Macromolecule skin penetration enhancer as well as preparation method and applications thereof

A technology of absorption enhancer and polymer, applied in the field of polymer transdermal absorption enhancer and its preparation, can solve the problems of high cost, toxicity of body organs, difficulty in production and the like

Active Publication Date: 2013-05-15
武汉天时维璟微生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these commonly used transdermal absorption enhancers have their own shortcomings, such as irritation to the skin

Method used

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  • Macromolecule skin penetration enhancer as well as preparation method and applications thereof
  • Macromolecule skin penetration enhancer as well as preparation method and applications thereof
  • Macromolecule skin penetration enhancer as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0044] see figure 1 , figure 2 , the preparation method of above-mentioned macromolecule transdermal absorption accelerator, comprises the following operations:

[0045] 1) After dissolving hydroxypropyl β-cyclodextrin in water, add glycidyl methacrylate under a protective atmosphere, stir in a water bath at 40-60°C, and the sugar unit of hydroxypropyl β-cyclodextrin will open glycidyl methacrylate The epoxy bond of the ester is connected with it, and HP-β-CD-GMA is obtained after full reaction.

[0046] The molar ratio of hydroxypropyl β-cyclodextrin to glycidyl methacrylate is 1:6.5-8.

[0047] 2) Add polyethyleneimine to HP-β-CD-GMA, stir in a water bath at 40-60°C, the double bond in HP-β-CD-GMA and the amino group of polyethyleneimine are connected by Schiff base reaction , HP-β-CD-GMA-PEI was obtained after full reaction.

[0048]The molar ratio of hydroxypropyl β-cyclodextrin to polyethyleneimine is 1:6.5-8.

[0049] 3) Put the prepared HP-β-CD-GMA-PEI into a dial...

Embodiment 1

[0052] Weighed HP-β-CD1g and dissolved it in 20ml of deionized water, added 5ml of GMA dropwise under nitrogen protection, and stirred in a water bath at 44°C for 48 hours to obtain HP-β-CD-GMA;

[0053] Add 15ml PEI dropwise to the above product under nitrogen protection, stir in a water bath at 40°C for 48 hours, put the obtained product into a dialysis bag with a molecular weight of 3.5KDa, and dialyze it with flowing pure water for more than 48 hours, then freeze the remaining liquid in the dialysis bag After drying for 72 hours, HP-β-CD-GMA-PEI was obtained.

Embodiment 2

[0055] Weigh 0.01mol of HP-β-CD and dissolve it in 100ml of deionized water, add 0.07mol of GMA dropwise under nitrogen protection, and stir in a water bath at 50°C for 48 hours to obtain HP-β-CD-GMA;

[0056] Add 0.07molPEI dropwise to the above product under nitrogen protection, stir in a water bath at 40°C for 48 hours, put the product into a dialysis bag with a molecular weight of 3.5KDa, and freeze-dry the remaining liquid in the dialysis bag for 72 hours, namely HP-β-CD-GMA-PEI was obtained.

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PUM

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Abstract

The invention discloses a macromolecule skin penetration enhancer as well as a preparation method and applications thereof. The preparation method comprises the followings step of: linking HP-beta-CD (hydroxypropyl-beta-cyclodextrin) with PEI (polyethyleneimine) by utilizing GMA (glycidyl methacrylate), thereby synthesizing the novel skin penetration enhancer, namely HP-beta-CD-GMA-PEI. Through HP-beta-CD-GMA-PEI treatment, cuticle protein cell viability is improved, so that a keratin accumulation structure becomes loose, and the degree of freedom of the corresponding carbon motion is improved, so that the keratin carbon motion is accelerated. Under the same concentration, compared with azone, the HP-beta-CD-GMA-PEI has a better skin penetration effect, and when the concentration is increased by one time, the skin penetration effect is better.

Description

technical field [0001] The invention belongs to the technical field of transdermal absorption accelerators, and relates to a polymer transdermal absorption accelerator and its preparation method and application. Background technique [0002] Transdermal drug delivery systems (transdermal drug delivery systems) refer to new preparations for transdermal administration. This kind of preparation is usually administered through skin application. Transfer to various tissues or diseased parts, and play a role in treating or preventing diseases. The transdermal drug delivery system has the unique advantages of avoiding the degradation of the drug in the gastrointestinal tract, the first-pass effect of the liver, and the ability to administer or withdraw the drug at any time. Therefore, it has been continuously improved and developed rapidly since its inception. However, due to the relatively low transdermal absorption rate and transdermal drug dosage of many drugs, they cannot meet...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K9/00C08G81/00C08B37/16
Inventor 王珂邢建峰董凯许维
Owner 武汉天时维璟微生物科技有限公司
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