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CN102872013A - Anti-parasitic disease compound Triclabendazole granule for flocks and herds and preparation method for anti-parasitic disease compound Triclabendazole granule - Google Patents

Anti-parasitic disease compound Triclabendazole granule for flocks and herds and preparation method for anti-parasitic disease compound Triclabendazole granule Download PDF

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Publication number
CN102872013A
CN102872013A CN2012104163507A CN201210416350A CN102872013A CN 102872013 A CN102872013 A CN 102872013A CN 2012104163507 A CN2012104163507 A CN 2012104163507A CN 201210416350 A CN201210416350 A CN 201210416350A CN 102872013 A CN102872013 A CN 102872013A
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China
Prior art keywords
triclabendazole
granule
compound recipe
parasitic disease
described adjuvant
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Pending
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CN2012104163507A
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Chinese (zh)
Inventor
元军英
范培柱
要瑞丽
范培松
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TIANJIN BIJIA PHARMACEUTICAL GROUP CO Ltd
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TIANJIN BIJIA PHARMACEUTICAL GROUP CO Ltd
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Priority to CN2012104163507A priority Critical patent/CN102872013A/en
Publication of CN102872013A publication Critical patent/CN102872013A/en
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Abstract

The invention belongs to the technical field of drug preparation and particularly relates to an anti-parasitic disease compound Triclabendazole granule for flocks and herds and a preparation method for the anti-parasitic disease compound Triclabendazole granule. The anti-parasitic disease compound Triclabendazole granule for the flocks and herds comprises the following components in parts by mass: 2.5-5 parts of Triclabendazole, 1-3 parts of levamisole hydrochloride and the balance auxiliary material. Compared with the prior art, the anti-parasitic disease compound Triclabendazole granule for the flocks and herds has the beneficial effects that as the Triclabendazole and the levamisole hydrochloride are combined for use, a disinsectization effect is better than that achieved by the addition of single components in the same proportion. Moreover, the recurrence rate is obviously reduced.

Description

A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide granule and preparation method thereof
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 granule and preparation method thereof.
Background technology
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, and 24-36 hour blood medicine peaking behind goat and the sheep triclabendazole for oral administration, the blood medicine peak value of its prototype and metabolite thereof are 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, approximately have 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.
But triclabendazole is used for the treatment of separately the cattle and sheep that infect fasciola and exists the drawback that indivedual residual, colony shows effect repeatedly.Because the gregarious habit of cattle and sheep is if any the residual recurrence that very easily causes colony.Therefore strive for that radical cure is problem demanding prompt solution.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, propose a kind of safe and efficient, compatibility rationally, the anthelmintic scope is wide and radical rate is high, mouthfeel is good, convenient drug administration, the simple a kind of cattle and sheep of technique be with the sick compound recipe triclabendazole of parasiticide granule and preparation method thereof.
The present invention realizes that the technical scheme of purpose is:
A kind of cattle and sheep contain following component and mass fraction thereof: triclabendazole 2.5-5 part with the sick compound recipe triclabendazole of parasiticide granule; Levamisole hydrochloride 1-3 part; All the other are adjuvant.
A kind of cattle and sheep sick compound recipe triclabendazole of parasiticide granule and preparation method thereof, step is:
⑴ 1/10 of the starch total amount made gelatinized corn starch during will write out a prescription, for subsequent use;
⑵ mix triclabendazole, levamisole hydrochloride, dextrin, sucrose, mannitol and the remaining starch of recipe quantity 20 minutes;
⑶ make soft material with ⑴ and ⑵ wet method, requires to hold agglomerating finger pressure namely loose, and 17 mesh sieves are granulated;
With obtain granule 65-75 ℃ dry 2-3 hour, the inspection of semifinished product, 17 mesh sieve granulate;
⑸ fragrant with the world, aspartame joins among the granule ⑷, always mixed 20 minutes;
⑹ packing namely gets compound recipe triclabendazole granule.
World perfume, aspartame and mannitol can be covered bitter taste of drug, improve mouthfeel and grains of sand sense, increase the domestic animal animal to the compliance of medicine, reduce loaded down with trivial details step and the administration time of raiser's administration.Granule is drying agent, produce and use procedure in be difficult for the generation dust, have steady quality, transportation, store, carry, use all more convenient; Mechanization production, output is large, and cost is low, and sanitary standard also easily reaches.
Compared with prior art, beneficial effect of the present invention is: triclabendazole and levamisole hydrochloride share, and anthelminthic effect is higher than the addition of single in proportion prescription, and obviously reduce relapse rate.
 
