CN106511267A - Compound moxidectin drops as well as preparation method and application thereof - Google Patents

Compound moxidectin drops as well as preparation method and application thereof Download PDF

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Publication number
CN106511267A
CN106511267A CN201710041410.4A CN201710041410A CN106511267A CN 106511267 A CN106511267 A CN 106511267A CN 201710041410 A CN201710041410 A CN 201710041410A CN 106511267 A CN106511267 A CN 106511267A
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moxidectin
drop
compound recipe
drops
preparation
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Inventor
元晓琪
寇贺红
吴桂英
蒲静君
李汶潓
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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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention provides compound moxidectin drops as well as a preparation method and application thereof. The compound moxidectin drops have the advantages that moxidectin and ingredients with insecticidal effect, such as imidacloprid, are compounded and used, so that the drops have good insecticidal effect; meanwhile, in the drops, propylene glycol, moringa seed oil and eucalyptus oil are taken as transdermal agents, wherein the moringa seed oil and the eucalyptus oil are natural plant essential oil with fragrance and can cover up peculiar smell in the drops and improve sense of a user; and further the drops can be used for killing endoparasite and ectoparasite of animals due to good insecticidal effect. In the preparation method, the components of the drops are taken as raw materials and mixed to prepare corresponding drops, so that the preparation method provided by the invention has the advantages of simplicity, high efficiency, good insecticidal effect of the obtained drops, and the like.

Description

Compound recipe Moxidectin drop and its preparation method and application
Technical field
The present invention relates to field of pesticides, in particular to compound recipe Moxidectin drop and its preparation method and application.
Background technology
With Chinese society expanding economy and the acceleration of urbanization process, the independence of urbanite family, closure, Personalized and senescence problem becomes increasingly conspicuous, and the leisure of resident, consumption and emotion sustenance mode are also in diversified development, and raising is doted on Thing is surging forward in China city.
In recent years, the pet industry growth momentum of China is swift and violent.According to conservative estimation, the number of animals raised of domestic only pet dog is just Jing has exceeded 10,000,000, and the raising petss quantity in the city such as Beijing, Shanghai has also reached the rank of million.
Flourishing along with pet industry, pet health situation but allows of no optimist, flea, cattle Tickss, acarid, skin The infecting both domestic animals and human parasite and zoonosiss that disease, the plague, Lyme disease etc. are brought by house pet and cat is also more and more.Due to people and House pet gets close in life very much, and these disease pests are easy to secondary propagation is carried out in kinsfolk by house pet.
External medicament parasite killing is carried out to house pet, is to solve this problem mode the most quick and easy, it is each in prior art The research of class medicament bathing, medicine liquid spray or drop was also never interrupted.
But, although people achieve suitable progress in the research of outer insecticide in animal body, but, on the one hand, Due to the drug-fast generation of parasite, the application effect of existing insecticide weakens year by year, it has to which the annual insecticide that increases is used Amount, this not only causes the raising of cost, also result in the pollution and the threat increasing to health of environment;It is another Aspect, existing parasite killing strange smell are larger, after administration either for animal, especially for doting on mankind's Long Term Contact daily For thing, or user, there is more serious stimulus to the sense organ.
In view of this, it is special to propose the present invention.
The content of the invention
The first object of the present invention is to provide a kind of compound recipe Moxidectin drop, by will not former times gram in described drop Fourth, and the composition compounding use with insecticidal effect such as imidacloprid, so that drop of the present invention has good parasite killing effect Really;Meanwhile, the present invention in, with Propylene Glycol, seed oil of Moringa oleigera, eucalyptus oil as transdermal agent, wherein seed oil of Moringa oleigera and eucalyptus oil be with Fragranced natural plant essential oils, can cover the abnormal flavour in drop, improve the sense organ of user.
Moxidectin:Moxidectin is a kind of Macrolide anthelmintic antibiotic, with characteristics such as wide spectrum, efficient, low toxicities, Meanwhile, Moxidectin to no skin irritation, to the safe of animal.
