CN102895180A - Parasitic disease resistant compound triclabendazole transdermal solution for cattle and sheep and preparation method thereof - Google Patents
Parasitic disease resistant compound triclabendazole transdermal solution for cattle and sheep and preparation method thereof Download PDFInfo
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- CN102895180A CN102895180A CN2012103794333A CN201210379433A CN102895180A CN 102895180 A CN102895180 A CN 102895180A CN 2012103794333 A CN2012103794333 A CN 2012103794333A CN 201210379433 A CN201210379433 A CN 201210379433A CN 102895180 A CN102895180 A CN 102895180A
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Abstract
The invention relates to a parasitic disease resistant compound triclabendazole transdermal solution for cattle and sheep and a preparation method thereof. The transdermal solution consists of the following components in parts by volume: 25 to 35 parts of ethyl acetate, 20 to 30 parts of dimethyl sulfoxide, 2 to 6 parts of azone, 1 to 3 parts of isopropanol, and 50 to 70 parts of ethanol; every 100ml of solution contains 2.5 to 5 grams of triclabendazole and 0.5 to 2 grams of levamisole hydrochloride; and the finished product is prepared by weighing, preparing, circulating, filtering and filling. The method is simple in production equipment, easy to operate, convenient to use and suitable for expanded production; and the transdermal solution fills the blank of domestic veterinary drugs in certain dosage forms, innovates the administration route, and is widely applied to prevention and treatment of parasitic diseases such as fasciola hepatica and gastrointestinal nematodiasis of the cattle and the sheep.
Description
Technical field
The invention belongs to field of medicine preparing technology, the especially a kind of cattle and sheep sick compound recipe triclabendazole of parasiticide transdermal solution and preparation method thereof.
Background technology
Preparation capable of permeating skin is the novel form of percutaneous dosing, and namely the transdermal blood capillary of medicine enters whole body and reaches effective blood drug concentration through blood circulation, and medicine is in each tissue or diseased region performance treatment or prophylactic effect.Compare with ordinary preparation, preparation capable of permeating skin has to be avoided crossing effect and gastrointestinal deactivation etc. by the side effect of the initiations such as oral administration and gastrointestinal administration, the advantage of keeping constant blood drug level, prolonging three aspects such as effective acting time such as liver.
Triclabendazole is the medicine that is exclusively used in anti-fasciola in the benzimidazole, and the liver-plate shape trematodiasis of various ages in days is all had obvious repelling and killing efficacy.To ruminant distoma hepaticum such as cattle, sheep and goats, all effective to cattle Fasciola gigantica, deer distoma hepaticum, deer Fasciola gigantica and Hepar Equi sheet trematodiasis etc.This product is for oral administration easily from gastrointestinal absorption.Bioavailability is higher, 24-36 hour blood medicine peaking behind goat and the sheep triclabendazole for oral administration, and dog and rabbit reached blood medicine peak value in rear 8 hours for oral administration, and the blood medicine peak value of its prototype and metabolite thereof is 5-20 times of other benzimidazole anthelmintics.This product major part in cattle, sheep, dog and rabbit body is oxidized to sulfoxide, sulfone, ketone and 4-hydroxy derivatives, these derivants and albumin bound, and in blood plasma, continue more than 7 days.After the sheep medication 10 days, have approximately 95% medicine to be discharged by feces, 2% through the urine discharge, by the less than 1% of milk discharge.This product is discharged slowly, and the half-life of goat, sheep is about 22 days.
Levamisole hydrochloride is a kind of wide spectrum nematicide, and most of nematicides of horse, cattle, sheep, pig, dog and chicken are had activity.Mechanism is parasympathetic and the sympathetic ganglion of excited responsive anthelmintic, shows as nicotinic action, by blocking-up Fumaric acid and succinate oxidation effect, disturbs the carbohydrate metabolism of nematicide, and the anesthesia anthelmintic is discharged living worm body.Except having anthelmintic activity, can also obviously improve immunoreation.Adult to abomasum nematicide, small intestinal nematicide, large intestine nematicide and the thread lungworm of cattle and sheep has good activity.
