CN1943554A - Avermectins transdermal agent and preparing method - Google Patents

Avermectins transdermal agent and preparing method Download PDF

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Publication number
CN1943554A
CN1943554A CN 200610014920 CN200610014920A CN1943554A CN 1943554 A CN1943554 A CN 1943554A CN 200610014920 CN200610014920 CN 200610014920 CN 200610014920 A CN200610014920 A CN 200610014920A CN 1943554 A CN1943554 A CN 1943554A
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CN
China
Prior art keywords
avermectins
transdermal agent
avilamycin
azone
propylene glycol
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN 200610014920
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Chinese (zh)
Inventor
王连民
刘珂飞
张立花
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Tianjin Shengji Group Co Ltd
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Tianjin Shengji Group Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tianjin Shengji Group Co Ltd filed Critical Tianjin Shengji Group Co Ltd
Priority to CN 200610014920 priority Critical patent/CN1943554A/en
Publication of CN1943554A publication Critical patent/CN1943554A/en
Pending legal-status Critical Current

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  • Medicinal Preparation (AREA)

Abstract

The invention discloses a Avermectini transdermal medication and its preparation process, said medication is prepared as follows: alcohol of 40-60g and consistency of 95% heating to 30-60DEG C; adding Avermectini B1 0.2-0.7m, mixing till soluble; adding propylene glycol 25-50g and azone 2-5g successively and mixing.

