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Application of N-arginine chitosan as percutaneous sorbefacient

A technology of absorption enhancer, arginine, applied in the field of biomedicine

Inactive Publication Date: 2010-07-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of derivatives of arginine and chitosan as transdermal penetration enhancers has not been reported in literature and patents at home and abroad.

Method used

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  • Application of N-arginine chitosan as percutaneous sorbefacient
  • Application of N-arginine chitosan as percutaneous sorbefacient
  • Application of N-arginine chitosan as percutaneous sorbefacient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Implementation example 1: Experimental research on the promotion of adefovir transdermal absorption by N-arginine chitosan

[0019] 1. Synthesis of N-arginine chitosan

[0020] (1) BOC protection of arginine side chain amino group: Weigh 5 grams of arginine and dissolve it in 200ml deionized water, and then weigh 4 grams of Boc anhydride and dissolve it in 200ml tetrahydrofuran, and add arginine to the tetrahydrofuran solution dissolved in Boc anhydride In the aqueous acid solution, stir evenly, add dropwise 1mol / L NaOH solution to adjust the pH value to 9-10, stir and react at room temperature for 24 hours, put the reaction solution on a rotary evaporator to remove the tetrahydrofuran-water mixture, and obtain N-tert-butyl Oxycarbonyl arginine, take 200ml deionized water and dissolve it.

[0021] (2) Synthesis of N-arginine chitosan: take by weighing 10 grams of chitosan with a deacetylation degree of 90% and a molecular weight of 10,000, add it to 1% glacial acetic a...

Embodiment 2

[0032] Implementation example 2 insulin

[0033] 1, the synthesis of N-arginine chitosan: with embodiment 1.

[0034] 2. Transdermal experiment

[0035] Preparation of sample solution: Weigh 30mg of insulin and dissolve it in 18ml (0.1mol / L) HCl solution, divide the drug solution into 6 parts on average, adjust the pH value of the solution to 7 with 1mol / L NaOH, add distilled water to the full amount Take arginine, polysaccharide, derivatives of arginine and chitosan, and 60 mg of N-arginine chitosan after refining and purification, and dissolve them in the above solution to obtain arginine, poly Derivatives of sugar, arginine and chitosan and insulin solution at 2% concentration of N-arginine chitosan.

[0036] Transdermal test: take the above-prepared solution for transdermal test, and the test method is the same as in Example 1.

[0037] 3. Experimental results and data

[0038] Using different molecular weight chitosan, mixture of chitosan and arginine, and N-arginine ch...

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Abstract

The invention belongs to biomedical field, particularly relates to an application of a chitosan derivative N-arginine chitosan as percutaneous sorbefacient. The invention has advantages of providing a chitosan derivative which has simple structure and biodegradable property and can well promote percutaneous absorption of macromoleculare medicines and medicines with poor permeability.

Description

Technical field: [0001] The invention belongs to the field of biomedicine, and specifically relates to the application of N-arginine chitosan in promoting drug transdermal absorption. Background technique: [0002] The drug transdermal drug delivery system has the unique advantages of avoiding the degradation of the drug in the gastrointestinal tract and the first-pass effect of the liver, as well as giving or withdrawing the drug at any time. Therefore, it has been continuously improved and developed rapidly since its inception. . However, because the transdermal rate and transdermal drug dosage of many drugs are very low, which cannot meet the clinical treatment requirements, improving the transdermal delivery of drugs has become the key to the development of transdermal drug delivery systems. Commonly used methods to solve this problem include pharmaceutical methods, chemical methods, and physical methods, and the use of transdermal absorption enhancers is the most widel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K45/00A61K9/00A61K9/06A61K9/70
Inventor 吕慧侠周建平陈箐青张振海
Owner CHINA PHARM UNIV
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