CN102302454A - Animal intestinal slow-releasing parasiticide and preparation method - Google Patents

Animal intestinal slow-releasing parasiticide and preparation method Download PDF

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Publication number
CN102302454A
CN102302454A CN201110207876A CN201110207876A CN102302454A CN 102302454 A CN102302454 A CN 102302454A CN 201110207876 A CN201110207876 A CN 201110207876A CN 201110207876 A CN201110207876 A CN 201110207876A CN 102302454 A CN102302454 A CN 102302454A
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aqueous solution
animal
intermediate layer
top layer
binding agent
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CN201110207876A
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CN102302454B (en
Inventor
刘鼎阔
王立红
张勇
董惠峰
张俊霞
张凤洪
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Tianjin aotailai Biotechnology Co., Ltd
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Dingzheng Animal Pharmaceutical Tianjin Co Ltd
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Priority to PCT/CN2012/078997 priority patent/WO2013013603A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5036Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention relates to an animal intestinal slow-releasing parasiticide, comprising a drug particle, a middle layer and a surface layer, wherein the middle layer is wrapped on the outer surface of the drug particle, and the surface layer is wrapped on the outer surface of the middle layer. The invention adopts a structure of three layers that the middle layer is wrapped on the outer surface of the drug particle and the surface layer is wrapped on the outer surface of the middle layer, the slow-releasing effect of the drug is achieved by the middle layer and the surface layer, therefore, the drug is avoided to be decomposed and destructed in stomach, the stimulation and adverse reaction to the stomach caused by the drug is also prevented, furthermore the drug keeps a high concentration in blood for a long time in animal bodies, the stability and the bioavailability of the drug are both high, the retention time is long, the administration frequency and amount are reduced, and the parasites in the animal bodies can be prevented for a long time or be killed.

