CN1158724A - Veterinary antiparasitic lincture contg. avermectin or invermectin - Google Patents

Veterinary antiparasitic lincture contg. avermectin or invermectin Download PDF

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CN1158724A
CN1158724A CN 96120433 CN96120433A CN1158724A CN 1158724 A CN1158724 A CN 1158724A CN 96120433 CN96120433 CN 96120433 CN 96120433 A CN96120433 A CN 96120433A CN 1158724 A CN1158724 A CN 1158724A
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avilamycin
linctus
veterinary antiparasitic
ethyl acetate
surfactant
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王玉万
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Abstract

The licture contains following components: ethyl acetate 5-15%, lanolin 10-60%, vaseline 10-50%, surfactant 0.3-20%, preservative 0.5-2%, dose 0.1-2% and avermectin or ivermectin 0.5-10%. It may also contain 1,2-propanediol, carboxymethyl cellulose, ethoxyl cellulose, talcum powder and other matter. Added imidazole medicine it can spread its worm-killing spectrum.

Description

The veterinary antiparasitic linctus that contains avilamycin or Ivermectin HCL
The present invention relates to the veterinary antiparasitic linctus, particularly a kind of veterinary antiparasitic linctus that contains avilamycin or Ivermectin HCL.
Found avilamycin (Avermectin) and Ivermectin HCL (Lvermectin) in 76 years, avilamycin is the metabolite of streptomycete (Streptomyces avermitilis), and Ivermectin HCL is the reduzate of avilamycin.Avilamycin and Ivermectin HCL have wide spectrum, anti-insect activity efficiently, and the eighties, U.S. Merck company succeeded in developing agricultural insecticide and anti-parasite medicine for animal use with these two kinds of materials, and put on market.
The mixture that avilamycin (Avermectin) is made up of eight quite similar homologues of structure.That is: Avermectin, A 1a, A 1b, A 2A, A 2b, B 1a, B 1b, B 2A, B 2bThe structural formula of relevant avilamycin is represented by following general formula:
Figure A9612043300041
Eight quite similar homologues compositions of structure are stated table 1 as follows in the above-mentioned general formula.
Table 1
Figure A9612043300051
In eight components of above-mentioned avilamycin, B 1AComponent is the component that insecticidal activity is the highest, insecticidal spectrum is the widest.But because of B 1AAnd B 1BIn suitability for industrialized production, be difficult to separate effectively, so that be widely used now is B 1AAnd B 1BRespectively account for certain proportion (B 1AAccount for more than 80% B 1BAccount for below 20%) the avilamycin mixture, be referred to as Avermectin B 1(being called for short AVM), and the hydrogenating reduction product Ivermectin HCL (IVM) of AVM.AVM and IVM have been widely used in the prophylactic treatment of the parasitic disease of animal in plant protection in the agricultural production and the animal husbandry.It all has the extremely strong effect of killing to extensively parasitizing animal body outer demodicid mite, Ticks, louse, fly larvae and intravital nematicide.
The most common dosage form is the back liniment of using with injection, powder, tablet, capsule and the cattle of avilamycin and Ivermectin HCL preparation at present, but the use inconvenience that has in the above-mentioned dosage form (as injection, powder, tablet etc.), the use cost height that has (using the back liniment) as cattle.
The object of the invention provides a kind of veterinary antiparasitic linctus that contains avilamycin or Ivermectin HCL, and this dosage form has to be used very conveniently, and cost is low, good effect, advantage such as insecticidal spectrum is extensive.
