CN1069033C - Anti-parasite oral spray containing evericin and ivermectin for sheep - Google Patents
Anti-parasite oral spray containing evericin and ivermectin for sheep Download PDFInfo
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- CN1069033C CN1069033C CN98124497A CN98124497A CN1069033C CN 1069033 C CN1069033 C CN 1069033C CN 98124497 A CN98124497 A CN 98124497A CN 98124497 A CN98124497 A CN 98124497A CN 1069033 C CN1069033 C CN 1069033C
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- mouth sprays
- avilamycin
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Abstract
The present invention relates to an antiparasitic oral cavity spray containing abamectin or ivermectin for sheep. The antiparasitic oral cavity spray can be divided into a solution type and an emulsion type and contains the following components and contents (weight percentage, the following is the same): the solution type: 0.1 to 15% of abamectin or ivermectin, 0 to 80% of surfactant, and solvent or vegetable oil as the rest; the emulsion type: 0.1 to 15% of abamectin or ivermectin, 0.1 to 80% of surfactant, 2 to 80% of solvent, 0.1 to 5% of stabilizing agent and water as the rest. In the formula, the best concentration scope of abamectin or ivermectin is from 0.5 to 4%.
Description
The present invention relates to a kind of sheep that contains avilamycin or ivermectin and use anti-parasite oral spray, the invention belongs to anti-parasite medicine for animal use.
The eighties U.S. MERCK company successfully is developed to anti-parasite medicine for animal use with avilamycin and ivermectin, be used to kill parasites such as nematicide and external demodicid mite in the body of animal, Ticks, louse, fly larvae, used oral agents has powder, tablet, capsule, oral liquid, wherein uses more convenient with oral liquid.(William C.Campbell,“Ivermectin and Abamectin”,Springer-Verlag,New York Inc,1989,p215-229)。But when using oral liquid, need a kind of special continuous liquid filling device, use cost is increased greatly.For this reason, we develop a kind of avilamycin and ivermectin mouth sprays, and it is easy to use, only need a kind of special valve system during use, use cost is reduced, and absorb good.
The object of the present invention is to provide a kind of sheep that contains avilamycin or ivermectin to use anti-parasite oral spray.
The object of the present invention is achieved like this:
This spray is a solution-type, and specifically form content following (percetage by weight, down together): avilamycin or ivermectin 0.1-15%, surfactant 0-80%, all the other are solvent or vegetable oil.
This spray is an emulsion-type, and it is as follows specifically to form content: avilamycin or ivermectin 0.1-15%, surfactant 0.1-80%, solvent 2-80%, stabilizing agent 0.1-5%, all the other are water.
In described solution dosage and the emulsion-type spray, the optimum concentration range of avilamycin or ivermectin is 0.5-4%.
Described surfactant comprises anion surfactant, cationic surfactant, nonionic surfactant and amphoteric surfactant, special surface activating agent for available surfactant pharmaceutically.
Described anion surfactant comprises sulfuric acid, carboxylate, sulfonate, phosphate ester salt.
Described cationic surfactant comprises amine salt type cationic surfactant, quaternary ammonium salt cationic surfactant.
Described nonionic surfactant comprises polyethylene glycol type, Tweens, polyoxyethylene aliphatic alcohol ether, polyethenoxy alkylphenols, polyvinylpyrrolidone.
Described amphoteric surfactant comprises amino acid type amphoteric surface active agent, betaine type amphoteric surfac-tant, imidazoline type amphoteric surfactant, amine oxide.
Described special surface activating agent comprises fluorine surfactant, silicon surface active agent.
Tween series in the described nonionic surfactant is selected from tween 80, Tween-60, Tween-40, tween 20, span series and is selected from Arlacel-20, Arlacel-40, Arlacel-80.
Described solvent comprises ethanol, isopropyl alcohol, 1,2-propylene glycol, glycerol, n-butyl alcohol, isobutanol, ethyl acetate, methyl acetate, acetone, butanone, dimethyl acetylamide, dimethyl formamide organic solvent, this this solvent can use separately, but also two or more uses simultaneously.
Described vegetable oil comprises Semen Maydis oil, Oleum sesami, Oleum Glycines, rapeseed oil, Oleum Gossypii semen, Oleum Ricini, Oleum Arachidis hypogaeae semen, Oleum Helianthi, almond oil.
