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A kind of monosialotetrahexosyl ganglioside microsphere and preparation method thereof

A technology of ganglioside and monosialic acid, which is applied in the field of monosialotetrahexosylganglioside microspheres and its preparation, can solve the problems of poor patient compliance, reduce toxic and side effects, improve curative effect, and avoid long-term The effect of frequent dosing

Inactive Publication Date: 2012-02-01
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, common GM-1 preparations need to be administered repeatedly to maintain the effective concentration in the cerebrospinal fluid, and the patient's compliance is poor.

Method used

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  • A kind of monosialotetrahexosyl ganglioside microsphere and preparation method thereof
  • A kind of monosialotetrahexosyl ganglioside microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Preparation of monosialotetrahexosylganglioside microspheres

[0019] 0.5ml 20mg / ml PLGA dichloromethane solution was used as the organic phase, and 0.1ml 80mg / ml monosialotetrahexosylganglioside solution was added as the inner aqueous phase, and vortex emulsified for 60s to obtain O / W type primary emulsion Add it dropwise to 10ml 30mg / mL external water phase polyvinyl alcohol ultrapure aqueous solution and shear at high speed for 120s to form a double emulsion; stir at low speed for 3 hours to completely volatilize the organic solvent; centrifuge, discard the upper liquid, wash 3 times with distilled water, Monosialotetrahexosylganglioside microspheres were obtained, and vacuum-dried for 72 hours to obtain monosialotetrahexosylganglioside dry powder; wherein, the vortex speed was 800r / min, and the high-speed shear speed was 20000r / min. min.

Embodiment 2

[0020] Example 2: Preparation of monosialotetrahexosylganglioside microspheres

[0021] 0.5ml 60mg / ml PLGA dichloromethane solution was used as the organic phase, and 0.067ml 120mg / ml monosialotetrahexosyl ganglioside solution was added as the inner aqueous phase, and vortex emulsified for 90s to obtain O / W type primary emulsion Add it dropwise to 10ml50mg / mL external water phase polyvinyl alcohol ultrapure aqueous solution at high speed for 15s to form double emulsion; stir at low speed for 3 hours to completely volatilize the organic solvent; centrifuge, discard the upper liquid, and wash 3 times with distilled water to obtain Monosialotetrahexosylganglioside microspheres were vacuum-dried for 72 hours to obtain monosialotetrahexosylganglioside microspheres dry powder; wherein, the vortex speed was 1500r / min, and the high-speed shear speed was 33000r / min .

Embodiment 3

[0022] Example 3: Preparation of monosialotetrahexosylganglioside microspheres

[0023] 0.5ml 80mg / ml PLGA solution in dichloromethane was used as the organic phase, and 0.05ml 160mg / ml monosialotetrahexosylganglioside solution was added as the inner aqueous phase, and vortex emulsified for 120s to obtain an O / W type primary emulsion ; Add it dropwise to 10ml10mg / mL external water phase polyvinyl alcohol ultrapure aqueous solution and shear at high speed for 30s to form double emulsion; Stir at low speed for 3 hours to completely volatilize the organic solvent; Centrifuge, discard the upper liquid, and wash 3 times with distilled water to obtain Monosialotetrahexosylganglioside microspheres were vacuum-dried for 72 hours to obtain monosialotetrahexosylganglioside microspheres dry powder; wherein, the vortex speed was 2000r / min, and the high-speed shear speed was 8000r / min .

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Abstract

The invention discloses a monosialote rahexosylganglioside (GM-1) microsphere, comprising monosialote rahexosylganglioside, carrier material, emulsifier and water, wherein the concentration of the components is: monosialote rahexosylganglioside 80 to 240 mg / ml, carrier material 20 to 200 mg / ml and emulsifier 10 to 50 mg / ml. The monosialote rahexosylganglioside microsphere of the invention can be used for injection and has uniform quality and appearance, with the average grain diameter being 1 to 15 microns and the encapsulating rate higher than 80%. The monosialote rahexosylganglioside microsphere has obvious slow release function, obviously decreases the dose times and increases the adaptation of sufferer.

Description

technical field [0001] The invention relates to a monosialotetrahexosyl ganglioside microsphere and a preparation method thereof. Background technique [0002] Monosialotetrahexosyl ganglioside (GM-1), one of the most important gangliosides, can promote the growth, differentiation and regeneration of nerve cells cultured in vitro; it can regulate nerve growth factors; it can promote Neuronal axon and dendritic proliferation, lateral process formation; inhibit cell degeneration, strengthen neurotrophy, reduce the death of damaged cell bodies, and promote neuron regeneration and functional recovery. It is mainly used for the treatment of vascular or traumatic central nervous system diseases, including brain trauma, spinal cord trauma, stroke, hypoxic-ischemic encephalopathy, white matter injury of premature infants, Parkinson's disease, etc. [0003] At present, it is mainly administered through intramuscular injection or intravenous infusion for a long time and in large dose...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/7032A61K47/34A61K47/36A61K47/42A61P25/00A61P25/16A61K47/10A61K47/26
Inventor 张娜刘永军姜庆城刘莉姜书梅
Owner SHANDONG UNIV