Seed oil of Moringa oleigera:Moringa (MoringaoleiferaLam), also known as drumstick tree, is Moringaceae (Moringaceae) Moringa Belong to tropical perennial deciduous tree, because its tree root has acid, so Moringa of gaining the name.Moringa quintessence oil is carried from Moringa dry powder A kind of volatile oil for taking out, containing abundant unsaturated fatty acid, therefore which has good transdermal effect.Additionally, according to the study Data shows that there is seed oil of Moringa oleigera antibacterial, antiinflammatory, antifungal etc. to act on, and have therapeutical effect to people's tinea corporis, mycosises.Example Such as, prior art:A kind of insecticide (application number:201310107896.9) disclose leaf of Moringa liquid and azone are mixed with The technical scheme of insecticide.
Eucalyptus oil:Eucalyptus oil, also known as cajuputole, eucalyptole, is a kind of colourless oil liquid, Eucalyptus oil, cajuput oil, Extract in the materials such as Oleum Camphora, laurel, be widely used in medicine.Eucalyptus oil is fat-soluble strong, in recent years as saturating The research of leather agent is more and more.Which also has certain mould proof and sterilization and anticorrosion effect simultaneously, and Jing is saturating frequently as parasiticide The ancillary drug of skin medicine.For example, prior art:A kind of compound percutaneous solution of the Chinese medicine and western medicine and preparation method thereof (patent No.: CN201210554917.7) disclose the skill that doractin, eucalyptus oil, azone prepare the compound percutaneous solution for curing house pet tinea Art scheme.
The discovery of Jing inventor Jing numerous studies, seed oil of Moringa oleigera and eucalyptus oil, Moxidectin fit applications, are remarkably improved not The parasiticide effect of former times gram fourth;Meanwhile, study through penetrating absorption, find the addition of Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil It is remarkably improved the transdermal effect of Moxidectin.
The second object of the present invention is the preparation method of the compound recipe Moxidectin drop for providing described, in the method, is led to Cross and instant component as raw material and is mixed to prepare corresponding drop, with preparation method is simple, efficiency high and obtained Drop good disinsection effect the advantages of.
Third object of the present invention is to provide the application of the compound recipe Moxidectin drop, and drop of the present invention has good Good insecticidal effect, it is thus possible to for the killing of animal endoparasite and ectoparasite.
In order to realize the above-mentioned purpose of the present invention, spy employs the following technical solutions:
A kind of compound recipe Moxidectin drop, according to percent by weight, the compound recipe Moxidectin drop is mainly by following Component is made:
Moxidectin 0.5~5%;
Imidacloprid 5~12%;
Propylene Glycol 1~5%;
Seed oil of Moringa oleigera 1~4%;
Antioxidant 0.1~0.5%;
Eucalyptus oil 0.5~2%;
Solvent 75~95%;
Optionally, in the present invention, the compound recipe Moxidectin drop still further comprises Permethrin.
Optionally, in the present invention, according to percent by weight, compound recipe Moxidectin of the present invention is by following components system Into:
Moxidectin 0.5~5%;
Imidacloprid 5~12%;
Permethrin 3~8%
Propylene Glycol 1~5%;
Seed oil of Moringa oleigera 1~4%;
Antioxidant 0.1~0.5%;
Eucalyptus oil 0.5~2%;
Solvent 75~90%.
Optionally, in the present invention, the antioxidant is BHA and/or BHT.
Optionally, in the present invention, the solvent is alpha-pyrrolidone;And/or dimethyl sulfoxide;And/or dimethyl formyl Amine;And/or dimethyl acetylamide;And/or ethanol.
Meanwhile, present invention also offers the preparation method of the compound recipe Moxidectin drop, the compound recipe Moxidectin drop Agent is mixed with by heretofore described component and is obtained.
Optionally, the method for the invention comprises the steps:
1) imidacloprid is dissolved with most of solvent;
2) Moxidectin is added into step 1) in resulting solution, and continue stirring mixing;
3) to step) Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil are added in resulting solution, and continue stirring mixing;
4) by BHA and/or BHT with residual solvent dissolving after, by resulting solution and step 3) resulting solution mixes, and obtains final product institute State compound recipe Moxidectin drop.