Described stabilizing agent comprises xanthan gum, arabic gum, hydroxyethyl-cellulose, hydroxypropyl cellulose, methylcellulose, sodium carboxymethyl cellulose, polyvinyl alcohol.
Preparation process is:
Solution-type: at first with solvent or vegetable oil dissolving avilamycin or ivermectin, add or do not add surfactant, stir, at last after testing, the packing warehouse-in;
Emulsion-type: at first use dissolution with solvents avilamycin or ivermectin, add the surfactant mixing again, add stabilizing agent and water then, stir, at last after testing, packing warehouse-in;
Preparation is loaded in the container of being furnished with the Special valve system, presses valve with hands during use and by pressure liquid in the bottle is accurately quantitatively extruded, liquid is sprayed in the sheep oral cavity or in the liquid stream mode with the droplet shape and sprays in the sheep oral cavity.
Mouth sprays of the present invention can be divided into solution and emulsion-type, specifically forms content and is (percetage by weight):
Solution-type: avilamycin or ivermectin 0.1-15%, surfactant 0-80%, all the other are solvent or vegetable oil.
Emulsion-type: avilamycin or ivermectin 0.1-15%, surfactant 0.1-80%, solvent 2-80%, stabilizing agent 0.1-5%, all the other are water.
The optimum concentration range of avilamycin or ivermectin is 0.5-4% in the prescription.
Described avilamycin is the tunning of A Foman streptomycete Streptomyces avermitilis, the mixture of being made up of eight quite similar homologues of structure, i.e. Avermectin A
1a, A
1b, A
2a, A
2b, B
1a, B
1b, B
2a, B
2b, generally use B more
1a, B
1bMixture, it can adopt prior art extract and separate (William C.Campbell, " Ivermectin andAbamectin ", Springer-Verlag, New York Inc, 1989, p1-23)
Described ivermectin be avilamycin two hydroperoxide derivatives (William C.Campbell, " Ivermectin and Abamectin ", Springer-Verlag, New York Inc, 1989, p1-23)
Described surfactant comprises anion surfactant for available surfactant pharmaceutically, for example sulfuric acid, carboxylate, sulfonate, phosphate ester salt; Cationic surfactant such as amine salt type cationic surfactant, quaternary ammonium salt cationic surfactant, nonionic surfactant is selected from polyethylene glycol type, Tweens, polyoxyethylene aliphatic alcohol ether, polyethenoxy alkylphenols, polyvinylpyrrolidone, with amphoteric surfactant chloro acid type amphoteric surfactant for example, the betaine type amphoteric surfac-tant, the imidazoline type amphoteric surfactant, amine oxide, special surface activating agent such as fluorine surfactant, silicon surface active agent etc., consider that from cost and stability the tween series of using nonionic surfactant as tween 80 more, Tween-60, Tween-40, tween 20 etc., span series is as Arlacel-20, Arlacel-40, Arlacel-80 etc.
Described solvent comprises ethanol, isopropyl alcohol, 1, organic solvents such as 2-propylene glycol, glycerol, n-butyl alcohol, isobutanol, ethyl acetate, methyl acetate, acetone, butanone, dimethyl acetylamide, dimethyl formamide, this this solvent can use separately, but also two or more uses simultaneously.
Described vegetable oil comprises Semen Maydis oil, Oleum sesami, Oleum Glycines, rapeseed oil, Oleum Gossypii semen, Oleum Ricini, Oleum Arachidis hypogaeae semen, Oleum Helianthi, Semen Armeniacae Amarum wet goods.
Described stabilizing agent comprises xanthan gum, arabic gum, hydroxyethyl-cellulose, hydroxypropyl cellulose, methylcellulose, Carboxymethyl cellulose sodium, polyvinyl alcohol.
The preparation method of mouth sprays of the present invention may further comprise the steps:
Solution-type: at first with solvent or vegetable oil dissolving avilamycin or ivermectin, add or do not add surfactant, stir, at last after testing, the packing warehouse-in.
Emulsion-type; At first use dissolution with solvents avilamycin or ivermectin, add the surfactant mixing again, add stabilizing agent and water then, stir, at last after testing, packing warehouse-in.
