US2023330017A1PendingUtilityA1

Liquid formulation comprising paeonol and apocynin

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Assignee: AKL RES & DEVELOPMENT LTDPriority: Nov 23, 2017Filed: Jun 1, 2023Published: Oct 19, 2023
Est. expiryNov 23, 2037(~11.3 yrs left)· nominal 20-yr term from priority
Inventors:Nicholas John Larkins
A61K 9/08A61K 31/12A61K 47/10A61K 47/14A61K 36/65A61K 9/4858A61K 36/24A61K 9/48A61K 36/539A61P 25/28A61P 29/00A61K 31/085Y02A50/30A61K 36/68A61K 36/708A61K 36/898A61K 2300/00A61P 25/00A61K 9/0087
60
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Claims

Abstract

A stable liquid formulation is provided. The liquid formulation includes a composition of active ingredients paeonol and apocynin. Methods of production of such a formation and treatment of diseases administering such a formulation are also provided.

Claims

exact text as granted — not AI-modified
1 . A liquid formulation comprising active compounds 2-hydroxy-4-methoxyacetophenone (paeonol) or isomer thereof and 4-hydroxy-3-methoxyacetophenone (apocynin) or isomer thereof wherein the ratio by weight of paeonol to apocynin is from 3:2 to 9:1. 
     
     
         2 . A formulation according to  claim 1  further comprising at least one excipient wherein the ratio by weight of total active compounds to excipient is from 2:3 to 19:1. 
     
     
         3 . A formulation according to  claim 2  wherein the excipient is a glycol or glycol derivative, a polyhydric alcohol, or an ester and/or ether thereof. 
     
     
         4 . A formulation according to  claim 2  wherein the excipient is a glycol. 
     
     
         5 . A formulation according to  claim 2  wherein the excipient is a polyethylene glycol. 
     
     
         6 . A formulation according to  claim 2  wherein the excipient is polyethylene glycol 400. 
     
     
         7 . A formulation according to  claim 1  wherein the ratio by weight of paeonol or isomer thereof to apocynin or isomer thereof is from 80:20 to 77.7:22.3. 
     
     
         8 . A formulation according to  claim 2  wherein the ratio by weight of total active compounds to excipient is 64:36. 
     
     
         9 . A formulation according to  claim 1  wherein the formulation is stable at room temperature. 
     
     
         10 . A formulation according to  claim 1  wherein the formulation is made from a eutectic mixture of 2-hydroxy-4-methoxyacetophenone (paeonol) or isomer thereof and 4-hydroxy-3-methoxyacetophenone (apocynin) or isomer thereof. 
     
     
         11 . A liquid formulation comprising active compounds 2-hydroxy-4-methoxyacetophenone (paeonol) or isomer thereof and 4-hydroxy-3-methoxyacetophenone (apocynin) or isomer thereof wherein the ratio by weight of paeonol to apocynin is from 3:2 to 9:1, the formulation further comprising at least one excipient wherein the ratio by weight of total active compounds to excipient is from 2:3 to 19:1. 
     
     
         12 . A liquid formulation made from a eutectic mixture comprising active compounds paeonol or isomer thereof and apocynin or isomer thereof. 
     
     
         13 . A formulation according to  claim 12  further comprising at least one excipient. 
     
     
         14 . A formulation according to  claim 13  wherein the excipient is a glycol or glycol derivative, a polyhydric alcohol, or an ester and/or ether thereof. 
     
     
         15 . A formulation according to  claim 13  wherein the excipient is a glycol. 
     
     
         16 . A formulation according to  claim 13  wherein the excipient is a polyethylene glycol. 
     
     
         17 . A formulation according to  claim 13  wherein the excipient is polyethylene glycol 400. 
     
     
         18 . A formulation according to  claim 13  wherein the ratio by weight of total active compounds to excipient is from 2:3 to 19:1. 
     
     
         19 . A formulation according to  claim 13  wherein the ratio by weight of total active compounds to excipient is 64:36. 
     
     
         20 . A formulation according to  claim 12  wherein the ratio by weight of paeonol or isomer thereof to apocynin or isomer thereof is from 3:2 to 9:1. 
     
     
         21 . A formulation according to  claim 12  wherein the ratio by weight of paeonol or isomer thereof to apocynin or isomer thereof is from 80:20 to 77.7:22.3. 
     
     
         22 . A formulation according to  claim 12  wherein the formulation is stable at room temperature. 
     
     
         23 . A formulation according to  claim 1  for the treatment of inflammatory disease. 
     
     
         24 . A formulation according to  claim 1  for the treatment of neurodegenerative disease. 
     
     
         25 . A method of treatment of inflammatory disease and/or neurodegenerative disease comprising a step of administering to a patient in need thereof a formulation according to  claim 1 . 
     
     
         26 . A formulation made from a eutectic mixture comprising active compounds paeonol or isomer thereof and apocynin or isomer thereof. 
     
     
         27 . A formulation according to  claim 26  wherein the formulation is a liquid. 
     
     
         28 . The formulation according to  claim 2  wherein the ratio by weight of total active compounds to excipient is from 2:3 to 9:1. 
     
     
         29 . The formulation according to  claim 11  wherein the ratio by weight of total active compounds to excipient is from 2:3 to 9:1. 
     
     
         30 . The formulation according to  claim 13  wherein the ratio by weight of total active compounds to excipient is from 2:3 to 9:1.

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