CN1193510A - Oily injection for preventing animals from parasites - Google Patents

Oily injection for preventing animals from parasites Download PDF

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Publication number
CN1193510A
CN1193510A CN98101716A CN98101716A CN1193510A CN 1193510 A CN1193510 A CN 1193510A CN 98101716 A CN98101716 A CN 98101716A CN 98101716 A CN98101716 A CN 98101716A CN 1193510 A CN1193510 A CN 1193510A
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China
Prior art keywords
injection
ivermectin
oil
avilamycin
oily injection
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CN98101716A
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Chinese (zh)
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王玉万
戴晓曦
潘贞德
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Individual
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Priority to CN98101716A priority Critical patent/CN1193510A/en
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Abstract

An oily injection as veterinary medicine for treating parasitosis contains vegetable oil or mineral oil as solvent (60-95%), avilamycin or ivermectin (0.1-10%) and cosolvent, and features high stability and effect, low cost, good suction and less damage to tissue.

Description

A kind of oily injection for preventing animals from parasites
The invention belongs to anti-parasite medicine for animal use, or rather, is a kind of oily injection for preventing animals from parasites that contains avilamycin or ivermectin.
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 interior nematicide of animal body and external demodicid mite, Ticks, louse, fly, maggot, used dosage form comprises powder, tablet, paste, oral liquid and injection, with injection curative effect the best.Making the used solvent of injection mainly is: 1,2-propylene glycol, glycerol formal etc., and 1,2-propylene glycol content in preparation too much has certain damage to tissue site, can cause injection site portion of tissue necrosis (Luo Mingsheng etc., " pharmaceutical necessities complete works ", Sichuan science tech publishing house during tight getting, 1993, P300); The glycerol formal price is more expensive, and consumption is many more in preparation, and production cost is just high more.
The objective of the invention is to overcome the shortcoming of prior art, propose that a kind of production cost is low, little to degree of tissue damage, the reliable solvent of drug effect makes anti-parasite medicine for animal use.
Realize the main technical schemes of purpose of the present invention: as main dispersing medium, make the oily injection that contains avilamycin (AVM) or ivermectin (IVM) with vegetable oil or mineral oil.
The concrete prescription of the present invention antibiosis worm for animals medicine and content (by weight percentage): avilamycin or ivermectin 0.1-10%, vegetable oil or mineral oil 60-95%, all the other are cosolvent; The best content of forming; All the other are cosolvent for avilamycin or ivermectin 0.5-2%, vegetable oil or mineral oil 80-93%.
Described avilamycin is the tunning of A Foman mycete (Streptomyces avremitilis), the mixture of being made up of eight quite similar homologues of structure, i.e. AvermectinA 1a, A 1b, A 2a, A 2b, B 1a, B 1b, B 2a, B 2bThe general B that uses more 1a, B 1bMixture, it can adopt existing technology extract and separate (William C.Campbell, " Ivermectinand Abamectin ", Springer-Verlag, New York Inc, 1989, P1-23).
Described ivermectin be avermitilis strain derivant (William C.Campbell, " Ivermectin and Abamectin " Springer-Verlag, New, York Inc, 1989, P1-23).
Described vegetable oil comprises Semen Maydis oil, Oleum sesami, Oleum Glycines, Oleum Arachidis hypogaeae semen, Oleum Ricini, rapeseed oil, Oleum Gossypii semen.
Described mineral oil is liquid paraffin.
Described cosolvent comprises ethanol, ethyl acetate, acetone.
The preparation method of the present invention's oil injection may further comprise the steps:
1. with an amount of cosolvent dissolving avilamycin or ivermectin;
2. add vegetable oil or mineral oil, stir;
3. detection, sterilization, packing warehouse-in.
The advantage of injection of the present invention:
Owing to adopt vegetable oil or mineral oil as making avilamycin merit ivermectin injection solvent, therefore production cost is lower, to the little and good absorbing of injection site tissue loss, stability of formulation is good, and anthelminthic effect with 1, avilamycin or ivermectin that 2-propylene glycol etc. is done solvent manufacturing are identical.
Further specify characteristics of the present invention below by instantiation:
Example 1
The preparation of this example ten days contains the oily injection of avilamycin 0.2%.
Get 0.21 kilogram of avilamycin (purity 95%), place 200 liters of batch tanks, add 10 liters of ethanol (pharmaceutical grade), stir, the dissolving back adds Oleum sesami (decolouring pharmaceutical grade) to 100 liters, stir, the sterilization of qualified after measured back, packing promptly obtain 0.2% avilamycin oil injection.
Example 2
The ivermectin oil injection of this example ten days preparation 9.5%.
Get 9.79 kilograms of ivermectins (purity 97%), place 200 liters of preparing tanks, add 10 liters of acetass, stir make it dissolving after, add Semen Maydis oil to 100 liter, stirring and evenly mixing, packing, sterilization promptly get 9.5% the oily injection of ivermectin.
Example 3
This example is the ivermectin oil injection of preparation 1%, and promptly ivermectin (purity is 97%) is 1.03 kilograms, places 200 liters of preparing tanks, add 20 liters of acetone stir make it dissolving after, add Semen Maydis oil to 100 liter, stirring and evenly mixing, packing, sterilization promptly gets 1% ivermectin oil injection.
Example 4
This example to oily injection of the present invention with 1, the 2-propylene glycol is the comparison that 1% avilamycin that makes of solvent or ivermectin injection are made the insecticidal activity aspect, the results are shown in Table 1.
The same group sheep of choosing the natural infection nematicide is divided into 4 groups at random, 4 groups of sheep are pressed avilamycin, ivermectin oil injection and commercially available avilamycin, the ivermectin injection of body weight subcutaneous injection 0.2mg/kg 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.
As shown in Table 1, oily injection of the present invention with 1, the 2-propylene glycol is the anthelminthic effect unanimity of solvent preparation avermitilis strain poison or ivermectin injection, and has no adverse reaction behind the animal using dosage 0.2mg/kg, illustrates that oily to penetrate liquid be safe to animal.
Example 5
This example is done the comparison of blood medicine kinetics aspect to 1% avilamycin of the present invention oil injection and commercially available 1% abamectin injection (with 1, the 2-propylene glycol is made solvent).
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.By drawing pharmaceutical concentration-time curve, and the result who calculates each materia medica parameter shows, the blood medicine peak concentration basically identical of the injection of two kinds of different solvents systems, the oil injection has peak time to be later than with 1, the 2-propylene glycol is made the injection of solvent, the persistent period of oil injection, it is long that the 2-propylene glycol is made the injection of solvent, shows that oily injection has slow releasing function than 1.
Example 6
This example is made toxicity research relatively to 1% avilamycin of the present invention and commercially available 1% abamectin injection (with 1, the 2-propylene glycol is made solvent).
Get healthy mice, establish various dose respectively, observe the dead animal number, calculate LD by simplifying karber's method 50The result shows, oily injection and 1, the LD of the injection of 2-propylene glycol preparation 50Unanimity is clinically tested oily injection through 1000 sheep and is not had untoward reaction.
In sum, oily injection of the present invention and commercially available 1,2-propylene glycol, glycerol formal are made the avilamycin of solvent preparation or the anthelminthic effect of ivermectin injection is consistent with toxicity, but the every milliliter of solvent cost of avermitilis strain injection with the vegetable oil preparation is a 0.015-0.020 unit, and with 1, the 2-propylene glycol is that the avilamycin made of solvent or every milliliter of solvent cost of ivermectin injection do not wait in 0.10-0.30 unit that (glycerol formal of adding is many more, cost is high more, but what add lacks, absorb badly, side reaction is big).This shows that from manufacturing cost, aspects such as clinical efficacy are taken all factors into consideration, utilize vegetable oil to be much better than with 1 for the avilamycin or the ivermectin oil injection of solvent, 2-propylene glycol, glycerol formal etc. are the avilamycin or the ivermectin injection of solvent.
Oily AVM/IVM injection of table 1. and common AVM/IVM injection 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
AVM oil injection in the example 1 ???0.2 ??100 ????100 ??100 ??100
IVM oil injection in the example 3 ???0.2 ??100 ????100 ??100 ??92.5
1%Ivomec* ???0.2 ??100 ????100 ??100 ??92.0
1% A Fuding injection * ???0.2 ??100 ????100 ??100 ??92.0
* 1%Ivonec is commercially available ivermectin injection (production of U.S. MSD Corp.), and 1% A Fuding injection is commercially available abamectin injection (New Tech. Development General Co., Beijing Agriculture Univ.'s production).