In order to achieve the above object, the present invention is by the following technical solutions:
Veterinary antiparasitic linctus (1) comprises following component: ethyl acetate 5-15%; Lanoline 10-60%; Vaseline 10-50%; Surfactant 0.3-20%; Correctives 0.1-2%; Antiseptic 0.5-2% (percentage by weight); AVM and IVM0.5-10%.
Veterinary antiparasitic linctus (11) comprises following component: ethyl acetate 5-15%; Surfactant 1-20%; Carboxymethyl cellulose 20-50% or hydroxyethyl-cellulose 20-50%; Water 5-15%; Pulvis Talci 5-25%; AVM or IVM0.5-5%.Linctus also can add an amount of correctives in (11).
Make compound linctus with AVM and IVM and imidazoles are composite, can enlarge insecticidal spectrum.Can kill parasites such as interior nematicide of body and external Ticks, louse, demodicid mite, fly larvae, can also kill cestode, trematodiasis etc. in the body, thereby drug cost is reduced, and reduce animal anthelmintic number of times.
Therefore the linctus that contains the imidazoles medicine of the present invention is formed: ethyl acetate 5-15%; Surfactant 1-10%; Lanoline 5-20%; Vaseline 5-20%; AVM or IVM1-3%; Imidazoles 25-70%.Also can add an amount of correctives.
In above-mentioned several veterinary antiparasitic linctus, AVM that is adopted or IVM purity are higher, and all about 90%, for this reason, the cost height the experiment proved that purity content, can adopt to contain avilamycin A 1, A 2, B 1, B 2Oily mixture substitute AVM or IVM prepares linctus.The preparation method of oily mixture is as follows: with the production streptomyces strain (Cstreptomyces avermitilis) of AVM, bacterial strain gets mycelium through 9 days fermentation after-filtration, with mycelium with organic solvent lixiviate, filtrations such as acetone or ethyl acetate, reclaim lixiviating solution, decolouring is also removed toxic substance (as oligomycin etc.) and afterwards, is evaporated to the ointment shape.In this ointment shape mixture, contain Avermectin A 13-10%, A 28-25%, B 16-25%, B 23-10%, lipid 10-30%, water 5-10%.Oily mixture by above method preparation adds surfactant 1-10%, lanoline 5-40%, ethyl acetate 5-10%, vaseline 20-40%, correctives 0.5-2% again, promptly can be made into linctus.
In above-mentioned several linctus prescriptions, the surfactant that is adopted can be a nonionic surfactant, also can be anionic.Surfactant commonly used has: polysorbas20-80; Span20-80; TX60-100 etc.
Excipient substrate such as the lanoline in the above-mentioned linctus, vaseline can use materials such as carboxymethyl cellulose, hydroxyethyl-cellulose, silicone, Cera Flava, calcium phosphate, Pulvis Talci to substitute.
Linctus of the present invention is compared with existing pharmaceutical dosage form has following advantage:
Tablet, powder and the injection used with cattle, sheep compare, and this linctus production technology is simple, and production cost is low, and is extremely easy to use.Compare with the back liniment with cattle commonly used, have the minimum advantage of dosage again, than cattle doubly, and on ease of use and drug effect, be equal to the back liniment with cattle with the low 1-1.5 of back liniment use cost.
The invention will be further described below in conjunction with example:
Example 1:
Take by weighing 70 gram AVM or IVM (purity 90%) and place material-compound tank, add 150 milliliters of ethyl acetate, be heated to 50-60 ℃, make it to dissolve fully, add 130 yuan of Tween 80s and 150 gram Span80 again, thoroughly add dissolved lanoline 700 grams and dissolved white vaseline 1200 grams behind the mixing, add correctives 1% at last, antiseptic 1%, thorough mixing, quality testing, packing, vanning warehouse-in.
