Stable aqueous capsaicin injectable formulations and medical uses thereof
AssigneeCentrexion Therapeutics Corporation
InventorsDrazen Ostovic, Gary Fred Musso
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Abstract
The invention provides stable, aqueous capsaicin injectable formulations, a unit dose containing such injectable formulations, medical kits, and methods for using such injectable formulations and unit doses to treat patients suffering from pain, such as osteoarthritic knee pain. The stable, aqueous capsaicin injectable formulations may contain, for example, capsaicin, a solubilizing agent (e.g., a polyethylene glycol ester of a (C15-C25) hydroxyalkanoic acid), an antioxidant, and water.
Claims30
An aqueous, capsaicin injectable formulation, comprising
- a. about 0.04% (w/w) to about 0.06% (w/w) of capsaicin;
- b. about 0.5% (w/w) to about 1.5% (w/w) of a solubilizing agent, wherein the solubilizing agent comprises
- and polyethylene glycol;
- c. about 0.005% (w/w) to about 0.015% (w/w) of an antioxidant;
- d. about 0.2% (w/w) to about 1% (w/w) of an alkali metal acetate;
- e. about 0.01% (w/w) to about 0.05% (w/w) of a chelating agent;
- f. about 0.3% (w/w) to about 0.9% (w/w) of a tonicity modifier;
- g. at least 96% (w/w) water;
- and
- having a pH in the range of about 5 to about 6;
- wherein the formulation contains less than 1% (w/w) of capsaicin-dimer having the following structure:
An aqueous, capsaicin injectable formulation, comprising
- a. about 0.04% (w/w) to about 0.06% (w/w) of capsaicin;
- b. about 0.8% (w/w) to about 1.2% (w/w) of a solubilizing agent, wherein the solubilizing agent comprises (a) about 70% (w/w) of a mixture of
- and (b) about 30% (w/w) polyethylene glycol;
- c. about 0.005% (w/w) to about 0.015% (w/w) of dibutylhydroxytoluene;
- d. about 0.2% (w/w) to about 1% (w/w) of sodium acetate;
- e. about 0.01% (w/w) to about 0.05% (w/w) of ethylenediaminetetraacetic acid or a salt thereof;
- f. about 0.3% (w/w) to about 0.9% (w/w) of sodium chloride;
- g. at least 96% (w/w) water;
- and
- having a pH in the range of about 5 to about 6;
- wherein the formulation contains less than 1% (w/w) of capsaicin-dimer having the following structure:
Dependencies are inferred from the claim text.