Stabilization of epinephrine formulations
AssigneeYs Pharmtech
InventorYosyong SURAKITBANHARN
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Abstract
The disclosure herein relates to the innovative epinephrine formulations in aqueous solution of medicinal products that enhance the physicochemical stabilities of epinephrine and extend the product shelf life. In some instances, the formulations comprise epinephrine or a salt thereof, a complexing agent, and a “non-sulfite” antioxidant. The epinephrine formulations substantially demonstrated the superior physicochemical stabilities to conventional sulfite formulation of commercial medications currently available. In some instances, sulfite-free formulations further provide further benefit (e.g., safety benefits) to sulfite-sensitive patients. The compositions, methods for preparing the formulations, and methods of using the same (e.g., in the treatment of anaphylaxis) are also provided.
Claims51
A pharmaceutical composition comprising:
- epinephrine;
- one or more antioxidant, the antioxidant being present in the composition in an amount of about 0.07 wt. % or less (e.g., about 0.05 wt. % or less, about 0.04 wt. % or less, about 0.035 wt. % or less, or the like, such as down to about 0.005 wt. % or down to about 0.01 wt. %) (e.g., on a free base basis);
- and
- an aqueous medium;
- wherein the pharmaceutical composition has a pH of at least 3.5.
A pharmaceutical composition comprising:
- epinephrine;
- and
- one or more antioxidant, the one or more antioxidant being present in the composition in an antioxidant-to-epinephrine weight ratio of about 7:10 or less (e.g., less than 1:2).
A method for treating anaphylaxis, anaphylactic shock, or the symptoms thereof, the method comprising administering to an individual in need thereof a therapeutically effective amount of a composition of any one of the preceding claims.
A method of inhibiting the systemic distribution of locally administered anesthetic by administering the anesthetic concomitantly with (i) epinephrine and (ii) an antioxidant (e.g., cysteine) to an individual in need of a local anesthetic, wherein the epinephrine and antioxidant are administered in an antioxidant-to-epinephrine ratio of less than 1:2 (e.g., less than 1:5, or about 1:10), wherein the epinephrine is formulated at a pH of at least 3.5.
A method of inhibiting the systemic distribution of locally administered anesthetic by administering the anesthetic in a composition with (i) epinephrine and (ii) an antioxidant (e.g., cysteine) to an individual in need of a local anesthetic, wherein the composition comprises less than 0.05 wt. % antioxidant, wherein the epinephrine is formulated at a pH of at least 3.5.
Dependencies are inferred from the claim text.