The advantage of mouth sprays of the present invention:
Mouth sprays preparation of the present invention is easy to use than other oral formulations, production cost is low, and absorbs good.
Further describe characteristics of the present invention with example below, but do not limit the scope of the invention.
Embodiment 1
Present embodiment is the mouth sprays that preparation contains avilamycin 0.5%.
Get 0.53 kilogram of avilamycin (purity 95%), place 200 liters of batch tanks, add 5 liters of dimethyl acetylamide, stir and to make it after the dissolving, add ethanol to 100 liter, stir, promptly get 0.5% avilamycin mouth sprays through the after the assay was approved packing.
Usage and consumption: the avilamycin mouth sprays is loaded in the bottle of being furnished with valve system, and sheep with 0.4 milliliter of spray, can be killed interior nematicide of sheep body and external demodicid mite, Ticks, louse, fly larvae etc. by per 10 kg body weight spray.
Embodiment 2
Present embodiment is the ivermectin mouth sprays of preparation 15%.
Get 15.5 kilograms of ivermectins (purity 97%), place 200 liters of preparing tanks, add 10 liters of ethyl acetate stir make it dissolving after, add 80 liters of tween 80s, add Semen Maydis oil to 100 liter then, stirring and evenly mixing, packing promptly gets 15% ivermectin mouth sprays.
Embodiment 3
Present embodiment is the avilamycin mouth sprays of preparation 0.2%.
Get 0.21 kilogram of avilamycin (purity is 95%), place 200 liters of preparing tanks, add 5 liters of acetone stir make it dissolving after, add 80 liters of Tween-60 mixings, add 0.2% xanthan gum solution to 100 liter then, stirring and evenly mixing, packing promptly gets 0.5% avilamycin mouth sprays.
Embodiment 4
Present embodiment is the ivermectin mouth sprays of preparation 14.5%.
Get 15.4 kilograms of ivermectins (purity is 94%), place 200 liters of preparing tanks, add 40 liters of ethyl acetate stir make it dissolving after, add 2 liters of Arlacel-80 mixings, add 3% sodium carboxymethyl cellulose solution to 100 liter then, stirring and evenly mixing, packing promptly get 14.5% ivermectin mouth sprays.
Embodiment 5
Present embodiment is done the comparison of insecticidal activity aspect to mouth sprays of the present invention and common avilamycin or ivermectin oral formulations, the results are shown in Table 1.
The same group sheep of choosing the natural infection nematicide is divided into 5 groups at random, 5 groups of sheep are pressed avilamycin, ivermectin mouth sprays and the commercially available avilamycin oral formulations of the oral 0.2mg/kg of body weight separately respectively, each treated animal is respectively at the forward and backward worm's ovum number of counting respectively in the feces of test, and the calculating deworming rates.And the observation medicine has no side effect to animal.
Table 1. avilamycin or ivermectin mouth sprays and other oral formulations are to the effect of all kinds of nematicide worm's ovums of sheep (larva)
| Dosage form | Dosage (mg/kg) | Deworming rates (%) | |||
| Haemonchus contortus | Trichostrongylus colubriformis | Strongyloides papillosus | The first nematicide of sheep's wool | ||
| Avilamycin mouth sprays among the embodiment 1 | 0.2 | 100 | 100 | 98.7 | 92.2 |
| 0.08% avilamycin oral liquid | 0.2 | 100 | 100 | 100 | 91.4 |
| The avilamycin tablet | 0.2 | 100 | 97.4 | 98.2 | 88.7 |
| The avilamycin powder | 0.2 | 100 | 96.3 | 97.4 | 89.1 |
| The avilamycin capsule | 0.2 | 100 | 98.1 | 97.9 | 87.8 |
Annotate: 0.08% avilamycin oral liquid is commercially available avilamycin oral liquid (French Virbac company produce).Avilamycin powder, tablet, capsule are the commercially available prod, and New Tech. Development General Co., Beijing Agriculture Univ. produces.As shown in Table 1, mouth sprays of the present invention is consistent with the anthelminthic effect of common avilamycin oral liquid.And animal has no adverse reaction after using recommended dose (0.2mg/kg), illustrates that mouth sprays is safe to animal.
Embodiment 6
Present embodiment is done the comparison of blood medicine kinetics aspect to the mouth sprays of the embodiment of the invention 1 and commercially available avilamycin powder, tablet, capsule, oral liquid.
