent, and the insect reduction rate is more than or equal to 60 percent; the pest-reducing rate is less than 60 percent.
Usage and dosage: according to the above description.
The formula:
TABLE 9 results of insect reduction rates in dogs and cats following drug administration
The relevant clinical symptoms of the experimental animals are observed and recorded daily, and the data in the table 9 show that 1d after the administration, the insect-reducing effect of the example 3 is most obvious; 3d after the medicine is taken, the symptoms of the parasitic infection are greatly improved, and most of the effects of clinical cure can be achieved; the number of 7d parasites was essentially zero.
It is to be understood that the invention is not limited in its application to the examples described above, but is capable of modification and variation in light of the above teachings by those skilled in the art, and that all such modifications and variations are intended to be included within the scope of the appended claims.

Claims (10)

1. The moxidectin compound preparation is characterized by comprising the following components in percentage by mass: 0.4% -2.5% moxidectin, 0.4% -3.5% imidacloprid, 0.3% -1% non-prednisone, 10% -40% oil phase solvent, 20% -60% emulsifying agent, 10% -30% co-emulsifying agent and 0.05% -0.2% antioxidant.
2. The moxidectin compound preparation according to claim 1, characterized in that the moxidectin compound preparation comprises, in mass percent: 0.4% -1.4% moxidectin, 0.8% -3.5% imidacloprid, 0.3% -0.7% non-prednisone, 10% -28% oil phase solvent, 18% -52% emulsifying agent, 11% -21% co-emulsifying agent and 0.05% -0.1% antioxidant.
3. The moxidectin compound preparation according to claim 1 or 2, characterized in that the emulsifier is one or two of tween-80 and castor oil polyoxyethylene ether-40.
4. The moxidectin compound preparation according to claim 1 or 2, characterized in that the co-emulsifier is one or two of 1, 2-propanediol and isopropanol.
5. The moxidectin compound preparation according to claim 1 or 2, characterized in that the antioxidant is one or two of dibutyl hydroxy toluene and butyl hydroxy anisole.
6. A process for the preparation of a moxidectin compound formulation as claimed in any one of claims 1 to 5, comprising the steps of:
sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in an oil phase solvent, and magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution A;
mixing an emulsifying agent and a coemulsifier, and magnetically stirring to obtain a solution B;
mixing the solution A and the solution B, and canning to obtain the moxidectin compound preparation.
7. A process for the preparation of a moxidectin compound formulation as claimed in any one of claims 1 to 5, comprising the steps of:
mixing an oil phase solvent, an emulsifier and a co-emulsifier, and magnetically stirring to obtain a solution C;
and sequentially dissolving moxidectin, imidacloprid, non-prednisone and an antioxidant in the solution C, magnetically stirring until the moxidectin, the imidacloprid, the non-prednisone and the antioxidant are completely dissolved to obtain a solution D, and filling to obtain the moxidectin compound preparation.
8. The method for preparing moxidectin complex formulation of claim 7, further comprising the step of adding purified water prior to filling.
9. The application of the moxidectin compound preparation is characterized in that the moxidectin compound preparation in any one of claims 1-5 is used for preparing an insect repellent for animals.
10. The use according to claim 9, wherein the animal is a canine or a feline.
CN202310794009.3A 2023-06-29 2023-06-29 Moxidectin compound preparation and preparation method and application thereof Pending CN116808033A (en)

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