A selamectin topical solution for pets, and a preparation method and application thereof

Abstract

The present application belongs to the technical field of pet insecticide, and discloses a kind of pet external use selamectin drop, preparation method and application thereof.The rosemary volatile oil, selamectin and gardenia fruit extract are combined, which can effectively reduce the use amount of selamectin, avoid the use of penetration enhancer (traditional formula needs to add penetration enhancer, such as dipropylene glycol methyl ether and other components), dissolve the lipid layer of insect exoskeleton or microbial cell membrane, destroy the membrane structure integrity, thereby promote the penetration of other components, the gardenia fruit extract can combine with microbial cell membrane protein, change the membrane permeability, further improve the penetration of other components, improve the utilization rate, and the gardenia fruit extract, bacterial protein and nucleic acid synthesis are inhibited, and selamectin kills parasites by interfering with the conduction of insect nerve signal, the mechanism of action of the three is mutually synergistic, and each other is synergistic, which improves the insecticidal and bacteriostatic effect.

Description

TECHNICAL FIELD

[0001] The present application relates to the technical field of pet insecticide, in particular to a kind of pet external selamectin drop and its preparation method and application. BACKGROUND

[0002] With the increasing concern of pet health problems, external parasites (such as scabies, Demodex, ear mite, and so on) and skin diseases (such as bacterial dermatitis, fungal dermatosis, and so on) of pets become common problems.

[0003] Parasitic diseases have always been an important factor affecting the health of dogs and cats. Parasites can directly infect dogs and cats, causing skin inflammation, weight loss, and damage to the quality of fur. On the other hand, many spiders and insects can act as transmitters of some infectious diseases and parasitic diseases, leading to the occurrence of insect-borne diseases. Therefore, controlling and eliminating internal and external parasites of dogs and cats is of great significance to protect human and dog and cat health. However, most of the existing external drugs have the disadvantages of insignificant treatment effect, long treatment cycle, unsuitability for long-term use, or easy to cause pets to develop drug resistance. SUMMARY

[0004] The present application provides a kind of pet external selamectin drop and its preparation method and application The drop described in the present application has excellent acaricidal and antibacterial effects, and can effectively treat parasitic diseases.

[0005] The present application solves the technical problem by adopting the following technical solution:

[0006] A kind of pet external selamectin drop, comprising the following components by weight percentage: 0.05-0.4% antioxidant, 0.5-1.2% glycyrrhizic acid dipotassium, 1.5-4% rosemary volatile oil, 3-6% selamectin, 3-8.5% gardenia fruit extract, 5-20% 1,2-propanediol, and the balance solvent.

[0007] Rosemary volatile oil: rosemary essential oil can dissolve the lipid layer of insect exoskeleton or microbial cell membrane, destroy the membrane structure integrity. It can cause paralysis of the worm by inhibiting acetylcholinesterase (AChE) activity and interfering with nerve signal transmission. At the same time, rosemary essential oil has excellent antioxidant and anti-inflammatory effects, and can repair skin inflammation caused by parasitic or bacterial infection.

[0008] Selamectin has a broad-spectrum antibacterial effect, and at the same time, selamectin can enhance the activity of glutamate-gated chloride channel (GluCl) of invertebrate neurons, leading to hyperpolarization of nerve and muscle of the worm, causing paralysis and death. Selamectin has excellent killing effect on a variety of parasites such as fleas, ticks, mites, and nematodes.

[0009] Gardenia fruit extract: it can kill bacteria and parasites by destroying bacterial cell membranes and inhibiting the synthesis of bacterial proteins and nucleic acids. Gardenia fruit extract can bind to microbial cell membrane proteins, change membrane permeability, promote the penetration of other components, and improve the utilization rate of other components.

