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Compound Tilmicosin nanoemulsion antibacterial agent and preparation method thereof

A technology for tilmicosin and an antibacterial drug, applied in the field of veterinary medicine, can solve the problems of low bioavailability, short half-life in vivo, incomplete absorption, etc., and achieve the effects of simple preparation method, reduced toxic and side effects, and rapid absorption

Inactive Publication Date: 2011-03-09
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because tilmicosin is insoluble in water, the traditional preparation used now is tilmicosin phosphate, which is easily destroyed by gastric acid after oral administration, has incomplete absorption, low bioavailability, and short half-life in the body. In addition, it is harmful to the heart. certain toxicity

Method used

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  • Compound Tilmicosin nanoemulsion antibacterial agent and preparation method thereof
  • Compound Tilmicosin nanoemulsion antibacterial agent and preparation method thereof
  • Compound Tilmicosin nanoemulsion antibacterial agent and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Preparation of compound tilmicosin nanoemulsion with a drug concentration of tilmicosin of 0.01%

[0023] Tilmicosin 0.010g

[0024] Florfenicol 0.001g

[0025] Dimethyl sulfoxide 0.004g

[0026] RH-40 13.380g

[0027] IPM 2.430g

[0028] Distilled water 84.175g

[0029] The specific preparation method is as follows:

[0030] 1) first tilmicosin is completely dissolved in the mixture of surfactant or co-surfactant or co-surfactant and tilmicosin co-solvent;

[0031] 2) Dissolving Florfenicol in the Florfenicol co-solvent, stirring to dissolve it;

[0032] 3) Mix the solution prepared in step 1) and step 2), and stir evenly;

[0033] 4) If step 2) contains surfactant, add oil directly and stir evenly; if it does not contain surfactant, add surfactant and stir evenly, then add oil and stir well; finally add distilled water dropwise slowly, drop Stir continuously while adding, until a uniform and transparent system is formed, and the tilmicosin nanoemulsi...

Embodiment 2

[0034] Example 2 Preparation of tilmicosin nanoemulsion with a concentration of tilmicosin of 0.15%

[0035] Tilmicosin 0.150g

[0036] Florfenicol 0.003g

[0037] Dimethyl sulfoxide 0.012g

[0038] RH-40 27.000g

[0039] IPM 3.000g

[0040] Distilled water 69.835g

Embodiment 3

[0041] Example 3 Preparation of Tilmicosin Nanoemulsion with a Drug Concentration of 0.95%

[0042] Tilmicosin 0.950g

[0043] 1,2-propylene glycol 10.000g

[0044] Florfenicol 0.005g

[0045] Dimethyl sulfoxide 0.020g

[0046] RH-40 22.500g

[0047] IPM 2.500g

[0048] Distilled water 64.025g

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Abstract

The invention discloses a compound Tilmicosin nanoemulsion antibacterial medicament with a particle size of 1-100 nm, which comprises, by mass, 0.01%-15.2% of Tilmicosin, 0.001%-2.12% of Florfenicol, 13.38%-36% of surfactant, 0%-26.5% of cosurfactant, 2.43%-5.32% of oil, 0.004%-2.12% of Florfenicol solubilizer, 0%-2.07% of Tilmicosin solubilizer and 14.89%-84.17% of distilled water. The sum of the mass percentages of the above components is 100%. The medicament is primrose, clear and transparent liquid in appearance and is characterized by low viscidity, good stability, high dispersibility, quick absorption and the like. The medicament has the advantages of higher bioavailability, longer half-life in a body, lower toxicity and sustained releasing and targeting effect.

Description

technical field [0001] The invention belongs to the field of veterinary medicines, and relates to a new dosage form of veterinary antibacterial drugs, in particular to a compound tilmicosin nanoemulsion antibacterial drug and a preparation method thereof. technical background [0002] Tilmicosin is a special-purpose macrolide antibiotic for livestock and poultry, which has inhibitory effects on Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc., especially for Actinobacillus pleuropneumoniae, hemolytic Pasteurella and mycoplasma have the strongest effect. Because the main target organs of tilmicosin are the lungs and breasts, and the drug concentration is high, it is mainly used for respiratory tract infections in livestock and poultry and mastitis in dairy cows. However, because tilmicosin is insoluble in water, the traditional preparation used now is tilmicosin phosphate, which is easily destroyed by gastric acid after oral administratio...

Claims

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Application Information

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IPC IPC(8): A61K31/706A61K31/165A61K9/107A61P31/04A61P11/00A61P15/00
Inventor 欧阳五庆王璟李雅
Owner NORTHWEST A & F UNIV
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