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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- surfactant
- ivermectin
- mouth sprays
- avilamycin
- sprays according
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- AZSNMRSAGSSBNP-UHFFFAOYSA-N 22,23-dihydroavermectin B1a Natural products C1CC(C)C(C(C)CC)OC21OC(CC=C(C)C(OC1OC(C)C(OC3OC(C)C(O)C(OC)C3)C(OC)C1)C(C)C=CC=C1C3(C(C(=O)O4)C=C(C)C(O)C3OC1)O)CC4C2 AZSNMRSAGSSBNP-UHFFFAOYSA-N 0.000 title claims abstract description 41
- SPBDXSGPUHCETR-JFUDTMANSA-N 8883yp2r6d Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O[C@@H]([C@@H](C)CC4)C(C)C)O3)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1C[C@H](C)[C@@H]([C@@H](C)CC)O[C@@]21O[C@H](C\C=C(C)\[C@@H](O[C@@H]1O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C1)[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\1)O)C[C@H]4C2 SPBDXSGPUHCETR-JFUDTMANSA-N 0.000 title claims abstract description 41
- 229960002418 ivermectin Drugs 0.000 title claims abstract description 41
- 241001494479 Pecora Species 0.000 title claims abstract description 16
- 230000002141 anti-parasite Effects 0.000 title claims abstract description 10
- 229940041678 oral spray Drugs 0.000 title claims description 6
- 239000000668 oral spray Substances 0.000 title claims description 6
- 239000007921 spray Substances 0.000 claims abstract description 50
- 239000004094 surface-active agent Substances 0.000 claims abstract description 28
- 239000002904 solvent Substances 0.000 claims abstract description 20
- 239000003381 stabilizer Substances 0.000 claims abstract description 10
- 235000015112 vegetable and seed oil Nutrition 0.000 claims abstract description 10
- 239000008158 vegetable oil Substances 0.000 claims abstract description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000000839 emulsion Substances 0.000 claims abstract 5
- 229930192734 Avilamycin Natural products 0.000 claims description 48
- 239000004190 Avilamycin Substances 0.000 claims description 48
- XIRGHRXBGGPPKY-OTPQUNEMSA-N [(2r,3s,4r,6s)-6-[(2'r,3's,3ar,4r,4'r,6s,7ar)-6-[(2s,3r,4r,5s,6r)-2-[(2r,3s,4s,5s,6s)-6-[(2r,3as,3'ar,6'r,7r,7's,7ar,7'ar)-7'-acetyl-7'-hydroxy-6'-methyl-7-(2-methylpropanoyloxy)spiro[4,6,7,7a-tetrahydro-3ah-[1,3]dioxolo[4,5-c]pyran-2,4'-6,7a-dihydro-3ah- Chemical compound O([C@H]1[C@H](O)C[C@@H](O[C@@H]1C)O[C@H]1[C@H](O)CC2(O[C@]3(C)C[C@@H](O[C@H](C)[C@H]3O2)O[C@H]2[C@@H](OC)[C@@H](C)O[C@H]([C@@H]2O)O[C@H]2[C@H](O)[C@H](OC)[C@H](OC3[C@@H]([C@@H]4O[C@]5(O[C@H]4CO3)[C@@H]3OCO[C@H]3[C@@](O)([C@@H](C)O5)C(C)=O)OC(=O)C(C)C)O[C@@H]2COC)O[C@@H]1C)C(=O)C1=C(C)C(Cl)=C(O)C(Cl)=C1OC XIRGHRXBGGPPKY-OTPQUNEMSA-N 0.000 claims description 48
- 229960005185 avilamycin Drugs 0.000 claims description 48
- 235000019379 avilamycin Nutrition 0.000 claims description 48
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 14
- 238000003756 stirring Methods 0.000 claims description 14
- 239000002280 amphoteric surfactant Substances 0.000 claims description 12
- -1 phosphate ester salt Chemical class 0.000 claims description 12
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 11
- 239000003093 cationic surfactant Substances 0.000 claims description 11
- 210000000582 semen Anatomy 0.000 claims description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 9
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 9
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 9
- 238000002156 mixing Methods 0.000 claims description 8
- 239000002736 nonionic surfactant Substances 0.000 claims description 8
- 229920000136 polysorbate Polymers 0.000 claims description 7
- 238000012360 testing method Methods 0.000 claims description 7
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- ZXEKIIBDNHEJCQ-UHFFFAOYSA-N isobutanol Chemical compound CC(C)CO ZXEKIIBDNHEJCQ-UHFFFAOYSA-N 0.000 claims description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 5
- 230000003213 activating effect Effects 0.000 claims description 5
- 239000003945 anionic surfactant Substances 0.000 claims description 5
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
- WFKAJVHLWXSISD-UHFFFAOYSA-N isobutyramide Chemical compound CC(C)C(N)=O WFKAJVHLWXSISD-UHFFFAOYSA-N 0.000 claims description 4
- 239000003921 oil Substances 0.000 claims description 4
- 235000019198 oils Nutrition 0.000 claims description 4
- 239000000230 xanthan gum Substances 0.000 claims description 4
- 235000010493 xanthan gum Nutrition 0.000 claims description 4
- 229920001285 xanthan gum Polymers 0.000 claims description 4
- 229940082509 xanthan gum Drugs 0.000 claims description 4
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 claims description 3
- ZEMPKEQAKRGZGQ-AAKVHIHISA-N 2,3-bis[[(z)-12-hydroxyoctadec-9-enoyl]oxy]propyl (z)-12-hydroxyoctadec-9-enoate Chemical compound CCCCCCC(O)C\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CC(O)CCCCCC)COC(=O)CCCCCCC\C=C/CC(O)CCCCCC ZEMPKEQAKRGZGQ-AAKVHIHISA-N 0.000 claims description 3
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims description 3
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 3
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 3
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 3
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 claims description 3
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 3
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
- 229920001213 Polysorbate 20 Polymers 0.000 claims description 3
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 3
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims description 3
- 235000019484 Rapeseed oil Nutrition 0.000 claims description 3
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims description 3
- 235000010489 acacia gum Nutrition 0.000 claims description 3
- 239000001785 acacia senegal l. willd gum Substances 0.000 claims description 3