Optionally, the present invention in, step 2) in may further include step 2) add Moxidectin while, be additionally added Permethrin, and it is stirred together for the step of mixing.
Optionally, the present invention in, step 3) described in continue stirring mixing time be 20~30min.
Optionally, in the present invention, step 4) in may further include solution is mixed after, gained mixed solution is entered into one The step of step is filtered.
Further, present invention also offers application of the compound recipe Moxidectin drop in animal anthelmintic.
Optionally, in the present invention, the animal is poultry or livestock or house pet.
Compared with prior art, beneficial effects of the present invention are:
(1) in the present invention, by the active ingredient compounding use such as Moxidectin, imidacloprid, so that of the invention Drop has good insecticidal effect, while will not also develop immunity to drugs;
(2), in the present invention, transdermal agent contains crude vegetal seed oil of Moringa oleigera, eucalyptus oil, can be effectively improved drop of the present invention The use sense organ of agent;Meanwhile, in the present invention, eucalyptus oil is used cooperatively with seed oil of Moringa oleigera, it is also possible to effectively improve medicine of the present invention The osmotic effect of effect composition, while the killing effect to insects such as parasites can also be effectively improved.
Specific embodiment
Embodiment of the present invention is described in detail below in conjunction with embodiment, but those skilled in the art will Understand, the following example is merely to illustrate the present invention, and is not construed as limiting the scope of the present invention.It is unreceipted concrete in embodiment Condition person, the condition advised according to normal condition or manufacturer are carried out.Agents useful for same or the unreceipted production firm person of instrument, are The conventional products that commercially available purchase is obtained can be passed through.
Compound recipe Moxidectin drop of the present invention, is in the animal body with Moxidectin and imidacloprid etc. as active ingredient Outer parasite killing drop, according to percent by weight, the drop is mainly made up of following components:Moxidectin 0.5~5%, for example Can be, but be not limited to 1,1.5,2,2.5,3,3.5 or 4% etc.;Imidacloprid 5~12%, can for example be, but be not limited to 6, 8th, 10 or 11% etc.;Propylene Glycol 1~5%, for example, can be, but be not limited to 2,3 or 4% etc.;Seed oil of Moringa oleigera 1~4%, example Can such as be, but be not limited to 2,3 or 4% etc.;Eucalyptus oil 0.5~2%, for example, can be, but be not limited to 1,1.5 or 2% Deng;Antioxidant 0.1~0.5%, for example, can be, but be not limited to 0.2,0.3 or 0.4% etc.;Solvent 75~95%, for example Can be, but be not limited to 78,80,83,85,90 or 92% etc.;
Wherein, in the Moxidectin drop component, antioxidant is BHA and/or BHT;Wherein BHT is 2,6-, bis- uncles Butyl -4- methylphenols, BHA is Butylated hydroxyanisole;
Wherein, the solvent is alpha-pyrrolidone;And/or dimethyl sulfoxide;And/or dimethylformamide;And/or two Methylacetamide;And/or ethanol.
Further, drop of the present invention can also including Permethrin etc. other active ingredient, it is this including Permethrin Compound recipe Moxidectin drop, according to raw material weight percent meter, be by made by following components:Moxidectin 0.5~5%, Can for example be, but be not limited to 1,1.5,2,2.5,3,3.5 or 4% etc.;Imidacloprid 5~12%, for example, can be, but not limit In 6,8,10 or 11% etc.;Permethrin 3~8%, for example, can be, but be not limited to 4,4.5,5,6 or 8% etc.;Propylene Glycol 1 ~5%, can for example be, but be not limited to 2,3 or 4% etc.;Seed oil of Moringa oleigera 1~4%, for example, can be, but be not limited to 2,2.5 Or 3% etc.;Antioxidant 0.1~0.5%, for example, can be, but be not limited to 0.2,0.3 or 0.4% etc.;Eucalyptus oil 0.5 ~2%, can for example be, but be not limited to 1,1.5 or 2% etc.;Solvent 75~90%, can for example be, but be not limited to 82, 85th, 87 or 89% etc.;
Likewise, in the Moxidectin drop component, antioxidant is BHA and/or BHT,;Wherein BHT is 2,6- bis- Tert-butyl-4-methyl-Phenol, BHA are Butylated hydroxyanisole;
Wherein, the solvent is alpha-pyrrolidone;And/or dimethyl sulfoxide;And/or dimethylformamide;And/or two Methylacetamide;And/or ethanol.
