CN105748403A - A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof - Google Patents
A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof Download PDFInfo
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- CN105748403A CN105748403A CN201410793149.XA CN201410793149A CN105748403A CN 105748403 A CN105748403 A CN 105748403A CN 201410793149 A CN201410793149 A CN 201410793149A CN 105748403 A CN105748403 A CN 105748403A
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- Prior art keywords
- ivermectin
- oral liquid
- water
- animals
- tween
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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 49
- 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 49
- 229960002418 ivermectin Drugs 0.000 title claims abstract description 49
- 239000007788 liquid Substances 0.000 title claims abstract description 47
- 238000000034 method Methods 0.000 title abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 53
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims abstract description 36
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims abstract description 12
- 229920000053 polysorbate 80 Polymers 0.000 claims abstract description 12
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims abstract description 10
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims abstract description 10
- 235000019799 monosodium phosphate Nutrition 0.000 claims abstract description 10
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims abstract description 10
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 claims abstract description 10
- 241001465754 Metazoa Species 0.000 claims description 26
- 238000003756 stirring Methods 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 13
- 229940033663 thimerosal Drugs 0.000 claims description 9
- 238000004519 manufacturing process Methods 0.000 abstract description 3
- 210000002200 mouth mucosa Anatomy 0.000 abstract description 2
- 239000002904 solvent Substances 0.000 abstract description 2
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 229910000397 disodium phosphate Inorganic materials 0.000 abstract 1
- 235000019800 disodium phosphate Nutrition 0.000 abstract 1
- 229960004906 thiomersal Drugs 0.000 abstract 1
- 239000005645 nematicide Substances 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 241001494479 Pecora Species 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229930192734 Avilamycin Natural products 0.000 description 1
- 239000004190 Avilamycin Substances 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 102000002322 Egg Proteins Human genes 0.000 description 1
- 108010000912 Egg Proteins Proteins 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 208000002720 Malnutrition Diseases 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 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 description 1
- 208000007502 anemia Diseases 0.000 description 1
- 230000000507 anthelmentic effect Effects 0.000 description 1
- 230000002141 anti-parasite Effects 0.000 description 1
- 229960005185 avilamycin Drugs 0.000 description 1
- 235000019379 avilamycin Nutrition 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 230000000749 insecticidal effect Effects 0.000 description 1
- 230000001071 malnutrition Effects 0.000 description 1
- 235000000824 malnutrition Nutrition 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 208000015380 nutritional deficiency disease Diseases 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 210000004681 ovum Anatomy 0.000 description 1
- 244000045947 parasite Species 0.000 description 1
- 230000024241 parasitism Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 239000000273 veterinary drug Substances 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof are disclosed. Each 1000 mL of the oral liquid comprises 0.1-2 g of ivermectin, 1-20 mL of ethyl acetate, 50-150 mL of Tween-80, 1-10 g of sodium hydrogen phosphate, 1-10 g of sodium dihydrogen phosphate and 0.001-1 g of thiomersal, with the balance being water. The oral liquid adopts the water as a solvent, the ivermectin is low in solubility in water, but a solution can be uniform through adding the water after the ethyl acetate and the tween-80 which are high in dose are utilized to promote solution of the ivermectin, and therefore the ivermectin oral liquid is uniform, stable and long in shelf life, and is nonirritant to mouth mucosa, lower in production cost and good in absorption when being compared to oil oral liquids.
Description
Technical field
The invention belongs to veterinary drug field of pharmaceutical technology, be specifically related to a kind of ivermectin water solublity oral liquid for animals and preparation method thereof.
Background technology
Nematicide generally occurs when the decline of domestic animal resistance or malnutrition, parasitize the nematicide in the domestic animal body such as cattle, sheep and can constantly draw its nutrient substance, discharge toxin, and then reduce immunity of organisms, occur becoming thin, anemia by the hair slightly disease such as disorderly, infect severe patient and can cause mortality.Nematicide polypide parasitism in host and when dividing a word with a hyphen at the end of a line, often causes comparatively serious mechanical damage and stimulation, causes bleeding and inflammation host.
Avilamycin is successfully developed into anti-parasite medicine for animal use with ivermectin by MERCK company of the eighties U.S., for killing the parasites such as internal nematicide and external wax, board, louse, the fly larvae of animal, dosage form used has powder, tablet, paste, oral liquid and injection etc., wherein uses more convenient with oral liquid.Ivermectin dissolubility in water is low, but has fat-solubility, and therefore, ivermectin oral liquid on the market is oil preparation oral liquid.Up to now, still there is no ivermectin water solublity oral liquid both at home and abroad, it is contemplated that, ivermectin water solublity oral liquid has wide market prospect.
