CN102106843B - Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof - Google Patents
Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof Download PDFInfo
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- CN102106843B CN102106843B CN2011100438417A CN201110043841A CN102106843B CN 102106843 B CN102106843 B CN 102106843B CN 2011100438417 A CN2011100438417 A CN 2011100438417A CN 201110043841 A CN201110043841 A CN 201110043841A CN 102106843 B CN102106843 B CN 102106843B
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Abstract
The invention relates to a slow-release lung targeted microcapsule preparation of florfenicol with a good targeted function and a slow-release function, and a preparation method thereof. The capsule selects gelatin, ethyecellulose or arabic gum as a material, and the florfenicol micropowder as a capsule core, wherein the mass ratio of the material to the capsule core is controlled to be (1:1)-(1:2); and the particle size of the florfenicol micropowder is controlled to be 2-10 mu m. The preparation method comprises the following steps: swelling the capsule material in water in advance, wherein, the weight concentration is controlled to be 10-20%; evenly suspending the florfenicol micropowder into an aqueous solution of the capsule material; manufacturing a microcapsule through a spray drying method, wherein, the air intake temperature is controlled between 80 and 110 DEG C, the air outlet temperature is controlled between 110 and 130 DEG C, and the spray flow is 0.3-0.6 litre per minute; and performing spray drying to prepare the microcapsule preparation which has the lung targeted function, can lead drugs to enrich into lung tissues, has better curative effects on lung infection, has a long-acting and slow-release function, decreases the times of drug administration, lowers the quantity of labor of cultivation workers, and lightens the stress reaction of animals.
Description
Technical field
The invention belongs to the veterinary drug preparation field, be specifically related to a kind of slow release lung targeted micro-capsule preparation and method for making thereof with florfenicol of good targeting and slow releasing function.
Background technology
Florfenicol (Florfenicol) Chinese: fluprofen; Florfenicol; Florfenicol; It is the broad spectrum antibiotic of the special-purpose chloromycetin of a kind of new veterinary successfully developed in the late nineteen eighties; Nineteen ninety goes on the market in Japan first; The furunculosis of this medicine treatment salmon of Norway in 1993 approval, nineteen ninety-five France, Britain, Austria, Mexico and Spain ratify to be used to treat cattle respiratory system bacterial disease.Also ratify feed additive in Japan and Mexico as pig, the bacterial disease (Qiu Yinsheng etc., 1996) of prevention and treatment pig, China has passed through examining of this medicine at present.The main florfenicol preparation of market sale has injection (it is 30%, 10% and 5% that main specifications contains florfenicol), powder (containing florfenicol 10%), solution (containing florfenicol 2.0%) and pre-mixing agent 4 kinds of dosage forms such as (containing florfenicol 5.0%).The Ministry of Agriculture with florfenicol, florfenicol pre-mixing agent (specification: 50g: florfenicol 5g), florfenicol injection (specification: 2ml: florfenicol 0.6g) etc. 2 kinds of dosage forms totally 2 specifications record and be national veterinary drug quality standard (2 00 3 editions).
Above conventional formulation is systemic administration on the one hand; Receive the influence of liver first pass effect, it is not high to be distributed in the relative lung tissue of whole body concentration in addition, is difficult to play therapeutical effect preferably for serious pulmonary infection; Receive the limitation of half-life on the other hand; Need be administered twice every day, and frequent drug administration had both increased culturist's workload, causes stronger stress to animal again.And microcapsule formulation has shown very big advantage since clinical practice, is that mainly it has good targeting and slow releasing function.Chinese patent CN101647788 has reported a kind of method of single coacervation preparation florfenicol microcapsule, and good taste masking and the effect that improves stability are arranged.
Summary of the invention
The objective of the invention is to overcome the deficiency that exists in the prior art and a kind of lung targeting that both had is provided; Can make medicine be enriched in animal lung tissue; Play better therapeutic to pulmonary infection, can play the effect of long-acting slow-release simultaneously, reduce administration number of times; Reduce the amount of labour of culturing the workman, alleviate the slow release lung targeted micro-capsule preparation and the method for making thereof of the florfenicol of animal stress.
The objective of the invention is to realize like this:
A kind of slow release lung targeted micro-capsule preparation of florfenicol, it is characterized in that: the capsule material is selected one of gelatin, ethyl cellulose, arabic gum for use, is capsule-core with the florfenicol micropowder; Mass ratio is controlled between the 1:1-1:2; The granularity of florfenicol micropowder is controlled in the 2-10 mu m range, and at first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%; Then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol.
A kind of method for making of slow release lung targeted micro-capsule preparation of florfenicol, it is characterized in that: the capsule material is selected one of gelatin, ethyl cellulose, arabic gum for use, is capsule-core with the florfenicol micropowder; Mass ratio is controlled between the 1:1-1:2; The granularity of florfenicol micropowder is controlled in the 2-10 mu m range, and at first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%; Then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol.