The preparation method of compound recipe Moxidectin drop of the present invention is more simple, is that the mixing of each component raw material i.e. can Drop of the present invention is obtained, specifically:
It is divided into what two parts were used as the solvent that solvent is used in the present invention, wherein most is in step 1) middle use In by imidacloprid, by stirring and dissolving, remaining is partially in step 4) in for dissolving BHA and/or BHT;
And in step 2) in, as the main raw material components of drop of the present invention have two kinds, thus in the preparation of this step Also difference in method, specifically, if not including Permethrin in raw material components, in this step, it is only necessary to by Moxidectin Add step 1) in resulting solution, and further stirring mixing;If in raw material components include Permethrin, by Moxidectin with And Permethrin adds step 1 jointly) in resulting solution, and further stirring mixing;
Step 3) in, it is the Propylene Glycol as transdermal agent, seed oil of Moringa oleigera and eucalyptus oil to be added in mixed solution, and after Continuous stirring mixing, the time for stirring mixing are preferably 20min;
Step 4) be then by BHA and/or BTH with the dissolving of the solvent of remainder after, in the mixed solution before addition, and It is again stirring for mixing;After mixing terminates, gained mixed liquor Jing filter paper or filter-cloth filtering can also be finally given the drop Agent;
The drop is further Jing after sampling observation is qualified, can carry out subpackage or canned, be sold and used.
Further, preparation method of the present invention can specifically be summarized as following steps:
1) imidacloprid is dissolved with most of solvent;
2) by Moxidectin, or Moxidectin and Permethrin, add step 1) in resulting solution, and it is mixed to continue stirring Close;
3) to step 2) add Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil in resulting solution, and continue stirring mixing 20~ 30min;
4) by BHA and/or BHT with residual solvent dissolving after, by resulting solution and step 3) resulting solution mixes, and by institute Obtain mixed solution and pass through filter paper or filter-cloth filtering, obtain final product the compound recipe Moxidectin drop.
Drop of the present invention can be used for the inside and outside parasite killing of the animals such as poultry, domestic animal.Preferably, drop of the present invention Suitable for the inside and outside parasite killing of domestic pets, for example, can be used for the inside and outside parasite killing of cat, Canis familiaris L. etc..It is further preferred that with not Former times gram fourth 2.5%, inside and outside parasite killing of the drop obtained by 10% proportioning of imidacloprid more suitable for pet dog;With Moxidectin 1%, inside and outside parasite killing of the drop obtained by 10% proportioning of imidacloprid more suitable for pet cat.
In specifically used method, drop can be dripped at parasite parasitism, or after can also dissolve drop, be adopted Large-area inside and outside parasite killing is carried out with the mode of dipping.
Embodiment 1
According to percetage by weight:2.5% Moxidectin, 10% imidacloprid, 2% Propylene Glycol, 2% seed oil of Moringa oleigera, 0.1% BHT, 1% eucalyptus oil, and the alpha-pyrrolidone of surplus, weigh appropriate each raw material respectively;
Then, it is prepared as follows Moxidectin drop:
1) imidacloprid is dissolved with most of alpha-pyrrolidone;
2) Moxidectin is added into step 1) in resulting solution, and continue stirring mixing;
3) to step 2) add Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil in resulting solution, and continue stirring mixing 20~ 30min;
4) by BHT with the dissolving of remaining alpha-pyrrolidone after, by resulting solution and step 3) resulting solution mixes, and by institute Obtain mixed solution and pass through filter paper or filter-cloth filtering, obtain final product the compound recipe Moxidectin drop of embodiment 1.
