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N-acetyl cysteine compositions and methods to improved the therapeutic efficacy of acetaminophen

A paracetamol and acetylcysteine ​​technology, applied in the field of N-acetylcysteine ​​composition and improving the therapeutic efficacy of paracetamol, can solve problems such as allowable dose limitation of treatment plan, limited treatment and the like

Inactive Publication Date: 2012-07-11
THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, physicians treating children with high fevers often find their treatment options limited by the currently allowed doses
Lowering this dose would further limit treatment for these cases
Likewise, treatment of severe pain may be limited by the maximum dose of acetaminophen that can be prescribed or recommended without causing toxicity

Method used

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  • N-acetyl cysteine compositions and methods to improved the therapeutic efficacy of acetaminophen
  • N-acetyl cysteine compositions and methods to improved the therapeutic efficacy of acetaminophen
  • N-acetyl cysteine compositions and methods to improved the therapeutic efficacy of acetaminophen

Examples

Experimental program
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Effect test

Embodiment approach

[0063] According to one embodiment, the molar ratio of APAP:NAC in the composition of the invention is 1:15 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:10 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:5 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:4 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:3 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:2 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:1 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:0.5 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:0.25 (w / w). According to another embodiment, the molar ratio of APAP:NAC in said composition is 1:0.125 (w / w). Accor...

Embodiment 1

[0157] Example 1. Veterinary use of compositions comprising acetaminophen-N-acetylcysteine

[0158] Veterinarians have experimented with many preparations to provide pain relief in a variety of animal species. Many of these species are more susceptible to the toxic effects of acetaminophen than humans. For example, toxicity was demonstrated in dogs at doses >40 mg / kg compared to doses >140 mg / kg in humans. The most severe toxicity was in felines, where acetaminophen toxicity and death were demonstrated in felines at doses as low as 5-10 mg / kg. This toxicity limits the therapeutic use of acetaminophen in animals.

[0159] According to the present invention, animals needing antipyretic or analgesia are treated with a unit dose of APAP and a therapeutically enhanced amount of NAC so that paracetamol and N-acetylcysteine ​​are contained in the composition of paracetamol and N-acetylcysteine. -The molar ratio of acetylcysteine ​​is in the condition existing composition treatment...

Embodiment 2

[0160] Example 2. Long-term use of an acetaminophen-NAC composition in an adult patient to control osteoarthritis pain

[0161] Adult patients take a standard dose of 1000 mg of acetaminophen four times daily for osteoarthritis pain. The patient obtained the same pain relief by taking 750 mg of acetaminophen-NAC four times a day, and the efficacy of the acetaminophen-NAC formulation did not diminish during long-term use of the acetaminophen-NAC composition.

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Abstract

The present invention relates to compositions for improving the efficacy of acetaminophen comprising a unit dose of acetaminophen and a therapeutic efficacy-enhancing amount of N- acetylcysteinc, such that acetaminophen and N-acctylcysteinc are present in the composition in a molar ratio of acetaminophen to N-acetyl cysteine ranging from about 1:15 to about 1:0.000977, and use of such compositions for analgesic and antipyretic applications.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority to US Provisional Application No. 61 / 225,679, filed July 15, 2009, which is incorporated herein by reference in its entirety. field of invention [0003] The present invention relates to compositions for improving the efficacy of acetaminophen preparations comprising a therapeutically efficacy-improving amount of N-acetylcysteine ​​and a unit dose of acetaminophen, and to such compositions with respect to analgesia and pain relief. The use of thermal application, whereby the formulation of the composition can enhance the therapeutic efficacy of acetaminophen when administered at standard doses, and enable the administration of substandard doses of acetaminophen to achieve the same level as in standard acetaminophen Potency equivalent to that obtained at the dose. Background technique [0004] Over the past 30 years, acetaminophen, presented in various formulations, has ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/12A01N37/44A61K31/195
CPCA61K9/0019A61K9/006A61K31/198A61K31/167A61K9/0031A61K9/0014A61K9/2095A61K9/0043A61K9/0053A61K2300/00A61P29/00A61P43/00
Inventor 莉奥诺·A··赫岑伯格詹姆斯·安德勒斯
Owner THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV
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