[0010] The present application creatively combines rosemary volatile oil, silafluofen and gardenia fruit extract, which can effectively reduce the use amount of silafluofen, avoid the use of penetration enhancers (traditional formula needs to add penetration enhancers such as dipropylene glycol methyl ether and other components), and promote the penetration of other components. Gardenia fruit extract can bind to microbial cell membrane proteins, change membrane permeability, further improve the penetration of other components, and improve the utilization rate. At the same time, gardenia fruit extract can inhibit the synthesis of bacterial proteins and nucleic acids, and silafluofen can kill parasites by interfering with the conduction of insect nerve signals. The three mechanisms of action are mutually synergistic, mutually reinforcing, reducing the possible drug resistance of single component, and improving the insecticidal and antibacterial effects.

[0011] As a preferred embodiment of the present application, the antioxidant includes at least one of butylated hydroxyanisole and 2,6-di-tert-butyl-p-cresol.

[0012] As a preferred embodiment of the present application, the solvent includes at least one of dimethyl sulfoxide, alpha-pyrrolidone, dimethylformamide and ethanol.

[0013] As a preferred embodiment of the present application, the preparation method of the rosemary volatile oil is as follows: rosemary powder is added to water, steam distillation is carried out to obtain an oil-water mixture, and the water phase is separated to obtain the rosemary volatile oil.

[0014] As a preferred embodiment of the present application, the particle size of the rosemary powder is 50-400 mesh.

[0015] The mass ratio of the rosemary powder to water is 1: (4-10).

[0016] The distillation time is 4-10 h.

[0017] As a preferred embodiment of the present application, the preparation method of the gardenia fruit extract is as follows:

[0018] Gardenia fruit powder, cellulase, beta-glucanase and xylanase are added to water, and enzymolysis is carried out to obtain an enzymolysis solution.

[0019] The enzymolysis solution is first ultrafiltered by an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then ultrafiltered by an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0020] As a preferred embodiment of the present application, the mass ratio of the Gardenia fruit powder, cellulase, beta-glucanase, xylanase, and water is 1: (0.01-0.02): (0.002-0.008): (0.001-0.005): (4-10).

[0021] As a preferred embodiment of the present application, the particle size of the Gardenia fruit powder is 50-400 mesh.

[0022] The enzymolysis temperature is 45-52 DEG C, and the enzymolysis time is 2-6 h.

[0023] The present application also provides a preparation method of the pet external use selamectin drop, comprising the following steps:

[0024] The rosemary volatile oil, 1, 2-propylene glycol, and solvent are uniformly mixed, and then the antioxidant, dipotassium glycyrrhizinate, selamectin, and Gardenia fruit extract are added and uniformly stirred to obtain the pet external use selamectin drop.

[0025] The present application also provides an application of the pet external use selamectin drop in the preparation of a pet external disinfection medicine, characterized in that the external disinfection medicine comprises a pet parasiticide medicine, a pet trematodiasis medicine, or a pet cestodiasis medicine.

[0026] The present application has the following beneficial effects: the rosemary volatile oil, selamectin, and Gardenia fruit extract are combined in the present application, which can effectively reduce the use amount of selamectin, avoid the use of penetration enhancers (traditional formulations need to add penetration enhancers such as dipropylene glycol methyl ether and other components), dissolve the lipid layer of the exoskeleton of insects or the cell membrane of microorganisms, destroy the membrane structure integrity, thereby promoting the penetration of other components, and improve the utilization rate. DETAILED DESCRIPTION

[0027] In order to make the purpose, technical scheme and advantages of the embodiments of the present application more clear, the technical scheme in the embodiments of the present application will be described clearly and completely below. Obviously, the described embodiments are part of the embodiments of the present application, rather than all the embodiments. Based on the embodiments in the present application, all other embodiments obtained by those skilled in the art without creative labor fall within the protection scope of the present application.

[0028] In the present application, the open technical features include the closed technical solution consisting of the listed features, and also include the open technical solution containing the listed features.