The specific embodiment
A kind of cattle and sheep contain following component and mass fraction thereof: triclabendazole 2.5-5 part with the sick compound recipe triclabendazole of parasiticide granule; Levamisole hydrochloride 1-3 part; All the other are adjuvant.
Described adjuvant has the fragrant 1-3 part in the world; (mass fraction, as follows.)
Described adjuvant has aspartame 1-2 part;
Described adjuvant has dextrin 20-30 part;
Described adjuvant has sucrose 10-20 part;
Described adjuvant has mannitol 0.5-2 part;
Described adjuvant has starch 40-60 part.
The described world is fragrant to be used for raiseeing.
 
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.
Triclabendazole 2.5-5 part; Levamisole hydrochloride 1-3 part;
The fragrant 1-3 part in the world; Aspartame 1-2 part;
Dextrin 20-30 part; Sucrose 10-20 part;
Mannitol 0.5-2 part; Starch 40-60 part.
Among the following embodiment, every bag of 100g contains triclabendazole 2.5-5g, hydrochloric levamisole 1-3g.
The every packed 100g granule of embodiment 1:(, following examples are same):
Triclabendazole 2.5kg
Levamisole hydrochloride 3 kg
Fragrant 1.5 kg in the world
Aspartame 1 kg
Dextrin 30 kg
Sucrose 20 kg
Mannitol 2 kg
Starch 40 kg
The crude drug of compound recipe triclabendazole granule 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.
Preparation method comprises the steps:
⑴ 1/10 of the starch total amount made gelatinized corn starch during will write out a prescription, for subsequent use;
⑵ mix triclabendazole, levamisole hydrochloride, dextrin, sucrose, mannitol and the remaining starch of recipe quantity 20 minutes;
⑶ make soft material with ⑴ and ⑵ wet method, requires to hold agglomerating finger pressure namely loose, and 17 mesh sieves are granulated;
With obtain granule 65-75 ℃ dry 2-3 hour, the inspection of semifinished product, 17 mesh sieve granulate;
⑸ fragrant with the world, aspartame joins among the granule ⑷, always mixed 20 minutes;
⑹ packing namely gets compound recipe triclabendazole granule.
Embodiment 2:
Prescription:
Triclabendazole 5 kg
Levamisole hydrochloride 1 kg
Fragrant 3 kg in the world
Aspartame 2 kg
Dextrin 20 kg
Sucrose 10 kg
Mannitol 0.5 kg
Starch 58.5k g.
 
The step of preparation method is same as embodiment 1.
Embodiment 3:
Prescription:
Triclabendazole 3.75 kg
Levamisole hydrochloride 1.5 kg
Fragrant 1.75 kg in the world
Aspartame 1.5 kg
Dextrin 20 kg
Sucrose 10 kg
Mannitol 1.5 kg
Starch 60kg
Preparation method is with embodiment 1.
 