Embodiment 2
According to percetage by weight:1% Moxidectin, 10% imidacloprid, 2% Propylene Glycol, 2% seed oil of Moringa oleigera, 0.1%BHT, 1% eucalyptus oil, and the alpha-pyrrolidone of surplus, weigh appropriate each raw material respectively;
Then, the compound recipe Moxidectin drop of embodiment 2 is prepared according to 1 methods described of embodiment.
Embodiment 3
According to percetage by weight:2.5% Moxidectin, 10% imidacloprid, 5% Permethrin, 2% Propylene Glycol, 2% moringa seeds Oil, 0.1%BHT, 1% eucalyptus oil, and the alpha-pyrrolidone of surplus, weigh appropriate each raw material respectively;
Then, it is prepared as follows Moxidectin drop:
1) imidacloprid is dissolved with most of alpha-pyrrolidone;
2) Moxidectin and Permethrin are added into step 1) in resulting solution, and continue stirring mixing;
3) to step 2) add Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil in resulting solution, and continue stirring mixing 20~ 30min;
4) by BHT with the dissolving of remaining alpha-pyrrolidone after, by resulting solution and step 3) resulting solution mixes, and by institute Obtain mixed solution and pass through filter paper or filter-cloth filtering, obtain final product the compound recipe Moxidectin drop of embodiment 3.
Embodiment 4
According to percetage by weight:1% Moxidectin, 10% imidacloprid, 5% Permethrin, 2% Propylene Glycol, 2% moringa seeds Oil, 0.1%BHT, 1% eucalyptus oil, and the alpha-pyrrolidone of surplus, weigh appropriate each raw material respectively;
Then, the compound recipe Moxidectin drop of embodiment 4 is prepared according to 3 methods described of embodiment.
1 ill dog therapeutic effect of experimental example
House pet field selects the suitable ill dog 30 of medical history, the state of an illness (being only dog of the Jing Disease Diagnosis of Veterinary with dog acaricide), 3 groups are randomly divided into, respectively test group 1, test group 2 and matched group, 10 per group.Test group 1 gives the embodiment of the present invention 1, 1ml is given by every 5kg body weight, is dripped between dog dorsal scapular bone, medication 1 time, observe Cure;Test group 2 gives this Bright embodiment 3, gives 1ml by every 5kg body weight, drips between dog dorsal scapular bone, medication 1 time, observes Cure;Matched group Dog not medication, the sick heat condition of observation.
As a result show, after test group 1,2 sick dog medication of test group, symptom is clearly better within the 2nd day, or worm is reduced, and is suffered from dog and is grabbed Number of times of itching is significantly reduced, and depilation stops, and skin color is switched to pink, inflammatory symptom mitigation by flushing, and frass reduces the 4th day within 3 days Dermatitis disappears substantially, starts to grow virgin wool, and without the phenomenon that scratches, after the 7th day, skin color switchs to normally, without breakage, and matched group Suffer from the daily symptom of dog symptom to be not improved, develop in state is increased.
Meanwhile, over the course for the treatment of with treatment after, experimental dog drinking water diet is normal, any abnormal conditions does not occur; During medication, find drop of the present invention has no pesticide abnormal flavour, and sense organ is good.
2 drop insecticidal effect of the present invention of experimental example
In certain pet market, the pet cat at 500 12~24 healthy monthly ages is randomly selected, 5 groups is randomly divided into, per group 100;
Trial drug:The embodiment of the present invention 2 and embodiment 4;
Positive control medicine 1:Medicine of the embodiment 2 without the preparation capable of permeating skin containing natural plant essential oils, i.e.,:1% not former times Gram fourth, 10% imidacloprid, 0.1%BHT, and the alpha-pyrrolidone of surplus, prepare according to 2 method of embodiment.
