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Galanthamine long-acting release injectable microsphere composite and preparation method thereof

A technology of galantamine and galantamine base, which is applied in the direction of drug combination, active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, etc., and can solve problems such as the effect of acupuncture

Active Publication Date: 2012-01-04
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The reason is that the design purpose of the microcapsule instrument is to prepare APA microcapsules, and the particle size requirement is more than 300-500 μm, while the particle size requirement of injection microspheres is much smaller, with an average particle size of about 100 μm, generally less than 200 μm, otherwise, The needle passability of clinical injection administration of microsphere injection will be affected

Method used

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  • Galanthamine long-acting release injectable microsphere composite and preparation method thereof
  • Galanthamine long-acting release injectable microsphere composite and preparation method thereof
  • Galanthamine long-acting release injectable microsphere composite and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1: Galantamine PLGA microspheres were prepared by a vibrating nozzle method.

[0039] Precisely weigh about 55 mg of galantamine base, about 1000 mg of PLGA (monomer ratio LA:GA 50:50, molecular weight 12000) and add it to 5 ml of dichloromethane, vortex to dissolve completely, and make the dispersed phase. The dispersed phase was transferred to a 20ml glass syringe. Microspheres were prepared by vibrating nozzle method combined with emulsification method (O / W)-solvent evaporation method. The preparation instrument adopts the improved vibrating nozzle method microsphere instrument, and the process parameters are as follows: the aperture of the nozzle is 50 μm, the vibration frequency is 2000 Hz, the electric field voltage is 500 V, and the flow rate of the dispersed phase liquid is 1 ml / min, so that the nozzle can produce uniform and continuous droplets. Drop into the continuous phase of 200ml of 5% PVA17-88 aqueous solution, stir with medium-speed magnetic ...

Embodiment 2

[0040] Example 2: Preparation of galantamine PLGA microspheres by vibrating nozzle method.

[0041] Precisely weigh about 130 mg of galantamine base, about 1000 mg of PLGA (monomer ratio LA:GA 50:50, molecular weight 12000) and add it to 20 ml of ethyl acetate, vortex to dissolve completely, and make the dispersed phase. The dispersed phase was transferred to a 20ml glass syringe. Microspheres were prepared by vibrating nozzle method combined with emulsification method (O / W)-solvent evaporation method. The preparation equipment adopts the improved vibrating nozzle method microsphere instrument, and the process parameters are as follows: the aperture of the nozzle is 25 μm, the vibration frequency is 3000 Hz, the electric field voltage is 1000 V, and the flow rate of the dispersed phase liquid is 2 ml / min, so that the nozzle can produce uniform and continuous droplets , drop into the continuous phase of 200ml of 2% PVA17-50 aqueous solution, stir magnetically at a medium speed...

Embodiment 3

[0042] Embodiment 3: Preparation of galantamine PLGA microspheres by vibrating nozzle method.

[0043] Precisely weigh about 300mg of galantamine base, about 1000mg of PLGA (monomer ratio LA:GA 50:50, molecular weight 12000) and add it to 10ml of dichloromethane, vortex to dissolve completely, and make the dispersed phase. The dispersed phase was transferred to a 20ml glass syringe. Microspheres were prepared by vibrating nozzle method combined with emulsification method (O / W)-solvent evaporation method. The process parameters are as follows: the aperture of the nozzle is 50 μm, the vibration frequency is 2000 Hz, the electric field voltage is 1500 V, and the flow rate of the dispersed phase liquid is 1 ml / min, so that the nozzle can produce uniform and continuous droplets. In the phase, magnetically stir at a medium speed for 1 hour, then magnetically stir at a low speed for 4 hours, reduce pressure to promote the development of the organic solvent, collect the microspheres ...

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Abstract

The invention discloses galanthamine microspheres which contain 5-40wt% of basic group of galanthamine and 60-95wt % of polylactic acid / hydroxyacetic acid copolymer. The invention also provides a galanthamine long-acting release injectable microsphere composite which comprises the following components by weight percent: 60-90% of galanthamine microspheres, 5-25% of frozen dry proppant, 0.5-5% of suspending agent, 0.5-5% of wetting agent and 1-25% of osmotic pressure regulator. The invention combines the vibration nozzle method with the emulsion process (O / W)-solvent evaporation method so thatthe method has the advantage that the droplet-generating speed is fast, the efficiency is high, the containers used in preparation are easy to use in the aseptic operation, the production process canbe carried out continuously, the technology is applicable to scale-up application, etc.

Description

technical field [0001] The invention relates to an injection microsphere composition and a preparation method, more specifically, to a biodegradable galantamine long-acting injection sustained-release microsphere composition and a preparation method. Background technique [0002] Galantamine is a second-generation competitive cholinesterase inhibitor, which can pass through the blood-brain barrier, restore hindered neuromuscular conduction, and improve the paralysis of various peripheral neuromuscular disorders. In the early days, it was used to treat myasthenia gravis. In recent years, it has been found that galantamine can significantly improve the memory of elderly patients. It is mainly used for the treatment of mild, moderate and severe Alzheimer's disease (AD), and the curative effect is remarkable after 6 to 8 weeks of medication. , This product is suitable for benign memory disorders, improving the ability of patients to point to memory, associative learning, image r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/55A61K47/34A61K47/38A61K47/36A61P25/28
Inventor 刘善奎王海龙冯润良王芳谭晓军
Owner SHANDONG NEWTIME PHARMA
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