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Positively charged water-soluble 4-acetamidophenol having rapid skin penetration speed, and related compound prodrug thereof

A compound and composition technology, applied in skin diseases, organic chemistry, organic active ingredients, etc., can solve the problems of slow skin penetration

Inactive Publication Date: 2013-10-16
于崇曦 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the slow skin penetration of these drugs, it is difficult to achieve therapeutically effective plasma concentrations by means of formulations

Method used

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  • Positively charged water-soluble 4-acetamidophenol having rapid skin penetration speed, and related compound prodrug thereof
  • Positively charged water-soluble 4-acetamidophenol having rapid skin penetration speed, and related compound prodrug thereof
  • Positively charged water-soluble 4-acetamidophenol having rapid skin penetration speed, and related compound prodrug thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0051] Preparation of N-acetyl-4-aminophenyl diethylaminobutyrate hydrochloride

[0052] 15.1 g (0.1 mol) of paracetamol and 16 g (0.1 mol) of diethylaminobutyric acid were dissolved in 300 ml of dichloromethane. The reaction was cooled to 0°C with an ice bath. Add 20.6 g (0.1 mol) of N,N'-dicyclohexylcarbodiimide. The mixture was stirred at 0°C for 1 hour and at room temperature for 2 hours. The solids were removed by filtration. The dichloromethane solution was washed twice with 100ml of 5% sodium bicarbonate solution, and then washed three times with 100ml of water. The organic solution was dried over anhydrous sodium sulfate. Sodium sulfate was removed by filtration. 6 g of acetic acid was added to the reaction mixture with stirring. The solid product was collected by filtration. After drying, 27 g of the hygroscopic target product was obtained, with a yield of 82.1%. Solubility in water: 400mg / ml; Elemental analysis: C 16 h 25 ClN 2 o 3 ;Molecular weight: 328....

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Abstract

The invention discloses a prodrug compound represented by a structure formula 1, a composition or a preparation thereof, and a use of the prodrug compound in preparation of drugs for treatment of treatable conditions of non-steroidal anti-inflammation drugs in human or animals. The prodrug compound has a more rapid skin penetration speed compared with the corresponding parent drug. The invention further discloses a transdermal treatment application system, which at least contains one of the prodrug compound represented by the structure formula 1, or the composition, or the preparation.

Description

[0001] Divisional statement [0002] This application is a Chinese patent application filed on September 3, 2006 with the application number 200680055747.0 and the title of the invention is "Prodrugs of positively charged water-soluble acetaminophen and its related compounds with fast skin penetration rate" divisional application. technical field [0003] The present invention relates to positively charged, water-soluble prodrugs of acetaminophen, acetaminophen, and related compounds and their use in the treatment of any acetaminophen and acetaminophen-treated state in humans or animals Applications. Specifically, the present invention is directed to overcoming the side effects associated with the use of acetaminophen and its related compounds. These prodrugs can be administered orally or transdermally. Background technique [0004] N-acetyl-p-aminophenol (acetaminophen), 4-acetylaminophenyl salicylic acid (acetamoxalol) and their related compounds belong to the 4-aminoph...

Claims

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Application Information

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IPC IPC(8): C07C233/25A61K31/222A61P29/00A61P35/00A61P1/08A61P25/00A61P19/02A61P19/10A61P27/06A61P17/00A61P25/06A61P17/06A61P17/10
Inventor 于崇曦徐丽娜
Owner 于崇曦
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