Summary of the invention
In view of this, it is an object of the invention to provide a kind of ivermectin water solublity oral liquid for animals and preparation method thereof, ivermectin is made uniform and stable water solublity oral liquid, and production cost is lower, absorb good.
For reaching above-mentioned purpose, the present invention provides following technical scheme:
The ivermectin water solublity oral liquid for animals of the present invention, every 1000mL oral liquid is composed of the following components:
Ivermectin 0.1 ~ 2g；
Ethyl acetate 1 ~ 20mL；
Tween 80 50 ~ 150mL；
Disodium hydrogen phosphate 1 ~ 10g；
Sodium dihydrogen phosphate 1 ~ 10g；
Thimerosal 0.001 ~ 1g；
Surplus is water.
The optimization formula of the ivermectin water solublity oral liquid for animals of the present invention, every 1000mL oral liquid is composed of the following components:
Ivermectin 0.8g；
Ethyl acetate 9mL；
Tween 80 100mL；
Disodium hydrogen phosphate 4.5g；
Sodium dihydrogen phosphate 4g；
Thimerosal 0.01g；
Surplus is water.
Further, the pH value of described oral liquid is 5.7 ~ 6.5.
The preparation method of the ivermectin water solublity oral liquid for animals of the present invention, comprises the following steps:
(1) accurately weigh the ivermectin of recipe quantity, be stirred for dissolving by the ethyl acetate of recipe quantity, add the tween 80 of recipe quantity, after stirring, add water while stirring；
(2) adding after being dissolved by the thimerosal of recipe quantity with water in the solution system of step (1), after stirring, add water constant volume, adds disodium hydrogen phosphate and pH value is adjusted 5.7 ~ 6.5 by sodium dihydrogen phosphate, filter, obtain ivermectin water solublity oral liquid for animals.
The beneficial effects of the present invention is:
It is water that the present invention prepares the solvent of oral liquid, ivermectin dissolubility in water is low, after but the ethyl acetate of heavy dose and tween 80 hydrotropy dissolve ivermectin, add water and solution can be made uniform, therefore, ivermectin water solublity oral liquid prepared by the present invention is uniform and stable, shelf lives is long, and compared with oil preparation oral liquid, to oral mucosa nonirritant, production cost is lower, absorbs good.
Detailed description of the invention
The preferred embodiments of the present invention will be described in detail below.
Embodiment 1
The preparation method of the ivermectin water solublity oral liquid for animals of the present embodiment, comprises the following steps:
(1) accurately weigh 80g ivermectin, be stirred for dissolving by 900mL ethyl acetate, add 10L tween 80, after stirring, add water while stirring；
(2) add after 1g thimerosal being dissolved with water in the solution system of step (1), after stirring, add water and be settled to 100L, add disodium hydrogen phosphate 450g and sodium dihydrogen phosphate 400g, pH value is adjusted to 6.2, filters, obtain ivermectin water solublity oral liquid for animals.
Embodiment 2
The preparation method of the ivermectin water solublity oral liquid for animals of the present embodiment, comprises the following steps:
(1) accurately weigh 50g ivermectin, be stirred for dissolving by 400mL ethyl acetate, add 6L tween 80, after stirring, add water while stirring；
(2) add after 0.5g thimerosal being dissolved with water in the solution system of step (1), after stirring, add water and be settled to 100L, add disodium hydrogen phosphate 300g and sodium dihydrogen phosphate 400g, pH value is adjusted to 5.8, filters, obtain ivermectin water solublity oral liquid for animals.
Embodiment 3
The preparation method of the ivermectin water solublity oral liquid for animals of the present embodiment, comprises the following steps:
(1) accurately weigh 150g ivermectin, be stirred for dissolving by 1.5L ethyl acetate, add 15L tween 80, after stirring, add water while stirring；
(2) add after 50g thimerosal being dissolved with water in the solution system of step (1), after stirring, add water and be settled to 100L, add disodium hydrogen phosphate 900g and sodium dihydrogen phosphate 800g, pH value is adjusted to 6.5, filters, obtain ivermectin water solublity oral liquid for animals.