Description

A kind of animal and bird intestines slow release anthelmintic and preparation method thereof
Technical field
The invention belongs to the poultry technical field of pharmaceuticals, especially a kind of animal and bird intestines slow release anthelmintic and preparation method thereof.
The background technology parasite mainly is through consuming poultry endotrophic material, cause damage, make the utilization rate decline of poultry to feedstuff to poultry to the harm of poultry, thereby causes growth of animals or poultry slowly or nutrition for want of and death.In addition, parasitic disease can cause that also livestock and poultry production performance reduces, the quality of animal products reduces, bring problems such as other infectious disease, zoonosis to poultry.
At present; Each manufacturer develop have wide spectrum, the multiple anti-parasite medicine of characteristics such as safety; But these medicines can be destroyed at stomach, have reduced drug effect, and stomach is had tangible zest; And also not having the intravital parasite of control poultry that a kind of anti-parasite medicine can the long period so far, this has brought the technical difficulty of selection medicine for peasant household and plant.
Summary of the invention
The objective of the invention is to overcome the weak point of prior art, enteral slow release, long action time, stable high a kind of animal and bird intestines slow release anthelmintic are provided.
The technical scheme that the present invention adopts is:
A kind of animal and bird intestines slow release anthelmintic comprises drug particles, intermediate layer and top layer, and the intermediate layer is coated on the drug particles outer surface, and the top layer is coated on the outer surface in intermediate layer,
Said drug particles is mixed and made into by doing mixed thing and binding agent; Do mixed thing and comprise 2~4 parts lactose, 5~10 parts hydroxymethyl starch, 1~5 part microcrystalline Cellulose, 0.2~3 part sodium lauryl sulphate, 20~50 parts albendazole and 1~5 part ethopabate, binding agent comprises hydroxy methocel aqueous solution and ethanol;
Said intermediate layer comprises 10~50 parts mannitol and hydroxy methocel aqueous solution;
Said top layer comprises cellulose phthalate aqueous solution and ethanol.
And the concentration of the hydroxy methocel aqueous solution in said binding agent and the intermediate layer is 4%, and 95% ethanol is used on said binding agent and top layer.
And the concentration of the cellulose phthalate aqueous solution in the said top layer is 7~8%.
And hydroxy methocel aqueous solution and alcoholic acid weight ratio are 2: 8 in the said binding agent.
And cellulose phthalate aqueous solution and alcoholic acid weight ratio are 8: 2 in the said top layer.
Another object of the present invention provides a kind of method for preparing of animal and bird intestines slow release anthelmintic, and this method may further comprise the steps:
(1) by metering will do mix thing and binding agent mixing after, process drug particles;
(2) coat the intermediate layer at the drug particles outer surface;
(3) outer surface coats the top layer and processes semi-finished product in the intermediate layer;
(4) with making finished product after semi-finished product oven dry, the screening.
Advantage of the present invention and good effect are:
The present invention adopts three-decker, and in the outer surface coating intermediate layer of drug particles, outer surface coats the top layer in the intermediate layer; Realized the effect of medicament slow release through intermediate layer and top layer; Avoided medicine to destroy, also prevented stimulation and the untoward reaction of medicine, and medicine has kept the high blood drug level of long period in animal body stomach in the decomposition of gastric; Stability of drug and bioavailability are all very high; RT is long, has reduced administration number of times and dosage, can prevent or kill the intravital parasite of animal for a long time.
Description of drawings
Fig. 1 is a structural representation of the present invention.
The specific embodiment
Below in conjunction with embodiment, the present invention is further specified, following embodiment is illustrative, is not determinate, can not limit protection scope of the present invention with following embodiment.
A kind of animal and bird intestines slow release anthelmintic; Innovation of the present invention is: comprise drug particles 3, intermediate layer 2 and top layer 1; The intermediate layer is coated on the drug particles outer surface; The top layer is coated on the outer surface in intermediate layer; Drug particles is mixed and made into by doing mixed thing and binding agent, does mixed thing and comprises 2~4 parts lactose, 5~10 parts hydroxymethyl starch, 1~5 part microcrystalline Cellulose, 0.2~3 part sodium lauryl sulphate, 20~50 parts albendazole and 1~5 part ethopabate, and binding agent comprises hydroxy methocel aqueous solution and ethanol; The intermediate layer comprises 10~50 parts mannitol and hydroxy methocel aqueous solution; The top layer comprises cellulose phthalate aqueous solution and ethanol.
The concentration of the hydroxy methocel aqueous solution in binding agent and the intermediate layer is 4%; 95% ethanol is used on binding agent and top layer; The concentration of the cellulose phthalate aqueous solution in the top layer is 7~8%; Hydroxy methocel aqueous solution and alcoholic acid weight ratio are 2: 8 in the binding agent, and cellulose phthalate aqueous solution and alcoholic acid weight ratio are 8: 2 in the top layer.
The method for preparing of this animal and bird intestines slow release anthelmintic may further comprise the steps:
(1) 4 kilograms of lactose, 5 kilograms of hydroxymethyl starches, 2.3 kilograms of microcrystalline Cellulose, 2 kilograms of sodium lauryl sulphates, 20 kilograms of albendazoles and 4 kilograms of ethopabates are mixed and made into the dried thing that mixes.
(2) 0.12 kilogram of hydroxy methocel is dissolved in processes 4% hydroxy methocel aqueous solution in 2.88 kg of water, the ethanol of this hydroxy methocel aqueous solution and 12 kilogram 95% is mixed and made into binding agent.
(3) will do mix thing and binding agent mix homogeneously after, process drug particles through facility for granulating.
(4) 0.2 kilogram of hydroxy methocel is dissolved in processes 4% hydroxy methocel aqueous solution in 4.8 kg of water, behind this hydroxy methocel aqueous solution and 20 kilograms of mannitol mix homogeneously, evenly be coated on the drug particles outer surface that makes and form the intermediate layer.
(5) 30 kilograms of cellulose phthalates are dissolved in process 7.5% cellulose phthalate aqueous solution in 10 kg of water; With this cellulose phthalate aqueous solution with after 10 kilogram 95% ethanol mixes; Evenly be coated on the intermediate layer outer surface of the drug particles outer surface coating that makes, promptly make semi-finished product.
(6) with making finished product after semi-finished product oven dry, the screening.
The result of the animal and bird intestines slow release anthelmintic acid-resisting that makes test is as shown in table 1, and the result of animal and bird intestines slow release anthelmintic stability test is as shown in table 2, and the result of the test of animal and bird intestines slow release anthelmintic after by conventional administering mode is as shown in table 3.
Title The present invention The albendazole ordinary preparation
Content (mg/g) 82 83
PH value 1.5 following 4h content 2.1 1.3
PH value 7 following 0.5h content 80.3 78.4
Table 1: acid-resisting result of the test
Show that through test the present invention and ordinary preparation compare, the stomach juice-resistant destructiveness is stronger.
Figure BDA0000078066230000041
Table 2: the result of stability test
Show through test, good stability of the present invention, long-term storage does not have quality problems.
Figure BDA0000078066230000042
Table 3: the result of the test after the administration
Show that through test the present invention can keep higher blood drug level, bioavailability height can effectively prevent, kill endoparasite for a long time in vivo for a long time.
In sum, the outer surface of drug particles of the present invention coats the intermediate layer, and outer surface coats the top layer in the intermediate layer; Realized the effect of medicament slow release through intermediate layer and top layer, avoided medicine to destroy, also prevented stimulation and the untoward reaction of medicine stomach in the decomposition of gastric; And stability of drug and bioavailability are all very high; RT is long, has reduced administration number of times and dosage, can prevent or kill the intravital parasite of animal for a long time.