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims description 3
- 150000001412 amines Chemical class 0.000 claims description 3
- 229960003237 betaine Drugs 0.000 claims description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 3
- 150000007942 carboxylates Chemical class 0.000 claims description 3
- 238000004090 dissolution Methods 0.000 claims description 3
- 229910052731 fluorine Inorganic materials 0.000 claims description 3
- 239000011737 fluorine Substances 0.000 claims description 3
- 150000002333 glycines Chemical class 0.000 claims description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 3
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 3
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 3
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 3
- MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims description 3
- 229920000609 methyl cellulose Polymers 0.000 claims description 3
- 239000001923 methylcellulose Substances 0.000 claims description 3
- 235000010981 methylcellulose Nutrition 0.000 claims description 3
- 239000003960 organic solvent Substances 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- 229920001223 polyethylene glycol Polymers 0.000 claims description 3
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 3
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 3
- 229920000053 polysorbate 80 Polymers 0.000 claims description 3
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims description 3
- 239000010703 silicon Substances 0.000 claims description 3
- 229910052710 silicon Inorganic materials 0.000 claims description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims description 3
- 235000019489 Almond oil Nutrition 0.000 claims description 2
- 239000008168 almond oil Substances 0.000 claims description 2
- 150000001413 amino acids Chemical class 0.000 claims description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 2
- 210000000214 mouth Anatomy 0.000 abstract description 30
- IBSREHMXUMOFBB-JFUDTMANSA-N 5u8924t11h Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O3)C=C[C@H](C)[C@@H](C(C)C)O4)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\2)O)C[C@H]4C1 IBSREHMXUMOFBB-JFUDTMANSA-N 0.000 abstract description 6
- 239000005660 Abamectin Substances 0.000 abstract description 6
- 229950008167 abamectin Drugs 0.000 abstract description 6
- 239000003096 antiparasitic agent Substances 0.000 abstract 2
- 239000007788 liquid Substances 0.000 description 13
- 241001465754 Metazoa Species 0.000 description 8
- 238000012856 packing Methods 0.000 description 8
- 239000003814 drug Substances 0.000 description 7
- 238000009472 formulation Methods 0.000 description 6
- 239000002775 capsule Substances 0.000 description 5
- 239000005645 nematicide Substances 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- NWGKJDSIEKMTRX-AAZCQSIUSA-N Sorbitan monooleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NWGKJDSIEKMTRX-AAZCQSIUSA-N 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 241000238876 Acari Species 0.000 description 2
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 description 2
- LWZFANDGMFTDAV-BURFUSLBSA-N [(2r)-2-[(2r,3r,4s)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] dodecanoate Chemical compound CCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O LWZFANDGMFTDAV-BURFUSLBSA-N 0.000 description 2
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- AFSHKCWTGFDXJR-SQOHEDJBSA-N C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](OC)[C@H]3OC\2)O)C[C@H]4C1 Chemical compound C1=C[C@H](C)[C@@H]([C@@H](C)CC)O[C@]11O[C@H](C\C=C(C)\[C@@H](O[C@@H]2O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C2)[C@@H](C)\C=C\C=C/2[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](OC)[C@H]3OC\2)O)C[C@H]4C1 AFSHKCWTGFDXJR-SQOHEDJBSA-N 0.000 description 1
- 102000002322 Egg Proteins Human genes 0.000 description 1
- 108010000912 Egg Proteins Proteins 0.000 description 1
- 241000243974 Haemonchus contortus Species 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 241001468227 Streptomyces avermitilis Species 0.000 description 1
- 241000731783 Strongyloides papillosus Species 0.000 description 1
- 241000243796 Trichostrongylus colubriformis Species 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000010241 blood sampling Methods 0.000 description 1
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 description 1
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- 239000002552 dosage form Substances 0.000 description 1
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- 208000015181 infectious disease Diseases 0.000 description 1
- 230000000749 insecticidal effect Effects 0.000 description 1
- 229960002900 methylcellulose Drugs 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 244000045947 parasite Species 0.000 description 1
- 229940068984 polyvinyl alcohol Drugs 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
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.
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| Application Number | Priority Date | Filing Date | Title |
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| 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 |
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| CN98124497A CN1069033C (en) | 1998-11-13 | 1998-11-13 | Anti-parasite oral spray containing evericin and ivermectin for sheep |
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| CN1069033C true CN1069033C (en) | 2001-08-01 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3326608A1 (en) * | 2016-11-24 | 2018-05-30 | Nestlé Skin Health SA | Composition comprising avermectin compounds without solid fatty substances |
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| 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 |
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