[0029] In the present application, the numerical interval is continuous and includes the minimum value and the maximum value of the range, and each value between the minimum value and the maximum value, unless otherwise specified.

[0030] In the present application, the specific dispersion and stirring treatment method is not particularly limited.

[0031] The reagents or instruments used in the present application are not specified by the manufacturer, and are conventional products that can be obtained by purchase.

[0032] Example 1

[0033] A selamectin topical drop for pets comprises the following components by weight percentage: 0.2% butylated hydroxyanisole, 1% dipotassium glycyrrhizinate, 2% rosemary volatile oil, 5% selamectin, 6% gardenia fruit extract, 10% 1,2-propanediol, and the balance dimethyl sulfoxide.

[0034] The preparation method of the rosemary volatile oil is as follows: rosemary is crushed to 200 mesh to obtain rosemary powder, the rosemary powder is added to water, and water vapor distillation is carried out at 100 DEG C for 8h to obtain an oil-water mixture, after standing, the water phase is separated to obtain the rosemary volatile oil. The mass ratio of the rosemary powder to water is 1:8.

[0035] The preparation method of the gardenia fruit extract is as follows:

[0036] The gardenia fruit is crushed to 200 mesh to obtain gardenia fruit powder, the gardenia fruit powder, cellulase, beta-glucanase, and xylanase are added to water, and enzymatic hydrolysis is carried out at 48 DEG C for 5h to obtain an enzymatic hydrolysate; the mass ratio of the gardenia fruit powder to cellulase, beta-glucanase, xylanase, and water is 1:0.02:0.008:0.001:8.

[0037] The enzymatic hydrolysate is first ultrafiltered by an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then ultrafiltered by an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0038] The preparation method of the pet external use sirtinol drop, characterized in that, comprising the following steps: rosemary volatile oil, 1, 2-propylene glycol and dimethyl sulfoxide are uniformly mixed, then butylated hydroxyanisole, potassium glycyrrhizinate, sirtinol and gardenia fruit extract are added and uniformly stirred to obtain the pet external use sirtinol drop.

[0039] Example 2

[0040] A pet external use sirtinol drop, comprising the following components by weight percentage: 0.2% butylated hydroxyanisole, 1% potassium glycyrrhizinate, 1.5% rosemary volatile oil, 3% sirtinol, 8.5% gardenia fruit extract, 10% 1, 2-propylene glycol, and the balance dimethyl sulfoxide.

[0041] The preparation method of the rosemary volatile oil is as follows: rosemary is crushed to 200 meshes to obtain rosemary powder, the rosemary powder is added to water, and water vapor distillation is carried out at 100 DEG C for 8h to obtain an oil-water mixture, after standing, the water phase is separated to obtain the rosemary volatile oil. The mass ratio of the rosemary powder to water is 1:8.

[0042] The preparation method of the gardenia fruit extract is as follows:

[0043] The gardenia fruit is crushed to 200 meshes to obtain gardenia fruit powder, the gardenia fruit powder, cellulase, beta-glucanase and xylanase are added to water, and enzymolysis is carried out at 48 DEG C for 5h to obtain an enzymolysis liquid; the mass ratio of the gardenia fruit powder, cellulase, beta-glucanase, xylanase and water is 1:0.02:0.008:0.001:8.

[0044] The enzymolysis liquid is first subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 500 Da, then subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0045] The preparation method of the pet external use sirtinol drop, characterized in that, comprising the following steps: rosemary volatile oil, 1, 2-propylene glycol and dimethyl sulfoxide are uniformly mixed, then butylated hydroxyanisole, potassium glycyrrhizinate, sirtinol and gardenia fruit extract are added and uniformly stirred to obtain the pet external use sirtinol drop.

[0046] Example 3

[0047] A pet external use sirtinol drop, comprising the following components by weight percentage: 0.2% butylated hydroxyanisole, 1% potassium glycyrrhizinate, 4% rosemary volatile oil, 6% sirtinol, 3% gardenia fruit extract, 10% 1, 2-propylene glycol, and the balance dimethyl sulfoxide.

