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Application and preparation method of huperzine A gelatin nanoparticle loaded microspheres

A technology of huperzine A and nanoparticles, which is applied in the field of medicine, can solve the problems of easy aggregation and instability of nanoparticles, and achieve the effect of solving the problem of burst release

Active Publication Date: 2017-09-12
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Huperzine A microspheres have been reported in many patents and literatures, but they all have a problem that is difficult to solve is the phenomenon of sudden release of drugs, and the characteristics of easy aggregation and instability of nanoparticles are also very prominent

Method used

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  • Application and preparation method of huperzine A gelatin nanoparticle loaded microspheres
  • Application and preparation method of huperzine A gelatin nanoparticle loaded microspheres
  • Application and preparation method of huperzine A gelatin nanoparticle loaded microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of W / O / W Huperzine A Gelatin Nanoparticle Microspheres

[0037] (1) Dissolve 60mg of huperzine A and 100mg of Tween-80 in 10ml of deionized water with pH=5, and add 200mg of gelatin in a water bath at 50°C to fully swell. Under the condition of stirring at 300r / min, add 800 mg of absolute ethanol, then add 1000 mg of glutaraldehyde, stir and solidify, remove excess organic solvents by rotary evaporation under reduced pressure, including absolute ethanol and glutaraldehyde, then remove free drugs by ultrafiltration, concentrate , to get gelatin nanoparticle suspension.

[0038] (2) Take 0.2ml gelatin nanoparticle concentrate (equal to huperzine A 20mg) and add it dropwise to PLGA dichloromethane with a mass concentration of 15% at 12000rpm high-speed shear to form W / O type colostrum, colostrum Disperse the milk at 10000rpm into a 1% polyvinyl alcohol (PVA) aqueous solution to form a W / O / W double emulsion. The obtained double emulsion is stirred at 800rmp for...

Embodiment 2

[0041] Preparation of W / O / W Huperzine A Gelatin Nanoparticle Microspheres

[0042] (1) Dissolve 20mg of huperzine A and 50mg of Tween-20 in 10ml of deionized water with pH=5, and add 200mg of gelatin in a water bath at 50°C to fully swell. Under the condition of stirring at 300r / min, add 700mg of isopropanol, then add 800mg of formaldehyde, stir and solidify, remove excess organic solvents including isopropanol and formaldehyde by rotary evaporation under reduced pressure, then remove free drugs by ultrafiltration, concentrate, and get gelatin nano particle suspension.

[0043] (2) Take 0.2ml gelatin nanoparticle concentrate (equal to huperzine A 10mg) and add it dropwise to 20% PLGA dichloromethane at a high speed of 12000rpm to form W / O type colostrum, colostrum Disperse 10000rpm into a PVA aqueous solution with a concentration of 2% to form a W / O / W double emulsion. The obtained double emulsion was stirred at 800rmp for 3 hours to obtain solidified microspheres. The obtained ...

Embodiment 3

[0045] Preparation of O / W Huperzine A Gelatin Nanoparticle Microspheres

[0046] (1) Dissolve 10mg of huperzine A and 60mg of Tween-20 in 10ml of deionized water with pH=5, and add 100mg of gelatin in a water bath at 50°C to fully swell. Under the condition of stirring at 300r / min, add 1400mg of isopropanol, then add 1800mg of formaldehyde, stir and solidify, remove organic solvents including isopropanol and formaldehyde by rotary evaporation under reduced pressure, then remove free drugs by ultrafiltration, concentrate to obtain gelatin nanoparticle mixture Suspension.

[0047] (2) Freeze-dry the suspension of gelatin nanoparticles to obtain dry powder of gelatin nanoparticles (equal to huperzine A 5 mg). Disperse it into the dichloromethane of PLGA with a mass concentration of 15%, disperse the oil phase 12000rpm into the PVA aqueous solution with a mass concentration of 2%, to form an O / W emulsion, and stir the obtained emulsion at 800rmp for 2h to obtain solidified micros...

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Abstract

The invention discloses application and a preparation method of huperzine A gelatin nanoparticle loaded microspheres. According to drug release amount requirements of huperzine A and drug release characteristics of nanoparticles and microspheres, nanoparticles and microsphere preparations are combined so as to solve the problem of burst release of huperzine A sustained-release preparations, and sustained release is realized.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of a novel microsphere preparation loaded with gelatin nanoparticles. Background technique [0002] Alzheimer's disease (AD), commonly known as senile dementia, is a chronic neurodegenerative disease characterized by progressive memory loss and dementia. That is, in the state of no disturbance of consciousness, there are obstacles in memory, thinking, analysis and judgment, visuospatial recognition, emotion, etc. Its characteristic pathological changes are atrophy of the cerebral cortex, accompanied by deposition of β-amyloid protein, neurofibrillary tangles, reduction in the number of a large number of memory neurons, and the formation of senile plaques. Common cause of death. Clinically, it mainly manifests as comprehensive dementia such as memory impairment, aphasia, apraxia, agnosia, impairment of visuospatial skills, executive dysfunction, and personali...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/14A61K31/4748A61K47/34A61K47/32A61K47/42A61P25/28
CPCA61K9/0019A61K9/0043A61K9/146A61K9/1635A61K9/1647A61K9/1682A61K31/4748A61K36/11
Inventor 慕宏杰孙考祥王毅云楚永超
Owner YANTAI UNIV
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