Parasite mainly is by the nutrient substance in the consumption cattle and sheep body to the harm of cattle and sheep, causes mechanical damage, or lacks nutrition, and cattle and sheep are descended to the utilization rate of feedstuff, causes the cattle and sheep poor growth, and efficiency of feed utilization reduces.At present, parasiticide class drug use the most widely dosage form is injection, tablet and dashing agent, and wherein dashing agent is take external anthelmintic as main, and it is few really to use the mechanism of action of Transdermal absorption to carry out the medicine of inside and outside anthelmintic.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, the cattle and sheep of propose that a kind of route of administration is new, side effect is little, drug action longer duration, individual variation are little and easy to use are with the sick compound recipe triclabendazole of parasiticide transdermal solution and preparation method thereof.
The present invention realizes that the technical scheme of purpose is:
A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide transdermal solution, it is as follows to consist of component and content: volume parts
It is the 2.5-5%g/ml of above-mentioned medicinal liquid cumulative volume that triclabendazole adds quality;
It is the 0.5-2%g/ml of above-mentioned medicinal liquid cumulative volume that levamisole hydrochloride adds quality.
A kind of cattle and sheep preparation method of the sick compound recipe triclabendazole of parasiticide transdermal solution, it is characterized in that: the step of preparation is:
⑴ under agitation put into 35-40 ℃ of ethyl acetate to fully dissolving with the triclabendazole of recipe quantity, obtains triclabendazole solution, for subsequent use;
⑵ under agitation put into the levamisole hydrochloride of recipe quantity the ethanol of recipe quantity 1/3 to fully dissolving, obtains levamisole hydrochloride solution, for subsequent use;
⑶ with dimethyl sulfoxide, isopropyl alcohol, the azone of recipe quantity, mix homogeneously;
⑷ add ⑴ and ⑵ among the ⑶, is settled to full dose with remaining ethanol dilution after mixing;
⑸ to the qualified rear fill of clarity, namely get compound recipe triclabendazole transdermal solution with filtering with microporous membrane.
And described microporous filter membrane aperture is 1.2 μ m.
Advantage of the present invention and beneficial effect are:
1, the present invention has innovated the anti-parasite medicine route of administration, in its prescription azone and dimethyl sulfoxide medication after 12 hours transit dose reach 92.6%, transit dose is above standard, demonstrated fully the preparation advantage that percutaneous is absorbed in the parasiticide disease, the important breakthrough of the sick preparation processing technology of domestic parasiticide, for new way has been opened up in the sick treatment of domestic parasiticide.
2, the azone that relates in the present invention's prescription is novel dermal osmosis accelerator, it can increase skin to the percutaneous absorption of many dissimilar medicines, the medicinal liquid that contains azone of preparation enters the corium blood capillary through the appendages space and is absorbed, can effectively avoid liver to cross effect, reduce the medicine resolution ratio, avoid the peak valley phenomenon of drug absorption process, reduced the toxic and side effects that the factors such as medicine or dosage cause, prolong effective acting time, change the administration area, and effectively regulate dosage, reduce interindividual variation, have and use simply, convenient, characteristics are more suitable for the antiparasitic control in pastoral area than other dosage form efficiently.
3, the technique that the present invention relates to has simple, the processing ease of production equipment, advantage easy to use, as to be fit to expanding production, remedied domestic veterinary drug market in the blank of some dosage form, innovate route of administration, be widely used in the control of the parasitic disease such as control cattle and sheep distoma hepaticum, Biocontrol of Gastrointestinal Nematodes.
4, the azone that the present invention relates to is novel dermal osmosis accelerator, can increase skin to the percutaneous absorption of many dissimilar medicines, effectively avoid liver to cross effect, avoid the peak valley phenomenon of drug absorption process, reduced the relevant toxic and side effects that causes with dosage of medicine, prolong effective acting time, change the administration area, effectively regulate dosage, reduce interindividual variation, have use simply, characteristics easily and efficiently, be more suitable for the antiparasitic control in pastoral area and kill than other dosage form.
The specific embodiment
The invention will be further described below by specific embodiment, and following examples are descriptive, is not determinate, can not limit protection scope of the present invention with this.
Among the following embodiment, needing to add triclabendazole in every 100ml medicinal liquid is 2.5-5g, and levamisole hydrochloride is 0.5-2g.
Embodiment 1:
A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide transdermal solution, it consists of component and parts by weight are respectively:
The crude drug of compound recipe triclabendazole transdermal solution involved in the present invention is triclabendazole and levamisole hydrochloride, and wherein the triclabendazole another name is: 5-chloro-6-(2,3-dichlorophenoxy)-2-methyl mercapto-1H-benzimidazole; The levamisole hydrochloride another name is: (S)-(-)-6-phenyl-2,3,5, the 6-imidazolidine is [2,1-b] thiazole hydrochloride also.
