Oily injection containing antiparasitic agent/polyethylene glycol drug-loading microparticles

An anti-parasitic, drug-carrying particle technology, applied in anti-infective drugs, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as inconvenience of medication

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

The main disadvantage of this implant is that surgery is required to implant the

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1, preparation 6% ivermectin injection

[0025] Preparation composition: ivermectin 60g, PEG-20000 50g, H-HMC 40g, IPM added to 1 liter.

[0026] Preparation method: (1) Melt PEG at 60-70°C, add H-HMC and mix well, then add methanol about 3 times the amount of ivermectin, after H-HMC dissolves, add ivermectin, mix well , after the ivermectin dissolves, distill under reduced pressure, remove methanol, cool, solidify, pulverize, and pass through a 40-mesh sieve to obtain drug-loaded particles containing ivermectin. (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 20 μm, add the remaining medium, and use a high-shear homogenizer at about Under the condition of 5000rpm, after several times of homogenization, the ivermectin injection with a particle size of less than 20 μm was prepared.

Embodiment 2

[0027] Embodiment 2, preparation 3% Abamectin injection

[0028] Preparation composition: Abamectin 30g, PEG-10000 30g, HPMC 21g, soybean oil for injection added to 1 liter.

[0029] Preparation method: (1) Melt PEG at 60-70°C, add avermectin, HPMC and appropriate amount of methanol, mix well, dissolve it, cool, dry naturally after solidification, pulverize, pass through a 40-mesh sieve to obtain Drug-loaded microparticles of abamectin. (2) Disperse the drug-loaded particles in some 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 20 μm, add the remaining medium, and use a high-shear homogenizer to Under the condition of about 5000rpm, after repeated homogenization, the avermectin injection with a particle size of less than 20 μm was prepared.

Embodiment 3

[0030] Embodiment 3, preparation 18% acetamido abamectin injection

[0031] Preparation composition: acetamidoabamectin 180g, PEG-6000 90g, IPM added to 1 liter.

[0032]Preparation method: (1) Melt PEG at 60-70°C, add acetamidoabamectin and appropriate amount of ethanol, reflux to dissolve, distill under reduced pressure to remove ethanol, cool and solidify, pulverize, and pass through a 40-mesh sieve to obtain acetamide-containing Drug-loaded microparticles of kiabamectin. (2) Disperse the drug-loaded particles in part of the IPM, 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 at about Under the condition of 5000rpm, after repeated homogenization, the acetamidoabamectin injection with a particle size of less than 20 μm was prepared.

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Abstract

The invention provides an oily injection containing antiparasitic agent/polyethylene glycol drug-loading microparticles which is prepared by suspending drug-loading microparticles, which are composed of antiparasitic agent and solid polyethylene glycol, in an oily medium. The antiparasitic agent comprises ivermectin, abamectin, eprinomectin, doramectin, milbemycin oxime, moxidectin, albendazole oxide or hydrochloride thereof, oxfendazole or hydrochloride thereof, closantel base or sodium salt thereof; polyethylene glycol with molecular weight of more than 6,000is preferably selected for preparation of the oily injection; and one of isopropyl myristate, injection soybean oil, maize oil and tea seed oil is preferably selected for preparation of the oily injection.

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 antiparasitic drugs and solid polyethylene glycol, and dispersing the drug-loaded microparticles in an oily medium to prepare veterinary 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 ...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/10A61K47/34A61K47/38A61K47/44A61P33/00
Inventor 王玉万戴晓曦潘贞德任雅楠翁志飞沈力
Owner 王玉万
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