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Tilmicosin solid dispersible granule as well as preparation method and application thereof

A technology for tilmicosin and solid dispersion, which is applied in the field of tilmicosin solid dispersion particles and their preparation, can solve the problems of poor palatability of tilmicosin, irritation of gastric mucosa, poor palatability for animals, etc., and achieves improved bioavailability. The effect of low toxicity, small side effects and convenient medication

Active Publication Date: 2014-06-04
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Other preparations such as solutions, powders, premixes, etc. are all conventional oral preparations, and none of them can solve the problem of poor palatability of tilmicosin
[0004] The method of mixed feeding and administration is relatively simple for the prevention and treatment of highly infectious diseases, but tilmicosin itself tastes extremely bitter, and is irritating to the gastric mucosa, and the palatability of animals is poor. The existing tilmicosin formulations are directly mixed feeding is difficult

Method used

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  • Tilmicosin solid dispersible granule as well as preparation method and application thereof
  • Tilmicosin solid dispersible granule as well as preparation method and application thereof
  • Tilmicosin solid dispersible granule as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of Tilmicosin Solid Dispersion Granules

[0039] The preparation steps are as follows:

[0040] S1. Weigh each carrier auxiliary material according to the following formula ratio (based on the total mass as 100g):

[0041] Tilmicosin 10%;

[0042] Stearic acid 85%;

[0043] Paraffin 5%;

[0044] Heat to melt at 80°C and mix well;

[0045] S2. Add tilmicosin to the carrier auxiliary material obtained in S1, and stir evenly to obtain a mixed material;

[0046] S3. Cool the mixed material obtained in S2 to 70-90°C, and carry out the stage of fluidized bed spray granulation and spheroidization, and the temperature of the fluidized air in the granulation and spheroidization stage is 25°C;

[0047] S4. Cool, sieve, and collect to obtain 10% tilmicosin solid dispersion particles.

Embodiment 2

[0048] Example 2 Preparation of tilmicosin solid dispersion granule preparation

[0049] The preparation steps are as follows:

[0050] S1. Weigh each carrier auxiliary material according to the following formula ratio (based on the total mass as 100g):

[0051] Tilmicosin 20%;

[0052] Glyceryl Monostearate 75%;

[0053] Fat powder 5%;

[0054] Heat to melt at 70°C and mix well;

[0055] S2. Add tilmicosin to the carrier auxiliary material obtained in S1, and stir evenly to obtain a mixed material;

[0056] S3. Cool the mixed material obtained in S2 to 70-90°C, and carry out the stage of fluidized bed spray granulation and spheroidization, and the temperature of the fluidized air in the granulation and spheroidization stage is 20°C;

[0057] S4. Cool, sieve, and collect to obtain 20% tilmicosin solid dispersion granule preparation.

Embodiment 3

[0058] Example 3 Preparation of Tilmicosin Solid Dispersion Granules

[0059] The preparation steps are as follows:

[0060] S1. Weigh each carrier auxiliary material according to the following formula ratio (based on the total mass as 100g):

[0061] Tilmicosin 30%;

[0062] Fat powder 65%;

[0063] Paraffin 5%;

[0064] Heat to melt at 100°C and mix well;

[0065] S2. Add tilmicosin to the carrier auxiliary material obtained in S1, and stir evenly to obtain a mixed material;

[0066] S3. Cool the mixed material obtained in S2 to 70-90°C, and perform the stage of fluidized bed spray granulation and spheroidization, and the temperature of the fluidized air in the granulation and spheroidization stage is 30°C;

[0067] S4. Cool, sieve, and collect to obtain 30% tilmicosin solid dispersion granule preparation.

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Abstract

The invention discloses a tilmicosin solid dispersible granule as well as a preparation method and an application thereof. The tilmicosin solid dispersible granule consists of tilmicosin and a carrier accessory. The carrier accessory is one of glycerin monostearate, stearyl alcohol, saturated triglyceride, glycerinum simple lipid, paraffin wax, animal wax, vegetable wax or fatty powder or mixture thereof. The preparation method of the tilicosin solid dispersible granule comprises the following steps: weighing respective carrier accessories according to the formula proportion, heating, melting and mixing uniformly; adding the tilmicosin, stirring uniformly, cooling, pelleting through spraying of a fluidized bed, balling, cooling, sieving and collecting to obtain the tilmicosin solid dispersible granule. The tilmicosin solid dispersible granule solves the problem of medicine palatability, by feed mixing administration, the fluidity and dispersibility are good and medication is convenient; after animals take the granule, the medicine releases slowly, so that the safety is high; besides, the biological availability of tilmicosin medicine is enhanced, and the clinical using effect is remarkable.

Description

technical field [0001] The invention belongs to the technical field of preparation of animal medicines. More specifically, it relates to a tilmicosin solid dispersion granule, its preparation method and application. Background technique [0002] Tilmicosin is a semi-synthetic animal-specific macrolide antibiotic developed by Elanco in the 1980s, with tylosin as the precursor. Tilmicosin has strong antibacterial activity and a broad antibacterial spectrum, and has inhibitory effects on all Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, mycoplasma, spirochetes, etc. It is mainly used to treat infectious diseases caused by sensitive bacteria in cattle, goats, sheep, dairy cows, pigs, chickens, etc., especially for the treatment of livestock and poultry respiratory tract infection diseases. It has stronger activity than tylosin on Actinobacillus pleuropneumoniae, Pasteurella hemolytica, Pasteurella multocida and mycoplasma. Research in recent years has fo...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/706A23K1/17A61P31/04A61P31/14A23K20/195
Inventor 黄显会孔祥凯怀彬彬
Owner SOUTH CHINA AGRI UNIV
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