Claims (6)

1. animal and bird intestines slow release anthelmintic, it is characterized in that: comprise drug particles, intermediate layer and top layer, the intermediate layer is coated on the drug particles outer surface, and the top layer is coated on the outer surface in intermediate layer,
Said drug particles is mixed and made into by doing mixed thing and binding agent; Do mixed thing and comprise 2~4 parts lactose, 5~10 parts hydroxymethyl starch, 1~5 part microcrystalline Cellulose, 0.2~3 part sodium lauryl sulphate, 20~50 parts albendazole and 1~5 part ethopabate, binding agent comprises hydroxy methocel aqueous solution and ethanol;
Said intermediate layer comprises 10~50 parts mannitol and hydroxy methocel aqueous solution;
Said top layer comprises cellulose phthalate aqueous solution and ethanol.
2. a kind of animal and bird intestines slow release anthelmintic according to claim 1, it is characterized in that: the concentration of the hydroxy methocel aqueous solution in said binding agent and the intermediate layer is 4%, 95% ethanol is used on said binding agent and top layer.
3. a kind of animal and bird intestines slow release anthelmintic according to claim 1, it is characterized in that: the concentration of the cellulose phthalate aqueous solution in the said top layer is 7~8%.
4. according to claim 1 or 2 or 3 described a kind of animal and bird intestines slow release anthelmintics, it is characterized in that: hydroxy methocel aqueous solution and alcoholic acid weight ratio are 2: 8 in the said binding agent.
5. according to claim 1 or 2 or 3 described a kind of animal and bird intestines slow release anthelmintics, it is characterized in that: cellulose phthalate aqueous solution and alcoholic acid weight ratio are 8: 2 in the said top layer.
6. the method for preparing of a kind of animal and bird intestines slow release anthelmintic according to claim 1 is characterized in that: may further comprise the steps:
(1) by metering will do mix thing and binding agent mixing after, process drug particles;
(2) coat the intermediate layer at the drug particles outer surface;
(3) outer surface coats the top layer and processes semi-finished product in the intermediate layer;
(4) with making finished product after semi-finished product oven dry, the screening.
CN201110207876XA 2011-07-25 2011-07-25 Animal intestinal slow-releasing parasiticide and preparation method Expired - Fee Related CN102302454B (en)

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PCT/CN2012/078997 WO2013013603A1 (en) 2011-07-25 2012-07-23 Livestock intestinal sustained-release anthelmintic and preparation method therefor

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013013603A1 (en) * 2011-07-25 2013-01-31 鼎正动物药业(天津)有限公司 Livestock intestinal sustained-release anthelmintic and preparation method therefor
CN107296907A (en) * 2017-06-01 2017-10-27 江苏黄河药业股份有限公司 A kind of coating eraverm tablet and preparation method thereof
CN110833537A (en) * 2019-11-15 2020-02-25 三峡大学 Drug sustained-release material and application thereof to sustained-release material for treating proctitis

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1382445A (en) * 2001-04-23 2002-12-04 许晓全 Veterinary licking antihelmintic
CN101664417A (en) * 2009-09-08 2010-03-10 武威红牛农牧科技有限公司 Niclofolan-contained compound sustained-release animal parasiticide
CN101773467A (en) * 2010-01-20 2010-07-14 北京大北农动物保健科技有限责任公司 Milbemycin or milbemycin oxime sustained-release injection for animals and preparation method

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102302454B (en) * 2011-07-25 2012-12-12 鼎正动物药业(天津)有限公司 Animal intestinal slow-releasing parasiticide and preparation method

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1382445A (en) * 2001-04-23 2002-12-04 许晓全 Veterinary licking antihelmintic
CN101664417A (en) * 2009-09-08 2010-03-10 武威红牛农牧科技有限公司 Niclofolan-contained compound sustained-release animal parasiticide
CN101773467A (en) * 2010-01-20 2010-07-14 北京大北农动物保健科技有限责任公司 Milbemycin or milbemycin oxime sustained-release injection for animals and preparation method

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013013603A1 (en) * 2011-07-25 2013-01-31 鼎正动物药业(天津)有限公司 Livestock intestinal sustained-release anthelmintic and preparation method therefor
CN107296907A (en) * 2017-06-01 2017-10-27 江苏黄河药业股份有限公司 A kind of coating eraverm tablet and preparation method thereof
CN110833537A (en) * 2019-11-15 2020-02-25 三峡大学 Drug sustained-release material and application thereof to sustained-release material for treating proctitis

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WO2013013603A1 (en) 2013-01-31

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Effective date of registration: 20200701

Address after: Unit 516, block a, No. 3, Huatian Road, Huayuan Industrial Zone, Binhai New Area, Tianjin

Patentee after: Tianjin aotailai Biotechnology Co., Ltd

Address before: 300402, No. 1, Jing Yuan Road, Beichen Science Park, Jin Wai highway, Beichen District, Tianjin

Patentee before: S & E Animal Pharmaceutical (TianJin) Co.,Ltd.

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