Positive control medicine 2:Medicine of the embodiment 4 without the preparation capable of permeating skin containing natural plant essential oils, i.e.,:1% not former times Gram fourth, 10% imidacloprid, 5% Permethrin, 0.1%BHT, and the alpha-pyrrolidone of surplus, prepare according to 4 method of embodiment.
Before experiment, every group of pet cat body surface is cleaned, and cleans pet cat body surface;Then, respectively in every pet cat Anterior part of chest infects the cat flea of 100 or so;Then, after 2d is infected, respectively to 1-2 groups pet cat is with embodiment 2 and implements The compound recipe Moxidectin drop of example 4 is treated;3rd group gives positive control medicine 1 and is treated;4th group give it is positive right Treated according to medicine 2;5th group of pet cat does not receive treatment, only with clean water;
Therapeutic Method is as follows:By the compound recipe Moxidectin agent of the 2.5g embodiment of the present invention according to 1:100 ratio is mixed with water Close, then dipping treatment is carried out infecting position and peripheral part.
The cat flea infection conditions of each group pet cat are observed in administration 24,48 and 72h respectively, and count infection knot Really, criterion:Every pet cat if the quantity of cat flea exceeds 100 in the target of the visual field, is designated as nothing in checking process Effect;If the quantity of visual field cat flea is 30~50, it is designated as effectively;If not occurring cat flea in the visual field, recovery from illness is designated as.Control Therapeutic effect control is as follows:
From above-mentioned control, after medication 24h, the effective percentage and cure rate of 1~4 group of experimental group is all remarkably higher than unused Medicine group, illustrates that the present invention's is effective to killing endoparasite and ectoparasite.Meanwhile, from experimental data, the embodiment of the present invention 2 With embodiment 4, after medication 72h, up to 100%, cure rate is respectively 98% and 100% to effective percentage.And experimental group 3 and experimental group After 4 medication 72h, effective percentage is only 83% and 86%, and cure rate is only 79% and 83%;The effective percentage of experimental group 1 and experimental group 2 Experimental group 3 and experimental group 4 being all remarkably higher than with cure rate, the present invention being illustrated after addition transdermal agent, its anthelmintic drug action can Significantly increase, the mechanism that this effect occurs is inferred, is on the one hand the effect of transdermal, promote medicine and more enter animal machine Body, the availability of medicine are lifted, and the transdermal agent composition eucalyptus oil and seed oil of Moringa oleigera used by the present invention inherently has comparison good in addition Good anthelmintic action.
Meanwhile, over the course for the treatment of with treatment after, pet cat drinking water diet is normal, any abnormal conditions does not occur; During medication, it is found that the abnormal flavour of drop of the present invention is less, sense organ is preferable.
3 permeability effects of experimental example
The skin of pigletss abdominal part shaving is taken, and removes subcutaneous fat, tissue and blood capillary, it is then anti-with normal saline It is multiple to rinse, dry stand-by;
Appropriate Moxidectin is taken, and is dissolved with alpha-pyrrolidone, and so that the concentration of Moxidectin is 2.5%, Ran Houxiang Appropriate Propylene Glycol, eucalyptus oil and seed oil of Moringa oleigera are added in resulting solution, and causes three's concentration respectively 2%, 1% and 2%, and Using gained mixed solution as releasing agent, accepting agent is blank alpha-pyrrolidone solvent;
At normal temperatures, skin transdermal test in vitro absorption experiment is carried out, amount of release agent is 2ml, and accepting agent is 7ml, experiment temperature Spend for 37 DEG C, 5.0ml acceptable solutions are taken respectively in the 1st, 2,4,6,8,10,12h time points, while equivalent acceptable solution is supplemented, and profit With high effective liquid chromatography for measuring Moxidectin content, and calculate different time points Moxidectin unit area infiltration capacity.Knot Fruit is as follows:
Time (h) Unit area infiltration capacity (μ g/cm2)
1 59.39
2 103.54
4 135.48
6 178.31
8 203.94
10 248.67
12 279.71
Then, 2 parts of Moxidectins are taken, and is dissolved with appropriate alpha-pyrrolidone, and so that the concentration of Moxidectin is 2.5%;
Then, control (is designated as with eucalyptus oil (being designated as matched group 1), seed oil of Moringa oleigera (being designated as matched group 2) and Propylene Glycol respectively Group is 3) as penetrating agent, and is separately added in each part Moxidectin solution;
Wherein in matched group 1, in solution, the concentration of eucalyptus oil is 3.5%;In matched group 2, the concentration of solution seed oil of Moringa oleigera For 4%;In matched group 3, the concentration of Propylene Glycol is 4.5%;
Respectively using three groups of solution as releasing agent, accepting agent is blank alpha-pyrrolidone solvent;And respectively according to such as The upper identical method carries out Moxidectin unit area infiltration capacity, test result indicate that, the 12h unit areas of matched group 1 Infiltration capacity is 189.45 μ g/cm2;The 12h unit areas infiltration capacity of matched group 2 is 179.31 μ g/cm2;The 12h units of matched group 3 Area infiltration capacity is 162.19 μ g/cm2;.