Description

A kind of avermectins transdermal agent and preparation method
Technical field
The present invention relates to a kind of pharmaceutical composition, particularly relate to drug transdermal agent of a kind of anti-animal parasite disease and preparation method thereof.
Background technology
Colonize in the tame carcass such as cattle and sheep or the parasite of body surface can be caused the damage of organ, tissue to the host, capture nutrition or produce toxin, make that domestic animal such as cattle and sheep becomes thin, anemia, malnutrition, fertility performance descends, and severe patient can cause death.Can cause systemic toxicity and malnutrition as the sheep gastrointestinal nematode, endanger quite seriously, especially calf and sheep can cause large quantities of death.After cattle is infected, the farming ability drop, the milk cattle milk yield reduces, and this brings very big loss to animal husbandry, as untimely treatment, at last can be because of extremely weak and dead.Avilamycin is the novel Macrolide anti-parasite medicine that is produced by Avid kyowamycin.Avermectins medicine is because its excellent anthelmintic activity and higher safety, be considered at present that the best, most widely used general, a most salable class is novel, wide spectrum, efficient, safety and the little for animals anti-ecto-and endoparasites medicine of consumption, be widely used in veterinary clinic, in the control of poultry ecto-and endoparasites disease, brought into play important function.Drive away animal parasite in the general mode of for oral administration or drug administration by injection that adopts in the most of area of China at present, dosage forms such as pre-mixing agent, powder, solution, tablet, capsule, injection are generally arranged.But because the not compliance of domestic animal, so dosage forms such as pre-mixing agent, powder, solution, tablet, capsule exist the administration inconvenience, the shortcoming that first pass effect is big, and injection exists the shortcoming big to the domestic animal zest.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, a kind of avermectins transdermal agent is provided.
Second purpose of the present invention provides a kind of preparation method of avermectins transdermal agent.
Technical scheme of the present invention is summarized as follows:
A kind of avermectins transdermal agent is to make with following method: with the 40-60g concentration expressed in percentage by weight is that 95% ethanol is heated to 30-60 ℃; Add avilamycin B1 0.2-0.7mg stirring and dissolving; Add propylene glycol 25-50g successively, azone 2-5g stirs evenly.
Preferably: described 95% ethanol is 50g, and described avilamycin B1 is 0.5mg, and described propylene glycol is 40g, and described azone is 4g.
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 40-60g concentration expressed in percentage by weight to be that 95% ethanol is heated to 30-60 ℃; Add avilamycin B1 0.2-0.7mg stirring and dissolving; Add propylene glycol 25-50g successively, azone 2-5g stirs evenly.
Preferably: described 95% ethanol is 50g, and described avilamycin B1 is 0.5mg, and described propylene glycol is 40g, and described azone is 4g.
Advantage of the present invention: the present invention is owing to adopt preparation capable of permeating skin, and the carcass table medication of being in avoids oral drugs to be subjected to gastric acid, digestive enzyme and food effect when absorbing; Avoid the first pass effect of medicine; Sustainable control injection speed; And can make things convenient for interruption of the administration.
A kind of avermectins transdermal agent toxicity of the present invention is little, and cost is lower, and is easy to use, and treatment cattle parasitic disease can adopt direct cast or embrocates in body surface or embrocate in two in ear sides, and parasitic disease such as treatment sheep, dog, rabbit can adopt embrocates in two in ear sides.Because the stimulation that has changed administering mode, alleviated medicine can be used for treating domestic animal (as cattle, sheep, pig, dog, cat) parasitic disease.
The specific embodiment
The present invention is further illustrated below in conjunction with specific embodiment.
Embodiment 1
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 50g concentration expressed in percentage by weight to be that 95% ethanol is heated to 45 ℃; Add avilamycin B1 0.5mg stirring and dissolving; Add propylene glycol 40g successively, azone 4g stirs evenly.
Embodiment 2
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 40g concentration expressed in percentage by weight to be that 95% ethanol is heated to 30 ℃; Add avilamycin B1 0.2mg stirring and dissolving; Add propylene glycol 25g successively, azone 5g stirs evenly.
Embodiment 3
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 45g concentration expressed in percentage by weight to be that 95% ethanol is heated to 60 ℃; Add avilamycin B1 0.7mg stirring and dissolving; Add propylene glycol 50g successively, azone 2g stirs evenly.
Embodiment 4
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 50g concentration expressed in percentage by weight to be that 95% ethanol is heated to 40 ℃; Add avilamycin B1 0.3mg stirring and dissolving; Add propylene glycol 30g successively, azone 3g stirs evenly.
Embodiment 5
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 55g concentration expressed in percentage by weight to be that 95% ethanol is heated to 50 ℃; Add avilamycin B1 0.6mg stirring and dissolving; Add propylene glycol 45g successively, azone 4g stirs evenly.
Embodiment 6
A kind of preparation method of avermectins transdermal agent comprises the steps: with the 60g concentration expressed in percentage by weight to be that 95% ethanol is heated to 55 ℃; Add avilamycin B1 0.5mg stirring and dissolving; Add propylene glycol 35g successively, azone 3g stirs evenly.
Embodiment 7
Kill the sheep gastrointestinal nematode with a kind of avermectins transdermal agent of the present invention by the cast of 0.1ml/1kg body weight, the result is to the deworming rates of haemonchus contortus, hair garden nematicide, nematodirus, the first nematicide of hair, reach 100%, the deworming rates of oersted nematicide is respectively 9.7% and 100%.Be better than the subcutaneous injection administration with transdermal agent cast administering effect.
Embodiment 8
Kill the cattle parasite with a kind of avermectins transdermal agent of the present invention by the cast of 0.1ml/1kg body weight, can control parasitic infection such as psoroptes bovis, Bunostomum trigonoce phalum, the first nematicide of hair at duration of test (42 days) preferably.
Embodiment 9
The expeling rate of killing sheep gastrointestinal nematode adult by the cast of 0.1ml/1kg body weight with a kind of avermectins transdermal agent of the present invention is 99.85%, expeling rate to larva is 99.94%, expeling rate to the Protostrongylidae nematode larval is 100%, is 73.3% to the expeling rate of net filaria larva.
Embodiment 10
By 0.1ml/1kg body weight cast result worm's ovum negative conversion rate, worm's ovum slip and the deworming rates of gastrointestinal nematode is 100% with a kind of avermectins transdermal agent of the present invention, can all kills Oestrus ovis maggot, itch mite and sheep louse.
Embodiment 11
Use the avilamycin injection and treat the beef cattle mange and scab simultaneously by the cast of 0.1ml/1kg body weight, detect its effect by material anharmonic ratio, healing situation and average daily gain with a kind of avermectins transdermal agent of the present invention.Injection injection group and transdermal cast group cure rate are respectively 87.5% and 100%; The material anharmonic ratio was respectively 3.1: 1 and 2.4: 1; Average daily gain is respectively 0.79kg and 1.21kg, and the two compares difference extremely significantly (P<0.01) with the blank group.
The result shows, compares a kind of avermectins transdermal agent control of the present invention mange and scab better effects if with injection.
Embodiment 12
Use the avilamycin injection and press 0.1ml/1kg body weight cast treatment horse parasitic disease with a kind of avermectins transdermal agent of the present invention, the result shows that hematohidrosis disease, the horse botfly larva of a tapeworm or the cercaria of a schistosome, the circular section of horse nematicide, Trichonematidae nematicide, oxyuris equi etc. are all had significant repelling and killing efficacy.
Embodiment 13
Use the avilamycin injection and water 1 treatment psoroptes bovis and a mao louse by the 0.1ml/1kg body weight along dorsal line with a kind of avermectins transdermal agent of the present invention, after 7 days, acarid and hair louse slip are 100%, pruritus transference cure, effect obviously are better than using 0.5mg/kg body weight avilamycin subcutaneous injection group, and (after 7 days, the acarid slip is 98%, negative conversion rate is 90%, hair louse slip only is 60%, and does not have 1 example and turn out cloudy, and the pruritus symptom alleviates slightly).
Embodiment 14
Press the 0.1ml/1kg body weight with a kind of avermectins transdermal agent of the present invention, embrocate, 1 treatment dog ear demodicid mite, acaricide etc. in dog cat two in ear sides.Ear demodicid mite and acaricide slip are 100%, and the pruritus transference cure is after 7 days, and the acarid slip is 98%, and negative conversion rate is 90%, and the pruritus symptom alleviates slightly.