With sheep is laboratory animal, and 0.5,1,1.5,2,3,4,6,10,14,20 day difference blood sampling is measured blood drug level after administration.And draw pharmaceutical concentration-time curve, and calculate each pharmacokinetic parameters.The result shows that after the administration, blood medicine peak appears in mouth sprays mouth sprays in these several preparations at first, the peak blood drug level of various preparations is respectively: mouth sprays: 15-21 μ g/ml, oral liquid: 15-21 μ g/ml, powder and capsule: 8-13 μ g/ml, tablet 6-11 μ g/ml.
In sum, mouth sprays of the present invention is consistent with the anthelminthic effect of common avilamycin or ivermectin oral formulations, but consider from aspects such as production and use cost, easy to use and good absorbing, avilamycin or ivermectin mouth sprays are much better than common avilamycin or ivermectin oral formulations, have the wide development prospect.
Claims (15)
1. a sheep that contains avilamycin or ivermectin is used anti-parasite oral spray, it is characterized in that this spray is made up of the container of being furnished with valve of solution and this solution of splendid attire, the concrete composition content of described solution is as follows: avilamycin or ivermectin 0.1-15%, surfactant 0-80%, all the other are solvent or vegetable oil, and above-mentioned percent is percetage by weight.
2. a sheep that contains avilamycin or ivermectin is used anti-parasite oral spray, it is characterized in that this spray is made up of the container of being furnished with valve of Emulsion and this Emulsion of splendid attire, the concrete composition content of described Emulsion is as follows: avilamycin or ivermectin 0.1-15%, surfactant 0.1-80%, solvent 2-80%, stabilizing agent 0.1-5%, all the other are water, and above-mentioned percent is percetage by weight.
3. mouth sprays according to claim 1 and 2 is characterized in that in described solution dosage and the emulsion-type spray, the concentration of avilamycin or ivermectin is 0.5-4%.
4. mouth sprays according to claim 1 and 2 is characterized in that described surfactant comprises anion surfactant, cationic surfactant, nonionic surfactant and amphoteric surfactant, special surface activating agent for available surfactant pharmaceutically.
5. mouth sprays according to claim 4 is characterized in that described anion surfactant comprises sulfuric acid, carboxylate, sulfonate, phosphate ester salt.
6. mouth sprays according to claim 4 is characterized in that described cationic surfactant comprises amine salt type cationic surfactant, quaternary ammonium salt cationic surfactant.
7. mouth sprays according to claim 4 is characterized in that described nonionic surfactant comprises polyethylene glycol type, Tweens, polyoxyethylene aliphatic alcohol ether, polyethenoxy alkylphenols, polyvinylpyrrolidone.
8. mouth sprays according to claim 4 is characterized in that described amphoteric surfactant comprises amino acid type amphoteric surface active agent, betaine type amphoteric surfac-tant, imidazoline type amphoteric surfactant, amine oxide.
9. mouth sprays according to claim 4 is characterized in that described special surface activating agent comprises fluorine surfactant, silicon surface active agent.
10. mouth sprays according to claim 7 is characterized in that the Tweens in the described nonionic surfactant is selected from tween 80, Tween-60, Tween-40, tween 20.
11. mouth sprays according to claim 1 and 2, it is characterized in that described solvent comprises ethanol, isopropyl alcohol, 1,2-propylene glycol, glycerol, n-butyl alcohol, isobutanol, ethyl acetate, methyl acetate, acetone, butanone, dimethyl acetylamide, dimethyl formamide organic solvent, these solvents can use separately, but also two or more uses simultaneously.
12. mouth sprays according to claim 1 is characterized in that described vegetable oil comprises Semen Maydis oil, Oleum sesami, Oleum Glycines, rapeseed oil, Oleum Gossypii semen, Oleum Ricini, Oleum Arachidis hypogaeae semen, Oleum Helianthi, almond oil.
13. mouth sprays according to claim 2 is characterized in that described stabilizing agent comprises xanthan gum, arabic gum, hydroxyethyl-cellulose, hydroxypropyl cellulose, methylcellulose, sodium carboxymethyl cellulose, polyvinyl alcohol.