A kind of cattle and sheep comprise the steps: with the sick compound recipe triclabendazole of parasiticide transdermal solution
⑴ under agitation put into 35-40 ℃ of ethyl acetate to fully dissolving with the triclabendazole of recipe quantity, obtains triclabendazole solution, for subsequent use;
⑵ under agitation put into the levamisole hydrochloride of recipe quantity the ethanol of recipe quantity 1/3 to fully dissolving, obtains levamisole hydrochloride solution, for subsequent use;
⑶ with dimethyl sulfoxide, isopropyl alcohol, the azone of recipe quantity, mix homogeneously;
⑷ add ⑴ and ⑵ among the ⑶, arrives full dose with the ethanol dilution standardize solution after mixing;
⑸ to the qualified rear fill of clarity, it is saturating namely to get the compound recipe triclabendazole with filtering with microporous membrane
Skin solution.
Embodiment 2:
A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide transdermal solution, it consists of component and parts by weight are respectively:
The step of present embodiment preparation method is same as embodiment 1.
Embodiment 3:
A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide transdermal solution, it consists of component and parts by weight are respectively:
The step of the preparation method of present embodiment is same as embodiment 1.
Detect data: the azone in this pharmaceutical formulation and dimethyl sulfoxide medication are after 12 hours, and its transit dose reaches 92.6%, and transit dose is above standard.
Claims (3)
1. cattle and sheep are with the sick compound recipe triclabendazole of parasiticide transdermal solution, and it is characterized in that: it is as follows to consist of component and content: volume parts
It is the 2.5-5%g/ml of above-mentioned medicinal liquid cumulative volume that triclabendazole adds quality;
It is the 0.5-2%g/ml of above-mentioned medicinal liquid cumulative volume that levamisole hydrochloride adds quality.
2. cattle and sheep as claimed in claim 1 are with the preparation method of the sick compound recipe triclabendazole of parasiticide transdermal solution, and it is characterized in that: the step of preparation is:
⑴ under agitation put into 35-40 ℃ of ethyl acetate to fully dissolving with the triclabendazole of recipe quantity, obtains triclabendazole solution, for subsequent use;
⑵ under agitation put into the levamisole hydrochloride of recipe quantity the ethanol of recipe quantity 1/3 to fully dissolving, obtains levamisole hydrochloride solution, for subsequent use;
⑶ with dimethyl sulfoxide, isopropyl alcohol, the azone of recipe quantity, mix homogeneously;
⑷ add ⑴ and ⑵ among the ⑶, is settled to full dose with remaining ethanol dilution after mixing;
⑸ to the qualified rear fill of clarity, namely get compound recipe triclabendazole transdermal solution with filtering with microporous membrane.
3. cattle and sheep according to claim 2 are with the preparation method of the sick compound recipe triclabendazole of parasiticide transdermal, and it is characterized in that: described microporous filter membrane aperture is 1.2 μ m.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2012103794333A CN102895180A (en) | 2012-09-29 | 2012-09-29 | Parasitic disease resistant compound triclabendazole transdermal solution for cattle and sheep and preparation method thereof |
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| CN2012103794333A CN102895180A (en) | 2012-09-29 | 2012-09-29 | Parasitic disease resistant compound triclabendazole transdermal solution for cattle and sheep and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106176586A (en) * | 2016-07-22 | 2016-12-07 | 柳州市柳南区安顺养殖协会 | A kind of cattle and sheep parasiticide disease iodo-ether salicylamine transdermal solution |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2124904A (en) * | 1982-08-13 | 1984-02-29 | Ciba Geigy Ag | Synergistic anthelmintic compositions |
| CN1857727A (en) * | 2006-03-13 | 2006-11-08 | 新疆维吾尔自治区畜牧科学院兽医研究所 | Animal skin penetrant |
-
2012
- 2012-09-29 CN CN2012103794333A patent/CN102895180A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2124904A (en) * | 1982-08-13 | 1984-02-29 | Ciba Geigy Ag | Synergistic anthelmintic compositions |
| CN1857727A (en) * | 2006-03-13 | 2006-11-08 | 新疆维吾尔自治区畜牧科学院兽医研究所 | Animal skin penetrant |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106176586A (en) * | 2016-07-22 | 2016-12-07 | 柳州市柳南区安顺养殖协会 | A kind of cattle and sheep parasiticide disease iodo-ether salicylamine transdermal solution |
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Application publication date: 20130130 |