Claims (4)

1. avermectins transdermal agent is characterized in that making with following method: with the 40-60g concentration expressed in percentage by weight is that 95% ethanol is heated to 30-60 ℃; Add avilamycin B1 0.2-0.7mg stirring and dissolving; Add propylene glycol 25-50g successively, azone 2-5g stirs evenly.
2. a kind of avermectins transdermal agent according to claim 1 is characterized in that described 95% ethanol is 50g, and described avilamycin B1 is 0.5mg, and described propylene glycol is 40g, and described azone is 4g.
3. the preparation method of an avermectins transdermal agent, it is characterized in that comprising the steps: with the 40-60g concentration expressed in percentage by weight is that 95% ethanol is heated to 30-60 ℃; Add avilamycin B10.2-0.7mg stirring and dissolving; Add propylene glycol 25-50g successively, azone 2-5g stirs evenly.
4. the preparation method of a kind of avermectins transdermal agent according to claim 3 is characterized in that described 95% ethanol is 50g, and described avilamycin B1 is 0.5mg, and described propylene glycol is 40g, and described azone is 4g.
CN 200610014920 2006-07-27 2006-07-27 Avermectins transdermal agent and preparing method Pending CN1943554A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN 200610014920 CN1943554A (en) 2006-07-27 2006-07-27 Avermectins transdermal agent and preparing method

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN 200610014920 CN1943554A (en) 2006-07-27 2006-07-27 Avermectins transdermal agent and preparing method

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CN1943554A true CN1943554A (en) 2007-04-11

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106361686A (en) * 2015-07-21 2017-02-01 沈阳伟嘉牧业技术有限公司 Disophenol transdermal preparation, preparation method and medicinal applications thereof
CN107929230A (en) * 2017-12-26 2018-04-20 湖北回盛生物科技有限公司 A kind of external application avermectins transdermal agent and preparation method thereof
CN113209012A (en) * 2021-06-04 2021-08-06 湖南伟达科技有限公司 Avermectin transdermal solution and preparation method thereof

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106361686A (en) * 2015-07-21 2017-02-01 沈阳伟嘉牧业技术有限公司 Disophenol transdermal preparation, preparation method and medicinal applications thereof
CN107929230A (en) * 2017-12-26 2018-04-20 湖北回盛生物科技有限公司 A kind of external application avermectins transdermal agent and preparation method thereof
CN113209012A (en) * 2021-06-04 2021-08-06 湖南伟达科技有限公司 Avermectin transdermal solution and preparation method thereof

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Open date: 20070411