Clinical trial
The ivermectin water solublity oral liquid of embodiment 1 ~ 3 and ivermectin oil preparation oral liquid are done the comparison of insecticidal activity aspect: the same group sheep choosing natural infection nematicide carries out being randomly divided into 4 groups, 4 groups respectively by the ivermectin water solublity oral liquid of the embodiment 1 ~ 3 of respective bodyweight p 0.2mg/kg and ivermectin oil preparation oral liquid, each treated animal worm's ovum number in test forward and backward counting respectively feces, calculate deworming rates, and observe medicine animal is had no side effect, result is in Table 1.
As shown in Table 1, the ivermectin water solublity oral liquid of embodiment 1 ~ 3 is suitable with the anthelminthic effect of ivermectin oil preparation oral liquid, and animal has no adverse reaction after using recommended dose (0.2mg/kg), illustrates that animal is safe by the ivermectin water solublity oral liquid of embodiment 1 ~ 3.
What finally illustrate is, preferred embodiment above is only in order to illustrate technical scheme and unrestricted, although the present invention being described in detail by above preferred embodiment, but skilled artisan would appreciate that, in the form and details it can be made various change, without departing from claims of the present invention limited range.
Claims (4)
1. an ivermectin water solublity oral liquid for animals, it is characterised in that: every 1000mL oral liquid is composed of the following components:
Ivermectin 0.1 ~ 2g；
Ethyl acetate 1 ~ 20mL；
Tween 80 50 ~ 150mL；
Disodium hydrogen phosphate 1 ~ 10g；
Sodium dihydrogen phosphate 1 ~ 10g；
Thimerosal 0.001 ~ 1g；
Surplus is water.
2. ivermectin water solublity oral liquid for animals according to claim 1, it is characterised in that: every 1000mL oral liquid is composed of the following components:
Ivermectin 0.8g；
Ethyl acetate 9mL；
Tween 80 100mL；
Disodium hydrogen phosphate 4.5g；
Sodium dihydrogen phosphate 4g；
Thimerosal 0.01g；
Surplus is water.
3. ivermectin water solublity oral liquid for animals according to claim 1 and 2, it is characterised in that: the pH value of described oral liquid is 5.7 ~ 6.5.
4. the preparation method of the ivermectin water solublity oral liquid for animals described in claims 1 to 3 any one, it is characterised in that: comprise the following steps:
(1) accurately weigh the ivermectin of recipe quantity, be stirred for dissolving by the ethyl acetate of recipe quantity, add the tween 80 of recipe quantity, after stirring, add water while stirring；
(2) adding after being dissolved by the thimerosal of recipe quantity with water in the solution system of step (1), after stirring, add water constant volume, adds disodium hydrogen phosphate and pH value is adjusted 5.7 ~ 6.5 by sodium dihydrogen phosphate, filter, obtain ivermectin water solublity oral liquid for animals.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410793149.XA CN105748403A (en) | 2014-12-20 | 2014-12-20 | A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410793149.XA CN105748403A (en) | 2014-12-20 | 2014-12-20 | A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105748403A true CN105748403A (en) | 2016-07-13 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410793149.XA Pending CN105748403A (en) | 2014-12-20 | 2014-12-20 | A water-soluble ivermectin oral liquid for veterinary use and a preparing method thereof |
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| Country | Link |
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| CN (1) | CN105748403A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107802599A (en) * | 2017-12-08 | 2018-03-16 | 宁夏大学 | Development and application method of a kind of camel with drinking water type expelling parasite solution |
| EP3326608A1 (en) * | 2016-11-24 | 2018-05-30 | Nestlé Skin Health SA | Composition comprising avermectin compounds without solid fatty substances |
| CN119326713A (en) * | 2024-08-08 | 2025-01-21 | 河北威远药业有限公司 | A kind of preparation method of ivermectin aqueous solution |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1158251A (en) * | 1996-11-08 | 1997-09-03 | 王玉万 | Animal anti-parasite oral liquor containing avilamycin or envimycin |
-
2014
- 2014-12-20 CN CN201410793149.XA patent/CN105748403A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1158251A (en) * | 1996-11-08 | 1997-09-03 | 王玉万 | Animal anti-parasite oral liquor containing avilamycin or envimycin |
Cited By (3)
| 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 |
| CN107802599A (en) * | 2017-12-08 | 2018-03-16 | 宁夏大学 | Development and application method of a kind of camel with drinking water type expelling parasite solution |
| CN119326713A (en) * | 2024-08-08 | 2025-01-21 | 河北威远药业有限公司 | A kind of preparation method of ivermectin aqueous solution |
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Application publication date: 20160713 |
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