[0048] The preparation method of the rosemary volatile oil is as follows: rosemary is crushed to 200 meshes to obtain rosemary powder, the rosemary powder is added to water, and water vapor distillation is carried out at 100 DEG C for 8h to obtain an oil-water mixture, after standing, the water phase is separated to obtain the rosemary volatile oil. The mass ratio of the rosemary powder to water is 1:8.

[0049] The preparation method of the gardenia fruit extract is as follows:

[0050] The gardenia fruit is crushed to 200 meshes to obtain gardenia fruit powder, the gardenia fruit powder, cellulase, beta-glucanase and xylanase are added to water, and enzymolysis is carried out at 48 DEG C for 5h to obtain an enzymolysis liquid; the mass ratio of the gardenia fruit powder, cellulase, beta-glucanase, xylanase and water is 1:0.02:0.008:0.001:8.

[0051] The enzymolysis liquid is first subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0052] The preparation method of the pet external use sylvaticus drop is characterized by comprising the following steps: uniformly mixing rosemary volatile oil, 1,2-propylene glycol and dimethyl sulfoxide, then adding butylated hydroxyanisole, potassium glycyrrhizinate, sylvaticus and gardenia fruit extract, and uniformly stirring to obtain the pet external use sylvaticus drop.

[0053] Example 4

[0054] A pet external use sylvaticus drop comprises the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% potassium glycyrrhizinate, 2% rosemary volatile oil, 5% sylvaticus, 6% gardenia fruit extract, 10% 1,2-propylene glycol, and the balance dimethyl sulfoxide.

[0055] The preparation method of the rosemary volatile oil is as follows: rosemary is crushed to 200 meshes to obtain rosemary powder, the rosemary powder is added to water, and water vapor distillation is carried out at 100 DEG C for 8h to obtain an oil-water mixture, after standing, the water phase is separated to obtain the rosemary volatile oil. The mass ratio of the rosemary powder to water is 1:8.

[0056] The preparation method of the gardenia fruit extract is as follows:

[0057] The gardenia fruit is crushed to 200 meshes to obtain gardenia fruit powder, the gardenia fruit powder, cellulase, beta-glucanase and xylanase are added to water, and enzymolysis is carried out at 48 DEG C for 5h to obtain an enzymolysis liquid; the mass ratio of the gardenia fruit powder, cellulase, beta-glucanase, xylanase and water is 1:0.01:0.002:0.005:8.

[0058] The enzymatic hydrolysate is first ultrafiltered by using an ultrafiltration membrane with a molecular weight cut-off of 500 Da, then ultrafiltered by using an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0059] The preparation method of the pet external use silacin drop has the characteristics that it comprises the following steps: uniformly mixing rosemary volatile oil, 1,2-propylene glycol and dimethyl sulfoxide, then adding butylated hydroxyanisole, dipotassium glycyrrhizinate, silacin, gardenia fruit extract, and uniformly stirring to obtain the pet external use silacin drop.

[0060] Comparative Example 1

[0061] Comparative Example 1 is different from Example 1 in that Comparative Example 1 does not contain rosemary volatile oil, and the others are the same.

[0062] A pet external use silacin drop comprises the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% dipotassium glycyrrhizinate, 5% silacin, 6% gardenia fruit extract, 10% 1,2-propylene glycol, and the balance dimethyl sulfoxide.

[0063] Comparative Example 2

[0064] Comparative Example 2 is different from Example 1 in that Comparative Example 2 does not contain silacin, and the others are the same.

[0065] A pet external use drop comprises the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% dipotassium glycyrrhizinate, 2% rosemary volatile oil, 6% gardenia fruit extract, 10% 1,2-propylene glycol, and the balance dimethyl sulfoxide.