As can be seen here, the Penetration enhancing effect of compound penetrant of the present invention is more preferable.
Although with specific embodiment illustrate and describing the present invention, but it will be appreciated that without departing substantially from the present invention's Many other changes and modification can be made in the case of spirit and scope.It is, therefore, intended that in the following claims Including all such changes and modifications belonged in the scope of the invention.

Claims (10)

1. a kind of compound recipe Moxidectin drop, it is characterised in that according to percent by weight, the compound recipe Moxidectin drop master To be made up of following components:
Moxidectin 0.5~5%;
Imidacloprid 5~12%;
Propylene Glycol 1~5%;
Seed oil of Moringa oleigera 1~4%;
Antioxidant 0.1~0.5%;
Eucalyptus oil 0.5~2%;
Solvent 75~95%.
2. compound recipe Moxidectin drop according to claim 1, it is characterised in that the compound recipe Moxidectin drop also enters One step includes Permethrin.
3. compound recipe Moxidectin drop according to claim 2, it is characterised in that according to percent by weight, described multiple Square Moxidectin drop is made up of following components:
Moxidectin 0.5~5%;
Imidacloprid 5~12%;
Permethrin 3~8%
Propylene Glycol 1~5%;
Seed oil of Moringa oleigera 1~4%;
Antioxidant 0.1~0.5%;
Eucalyptus oil 0.5~2%;
Solvent 75~90%.
4. the compound recipe Moxidectin drop according to any one of claim 1-3, it is characterised in that described antioxidation Agent is BHA and/or BHT.
5. the compound recipe Moxidectin drop according to any one of claim 1-3, it is characterised in that described solvent is Alpha-pyrrolidone;And/or dimethyl sulfoxide;And/or dimethylformamide;And/or dimethyl acetylamide;And/or ethanol.
6. the preparation method of compound recipe Moxidectin drop any one of claim 1-5, it is characterised in that the compound recipe Moxidectin drop is that the component by any one of claim 1-5 is mixed with what is obtained.
7. preparation method according to claim 6, it is characterised in that methods described comprises the steps:
1) imidacloprid is dissolved with most of solvent;
2) Moxidectin is added into step 1) in resulting solution, and continue stirring mixing;
3) to step 2) Propylene Glycol, seed oil of Moringa oleigera and eucalyptus oil are added in resulting solution, and continue stirring mixing;
4) by BHA and/or BHT with residual solvent dissolving after, by resulting solution and step 3) resulting solution mixes, obtains final product described multiple Square Moxidectin drop.
8. preparation method according to claim 7, it is characterised in that step 2) in may further include step 2) add While Moxidectin, Permethrin is additionally added, and is stirred together for the step of mixing.
9. application of the compound recipe Moxidectin drop in animal anthelmintic any one of claim 1-5.
10. application according to claim 9, it is characterised in that the animal is poultry or livestock.
CN201710041410.4A 2017-01-18 2017-01-18 Compound moxidectin drops as well as preparation method and application thereof Pending CN106511267A (en)

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Application publication date: 20170322