- Patent Number:
11534,416
- Appl. No:
16/411861
- Application Filed:
May 14, 2019
- نبذة مختصرة :
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.
- Inventors:
NATIONAL DEFENSE EDUCATION AND RESEARCH FOUNDATION (Taipei, TW)
- Assignees:
NATIONAL DEFENSE EDUCATION AND RESEARCH FOUNDATION (Taipei, TW)
- Claim:
1. A method for reducing liver damage caused by acetaminophen (APAP), comprising administering to a subject in need thereof at least mannitol and sucralose and optionally menthol, in an amount effective in reducing liver damage caused by APAP, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg.
- Claim:
2. The method of claim 1 , wherein the liver damage includes necrosis or vacuolization occurred in the liver of the subject.
- Claim:
3. The method of claim 1 , wherein mannitol and sucralose are administered at a weight ratio of 1:1.
- Claim:
4. A method for administering acetaminophen (APAP) to a subject in need thereof, comprising administering to the subject acetaminophen, and at least mannitol and sucralose and optionally menthol in an amount effective in reducing liver damage caused by APAP, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg.
- Claim:
5. The method of claim 4 , wherein the liver damage includes necrosis or vacuolization occurred in the liver of the subject.
- Claim:
6. The method of claim 4 , wherein the acetaminophen, mannitol, sucralose and optionally menthol are administered separately, simultaneously or sequentially.
- Claim:
7. The method of claim 4 , wherein the acetaminophen, mannitol, sucralose and optionally menthol are formulated in a pharmaceutical composition.
- Claim:
8. The method of claim 7 , wherein the pharmaceutical composition is in a form of gel, solution, capsule, torches, or tablets, in a pharmaceutically acceptable dosage form.
- Claim:
9. The method of claim 4 , wherein the acetaminophen, mannitol, sucralose and optionally menthol are included in pharmaceutical kits, pharmaceutical packs or patient packs and acceptable container.
- Claim:
10. The method of claim 7 , wherein the pharmaceutical composition is a formulation consisting essentially of acetaminophen, mannitol and sucralose.
- Claim:
11. The method of claim 4 , wherein mannitol and sucralose are administered at a weight ratio of 1:1.
- Claim:
12. A method for reducing liver damage caused by acetaminophen (APAP), comprising administering to a subject in need thereof at least mannitol and sucralose and optionally at least one compound selected from the group consisting of Menthol, Eudragit S100, Pluronic F68, and Microcrystalline cellulose, in an amount effective in reducing liver damage caused by APAP, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg.
- Claim:
13. A method for administering acetaminophen (APAP) to a subject in need thereof, comprising administering to the subject acetaminophen and a compound as an inhibitor in an amount effective in reducing liver damage caused by APAP, wherein the compound is at least mannitol and sucralose and optionally at least one compound selected from the group consisting of Menthol, Eudragit S100, Pluronic F68, and Microcrystalline cellulose.
- Claim:
14. The method of claim 1 , wherein mannitol and sucralose are administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP.
- Claim:
15. The method of claim 4 , wherein mannitol and sucralose are administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP.
- Claim:
16. The method of claim 12 , wherein mannitol and sucralose are administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP.
- Claim:
17. The method of claim 13 , wherein mannitol and sucralose are administered in an amount effective to reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI) from APAP.
- Claim:
18. 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, and any combination thereof, in an amount effective in reducing liver damage caused by APAP, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg, provided that when sucralose is administered in an amount of 10 mg, it is administered in combination with mannitol in an amount of 10-250 mg.
- Claim:
19. A method for administering acetaminophen (APAP) to a subject in need thereof, comprising administering to the subject acetaminophen and a compound as an inhibitor in an amount effective in reducing liver damage caused by APAP, wherein the compound is selected from the group consisting of Mannitol, Sucralose, Menthol, and any combination thereof, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg, provided that when sucralose is administered in an amount of 10 mg, it is administered in combination with mannitol in an amount of 10-250 mg.
- Claim:
20. 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, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg, provided that when sucralose is administered in an amount of 10 mg, it is administered in combination with mannitol in an amount of 10-250 mg.
- Claim:
21. A method for administering acetaminophen (APAP) to a subject in need thereof, comprising administering to the subject acetaminophen and a compound as an inhibitor 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, wherein mannitol is administered in an amount of 10-250 mg and sucralose is administered in an amount of 10-250 mg, provided that when sucralose is administered in an amount of 10 mg, it is administered in combination with mannitol in an amount of 10-250 mg.
- Patent References Cited:
7101572 September 2006 Santos
10456371 October 2019 Hu
20140038921 February 2014 Hu
20200009097 January 2020 Hu
20210008101 January 2021 Hu
WO 2007/050631 May 2007
WO-2012142724 October 2012
- Other References:
Lee et al. 1996, JBC, vol. 271, No. 20, pp. 12063-12067. (Year: 1996). cited by examiner
- Primary Examiner:
McMillian, Kara R
- Attorney, Agent or Firm:
Birch, Stewart, Kolasch & Birch, LLP
- الرقم المعرف:
edspgr.11534416
No Comments.