14. the preparation method of the described mouth sprays of claim 1, it is characterized in that preparation process is: at first with solvent or vegetable oil dissolving avilamycin or ivermectin, add then or do not add surfactant, stir, the back is divided to pack into and is furnished with in the container of valve after testing.
15. the preparation method of the described mouth sprays of claim 2, it is characterized in that preparation process is: at first use dissolution with solvents avilamycin or ivermectin, add the surfactant mixing again, add stabilizing agent and water then, stir, back after testing branch is packed into and is furnished with in the container of valve.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98124497A CN1069033C (en) | 1998-11-13 | 1998-11-13 | Anti-parasite oral spray containing evericin and ivermectin for sheep |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98124497A CN1069033C (en) | 1998-11-13 | 1998-11-13 | Anti-parasite oral spray containing evericin and ivermectin for sheep |
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| Publication Number | Publication Date |
|---|---|
| CN1217187A CN1217187A (en) | 1999-05-26 |
| CN1069033C true CN1069033C (en) | 2001-08-01 |
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|---|---|---|---|
| CN98124497A Expired - Fee Related CN1069033C (en) | 1998-11-13 | 1998-11-13 | Anti-parasite oral spray containing evericin and ivermectin for sheep |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101579309B (en) * | 2009-06-23 | 2011-08-17 | 纽素乐必佳（天津）药业集团有限公司 | Anti-parasitic ivermectin transdermal solution used for livestock and preparation method thereof |
| CN103083228A (en) * | 2011-10-27 | 2013-05-08 | 天津生机集团股份有限公司 | Preparation method for ivermectin solution used for fowls |
| CN106692054A (en) * | 2016-10-20 | 2017-05-24 | 北京科百大科技有限责任公司 | Preparation of ivermectin pharmaceutical liquid preparation capable of resisting acid catalytic degradation |
| CN106732168A (en) * | 2016-12-15 | 2017-05-31 | 钦州市钦南区科学技术情报研究所 | A kind of surface activator composition and preparation method thereof |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1113433A (en) * | 1995-01-06 | 1995-12-20 | 北京农业大学 | Antiparasitic medicine |
| CN1146337A (en) * | 1996-08-19 | 1997-04-02 | 北京农业大学新技术开发总公司 | Anti-parasite oral liquid for animal containing avermectin or ivermectin |
| CN1158251A (en) * | 1996-11-08 | 1997-09-03 | 王玉万 | Animal anti-parasite oral liquor containing avilamycin or envimycin |
| CN1158724A (en) * | 1996-10-30 | 1997-09-10 | 王玉万 | Veterinary antiparasitic lincture contg. avermectin or invermectin |
| CN1193510A (en) * | 1998-04-23 | 1998-09-23 | 王玉万 | Oily injection for preventing animals from parasites |
| CN1194780A (en) * | 1997-03-27 | 1998-10-07 | 王玉万 | Plant protection pesticide containing avermectin |
| CN1194832A (en) * | 1997-03-27 | 1998-10-07 | 王玉万 | Antiparasitic medicine containing avermectin/ivermectin for animals |
-
1998
- 1998-11-13 CN CN98124497A patent/CN1069033C/en not_active Expired - Fee Related
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1113433A (en) * | 1995-01-06 | 1995-12-20 | 北京农业大学 | Antiparasitic medicine |
| CN1146337A (en) * | 1996-08-19 | 1997-04-02 | 北京农业大学新技术开发总公司 | Anti-parasite oral liquid for animal containing avermectin or ivermectin |
| CN1158724A (en) * | 1996-10-30 | 1997-09-10 | 王玉万 | Veterinary antiparasitic lincture contg. avermectin or invermectin |
| CN1158251A (en) * | 1996-11-08 | 1997-09-03 | 王玉万 | Animal anti-parasite oral liquor containing avilamycin or envimycin |
| CN1194780A (en) * | 1997-03-27 | 1998-10-07 | 王玉万 | Plant protection pesticide containing avermectin |
| CN1194832A (en) * | 1997-03-27 | 1998-10-07 | 王玉万 | Antiparasitic medicine containing avermectin/ivermectin for animals |
| CN1193510A (en) * | 1998-04-23 | 1998-09-23 | 王玉万 | Oily injection for preventing animals from parasites |
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| CN1217187A (en) | 1999-05-26 |
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