Consumption, usefulness: 1. when being used for cattle, sheep anthelmintic, getting (diameter 1.5mm cylinder) 2.5 centimeter length by per 50 kg body weight with the dipstick metering of getting it filled is that 0.4 gram is licked cream (containing 10 milligrams of active ingredients), is applied in cattle, sheep lip, is the best to be applied to the inboard.
2. get a certain amount of cream of licking, make liquid emulsion in the ratio adding hot water (more than 60 ℃) of 1: 25 (licking cream weight in grams/water volume milliliter).When being used for cattle, sheep anthelmintic, gavage 10 milliliters of Emulsions by per 50 kg body weight, available company gavages device and gavages.When being used for the pig anthelmintic, per 10 kg body weight using dosages are 3 milliliters, can add in the feedstuff and feed.
Example 2:
Take by weighing 110 gram AVM and IVM (purity 90%) and place material-compound tank, add 330 milliliters of ethyl acetate, be heated to 50-60 ℃, make it to dissolve fully, add 50 gram Tween 80s and 70 gram Span80 again, thoroughly mix with deployed hydroxyl second fungin 1200 grams (water 200 gram/hydroxyethyl-celluloses 1000 restrain) of deployed carboxymethyl cellulose 1200 grams (water 200 gram/carboxymethyl celluloses 1000 grams) of water or water again behind the mixing, and then to wherein adding 240 gram Pulvis Talci mixings, add correctives 1%, thorough mixing, quality testing, packing, vanning warehouse-in.
Consumption, usage: when being used for cattle, sheep anthelmintic, getting (diameter 1.5mm cylinder) 2.5 centimeter length by per 50 kg body weight with the dipstick metering of getting it filled is that 0.2 gram is licked cream (containing 10 milligrams of active ingredients), is applied in cattle, sheep lip, is the best to be applied to the inboard.
Example 3:
Take by weighing 44 gram AVM or IVM (purity 90%) and place material-compound tank, add 88 milliliters of ethyl acetate, be heated to 50-60 ℃, make it to dissolve fully, add 30 gram Tween 80s and 50 gram Span80 again, thoroughly add dissolved lanoline 500 grams and dissolved white vaseline 270 grams behind the mixing, add Albendazole 1000 grams and correctives 20 grams (glucose: NaCL: KCL=20: 10: 3) then, thorough mixing, quality testing, packing, the vanning warehouse-in.
Consumption, usage: when being used for cattle, sheep anthelmintic, getting (diameter 1.5mm cylinder) 2.5 centimeter length by per 50 kg body weight with the dipstick metering of getting it filled is that 0.5 gram is licked cream (containing 10 milligrams of active ingredients), is applied in cattle, sheep lip, is the best to be applied to the inboard.
Example 4:
Get ointment shape mixture 500 grams that contain avilamycin B110%, add 50 milliliters of ethyl acetate, be heated to 50-60 ℃ of thoroughly dissolving, add 30 gram Tween 80s and 50 gram Span80 again, add dissolved lanoline 130 grams and dissolved white vaseline 240 grams behind the mixing, add correctives 1% again, thorough mixing, quality testing, packing, vanning warehouse-in.
Usage and dosage: 1. when being used for cattle, sheep anthelmintic, getting (diameter 1.5mm cylinder) 2.5 centimeter length by per 50 kg body weight with the dipstick metering of getting it filled is that 0.2 gram is licked cream (containing 10 milligrams of active ingredients), is applied in cattle, sheep lip, is the best to be applied to the inboard.
2. get a certain amount of cream of licking, make liquid emulsion in the ratio adding hot water (more than 60 ℃) of 1: 50 (licking cream weight in grams/water volume milliliter).When being used for cattle, sheep anthelmintic, gavage 10 milliliters of Emulsions by per 50 kg body weight, the available device that gavages continuously gavages.When being used for the pig anthelmintic, per 10 kg body weight using dosages are 3 milliliters, can add in the feedstuff and feed.

