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A kind of tilmicosin drug inclusion compound and its preparation and application

A technology of tilmicosin and clathrate, which is applied in the field of veterinary biological products, can solve the problems of complex preparation process, many raw materials for coating liquid preparation, etc., achieve simple preparation process, low production cost, and reduce raw materials The effect of using

Active Publication Date: 2018-06-08
LUOYANG HUIZHONG ANIMAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the first method often uses technical means such as phase separation, spray drying, and double emulsion technology, and many accompanying problems, such as the use of toxic solvents, high temperature, strong acid and alkali, etc., can cause the decomposition of drugs
The second loading method is to divide the drug loading and the preparation of carrier particles into two steps, so the above-mentioned problems are avoided, but the drug loading amount in the medicament prepared by the second loading method is low, and the above two loading methods are currently The raw materials used in the method are all more, and the preparation process is also comparatively complicated
[0012] The above two methods use more raw materials for the preparation of core granules, and the preparation of coating liquid has more raw materials and the preparation process is complicated.

Method used

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  • A kind of tilmicosin drug inclusion compound and its preparation and application
  • A kind of tilmicosin drug inclusion compound and its preparation and application
  • A kind of tilmicosin drug inclusion compound and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: the preparation of tilmicosin drug inclusion compound

[0058] 1 Preparation of core particles loaded with tilmicosin

[0059] (1) The former powder of tilmicosin that takes 10g is put into 1000ml beaker, adds the 95% ethanol solution of 200ml, stirs until tilmicosin dissolves completely, the beaker that mixed solution is housed is placed on the magnetic stirrer, 25 ℃, 600r / min stirring constantly, slowly add 200ml of silica sol, the solution becomes turbid.

[0060] (2) After continuous stirring for 2 hours, the mixed solution was divided into 15ml centrifuge tubes, each tube was filled with 10ml solution, and centrifuged at 25°C and 8000r / min for 20min. Separate the supernatant from the precipitate.

[0061] (3) Place the precipitate in a constant temperature drying oven at 60°C, and after drying for 4 hours, take out the precipitate in all the centrifuge tubes and mix them together, and grind them through a 100-mesh sieve.

[0062] 2 Preparation of c...

Embodiment 2

[0069] Embodiment 2: The release performance test of tilmicosin drug inclusion compound

[0070] 1 Preparation of buffer

[0071] (1) Weigh 32.8g of sodium phosphate, add a small amount of purified water and stir to fully dissolve the sodium phosphate, add purified water to dilute to 1000ml, shake and shake to obtain a sodium phosphate solution with a concentration of 0.2mol / l.

[0072] (2) Measure 250ml of the above-mentioned sodium phosphate solution with a graduated cylinder, mix it evenly with a hydrochloric acid solution of 0.1mol / l with a concentration of 750ml, adjust the pH value to 6.86 with 2mol / l hydrochloric acid, and finally obtain a phosphate with a pH value of 6.86 buffer.

[0073] 2 Determination of sustained release rate

[0074] Accurately weigh the tilmicosin drug inclusion complex preparation 0.4g, tilmicosin former powder 0.12g and tilmicosin enteric-coated pellets 0.5g (ground into powder) prepared by embodiment 1 with a drug loading of 25%. shape). P...

Embodiment 3

[0077] Embodiment 3: the palatability test of tilmicosin drug inclusion compound

[0078] 1 Test drug and feed

[0079] The tilmicosin drug inclusion compound preparation with a drug loading of 25% prepared in Example 1.

[0080] Tilmicosin common premix, content 20%, batch number: 20130502, Henan Hemu Animal Pharmaceutical Co., Ltd.

[0081] Tilmicosin enteric-coated pellets, content 20%, batch number: W130711 Hubei Longxiang Pharmaceutical Co., Ltd.

[0082] Common feed for pig farms, Hefeng Feed.

[0083] 2 Experimental animals and groups

[0084] The test pigs were self-raised by the farm. Select 20 pigs with a body weight of 20-30kg and divide them into 4 groups with 5 pigs in each group. The first group is the test group, the second group is the 20% tilmicosin common premix control group, and the third group is the replacement group. Micoxin enteric-coated pellets, the fourth group is the normal feeding group.

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PUM

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Abstract

The invention relates to a drug inclusion compound of tilmicosin and its preparation and application. In the preparation method, the insoluble tilmicosin drug is first loaded onto nano-silica, and by adjusting the amount of tilmicosin and nano-silica sol in the preparation process of the inner core particles, a compound accounting for 80% of the total weight of the drug 90% of the inner core particles loaded with tilmicosin; and then coated with a coating solution made of resin, talcum powder, alcohol, surfactant, etc., to obtain the tilmicosin drug inclusion compound. After the drug inclusion compound is loaded with nano-silica, the drug concentration in saliva is reduced. At the same time, the drug-loaded particles are coated by inclusion technology, which not only achieves double taste-masking effects, but also plays a role in sustained release. role. In addition, the process of preparing the coating liquid in the present invention is simple, and after the coating is completed, the alcohol evaporates after being dried, so that the ingredients contained in the coating can be reduced without changing the coating effect.

Description

technical field [0001] The invention belongs to the technical field of veterinary biological products, and relates to a drug inclusion compound of tilmicosin and its preparation and application. Background technique [0002] Tilmicosin is a semi-synthesized macrolide antibiotic for livestock and poultry, which is a hydrolyzate of tylosin. The raw material drug is insoluble in water, has inhibitory effect on all Gram-positive bacteria, some Gram-negative bacteria, spirochetes, mycoplasma, mycoplasma, etc., has a wide antibacterial spectrum, strong antibacterial activity, and pathogens have low resistance to it ,, the drug has been approved for clinical use in Australia, Spain, the United States, France, Brazil, Malaysia, Italy and other countries. It mainly treats animal infectious diseases such as goats, dairy cows, pigs, and chickens, especially respiratory diseases. Actinobacillus, Pasteurella, have stronger antibacterial activity than tylosin. [0003] Tilmicosin is adm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/706A61K47/69A61K47/04A61P31/00A61P31/04
Inventor 张许科刘兴金张晓东
Owner LUOYANG HUIZHONG ANIMAL MEDICINE
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