Preparation method of ivermectin sustained-release microspheres

A technology of ivermectin and slow-release microspheres, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., and can solve problems such as short half-life, poor stability, and hindering applications. Achieve the effect of easy absorption, good stability and reduced dosage

Active Publication Date: 2012-01-04
INST OF MODERN PHYSICS CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life and poor stability of ivermectin injection, animals need to be administered in large quantities for a long time, which consumes a lot of manpower and material resources, which hinders its clinical application

Method used

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  • Preparation method of ivermectin sustained-release microspheres
  • Preparation method of ivermectin sustained-release microspheres
  • Preparation method of ivermectin sustained-release microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of ivermectin polylactic acid sustained-release microspheres.

[0030] Accurately weigh 0.5g of polylactic acid and 0.25g of drug ivermectin and dissolve in 20ml of a mixed solution of dichloromethane and acetone, the volume percentage of dichloromethane and acetone is 9:1, and ultrasonically ultrasonicate for 5 minutes to fully dissolve to form an oil phase , the relative molecular mass of polylactic acid is 10,000; at a temperature of -10°C to 30°C, inject the oil phase dropwise into 40ml containing 2.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween 80 Stir in the aqueous solution (water phase) at 2000rpm for 2min to form S / O / W 1 The first emulsion; then the resulting S / O / W 1 For the first time, inject the emulsion into 60ml aqueous solution containing 1.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween 80, stir at 400rpm for 4h until the organic solvent evaporates completely, forming S / O / W 2 second emulsion; again S / O / W 2 The second emulsio...

Embodiment 2

[0032] Accurately weigh 0.5g of polylactic acid and 0.25g of drug ivermectin and dissolve in 20ml of a mixed solution of dichloromethane and acetone (the volume percentage of dichloromethane and acetone is 9:1), and ultrasonically sonicate for 5 minutes to fully dissolve to make oil phase, the relative molecular mass of polylactic acid is 25,000; at a temperature of -10°C to 30°C, inject the oil phase dropwise into 40ml containing 2.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween Stir in 80 aqueous solution (water phase) at 2000rpm for 2min to form S / O / W 1 The first emulsion; then the resulting S / O / W 1 For the first time, inject the emulsion into 60ml aqueous solution containing 1.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween 80, stir at 500rpm for 4h until the organic solvent evaporates completely, forming S / O / W 2 second emulsion; again S / O / W 2 The second emulsion was centrifuged at 4000rpm for 20min, washed twice with deionized water, the microspheres were collected,...

Embodiment 3

[0034] Accurately weigh 0.5g of polylactic acid and 0.35g of drug ivermectin and dissolve in 20ml of a mixed solution of dichloromethane and acetone (the volume percentage of dichloromethane and acetone is 8:2), and ultrasonically sonicate for 5 minutes to fully dissolve to make oil phase, the relative molecular mass of polylactic acid is 10,000; at a temperature of -10°C to 30°C, inject the oil phase dropwise into 20ml containing 2.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween Stir in 80 aqueous solution (water phase) at 2000rpm for 2min to form S / O / W 1 The first emulsion; then the resulting S / O / W 1 For the first time, the emulsion was injected into 80ml of 1.0% (g / ml) polyvinyl alcohol and 0.1% (g / ml) Tween 80 aqueous solution, under the magnetic stirring of 500rpm for 4h until the organic solvent evaporated completely, forming S / O / W 2 second emulsion; again S / O / W 2 The second emulsion was centrifuged at 4000rpm for 20min, washed twice with deionized water, the microsp...

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Abstract

The invention relates to ivermectin sustained-release microspheres used as an animal medicine for animal injection, and a preparation method thereof. The invention belongs to an interdisciplinary field of biomedical polymer materials and controlled release preparations. The invention discloses ivermectin sustained-release microspheres, which are characterized in that: the ivermectin sustained-release microspheres have particle sizes of 0.1 to 10mum, a medicine loading capacity of 20% to 35%, and an entrapment rate of above 80%. The preparation method of the ivermectin sustained-release microspheres comprises steps that: a carrier material and the medicine ivermectin with a mass ratio of 1:1-10 are dissolved in an organic solvent; the solution is processed through supersonic wave or mechanical stirring, such that the solution is emulsified into an oil phase, wherein a volume ratio of oil phase to water phase is 1:5-10; under a temperature of -10 DEG C to 30 DEG C, the oil phase is injected into a water phase disperse medium solution step-by-step; constant-temperature magnetic stirring is carried out with a rotation speed of 400 to 10000rpm, the mixture is sufficiently emulsified, such that an S/O/W type emulsion is obtained; the emulsion is stirred under room temperature for 3 to 4 hours, such that the organic solvent is sufficiently volatilized; the obtained product is centrifuged, washed, collected, and is vacuum-dried with a pressure of 0.01 to 0.04MPa under room temperature for 10 to 12 hours or is lyophilized under a temperature of -0 DEG C to -20 DEG C. With the processes, ivermectin sustained-release microspheres with particle sizes of 0.1 to 10mum are obtained.

Description

technical field [0001] The invention relates to ivermectin sustained-release microspheres for animal medicine and animal health injection and a preparation method thereof, belonging to the cross research field of biomedical polymer materials and drug controlled release preparations. The method adopts the improved emulsion solvent evaporation method, uses the biodegradable polymer material polylactic acid (PLA) or polylactic acid-glycolic acid copolymer (PLGA) as the carrier to wrap ivermectin (IVM), and prepares it under the action of mechanical stirring Ivermectin sustained-release microspheres. Background technique [0002] In recent years, with the rapid development of animal husbandry, more and more different dosage forms of ivermectin have been developed, such as oral liquid, capsule, paste, injection, emulsion, spray, premixed Doses, pours, tablets, sustained release boluses, powders, etc. These drugs on the market have shown unique curative effects in clinical appli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/7048A61K47/34A61P33/00A61P33/10A61P33/14
Inventor 梁剑平李贵玉陆锡宏李雪虎
Owner INST OF MODERN PHYSICS CHINESE ACADEMY OF SCI
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