The present invention has following good effect:
Experimental data through to pig shows, the florfenicol microcapsule preparation is after oral, and the highly enriched lung tissue that is distributed in, and can keep higher concentration in a long time shows good targeting and slow releasing function.
Concrete experimental technique is following: choose 6 of health pig, male and female half and half, continuous 5 days oral florfenicol microcapsules; 12mg/kg body weight (in florfenicol), after beginning to take medicine respectively the 1st, 3; 6,9,12; Put to death a pig in 15,21 days, florfenicol metabolite florfenicol amine calculates the distributed density of medicine in each tissue in each tissue through detecting.First day result: 465ug/kg in the muscular tissue, subcutaneous fat 634 ug/kg, lungs 10230ug/kg, kidney 3270 ug/kg; The 9th day result: do not detect subcutaneous fat 196 ug/kg, lungs 5410ug/kg, kidney 485 ug/kg in the muscular tissue; The 12nd day result: subcutaneous fat 137 ug/kg, lungs 4630ug/kg, kidney 185 ug/kg; The 21st day result: subcutaneous fat 122 ug/kg, kidney 123 ug/kg.
Therefore, the present invention has and both has the lung targeting, can make medicine be enriched in animal lung tissue; Play better therapeutic to pulmonary infection, can play the effect of long-acting slow-release simultaneously, reduce administration number of times; Reduce the amount of labour of culturing the workman, alleviate the advantage of animal stress.
The specific embodiment
A kind of slow release lung targeted micro-capsule preparation of florfenicol, it is characterized in that: the capsule material is selected gelatin, ethyl cellulose or arabic gum etc. for use, and above-mentioned capsule material all is sophisticated industrial products, and is cheap.With the florfenicol micropowder is capsule-core, and the mass ratio of capsule material and florfenicol micropowder is controlled between the 1:1-1:2, and the granularity of florfenicol micropowder is controlled in the 2-10 mu m range; At first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%, then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol, and technology is simple to operation; Envelop rate is high, and the capsule type is intact.
A kind of method for making of slow release lung targeted micro-capsule preparation of florfenicol, it is characterized in that: the capsule material is selected one of gelatin, ethyl cellulose, arabic gum for use, is capsule-core with the florfenicol micropowder; The mass ratio of capsule material and florfenicol micropowder is controlled between the 1:1-1:2; The granularity of florfenicol micropowder is controlled in the 2-10 mu m range, and at first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%; Then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol.
Embodiment 1: the capsule material is selected ethyl cellulose for use; With the florfenicol micropowder is capsule-core, and the mass ratio of capsule material and florfenicol micropowder is controlled at 1:1, and 20 ㎏ Florfenicol raw material are processed micropowder; The granularity of micropowder is controlled in the 2-10 mu m range; Swelling is in 200 ㎏ water in advance with 20 ㎏ ethyl celluloses, and soaked overnight is processed ethyl cellulose solution.The florfenicol micropowder is joined in the ethyl cellulose solution, and high-shear emulsion machine is processed uniform suspension.90 ℃ of control EATs, 130 ℃ of leaving air temps, 0.5 liter of mist flow per minute, spray drying gets florfenicol microcapsule.Record: envelop rate >=98%, drug loading 48%.
Embodiment 2: the capsule material is selected arabic gum for use; With the florfenicol micropowder is capsule-core, and the mass ratio of capsule material and florfenicol micropowder is controlled at 1:2, and 40 ㎏ Florfenicol raw material are processed micropowder; The granularity of micropowder is controlled in the 2-10 mu m range; Swelling is in 100 ㎏ water in advance with 20 ㎏ arabic gums, and soaked overnight is processed gumwater.The florfenicol micropowder is joined in the gumwater, and high-shear emulsion machine is processed uniform suspension.110 ℃ of control EATs, 110 ℃ of leaving air temps, 0.3 liter of mist flow per minute, spray drying gets florfenicol microcapsule.Record: envelop rate >=98%, drug loading 49%.
Embodiment 3: the capsule material is selected gelatin for use; With the florfenicol micropowder is capsule-core, and the mass ratio of capsule material and florfenicol micropowder is controlled at 1:1, and 20 ㎏ Florfenicol raw material are processed micropowder; The granularity of micropowder is controlled in the 2-10 mu m range; Swelling is in 200 ㎏ water in advance with 20 ㎏ gelatin, and soaked overnight is processed gelatin solution.The florfenicol micropowder is joined in the gelatin solution, and high-shear emulsion machine is processed uniform suspension.80 ℃ of control EATs, 130 ℃ of leaving air temps, 0.6 liter of mist flow per minute, spray drying gets florfenicol microcapsule.Record: envelop rate >=98%, drug loading 49%.
