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Milk fragrance type tilmicosin enteric microcapsule and preparation method thereof

A tilmicosin and enteric-coated technology, which is applied in the field of milk-flavored enteric-coated microcapsules containing tilmicosin or tilmicosin phosphate and its preparation, can solve the problem of irritation, large particle size of the preparation, complex process, etc. question

Inactive Publication Date: 2014-06-11
RINGPU TIANJIN BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug molecule of tilmicosin has a strong bitter taste, the palatability is very poor when administered orally, and it is irritating to the stomach of animals, which has become the most important problem affecting the clinical use of tilmicosin
Patent CN101879141 discloses a taste-masking tilmicosin gastric-soluble granule preparation, but the preparation is irritating to the stomach of animals
Patent CN102319181 discloses a coating process of microcapsule-type animal medicines. The preparation of microcapsule-type animal medicines by this process is complex and costly, and the prepared microcapsules are single-layer coated. The auxiliary material microcrystalline cellulose As a filler or binder, the coating is easy to bite when the animal eats and eats the bitter taste of the main ingredient tilmicosin, which affects the palatability
Patent CN 102688220 discloses a method for preparing an odorless, enteric-coated tilmicosin microcapsule preparation. The preparation provided by the method has a large particle size and low bioavailability, and the preparation is odorless, which has no effect on increasing animal feed intake. Obvious effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Core layer preparation:

[0013] Weigh 30kg of tilmicosin phosphate, carry out ultrafine pulverization, add 30kg of dodecyl fatty acid, mix evenly at 60°C, put the mixture into a coating pan, add 20kg of 30% fructooligosaccharide liquid spray granulation, 50- Dry with hot air at 55°C to obtain the cystic core.

[0014] The compound enteric-coated capsule coating layer is prepared according to the following formula: 65L:

[0015] Weigh 10g of hydroxypropylmethylcellulose, 100g of hydroxypropylmethylcellulose succinate acetate, 10g of diethyl phthalate, 10g of Span 80, and 10g of milk flavor essence, add 75% ethanol to dilute to 1000ml, Instantly.

[0016] Encapsulation preparation conditions are as follows:

[0017] The capsule core layer and the capsule coating layer are mixed at a ratio of 2:1, and encapsulated under the following conditions: sterile air pressure 2kg / cm 2 , hot air temperature 40°C, fluidized bed velocity 0.5m 2 / min, the nozzle is 0.2m 2 / minut...

Embodiment 2

[0019] Core layer preparation:

[0020] Weigh 40kg of tilmicosin phosphate, carry out ultrafine pulverization, add 45kg of pentadecyl fatty acid, mix evenly at 80°C, put the mixture into a coating pan and add 30kg of 40% fructooligosaccharide liquid spray granulation, 50- Dry with hot air at 55°C to obtain the cystic core.

[0021] The compound enteric-coated capsule coating layer is prepared according to the following formula: 50L:

[0022] Weigh 20g of hydroxypropylmethylcellulose, 150g of hydroxypropylmethylcellulose succinate acetate, 15g of diethyl phthalate, 15g of Span 80, and 15g of milk essence, and add 80% ethanol to make up to 1000ml. Instantly.

[0023] Encapsulation preparation conditions are as follows:

[0024] The capsule core layer and the capsule coating layer are mixed at a ratio of 2:1, and encapsulated under the following conditions: sterile air pressure 4kg / cm 2 , hot air temperature 50℃, fluidized bed velocity 1m 2 / min, the nozzle is 0.4m 2 / minu...

Embodiment 3

[0026] Core layer preparation:

[0027] Weigh 35 kg of tilmicosin phosphate, carry out ultrafine pulverization, add 52.5 kg of octadecyl fatty acid, mix uniformly at 100 ° C, put the mixture into a coating pan and add 17.5 kg of 50% fructooligosaccharide liquid spray granulation, Dry with hot air at 50-55°C to obtain the core layer of the capsule.

[0028] Composite enteric-coated capsule coating layer is prepared as follows: 50L:

[0029] Weigh 50g of hydroxypropylmethylcellulose, 200g of hydroxypropylmethylcellulose succinate acetate, 50g of diethyl phthalate, 30g of Span 80, and 20g of milk essence, and add 85% ethanol to make it to 1000ml. Instantly.

[0030] Encapsulation preparation conditions are as follows:

[0031] The capsule core layer and the capsule coating layer are mixed at a ratio of 3:1, and encapsulated under the following conditions: sterile air pressure 6kg / cm 2 , hot air temperature 60℃, fluidized bed velocity 1.5m 2 / min, the nozzle is 0.8m 2 / minu...

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PUM

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Abstract

The invention relates to a milk fragrance type tilmicosin enteric microcapsule, and belongs to the technical filed of veterinary drugs. The tilmicosin enteric microcapsule is composes of a capsule core layer and a capsule coat layer; wherein the capsule core layer is composed of tilmicosin or tilmicosin phosphate and proper auxiliary materials, and the capsule coat layer is composed of a composite enteric material. The milk fragrance type tilmicosin enteric microcapsule can radically cover the bitterness of tilmicosin, and has a high encapsulation rate and a small microcapsule particle size.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a milk-flavored enteric-coated microcapsule containing tilmicosin or tilmicosin phosphate and a preparation method thereof. Background technique [0002] Tilmicosin is a semi-synthetic macrolide antibiotic for livestock and poultry developed by Elanco in the United States in the 1980s. It has strong antibacterial activity, low drug resistance, and a wide antibacterial spectrum. It is effective against all Gram-positive Bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc. have inhibitory effects, especially for a variety of mycoplasma and spirochetes. The drug has been approved for clinical use in Australia, Brazil, France, Malaysia, Italy, Spain, the United States and other countries for the treatment of infectious diseases in goats, cows, pigs, chickens and other animals. The drug molecule of tilmicosin has a strong bitter taste, the p...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/706A61K47/38A61P31/04
Inventor 王小武孙薇薇刘桂兰
Owner RINGPU TIANJIN BIOLOGICAL PHARMA
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