Claims (10)

1, a kind of A Weisu of containing for animals or add unguentum according to the plain parasiticide of dimension is characterized in that it comprises following component: ethyl acetate 5-15%, lanoline 10-60%, vaseline 10-50%, surfactant 0.3-20%, antiseptic 0.5-2%, correctives 0.1-2%, avilamycin B 1Crystallization product or Ivermectin HCL crystallization product 0.5-10%.
2, veterinary antiparasitic linctus as claimed in claim 1 is characterized in that described surfactant is selected from polysorbas20-80, Span20-80, one or more among the TX60-100.
3. veterinary antiparasitic linctus as claimed in claim 1 is characterized in that: described lanoline, vaseline excipient substrate are substituted by in carboxymethyl cellulose, hydroxyethyl-cellulose, silicone, Cera Flava, calcium phosphate, the Pulvis Talci one or more.
4. as veterinary antiparasitic linctus as claimed in claim 1, it is characterized in that also containing the imidazoles of 25-70%.
5. veterinary antiparasitic linctus as claimed in claim 1 is characterized in that licking the avilamycin B in the cream 1With containing avilamycin A 1, A 2, B 1, B 2Oily mixture substitute.
6. veterinary antiparasitic linctus as claimed in claim 1 is characterized in that containing avilamycin A in the said oily mixture 13-10%, avilamycin A 28-25%, avilamycin B 16-25%, avilamycin B 23-10%, lipid 10-30%, water 5-10%.
7. veterinary antiparasitic linctus as claimed in claim 6 is characterized in that said oily mixture prepares with following method:
Known production bacterial strain that will preparation avilamycin or Ivermectin HCL, after fermenting in 9 days, filter mycelium, with mycelium with organic molten Ji lixiviate, filtrations such as acetone or ethyl acetate, reclaim lixiviating solution, decolouring is also removed after the toxic substance, is evaporated to the ointment shape.
8, a kind of veterinary antiparasitic linctus is characterized in that it comprises following component (percentage by weight):
Ethyl acetate 5-15%
Surfactant 1-20%
Carboxymethyl cellulose 20-50%
Hydroxyethyl-cellulose 20-50%
Water 5-15%
Pulvis Talci 5-25%
Avilamycin or Ivermectin HCL 0.5-10%.
9, a kind of veterinary antiparasitic linctus is characterized in that it comprises following component (percentage by weight):
Ethyl acetate 5-15%
Surfactant 1-10%
Lanoline 5-20%
Vaseline 5-20%
Avilamycin or Ivermectin HCL 1-3%
Imidazoles 25-70%.
10, linctus for animals as claimed in claim 9 is characterized in that described imidazoles is an Albendazole.
CN 96120433 1996-10-30 1996-10-30 Veterinary antiparasitic lincture contg. avermectin or invermectin Pending CN1158724A (en)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1069033C (en) * 1998-11-13 2001-08-01 王玉万 Anti-parasite oral spray containing evericin and ivermectin for sheep
CN102231948A (en) * 2008-10-29 2011-11-02 托帕茨医药股份有限公司 Preservative system for emulsion-based therapeutic topical formulations
CN104288181A (en) * 2014-10-27 2015-01-21 武汉中博绿亚生物科技有限公司 Ointment for treating discomfort caused by expelling parasites on pet and preparation method of ointment
WO2017080520A1 (en) * 2015-11-13 2017-05-18 石家庄市兴柏生物工程有限公司 Method for extracting avermectin b2 from avermectin ointment
CN109700957A (en) * 2019-03-14 2019-05-03 临沂大学 A kind of avermectin Chinese herbal medicine extract cream and preparation method thereof for treating dog acarid disease

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1069033C (en) * 1998-11-13 2001-08-01 王玉万 Anti-parasite oral spray containing evericin and ivermectin for sheep
CN102231948A (en) * 2008-10-29 2011-11-02 托帕茨医药股份有限公司 Preservative system for emulsion-based therapeutic topical formulations
CN102231948B (en) * 2008-10-29 2015-08-19 托帕茨医药股份有限公司 For the preservative system of emulsion class treatment topical formulations
CN104288181A (en) * 2014-10-27 2015-01-21 武汉中博绿亚生物科技有限公司 Ointment for treating discomfort caused by expelling parasites on pet and preparation method of ointment
CN104288181B (en) * 2014-10-27 2018-05-04 武汉中博绿亚生物科技有限公司 It is a kind of to treat pet because expelling parasite causes paste for not relaxing and preparation method thereof
WO2017080520A1 (en) * 2015-11-13 2017-05-18 石家庄市兴柏生物工程有限公司 Method for extracting avermectin b2 from avermectin ointment
CN109700957A (en) * 2019-03-14 2019-05-03 临沂大学 A kind of avermectin Chinese herbal medicine extract cream and preparation method thereof for treating dog acarid disease
CN109700957B (en) * 2019-03-14 2021-04-06 临沂大学 Abamectin Chinese herbal medicine extract cream for treating dog acariasis and preparation method thereof

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