Embodiment 4: the capsule material is selected ethyl cellulose for use; With the florfenicol micropowder is capsule-core, and the mass ratio of capsule material and florfenicol micropowder is controlled at 1:2, and 40 ㎏ Florfenicol raw material are processed micropowder; The granularity of micropowder is controlled in the 2-10 mu m range; Swelling is in 100 ㎏ water in advance with 20 ㎏ ethyl celluloses, and soaked overnight is processed ethyl cellulose solution.The florfenicol micropowder is joined in the ethyl cellulose solution, and high-shear emulsion machine is processed uniform suspension.110 ℃ of control EATs, 120 ℃ of leaving air temps, 0.4 liter of mist flow per minute, spray drying gets florfenicol microcapsule.Record: envelop rate >=98%, drug loading 48%.
Claims (2)
1. the slow release lung targeted micro-capsule preparation of a florfenicol, it is characterized in that: the capsule material is selected one of gelatin, ethyl cellulose, arabic gum for use, is capsule-core with the florfenicol micropowder; Mass ratio is controlled between the 1:1-1:2; The granularity of florfenicol micropowder is controlled in the 2-10 mu m range, and at first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%; Then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol.
2. the method for making of the slow release lung targeted micro-capsule preparation of a florfenicol, it is characterized in that: the capsule material is selected one of gelatin, ethyl cellulose, arabic gum for use, is capsule-core with the florfenicol micropowder; Mass ratio is controlled between the 1:1-1:2; The granularity of florfenicol micropowder is controlled in the 2-10 mu m range, and at first swelling is in water in advance with the capsule material, and weight concentration is controlled between the 10%-20%; Then the florfenicol micropowder evenly is suspended in the capsule material aqueous solution; Make microcapsule through spray drying method, EAT is controlled between 80-110 ℃, and leaving air temp is controlled between 110-130 ℃; Mist flow per minute 0.3-0.6 liter, spray drying get the slow release lung targeted micro-capsule preparation of florfenicol.
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| CN2011100438417A CN102106843B (en) | 2011-02-24 | 2011-02-24 | Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof |
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| CN2011100438417A CN102106843B (en) | 2011-02-24 | 2011-02-24 | Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof |
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| CN102106843B true CN102106843B (en) | 2012-04-04 |
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Families Citing this family (4)
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| CN104510722A (en) * | 2013-09-27 | 2015-04-15 | 洛阳惠中兽药有限公司 | A florfenicol microcapsule, a preparing method thereof and applications of the florfenicol microcapsule |
| CN104784152B (en) * | 2014-01-20 | 2017-10-24 | 洛阳惠中兽药有限公司 | A kind of Thiamphenicol micro-capsule and preparation method and application |
| CN104288109B (en) * | 2014-10-28 | 2017-02-08 | 郑州合润生物制药有限公司 | Florfenicol supermolecule preparation and preparation method thereof |
| CN108210480A (en) * | 2016-12-13 | 2018-06-29 | 河南后羿实业集团有限公司 | A kind of preparation method of Tilmicosin micro-capsule |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1985812A (en) * | 2005-12-21 | 2007-06-27 | 天津市润拓生物技术有限公司 | Lung-targeting florfenicol microsphere for animal and birds and its preparing method |
| CN101647788A (en) * | 2009-06-26 | 2010-02-17 | 郑州后羿制药有限公司 | Florfenicol microcapsule and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1985812A (en) * | 2005-12-21 | 2007-06-27 | 天津市润拓生物技术有限公司 | Lung-targeting florfenicol microsphere for animal and birds and its preparing method |
| CN101647788A (en) * | 2009-06-26 | 2010-02-17 | 郑州后羿制药有限公司 | Florfenicol microcapsule and preparation method thereof |
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Inventor after: Guo Jianzhao Inventor after: Jiang Hongge Inventor after: Li Chunhui Inventor after: Zhu Yongxi Inventor after: Sun Meihe Inventor after: Wu Xiaona Inventor after: Chai Ruihong Inventor after: Lian Zhansheng Inventor after: Dong Yunlong Inventor before: Luo Zhenjun Inventor before: Jiang Erqiang Inventor before: Jiang Hongge Inventor before: Zhang Yongkui Inventor before: Wu Xiaoping |
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Effective date of registration: 20151028 Address after: 461670, eastern section of Binhe Road, Xuchang, Henan, Yuzhou Patentee after: XUCHANG TIANYUAN BIOLOGICAL TECHNOLOGY CO., LTD. Address before: 452500, No. 1, Huzhu Road, West Industrial Park, Xuchang, Henan, Yuzhou Patentee before: Henan Heima Animal Medicine Co., Ltd. |
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Granted publication date: 20120404 Termination date: 20180224 |