Claims (6)

1. an oily injection for preventing animals from parasites that contains avilamycin or ivermectin is characterized in that adopting vegetable oil or mineral oil to make main disperse medium, specifically forms content (by weight percentage):
Avilamycin or ivermectin 0.1-10%, vegetable oil or mineral oil 60-95%, all the other are cosolvent.
2. according to the described oily injection of claim 1, it is characterized in that forming content (by weight percentage): avilamycin or ivermectin 0.5-2%, vegetable oil or mineral oil 80-93%, all the other are cosolvent.
3. according to the described oily injection of claim 1, it 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.
4. according to the described oily injection of claim 1, it is characterized in that described mineral oil is liquid paraffin.
5. according to the described oily injection of claim 1, it is characterized in that cosolvent comprises ethanol, ethyl acetate, acetone.
6. the preparation method of the described oily injection of claim 1 is characterized in that preparation process is followed successively by: at first with cosolvent dissolving avilamycin or ivermectin, add vegetable oil or mineral oil again, stir, at last after testing, sterilization, packing warehouse-in.
CN98101716A 1998-04-23 1998-04-23 Oily injection for preventing animals from parasites Pending CN1193510A (en)

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CN98101716A CN1193510A (en) 1998-04-23 1998-04-23 Oily injection for preventing animals from parasites

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Cited By (4)

* 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
WO2004047803A1 (en) * 2002-11-27 2004-06-10 Eco Animal Health Ltd An injection of animal remedy including closantel or closantel sodium
CN103720652A (en) * 2014-01-07 2014-04-16 王玉万 Abamectin-drug-containing injection prepared from poloxamer and oily medium
CN103977017A (en) * 2014-06-03 2014-08-13 重庆布尔动物药业有限公司 Anti-parasitic injection for veterinary use and preparation method thereof

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
WO2004047803A1 (en) * 2002-11-27 2004-06-10 Eco Animal Health Ltd An injection of animal remedy including closantel or closantel sodium
CN103720652A (en) * 2014-01-07 2014-04-16 王玉万 Abamectin-drug-containing injection prepared from poloxamer and oily medium
CN103977017A (en) * 2014-06-03 2014-08-13 重庆布尔动物药业有限公司 Anti-parasitic injection for veterinary use and preparation method thereof
CN103977017B (en) * 2014-06-03 2016-09-07 重庆布尔动物药业有限公司 A kind of veterinary antiparasitic parenteral solution and preparation method thereof

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