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Oil injection containing nonsteroidal anti-inflammatory drugs/polyethylene glycol drug-loading particles

A non-steroidal anti-inflammatory, solid polyethylene glycol technology, applied in anti-inflammatory agents, drug combinations, non-central analgesics, etc.

Inactive Publication Date: 2014-04-09
王玉万
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But oily long-acting injections containing NSAID / PEG drug-loaded particles or NSAID / PEG / HPMC (or H-HPC) drug-loaded particles have not been reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1, preparation 10% ketoprofen injection

[0023] Preparation composition: Ketoprofen 100g, PEG-10000 50g, H-HPC 25g, IPM added to 1 liter.

[0024] Preparation method: (1) Melt PEG at 60-70°C, add H-HPC and mix well, then add methanol equivalent to 2 times the amount of ketoprofen, after H-HPC dissolves, add ketoprofen, mix well, After being dissolved, methanol is removed under reduced pressure, cooled, solidified, pulverized, and passed through a 40-mesh sieve to obtain drug-loaded particles containing ketoprofen. (2) Disperse the drug-loaded particles in part of the IPM, 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 8 μm, add the remaining medium, and use a high-shear homogenizer at about Under the condition of 5000rpm, after repeated homogenization, the ketoprofen injection with the particle size of drug-loaded particles less than 8 μm was prepared...

Embodiment 2

[0025] Embodiment 2, preparation 10% ibuprofen injection

[0026] Preparation composition: ibuprofen 100g, PEG-6000 60g, soybean oil for injection to 1 liter.

[0027] Preparation method: (1) Melt PEG at 60-70°C, add ibuprofen and ethanol equivalent to 3 times the amount of ibuprofen, mix thoroughly to dissolve, cool, dry naturally after solidification, pulverize, pass through 40 mesh sieve to obtain drug-loaded microparticles containing ibuprofen. (2) Disperse the drug-loaded particles in part of soybean 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 5 μm, add the remaining medium, and use a high-shear homogenizer to Under the condition of about 5000rpm, after several times of homogenization, the ibuprofen injection with a particle size of less than 5 μm was prepared.

Embodiment 3

[0028] Embodiment 3, preparation 12% indomethacin injection

[0029] Preparation composition: indomethacin 120g, PEG-4000 80g, tea seed oil for injection to 1 liter.

[0030] Preparation method: (1) Melt PEG at 60-70°C, add indomethacin and acetone equivalent to 3 times the amount of indomethacin, reflux to dissolve, remove acetone by distillation under reduced pressure, cool and solidify, crush, pass through 40 mesh Sieve to obtain drug-loaded microparticles containing indomethacin. (2) Disperse the drug-loaded particles in part of the tea seed 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 8 μm, add the remaining medium, and use a high-shear homogenizer Under the condition of about 5000rpm, after several times of homogenization, the indomethacin injection with a particle size of less than 8 μm was prepared.

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PUM

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Abstract

The invention discloses an oil injection containing nonsteroidal anti-inflammatory drugs / polyethylene glycol drug-loading particles prepared by forming drug-loading particles through nonsteroidal anti-inflammatory drugs and solid polyethylene glycol and suspending the drug-loading particles in an oil medium. The involved nonsteroidal anti-inflammatory drugs comprise naproxen, ketoprofen, ibuprofen, flunixin meglumine, diclofenac and indometacin. Preferentially, the polyethylene glycol with the molecular weight of more than 6000 is used for preparing the preparation. The preferential oil medium is selected from one of isopropyl myristate, soybean oil for injection, corn oil and tea-seed oil.

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 non-steroidal anti-inflammatory drugs and solid polyethylene glycol, and dispersing the drug-loaded microparticles in an oily medium to prepare an oily long-acting injection. 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/34A61K47/38A61K47/44A61P29/00A61K31/192A61K31/44A61K31/196A61K31/405
Inventor 王玉万戴晓曦潘贞德翁志飞任雅楠沈力
Owner 王玉万