US2023082397A1PendingUtilityA1

Acetaminophen compound composition without side effect to liver

71
Assignee: NATIONAL DEFENSE EDUCATION AND RES FOUNDATIONPriority: Nov 13, 2013Filed: Nov 23, 2022Published: Mar 16, 2023
Est. expiryNov 13, 2033(~7.3 yrs left)· nominal 20-yr term from priority
A61K 9/20A61K 47/22A61P 29/00A61K 47/38A61P 39/02A61K 47/26A61K 47/10A61K 31/167A61K 31/165A61K 47/12A61K 31/765A61K 47/32A61K 47/36A61K 47/14A61P 1/16A61K 9/06A61K 47/02A61K 9/48A61K 47/46
71
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Claims

Abstract

A new compound composition that is free of a side effect to a liver and used for alleviating the toxicity of an acetaminophen (APAP) medicament to the liver. The compound composition comprises (a) a pharmaceutically effective amount of acetaminophen and (b) a frequently-used safe and pharmaceutically acceptable excipient that can be combined with one or more than two medicaments that can reduce the toxicity of a drug via liver enzyme CYP2E1 metabolism to the liver. The compound is selected from the following group: Tween 20, microcrystalline cellulose, dicalcium phosphate, polyoxyethylene 23 lauryl ether, saccharin, mannitol, polyoxyethylene alkyl ether, sucralose, pyrrolidone, sodium starch glycolate, acrylic resin S100, carboxymethyl cellulose sodium, polyoxyethylene polyoxypropylene, menthol, low-substituted hydrocarbon propyl cellulose, pregelatinized starch, Dextrates NF hydrated, citric acid, polyoxyethylene castor oil, colloidal silica, polyethylene glycol monostearate aliphatic ester, sorbic acid, lemon oil, hydroxypropyl cellulose, sorbitol, acesulfame potassium, hypromellose phthalate, lactose monohydrate, maltodextrin, Brij 58, Brij 76, Tween 80, Tween 40, PEG 400, PEG 4000, PEG 2000, and the like, so as to reduce the side effect of the toxicity caused by acetaminophen to the liver.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method for reducing liver damage caused by acetaminophen (APAP), comprising
 administering to a subject in need thereof a compound selected from the group consisting of mannitol, sucralose, menthol, Eudragit S100, Pluronic F68, microcrystalline cellulose, and any combination thereof, in an amount effective in reducing liver damage caused by APAP.   
     
     
         2 . The method of  claim 1 , wherein the liver damage includes necrosis or vacuolization occurred in the liver. 
     
     
         3 . The method of  claim 1 , wherein the compound is selected from the group consisting of mannitol, sucralose, menthol and any combination thereof. 
     
     
         4 . The method of  claim 1 , wherein the compound includes at least mannitol and sucralose and optionally menthol. 
     
     
         5 . The method of  claim 1 , wherein the compound is mannitol, sucralose or a combination thereof. 
     
     
         6 . The method of  claim 1 , wherein the compound is a combination of mannitol and sucralose. 
     
     
         7 . The method of  claim 6 , wherein mannitol and sucralose are administered at a weight ratio of 1:1. 
     
     
         8 . The method of  claim 1 , wherein the compound is mannitol. 
     
     
         9 . The method of  claim 1 , wherein the compound is sucralose. 
     
     
         10 . The method of  claim 1 , wherein compound is administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP. 
     
     
         11 . A method for administering acetaminophen (APAP) to a subject in need thereof, comprising
 administering to the subject acetaminophen and a compound in an amount effective in reducing liver damage caused by APAP, wherein the compound is selected from the group consisting of mannitol, sucralose, menthol, Eudragit S100, Pluronic F68, microcrystalline cellulose, and any combination thereof.   
     
     
         12 . The method of  claim 11 , wherein the liver damage includes necrosis or vacuolization occurred in the liver. 
     
     
         13 . The method of  claim 11 , wherein the compound is selected from the group consisting of mannitol, sucralose, menthol and any combination thereof. 
     
     
         14 . The method of  claim 11 , wherein the compound includes at least mannitol and sucralose and optionally menthol. 
     
     
         15 . The method of  claim 11 , wherein the compound is mannitol, sucralose or a combination thereof. 
     
     
         16 . The method of  claim 11 , wherein the compound is a combination of mannitol and sucralose. 
     
     
         17 . The method of  claim 16 , wherein mannitol and sucralose are administered at a weight ratio of 1:1. 
     
     
         18 . The method of  claim 11 , wherein the compound is mannitol. 
     
     
         19 . The method of  claim 11 , wherein the compound is sucralose. 
     
     
         20 . The method of  claim 11 , wherein compound is administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP.

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