Choose and be diagnosed as 300 cattle of fasciola, 300 sheep and 300 goats through excrement inspection and respectively be divided into 3 groups, every group each 100 give respectively compound recipe triclabendazole granule (every bag of 100g is watered 200kg, mixed drink); Triclabendazole granule (every bag of 100g is watered 200kg, mixed drink); Levamisole hydrochloride tablets (is got 100, smash to pieces, be watered 200kg, mixed drink), detected once in per 5 days before the medication 15 days, medication and after the medication, average and count following table, calculate the effective percentage that it is used for anti-fasciola, and after 3 months, carry out excrement inspection worm's ovum repetition measurement to curing domestic animal, calculate relapse rate:
Figure 43575DEST_PATH_IMAGE001
Advantage of the present invention is:
1, the present invention's compatibility of drugs of having innovated the parasiticide disease uses, and triclabendazole, levamisole hydrochloride coupling are unexpectedly effective.
2, world perfume, aspartame and the mannitol that relates in the present invention's prescription rationally uses and optimal proportion adds, can cover bitter taste of drug, improve mouthfeel and grains of sand sense, increase the domestic animal animal to the compliance of medicine, reduce loaded down with trivial details step and the administration time of raiser's administration.And melting is good, and bioavailability is high.Have use simply, characteristics easily and efficiently, be more suitable for the antiparasitic control in pastoral area than other products and dosage form.
3, the technique that the present invention relates to has that production equipment is simple, processing ease, advantage easy to use, as to be fit to expanding production, remedied the blank of domestic veterinary drug market aspect anti-parasite medicine, innovate the compound medicine of reasonable compatibility, be widely used in the control of the parasitic disease such as control cattle and sheep distoma hepaticum, Biocontrol of Gastrointestinal Nematodes.

Claims (9)

1. cattle and sheep contain following component and mass fraction thereof: triclabendazole 2.5-5 part with the sick compound recipe triclabendazole of parasiticide granule; Levamisole hydrochloride 1-3 part; All the other are adjuvant.
2. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has the fragrant 1-3 part in the world.
3. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has aspartame 1-2 part.
4. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has dextrin 20-30 part.
5. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has sucrose 10-20 part.
6. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has mannitol 0.5-2 part.
7. compound recipe triclabendazole granule according to claim 1 is characterized in that, described adjuvant has starch 40-60 part.
8. compound recipe triclabendazole granule according to claim 2 is characterized in that, the described world is fragrant to be used for raiseeing.
9. cattle and sheep are with the sick compound recipe triclabendazole of parasiticide granule and preparation method thereof, and step is: 1/10 of the starch total amount made gelatinized corn starch during ⑴ will write out a prescription, for subsequent use;
⑵ mix triclabendazole, levamisole hydrochloride, dextrin, sucrose, mannitol and the remaining starch of recipe quantity 20 minutes;
⑶ make soft material with ⑴ and ⑵ wet method, requires to hold agglomerating finger pressure namely loose, and 17 mesh sieves are granulated;
With obtain granule 65-75 ℃ dry 2-3 hour, the inspection of semifinished product, 17 mesh sieve granulate;
⑸ fragrant with the world, aspartame joins among the granule ⑷, always mixed 20 minutes;
⑹ packing namely gets compound recipe triclabendazole granule.
CN2012104163507A 2012-10-26 2012-10-26 Anti-parasitic disease compound Triclabendazole granule for flocks and herds and preparation method for anti-parasitic disease compound Triclabendazole granule Pending CN102872013A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106821995A (en) * 2017-02-22 2017-06-13 佛山市南海东方澳龙制药有限公司 Triclabendazole preparation and its preparation method and application
CN113318079A (en) * 2021-05-13 2021-08-31 江西博莱大药厂有限公司 Method for improving dissolution rate of triclabendazole particles and dissolution rate detection method thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2124904A (en) * 1982-08-13 1984-02-29 Ciba Geigy Ag Synergistic anthelmintic compositions

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2124904A (en) * 1982-08-13 1984-02-29 Ciba Geigy Ag Synergistic anthelmintic compositions

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
严亚军等: "三氯苯达唑治疗并殖吸虫病的研究进展", 《中国寄生虫病防治杂志》, vol. 18, no. 6, 31 December 2005 (2005-12-31), pages 471 - 472 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106821995A (en) * 2017-02-22 2017-06-13 佛山市南海东方澳龙制药有限公司 Triclabendazole preparation and its preparation method and application
CN106821995B (en) * 2017-02-22 2020-08-21 佛山市南海东方澳龙制药有限公司 Triclabendazole preparation and preparation method and application thereof
CN113318079A (en) * 2021-05-13 2021-08-31 江西博莱大药厂有限公司 Method for improving dissolution rate of triclabendazole particles and dissolution rate detection method thereof
CN113318079B (en) * 2021-05-13 2024-01-09 江西博莱大药厂有限公司 Method for improving dissolution rate of triclabendazole particles and dissolution rate detection method thereof

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Application publication date: 20130116