[0066] Comparative Example 3

[0067] Comparative Example 3 is different from Example 1 in that Comparative Example 3 does not contain gardenia fruit extract, and the others are the same.

[0068] A pet external use silacin drop comprises the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% dipotassium glycyrrhizinate, 2% rosemary volatile oil, 5% silacin, 10% 1,2-propylene glycol, and the balance dimethyl sulfoxide.

[0069] Comparative Example 4

[0070] Comparative Example 4 is different from Example 1 in that Comparative Example 4 does not contain rosemary volatile oil (the total amount of rosemary volatile oil, silacin and gardenia fruit extract is the same), and the others are the same.

[0071] A pet external use silaquinone drop includes the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% glycyrrhizic acid dipotassium, 2% rosemary volatile oil, 5% silaquinone, 6% gardenia fruit extract, 10% 1,2-propanediol, and the balance dimethyl sulfoxide.

[0072] Comparative Example 5

[0073] Comparative Example 5 is different from Example 1 in that Comparative Example 5 does not contain silaquinone (the total amount of rosemary volatile oil, silaquinone, and gardenia fruit extract is the same), and the others are the same.

[0074] A pet external use drop includes the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% glycyrrhizic acid dipotassium, 4.5% rosemary volatile oil, 8.5% gardenia fruit extract, 10% 1,2-propanediol, and the balance dimethyl sulfoxide.

[0075] Comparative Example 6

[0076] Comparative Example 6 is different from Example 1 in that Comparative Example 6 does not contain gardenia fruit extract (the total amount of rosemary volatile oil, silaquinone, and gardenia fruit extract is the same), and the others are the same.

[0077] A pet external use silaquinone drop includes the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% glycyrrhizic acid dipotassium, 5% rosemary volatile oil, 8% silaquinone, 10% 1,2-propanediol, and the balance dimethyl sulfoxide.

[0078] Comparative Example 7

[0079] Comparative Example 7 is different from Example 1 in that Comparative Example 7 uses an equal amount of eucalyptus volatile oil to replace rosemary volatile oil, and the others are the same.

[0080] A pet external use silaquinone drop includes the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% glycyrrhizic acid dipotassium, 2% eucalyptus volatile oil, 5% silaquinone, 6% gardenia fruit extract, 10% 1,2-propanediol, and the balance dimethyl sulfoxide.

[0081] The preparation method of the eucalyptus volatile oil is: the eucalyptus is crushed to 200 mesh to obtain eucalyptus powder, the eucalyptus powder is added to water, and water vapor distillation is carried out at 100℃ for 8h to obtain an oil-water mixture, after standing, the water phase is separated to obtain eucalyptus volatile oil. The mass ratio of the eucalyptus powder to water is 1:8.

[0082] Comparative Example 8

[0083] A pet external use silatrane drop agent, comprising the following components in percentage by weight: 0.2% butylated hydroxyanisole, 1% glycyrrhizic acid dipotassium, 2% rosemary volatile oil, 5% silatrane, 6% sophora flavescens extract, 10% 1,2-propylene glycol, and the balance dimethyl sulfoxide.

[0084] The preparation method of the sophora flavescens extract is as follows:

[0085] The sophora flavescens is crushed to 200 mesh to obtain gardenia fruit powder, and the gardenia fruit powder, cellulase, beta-glucanase and xylanase are added into water for enzymolysis at 48 DEG C for 5h to obtain an enzymolysis solution; the mass ratio of the sophora flavescens powder, cellulase, beta-glucanase, xylanase and water is 1:0.01:0.002:0.005:8.

[0086] The enzymolysis solution is first subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the sophora flavescens extract.

[0087] Comparative Example 9

[0088] Comparative Example 9 is different from Example 1 in that the preparation method of the gardenia fruit extract of Comparative Example 9 is different from that of Example 1, and other aspects are the same.

