Flumazenil formulations for subcutaneous injection and methods of treatment using gaba receptor modulators
AssigneeBexson Biomedical, Inc.
InventorsJeffrey BECKER, Gregg PETERSON
Life of this patent
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Abstract
Provided herein are subcutaneous formulations of flumazenil that are useful for treating a variety of disease and disorders. The subcutaneous flumazenil formulations provided herein reduce injection site irritation and pain and allow for home administration to enhance patient compliance.
Claims40
A pharmaceutical composition, comprising:
- (i) flumazenil, or an isotopic variant thereof;
- or a pharmaceutically acceptable salt, solvate or hydrate thereof;
- and
- (ii) at least one pharmaceutically acceptable excipient,
- wherein the pharmaceutical composition is in a form for dosing or administration by subcutaneous injection;
- and
- wherein the concentration of flumazenil in the pharmaceutical composition is greater than 0.7 mg/mL.
A method of treating a disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of flumazenil, wherein the flumazenil is administered by subcutaneous injection in an amount of at least 0.5 mg/day from a single device for a period of time of at least 2 days, wherein the single device has a reservoir volume less than 30 mL.
The method of claim 28, wherein the flumazenil is administered at a rate of at least about μg/hr, at least about 60 μg/hr, at least about 80 μg/hr, at least about 100 μg/hr, at least about 150 μg/hr, at least about 200 μg/hr, or at least about 250 μg/hr.
A pharmaceutical composition, comprising:
- (i) a pharmaceutical compound, wherein the pharmaceutical compound is a GABAA receptor antagonist or modulator, a GABA receptor agonist, a GABA receptor partial agonist, a GABAA receptor negative allosteric modulator or inverse agonist, or salvinorin A, or an isotopic variant thereof;
- or a pharmaceutically acceptable salt, solvate or hydrate thereof;
- and
- (ii) at least one pharmaceutically acceptable excipient, wherein the at least one pharmaceutically acceptable excipient comprises a cyclodextrin substituted with at least one acidic functional group or a conjugate base thereof or a cyclodextrin substituted with at least one polar functional group,
- wherein the pharmaceutical composition is in a form for dosing or administration by subcutaneous injection.
A method of treating a disease or disorder in a subject in need thereof, comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical compound, wherein the pharmaceutical compound is GABAA receptor antagonist or modulator, a GABA receptor agonist, a GABA receptor partial agonist, a GABAA receptor negative allosteric modulator or inverse agonist, or salvinorin A, wherein the pharmaceutical compound is administered by subcutaneous injection from a single device for a period of time of at least 2 days, wherein the single device has a reservoir volume less than 30 mL.
Dependencies are inferred from the claim text.