NON-SEDATING ANTIHISTAMINE INJECTION FORMULATIONS AND METHODS OF USE THEREOF
First Claim
1. A method of increasing peak plasma concentration and/or providing immediate onset of plasma concentration of cetirizine in an individual in need of treatment for acute urticaria or angioedema associated with an acute allergic reaction, wherein the acute allergic reaction optionally includes anaphylaxis, comprisingadministering to the individual an intravenous injection of an injectable cetirizine composition containing 2 mg to 20 mg of cetirizine at a rate of 10 mg per 1.0-1.5 minutes or faster,wherein the peak plasma concentration (Cmax) of the intravenous injectable cetirizine composition is greater than twice the Cmax of a reference immediate-release oral cetirizine dosage form having the same number of mg of cetirizine as the injectable cetirizine composition, and wherein the area under the plasma time curve measured as AUC0-36hr and AUC0-inf is substantially the same for the intravenously injectable cetirizine composition and the reference immediate-release oral cetirizine dosage form.
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Accused Products
Abstract
Described herein are injectable compositions containing non-sedating or second and third generation antihistamines such as cetirizine/levocetirizine and methods of use thereof. Specifically, methods of treating acute urticaria or angioedema associated with an acute allergic reaction are disclosed. In certain embodiments, the injectable compositions are bioequivalent to currently marketed oral dosage forms with the same number of mg of cetirizine.
1 Citation
18 Claims
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1. A method of increasing peak plasma concentration and/or providing immediate onset of plasma concentration of cetirizine in an individual in need of treatment for acute urticaria or angioedema associated with an acute allergic reaction, wherein the acute allergic reaction optionally includes anaphylaxis, comprising
administering to the individual an intravenous injection of an injectable cetirizine composition containing 2 mg to 20 mg of cetirizine at a rate of 10 mg per 1.0-1.5 minutes or faster, wherein the peak plasma concentration (Cmax) of the intravenous injectable cetirizine composition is greater than twice the Cmax of a reference immediate-release oral cetirizine dosage form having the same number of mg of cetirizine as the injectable cetirizine composition, and wherein the area under the plasma time curve measured as AUC0-36hr and AUC0-inf is substantially the same for the intravenously injectable cetirizine composition and the reference immediate-release oral cetirizine dosage form.
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9. A method of decreasing the time for cetirizine to appear in the bloodstream of a patient in need of treatment for acute urticaria or angioedema associated with an acute allergic reaction, wherein the acute allergic reaction optionally includes anaphylaxis, comprising
administering to the patient an intramuscular injection of an injectable cetirizine composition containing 2 mg to 20 mg of cetirizine, wherein at least about 5 ng/mL of cetirizine appears in the patient'"'"'s bloodstream within about 4 minutes of administration.
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10. A method of treating a patient in need of injection with cetirizine, comprising
administering to the patient an intravenous injection of an injectable cetirizine composition containing 2 mg to 20 mg of cetirizine at a rate of 10 mg per 1.0-1.5 minutes or faster, to provide an immediate about 2 minute peak plasma concentration (Cmax) of the intravenous injectable cetirizine composition that is greater than twice the Cmax of a reference immediate-release oral cetirizine dosage form having the same number of mg of cetirizine as the injectable cetirizine composition, or administering an intramuscular injection of an injectable cetirizine composition containing 2 mg to 20 mg of cetirizine, wherein at least about 5 ng/mL of cetirizine appears in the patient'"'"'s bloodstream within about 4 minutes of administration.
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17. An injectable composition, comprising
2 to 20 mg of cetirizine per mL, 1 to 9 mg of sodium chloride per mL, 2 to 20 mg of benzyl alcohol per mL, and water q.s. to 100%, adjusted to a pH of about 5.5+/−
Specification