CN101879141B - Taste-masking tilmicosin gastric-soluble particle preparation - Google Patents

Taste-masking tilmicosin gastric-soluble particle preparation Download PDF

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Publication number
CN101879141B
CN101879141B CN 200910014963 CN200910014963A CN101879141B CN 101879141 B CN101879141 B CN 101879141B CN 200910014963 CN200910014963 CN 200910014963 CN 200910014963 A CN200910014963 A CN 200910014963A CN 101879141 B CN101879141 B CN 101879141B
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Prior art keywords
tilmicosin
gastric
masking
taste
coating material
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CN 200910014963
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CN101879141A (en
Inventor
王永军
吕淑荣
梁玉
李春杰
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Yantai aisijin Animal Health Products Co.,Ltd.
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YANTAI GREEN LEAF ANIMAL HEALTH PRODUCTS CO Ltd
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Abstract

The invention relates to a taste-masking tilmicosin gastric-soluble particle preparation, in particular to a gastric-soluble particle preparation consisting of a gastric-soluble coating material, a high-polymer carrier, a disintegrating agent and the like and aims to solve the problem of poor palatability of tilmicosin.

Description

A kind of taste-masking tilmicosin gastric-soluble particle preparation
Technical field
The present invention relates to a kind of taste-masking tilmicosin gastric-soluble particle preparation, relate generally to a kind of gastric-soluble particle preparation that utilizes gastric solubleness coating material, macromolecule carrier, disintegrating agent etc. to form, to reach a difficult problem that solves tilmicosin palatability difference.
Background technology
Tilmicosin is the derivant of tylosin behind acid hydrolysis, it is semi-synthetic Macrolide animal specific antibiotic, its molecular formula is C46HS0N2O13, molecular weight 869.15, it is approved for clinical in countries such as Australia, Brazil, France, Malaysia, Italy, Spain, the U.S..Tilmicosin has the antibacterial activity similar to Macrocyclolactone lactone kind medicine, and is effective with some gram negative bacterias and mycoplasma to gram positive bacteria.Especially the specific activity tylosin to Actinobacillus pleuropneumoniae, pasteurella, staphylococcus aureus, streptococcus pyogenes, streptococcus pneumoniae, corynebacterium pyogenes and livestock and poultry mycoplasma is stronger.Be mainly used in treating animals such as cattle, goat, sheep, milch cow, pig, chicken clinically by the microbial infectious disease of sensitivity, particularly livestock and poultry respiratory tract infection and responsive microbial mammitis of cow.
But, because the palatability of tilmicosin raw material own is poor, seriously restricted its application in livestock and poultry prevention and treatment.At present, common tilmicosin preparation has products such as solution, injection, powder, pre-mixing agent on the market.Because of injection by oral, do not have the problem of palatability difference, but because clinical practice is more loaded down with trivial details, when the disease large-scale outbreak, can not make the practical performance maximum effect of tilmicosin; Other preparations such as solution, powder, pre-mixing agent etc. all belong to oral conventional formulation, all fail to solve the difficult problem of tilmicosin palatability difference.
The present invention is intended to by preparation process, utilizes the gastric solubleness packaging technique, makes the preparation of gained in the oral process of animal disintegrate not take place, has only just disintegrate absorption when medicine arrives in the poultry stomach, to reach a difficult problem that solves palatability.
Given this, the inventor passes through lot of experiments, invented a kind of taste-masking tilmicosin gastric-soluble particle preparation of forming with gastric solubleness coating material, macromolecule carrier, disintegrating agent, this preparation stability is relatively good, can significantly improve the difficult problem of tilmicosin palatability difference through the present invention of clinical trial proof.
Summary of the invention
Taste-masking tilmicosin gastric-soluble particle preparation involved in the present invention by weight percentage, mainly is the tilmicosin by 10-70%, 2-15% gastric solubleness coating material, and the macromolecule carrier of 80%-20%, the disintegrating agent of 0.2-1% is formed.
Wherein said gastric solubleness coating material is mainly hydroxypropyl emthylcellulose, hydroxypropyl cellulose, polyethylene acetal diethylin acetic acid, dimethylaminoethyl acrylate methyl chloro acetic acid-neutral metering system acetate copolymer, wherein preferred hydroxypropyl emthylcellulose, hydroxypropyl cellulose or the two mixture, and adding proportion is 2-15% (making the label weightening finish), preferred 6-10%.
Described macromolecule carrier mainly comprises microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, Polyethylene Glycol etc., wherein preferred low-substituted hydroxypropyl cellulose, Polyethylene Glycol, and its shared prescription weight ratio is 80-20%.
Described disintegrating agent mainly comprises PVP, sodium carboxymethyl cellulose, and its shared prescription weight ratio is 0.2-1%, preferred 0.5-0.8%.
Taste-masking tilmicosin gastric-soluble particle preparation technology of the present invention is mixed in proportion tilmicosin, macromolecule carrier, cross 60 mesh sieves, disintegrating agent is joined in the suitable binders, granulate, cross 12 mesh sieves behind the gained particle drying, with fluidized bed coating described gastric solubleness coating material is carried out coating then, cross 10 mesh sieve granulate behind the particle drying and both got taste-masking tilmicosin gastric-soluble particle preparation.
The specific embodiment
Embodiment 1
10 parts of tilmicosins
80 parts of low-substituted hydroxypropyl celluloses
1 part of sodium carboxymethyl cellulose
9 parts of hydroxypropyl emthylcelluloses
Embodiment 2
40 parts of tilmicosins
55 parts of microcrystalline Cellulose
0.5 part of PVP
4.5 parts of hydroxypropyl emthylcelluloses
Embodiment 3
70 parts of tilmicosins
20 parts of Polyethylene Glycol
0.2 part of sodium carboxymethyl cellulose
8.8 parts of hydroxypropyl emthylcelluloses
Preparation method (above three embodiment are by this method preparation): tilmicosin, macromolecule carrier are mixed in proportion, cross 60 mesh sieves, disintegrating agent is joined in the suitable binders, granulate, cross 12 mesh sieves behind the gained particle drying, coating material is prepared into 10% coating aqueous solution, and the gastric solubleness coating material that will prepare with fluidized bed coating carries out coating then, crosses 10 mesh sieve granulate behind the particle drying and has both got taste-masking tilmicosin gastric-soluble particle preparation.

