Creatine, its derivatives, compositions and methods of use thereof

Pending Publication Date: 2022-10-13
YU RUEY J +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0107]A female subject, age 68, with worsening osteoarthritis of both knees, who had been advised to have surgical knee replacement, sought advice on possible alternative treatments. She was provided with the following formulations for topical applications: Formulation A:
[0109]Subject reported that the formulation A and formulation B were equally effective in providing pain relief, of estimated 80%, within 3-8 minutes after application to the knees and lasting for 4-5 hours. Pain relief has been sufficient for her to postpone consideration of knee replacement until the COVID-19 pandemic is subdued.
[0110]A female subject, age 62, with aggravating lower back pain of 2-3 years duration, was provided 8 ounces of Formulation A (Example 4) to be applied to the lower back in late afternoon when her lower back pain intensified from mild to substantial. Pain subsided completely within 3-4 minutes, not returning until early afternoon the next day, beginning as mild and worsening during the afternoon hours.
[0111]Subject w

Problems solved by technology

However, none of the prior art described the use of creatine derivatives of the current inve

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example

Example 1

Formulation Vehicles

[0104]As used in the present application, “WEP 442” represents water 40 parts, ethanol 40 parts and propylene glycol 20 parts by volume; “NEP 433” represents water 40 parts, ethanol 30 parts and propylene glycol 30 parts by volume; “WEP 244” represents water 20 parts, ethanol 40 parts and propylene glycol 40 parts by volume; “EP 55” represents an anhydrous composition with ethanol 50 parts and propylene glycol 50 parts by volume; and “WP 82” represents water 80 parts and propylene glycol 20 parts by volume.

Example

Example 2

Evaluation of Analgesic Effectiveness

[0105]Five scales were used to evaluate the efficacy of analgesic effect: 0 (zero) for no effect; 1+(25%), which represents partial relief of pain, itch, or eczema for less than 6 hours; 2+(50%), which represents substantial but incomplete relief of pain, itch, or eczema for less than 6 hours; 3+(75%), which represents complete relief of pain, itch, or eczema for less than 6 hours; and 4+(90-100%), which represents complete relief or eradication of pain, itch, or eczema for more than 6 hours

Example

Example 3

Preparation of Formulation of C12X4WEP442

[0106]HCl salt of ethyl creatinate 1 gram was dissolved in 24 ml of a solution prepared from water 40 parts, ethanol 40 parts and propylene glycol 20 parts by volume. L-arginine 0.15 gram was then added to the resulting solution raise the pH from 2.7 to 5.2. The formulation thus obtained contained 4% ethyl creatinate and was referred to as C12X4WEP442.

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Abstract

The application describes creatine or its derivatives, compositions comprising the same, and uses thereof for topical or systemic administration to treat pain, itch, or eczema, or inflammation associated with a cosmetic or medical condition, disorder or disease in a human subject, wherein the inflammation causes the pain, itch, or eczema. In addition, the application describes clinical use of these compounds and compositions which can reduce or eliminate erythema, edema and tissue distortions associated with inflammation.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority under 35 U.S.C. §119 to U.S. Provisional Patent Application No. 63 / 169,584, filed on April 1, 2021, and U.S Provisional Patent Application No. 63 / 241,130, filed on Sep. 7, 2021, the disclosures of which are herein incorporated by reference in their entireties.FIELD OF THE INVENTION[0002]The application describes creatine or its derivatives, compositions comprising the same, and uses thereof for topical or systemic administration to treat pain, itch, or eczema, or inflammation associated with a cosmetic or medical condition, disorder or disease in a human subject. In addition, the application describes clinical use of these compounds and compositions which can reduce or eliminate erythema, edema and tissue distortions associated with inflammation.BACKGROUND OF THE INVENTION[0003]Creatine is thought to improve strength, increase lean muscle mass, and help the muscles recover more quickly during exercise. Thi...

Claims

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Application Information

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IPC IPC(8): A61K31/195A61K45/06A61P29/00A61P17/06A61P17/00A61P25/06
CPCA61K31/195A61K45/06A61P29/00A61P17/06A61P17/00A61P25/06A61P17/04A61K31/198A61K31/22A61K9/0019A61K9/08A61K47/26
Inventor YU, RUEY J.VAN SCOTT, EUGENE J.
Owner YU RUEY J
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