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Vidarabine monophosphate microsphere drug delivery system and preparation method thereof

A technology of adenosine monophosphate and drug delivery system, applied in the field of medicine, can solve the problems of low patient compliance and short half-life, and achieve the effect of ensuring stable release, good dispersibility, and good sustained release effect.

Active Publication Date: 2015-07-15
GUANGDONG XIANQIANG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, adenosine vidarabine is mainly lyophilized powder injection and injection, which has a short half-life and requires multiple administrations, which brings great pain to patients and low patient compliance

Method used

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  • Vidarabine monophosphate microsphere drug delivery system and preparation method thereof
  • Vidarabine monophosphate microsphere drug delivery system and preparation method thereof
  • Vidarabine monophosphate microsphere drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 0.4g of chitosan (deacetylation degree 96%) and dissolve in 20mL of 2% acetic acid aqueous solution, let it stand, and remove air bubbles. Measure 0.1 g of polyethylene glycol 400 and 0.1 g of vidarabine monophosphate and add to the above solution to form the water phase. Take 100mL of liquid paraffin, add 5mL of Tween 80 and 0.5g of magnesium stearate as the oil phase. Slowly pour the water phase into the oil phase, mechanically stir at 1000rpm, add 2mL glutaraldehyde after complete emulsification, continue stirring for 4h to cross-link and solidify, collect the precipitate, wash with isopropanol and petroleum ether, and dry.

[0029] Under the electron microscope, it can be seen that the microspheres are round and spherical, and the results are shown in figure 1 .

[0030] Destroy the microspheres with 0.25mol / L hydrochloric acid, measure the content of vidarabine monophosphate in the microspheres by HPLC, and calculate the encapsulation efficiency according t...

Embodiment 2

[0036] Weigh 0.6g of chitosan (degree of deacetylation 96%) and dissolve in 20mL of 2% acetic acid aqueous solution, let stand, and remove air bubbles. Measure 0.2g of polyethylene glycol 400 and 0.06g of vidarabine monophosphate into the above solution to form the water phase. Take 60mL of liquid paraffin, add 2mL of Tween 80 and 0.2g of magnesium stearate as the oil phase. Slowly pour the water phase into the oil phase, stir mechanically at 1200rpm, add 1mL glutaraldehyde after complete emulsification, continue stirring for 6h to cross-link and solidify, collect the precipitate, wash with isopropanol and petroleum ether, and dry.

[0037] The encapsulation efficiency of the microspheres was calculated to be 76%.

Embodiment 3

[0039] Weigh 0.1 g of chitosan (deacetylation degree 96%) and dissolve in 20 mL of 2% acetic acid aqueous solution, let stand, and remove air bubbles. Measure 0.02g of polyethylene glycol 4000 and 0.1g of vidarabine monophosphate and add to the above solution to form the water phase. Take 40mL of liquid paraffin, add 1mL of Tween 80 and 0.1g of magnesium stearate as the oil phase. Slowly pour the water phase into the oil phase, stir mechanically at 1200rpm, add 0.2mL glutaraldehyde after the emulsification is complete, continue stirring for 2h to cross-link and solidify, collect the precipitate, wash with isopropanol and petroleum ether, and dry.

[0040] The encapsulation efficiency of the microspheres was calculated to be 37%.

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Abstract

The invention relates to a chitosan microsphere drug delivery system of vidarabine and a preparation method. The method is characterized by acquiring the the medicinal microsphere drug delivery system with a complete spherical shape, a uniform particle size, a high embedding rate, good dispersity and a sustained release property. The specific technical scheme is that: chitosan is taken as a membrane material, polyethylene glycol is adopted as a pore-forming agent, glutaraldehyde is employed as a crosslinking agent, and inverse emulsification-crosslinking method is used to prepare the drug carrying microspheres. The preparation method includes: dissolving the drug in an acidic aqueous solution of chitosan, adding polyethylene glycol and stirring them uniformly, and taking the mixture as an aqueous phase; adding the aqueous phase slowly into an oil phase containing a surface active agent and a dispersing agent, carrying out stirring and emulsifying to uniformity, and adding the crosslinking agent to undergo crosslinking solidification; and washing and drying the obtained product. The invention provides the vidarabine chitosan microsphere drug delivery system with a sustained-release property.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a preparation method of a microsphere drug delivery system, in particular to a vidarabine monophosphate microsphere drug delivery system and a preparation method. Background technique [0002] The invention relates to a preparation method of a microsphere drug delivery system, in particular to a vidarabine and its phosphate (monophosphate adenosine vidarabine) chitosan microsphere delivery system and a preparation method. Background technique [0003] Vidarabine has broad-spectrum antiviral activity. It has the strongest effect on herpes virus and herpes zoster virus, followed by varicella zoster virus, vaccinia virus and hepatitis B virus, and is effective on adenovirus, pseudorabies virus and some RNA tumor viruses. Ineffective against most RNA viruses. Phosphorylated by cellular enzymes to generate adenosine triphosphate, which can compete with deoxyadenosine triphosphate to inhibit ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/7076A61K47/36A61P31/14A61P31/20A61P31/22
Inventor 王学文李玲梅张志生孙晔杜丽丽陈超黄杰明
Owner GUANGDONG XIANQIANG PHARMA
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