Claims (1)

1. taste-masking tilmicosin gastric-soluble particle preparation, it is characterized in that, by weight percentage, main tilmicosin by 10-70%, 2-15% gastric solubleness coating material, the macromolecule carrier of 20%-80%, the disintegrating agent of 0.2-1% is formed, the gastric solubleness coating material is selected from hydroxypropyl emthylcellulose, hydroxypropyl cellulose, polyethylene acetal diethylin acetic acid, dimethylaminoethyl acrylate methyl chloro acetic acid-neutral metering system acetate copolymer, macromolecule carrier is selected from microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, Polyethylene Glycol, disintegrating agent is selected from PVP, sodium carboxymethyl cellulose, its preparation technology is:
A. tilmicosin, macromolecule carrier are mixed in proportion, cross 60 mesh sieves;
B. disintegrating agent is joined in the suitable binders, granulate, cross 12 mesh sieve granulate behind the gained particle drying;
C. the gastric solubleness coating material is prepared into certain density solution, with fluidized bed coating described gastric solubleness coating material is carried out coating then, cross 10 mesh sieves behind the particle drying, granulate namely gets taste-masking tilmicosin gastric-soluble particle preparation.
CN 200910014963 2009-05-05 2009-05-05 Taste-masking tilmicosin gastric-soluble particle preparation Active CN101879141B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
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Application Number Priority Date Filing Date Title
CN 200910014963 CN101879141B (en) 2009-05-05 2009-05-05 Taste-masking tilmicosin gastric-soluble particle preparation

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CN101879141A CN101879141A (en) 2010-11-10
CN101879141B true CN101879141B (en) 2013-07-17

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Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102688220B (en) * 2012-06-07 2014-07-30 湖州爱宝莱动物药业有限公司 Tilmicosin micro-capsule preparation and preparation method thereof
CN103083281B (en) * 2013-01-15 2015-01-07 广州格雷特生物科技有限公司 Enteric-coated tilmicosin slow-release micro-capsule preparation and preparation method thereof
CN104274411B (en) * 2014-10-28 2017-01-11 郑州合润生物制药有限公司 Tilmicosin micron preparation and preparation method thereof
CN104958764A (en) * 2015-06-05 2015-10-07 广西大学 Tilmicosin smell masking preparation and preparing method thereof
CN106074446B (en) * 2016-07-11 2019-03-22 郑州百瑞动物药业有限公司 Tilmicosin particle and preparation method thereof
CN108210936A (en) * 2016-12-13 2018-06-29 河南后羿实业集团有限公司 A kind of Tilmicosin inclusion compound and preparation method thereof
CN109464413A (en) * 2018-12-04 2019-03-15 中牧实业股份有限公司黄冈动物药品厂 A kind of Tilmicosin pellet and preparation method thereof

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CN1318369A (en) * 2000-04-17 2001-10-24 鲍长康 Preparation of oral coated medicine grains
JP2004035518A (en) * 2002-07-08 2004-02-05 Wyeth Lederle Japan Ltd Granular preparation for oral administration containing bitter taste-masked carbapenem antibiotic
CN101083977A (en) * 2004-10-12 2007-12-05 桑多斯股份公司 Taste-masking pharmaceutical compositions
CN1679525A (en) * 2005-01-12 2005-10-12 复旦大学 Oral disintegrant of compound paracetamol
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Address after: Road 264003 Shandong city of Yantai province Laishan District No. 32 Tong

Patentee after: Yantai aisijin Animal Health Products Co.,Ltd.

Address before: Road 264003 Shandong city of Yantai province Laishan District No. 32 Tong

Patentee before: YANTAI LUYE ANIMAL HEALTH PRODUCTS Co.,Ltd.