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Slow-release lung targeted microcapsule preparation of florfenicol and preparation method thereof

A florfenicol, lung-targeting technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, respiratory diseases, etc., can solve the problem of increasing the workload of farmers, animal stress response, etc. It can reduce the stress response of animals, improve the curative effect, and reduce the number of administrations.

Inactive Publication Date: 2011-06-29
XUCHANG TIANYUAN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] On the one hand, the above conventional preparations are used systemically and are affected by the first-pass effect of the liver. In addition, they are distributed in the whole body relative to the lung tissue at a low concentration, so it is difficult to play a good therapeutic effect on severe lung infections. On the other hand, they are affected by the half-life. Due to the limitation of the drug, it needs to be administered twice a day. Frequent administration not only increases the workload of the breeder, but also causes a strong stress response to the animals.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: the capsule material is selected from ethyl cellulose, with florfenicol micropowder as the capsule core, the mass ratio of capsule material and florfenicol micropowder is controlled at 1:1, and 20 kg of florfenicol raw material is made into micropowder , the particle size of the micropowder is controlled within the range of 2-10μm, pre-swell 20kg of ethylcellulose in 200kg of water, soak overnight to make ethylcellulose solution. Add the florfenicol micropowder into the ethyl cellulose solution, and make a homogeneous suspension by a high-shear emulsifier. Control the inlet air temperature at 90°C, the outlet air temperature at 130°C, the spray flow rate at 0.5 liters per minute, and spray dry to obtain the florfenicol microcapsules. Measured: encapsulation rate ≥ 98%, drug loading 48%.

Embodiment 2

[0015] Embodiment 2: the capsule material is selected from gum arabic, with florfenicol micropowder as the capsule core, the mass ratio of capsule material and florfenicol micropowder is controlled at 1:2, and 40 kg of florfenicol raw material is made into micropowder, micropowder The particle size is controlled within the range of 2-10μm, and 20kg of gum arabic is pre-swelled in 100kg of water and soaked overnight to make a gum arabic solution. The florfenicol micropowder was added to the gum arabic solution, and a high-shear emulsifier was used to make a uniform suspension. Control the inlet air temperature at 110°C, the outlet air temperature at 110°C, the spray flow rate at 0.3 liters per minute, and spray dry to obtain the florfenicol microcapsules. Measured: encapsulation rate ≥ 98%, drug loading 49%.

Embodiment 3

[0016] Embodiment 3: capsule material selects gelatin, takes florfenicol micropowder as capsule core, the mass ratio of capsule material and florfenicol micropowder is controlled at 1:1, 20 kg of florfenicol raw materials are made into micropowder, the micropowder The particle size is controlled within the range of 2-10μm. Pre-swell 20kg of gelatin in 200kg of water and soak overnight to make a gelatin solution. Add the florfenicol micropowder into the gelatin solution, and use a high-shear emulsifier to make a uniform suspension. Control the inlet air temperature at 80°C, the outlet air temperature at 130°C, the spray flow rate at 0.6 liters per minute, and spray dry to obtain the florfenicol microcapsules. Measured: encapsulation rate ≥ 98%, drug loading 49%.

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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 [0001] The invention belongs to the field of veterinary drug preparations, and in particular relates to a sustained-release lung-targeting microcapsule preparation of florfenicol with excellent targeting and sustained-release effects and a preparation method thereof. Background technique [0002] Florfenicol (Florfenicol) Chinese name: Fluprofen; It was first launched in Japan in 1990. In 1993, Norway approved the drug to treat salmon furunculosis. In 1995, France, the United Kingdom, Austria, Mexico and Spain approved it to treat bovine respiratory system bacterial diseases. In Japan and Mexico, it is also approved as a feed additive for pigs to prevent and treat bacterial diseases in pigs (Qiu Yinsheng et al., 1996). my country has now passed the approval of this drug. The main florfenicol preparations sold in the market include injections (main specifications containing 30%, 10% and 5% florfenicol), powders (containing 10% florfenicol), solutions (contain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/165A61K47/36A61K47/38A61K47/42A61P11/00A61P31/04
Inventor 罗振军蒋二强江红格张永奎吴小萍
Owner XUCHANG TIANYUAN BIOLOGICAL TECH CO LTD
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