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Oil injection containing antibacterial agents/polyethylene glycol drug-loading particles

A technology of drug-loaded particles and antibacterial drugs, which is used in antibacterial drugs, drug delivery, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2014-04-16
王玉万
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the commercially available injections containing these antibacterial drugs are prepared with water as the main solvent or organic solvents (such as 1,2-propanediol, dimethylacetamide, N-methylpyrrolidone, formalin glycerol, etc.) Solution-type preparations, there are also oil preparations prepared with vegetable oil or artificially synthesized oily compounds as the medium; the injections containing the above-mentioned antibacterial drugs disclosed in literature or patents include solution-type preparations, suspension-type preparations, emulsions, and contain different sustained-release preparations. Carrier long-acting injections, but oil-based long-acting injections containing solid PEG / antibacterial drug-loaded particles have not been reported

Method used

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  • Oil injection containing antibacterial agents/polyethylene glycol drug-loading particles

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1, preparation 8% ceftiofur hydrochloride injection

[0027] Preparation composition: every liter contains 90% ceftiofur hydrochloride 90g, PEG-10000 50g, H-HPC 25g, soybean oil for injection added to the final volume.

[0028] Preparation method: (1) Melt PEG at 60-70°C, add H-HPC and mix well, then add appropriate amount of methanol, after H-HPC dissolves and cool down to room temperature, add ceftiofur hydrochloride, mix well, remove under reduced pressure Clean methanol, cool, solidify, pulverize, and pass through a 40-mesh sieve to obtain drug-loaded particles containing ceftiofur hydrochloride. (2) Disperse the drug-loaded particles in some soybean oil, grind them through a colloid mill until the particle size is less than 50 μm, and further grind them with a sand mill until the particle size is less than 10 μm, add the remaining medium, and use a high-shear homogenizer to Under the condition of about 5000rpm, after several times of homogenization, cef...

Embodiment 2

[0029] Embodiment 2, preparation 8% cefquinol sulfate injection

[0030] Preparation composition: 90% cefquinol sulfate 90g, PEG-6000 90g, corn oil for injection is added to 1 liter.

[0031] Preparation method: (1) Melt PEG at 60-70°C, add cefquinol sulfate superfine powder, mix well, cool and solidify, pulverize, pass through a 40-mesh sieve to obtain drug-loaded particles containing cefquinol sulfate. (2) Disperse the drug-loaded particles in part of corn oil, grind them through a colloid mill until the particle size is less than 100 μm, and further grind them with a sand mill until the particle size is less than 20 μm, add the remaining medium, and use a high-shear homogenizer to Under the condition of about 5000rpm, after several times of homogenization, the ceftiofur hydrochloride injection with a particle size of less than 20 μm was prepared.

Embodiment 3

[0032] Embodiment 3, preparation 15% oxytetracycline hydrochloride injection

[0033] Preparation composition: every 100ml injection contains oxytetracycline hydrochloride 15g, PEG-10000 / HPMC (2:1) solid solution 6g, BHA 0.01g, BHT 0.01g, PG 0.005g, EDTA-2 sodium 0.15g, IPM added to the final volume.

[0034] Preparation method: disperse oxytetracycline hydrochloride and solid solution in part of IPM, grind with colloid mill and sand mill until the particle size is less than 10 μm, add antioxidant and remaining medium, and homogenize with high-shear homogenizer This preparation.

[0035]The preparation is intramuscularly injected into pigs, and the dosage is 15mg / kg b.w., and the blood drug concentration is still maintained in the effective concentration range (1-2 micrograms / m1) 48 hours after administration.

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Abstract

The invention discloses an oil injection containing antibacterial agents / solid polyethylene glycol drug-loading particles. The oil injection is prepared by consisting of the drug-loading particles through antibacterial agents and solid polyethylene glycol and suspending the drug-loading particles in an oil medium. The antibacterial agents comprise enrofloxacin, danofloxacin mesylate, Marbofloxacin, mequindox, tilmicosin, tylosin, oxytetracycline hydrochloride, ceftiofur hydrochloride, cefquinome sulfate, lincomycin hydrochloride, florfenicol, erythrocin and doxycycline hydrochloride; preferentially the polyethylene glycol with the molecular weight of more than 6000 is used for preparing the preparation; more preferentially, any one of isopropyl myristate, soybean oil for injection, corn oil and tea-seed oil is used for preparing the preparation. Hydroxypropyl methyl cellulose or high-substituted hydroxy propyl cellulose can be added into the preparation.

Description

technical field [0001] The invention belongs to the preparation technology of veterinary drug preparations, and in particular relates to preparing drug-loaded microparticles composed of antibacterial drugs and solid polyethylene glycol, and dispersing the drug-loaded microparticles in an oily medium to prepare oily long-acting injections. Background technique [0002] Polyethylene glycol (PEG) is a water-soluble polyether compound. PEG with a molecular weight less than 600 is a colorless transparent liquid, and PEG with a molecular weight greater than 1000 is in a solid state. PEG is widely used in pharmaceutical preparations. Low-molecular-weight (less than 600) PEG is used in the preparation of injections, mainly for solubilization, viscosity-increasing, and suspension-suspension, and it can stabilize emulsions when used in combination with emulsifiers. PEG in solid state is often used in the preparation of suppositories and ointments, and is also often used in the prepara...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/38A61K45/00A61K9/00A61P31/04
Inventor 王玉万潘贞德戴晓曦翁志飞任雅楠沈力
Owner 王玉万
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