[0089] The preparation method of the gardenia fruit extract is as follows:

[0090] The gardenia fruit is crushed to 200 mesh to obtain gardenia fruit powder, and the gardenia fruit powder, pectinase, trypsin and flavor protease are added into water for enzymolysis at 48 DEG C for 5h to obtain an enzymolysis solution; the mass ratio of the gardenia fruit powder, pectinase, trypsin, flavor protease and water is 1:0.01:0.002:0.005:8.

[0091] The enzymolysis solution is first subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

[0092] Test Example

[0093] 1. The mite killing rate is detected according to NY / T1151.2-2006.

[0094] 2. The test is carried out according to GB 15979-2002 "Hygienic Standard for Disposable Hygienic Products" Appendix C, and the test strain is Escherichia coli 8099.

[0095] Table 1

[0096]

[0097] As can be seen from Table 1, the drop agent has excellent mite killing and bacteriostatic effects, and can effectively treat parasitic diseases.

[0098] As can be seen from Comparative Example 1 and Comparative Examples 1-6, the rosemary volatile oil, silafluofen and gardenia fruit extract described in the present application have a significant synergistic effect in inhibiting bacteria and removing mites, and under the synergistic effect of the three, the mite removal effect is significantly improved. If any of the three is missing or any of the three is replaced by other ingredients, the mite removal and bacteria inhibition effect will be significantly reduced, and the treatment of parasites will be significantly reduced.

[0099] Finally, it should be noted that the above examples are used to illustrate the technical solutions of the present application, but not to limit the protection scope of the present application. Although the present application has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solutions of the present application can be modified or replaced by equivalents without departing from the essence and scope of the technical solutions of the present application.

Claims

1. A sirtuin topical drop for pets, characterized by, Comprise the following weight percentage of components: 0.2~0.4% antioxidant, 0.5~1.2% glycyrrhizic acid dipotassium, 1.5~4% rosemary volatile oil, 3~6% selamectin, 3~8.5% gardenia fruit extract, 5~20% 1,2-propanediol, the rest solvent; The antioxidant is butylated hydroxyanisole; The solvent is dimethyl sulfoxide; The preparation method of the gardenia fruit extract is: The gardenia fruit powder, cellulase, beta-glucanase and xylanase are added into water, and enzymolysis is carried out to obtain an enzymolysis liquid; The enzymolysis liquid is first subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 500 Da, and then subjected to ultrafiltration with an ultrafiltration membrane with a molecular weight cut-off of 5000 Da, and dried to obtain the gardenia fruit extract.

2. The sirtuins drop for external use of a pet according to claim 1, characterized by, The preparation method of the rosemary volatile oil is: the rosemary powder is added into water, and subjected to steam distillation to obtain an oil-water mixture, and the water phase is separated to obtain the rosemary volatile oil.

3. The topical sirtuin- containing drop for pets according to claim 2, wherein The particle size of the rosemary powder is 50~400 mesh; The mass ratio of the rosemary powder to water is 1: (4~10); The distillation time is 4~10 h.

4. The sirtuins drop for external use of a pet according to claim 1, characterized by, The mass ratio of the gardenia fruit powder, cellulase, beta-glucanase, xylanase and water is 1: (0.01~0.02): (0.002~0.008): (0.001~0.005): (4~10).

5. The sirtuins drop for external use of a pet according to claim 1, characterized by, The particle size of the gardenia fruit powder is 50~400 mesh; The enzymolysis temperature is 45~52℃, and the enzymolysis time is 2~6 h.

6. The method of producing the pet external use sirtuins drop of any one of claims 1 to 5, characterized by, Comprise the following steps: The rosemary volatile oil and 1,2-propanediol are mixed with a solvent, and then the antioxidant, glycyrrhizic acid dipotassium, selamectin and gardenia fruit extract are added and stirred uniformly to obtain the selamectin drop for pets.

7. The selamectin drop for pets of any one of claims 1~5 in the preparation of a pet external mite-killing and bacteriostatic medicine.

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