JPWO2021186437A5 - - Google Patents

Claims (21)

A pharmaceutical composition comprising an anti-anaphylactic adrenergic receptor agonist as an active agent in dry powder form for intranasal administration, the composition comprising at least one active agent in combination with at least one functional additive. a first type of solid particles and a second type of solid particles comprising a pharmaceutically acceptable carrier, wherein at least about 90% of the first type of particles have an average particle size of about 10 to 30 microns. less than about 10% of the first type of particles have an average particle size of about 10 microns or less, and the average particle size of the second type of particles is equal to or less than the average particle size of the first type of particles. A pharmaceutical composition having a larger than average particle size. 2. The pharmaceutical composition of claim 1, wherein the second type of particles has an average particle size of about 50-200 microns. 3. The at least one functional additive contained in the first type of particles and the carrier contained in the second type of particles are substantially free of excipients other than the carrier. Pharmaceutical composition. A pharmaceutical composition according to any one of claims 1 to 3, wherein the active agent is epinephrine, norepinephrine, dopamine or antihistamine, or any of their pharmaceutically acceptable salts or derivatives. 5. A pharmaceutical composition according to claim 4, wherein the active agent is epinephrine or a pharmaceutically acceptable salt thereof. 6. A pharmaceutical composition according to claim 4 or claim 5, wherein the active agent is epinephrine or a pharmaceutically acceptable bitartrate, hydrochloride, or borate salt thereof. The pharmaceutical composition according to any one of claims 1 to 6, wherein the functional additive is a buffer, a lubricant, or a lubricant. 8. The pharmaceutical composition according to claim 7, wherein the buffering agent is sodium dihydrogen phosphate. Pharmaceutical composition according to any one of claims 1 to 8, wherein the ratio of the at least one pharmaceutically active agent to the at least one functional additive in the first type of particles is predetermined. . A pharmaceutical composition according to any one of claims 1 to 9, wherein the carrier is either lactose monohydrate, lactose, a lactose functional analog, or any mixture of at least two thereof. The pharmaceutical composition according to any one of claims 1 to 9, wherein the carrier is dextrose, sorbitol, mannitol, maltitol, xylitol, cellulose or a cellulose derivative, and starch or a starch derivative. The pharmaceutical composition according to any one of claims 1 to 10, wherein the weight ratio of the first type of particles to the second type of particles is 1:9 to 9:1. An epinephrine pharmaceutical composition comprising as an active agent epinephrine or a pharmaceutically acceptable salt thereof in dry powder form for intranasal administration, the composition comprising: epinephrine in combination with a physiologically acceptable buffer; or a pharmaceutically acceptable salt thereof and a second type of solid particles comprising lactose monohydrate as a carrier, at least about 90% of the first type of particles comprising about having an average particle size of 10 to 30 microns, less than about 10% of the first type of particles have an average particle size of about 10 microns or less, and the second type of particles have an average particle size of about 10 microns or less; , larger than said first type of particles, and providing a nominally measured therapeutically effective amount of said epinephrine or a pharmaceutically acceptable salt thereof. 14. The epinephrine pharmaceutical composition according to claim 13, wherein the molar ratio of epinephrine bitartrate to sodium dihydrogen phosphate is 0.9:1. 15. The epinephrine pharmaceutical composition of claim 13 or 14, wherein the therapeutically effective amount of epinephrine corresponds to about 0.3 mg or 0.5 mg of epinephrine administered intramuscularly (i.m.). Disposable dosage unit form for intranasal administration to a subject of a pharmaceutical composition according to any one of claims 1 to 12, said dosage unit being loaded with a predetermined single dose of said composition. a disposable dosage unit form that provides a metered dose of a pharmaceutically active adrenergic receptor agonist to said subject. 15. A disposable dosage unit form for intranasal administration to a subject of a pharmaceutical composition according to claim 13 or 14, said dosage unit being filled with a predetermined single dose of said composition and containing a metered amount of epinephrine. a disposable dosage unit form that provides the subject with a dose of 16. A disposable dosage unit form for intranasal administration to a subject of a pharmaceutical composition according to claim 15, wherein the dosage unit is loaded with a predetermined single dose of the composition, about 0.3 mg or 0.5 mg. A disposable dosage unit form that provides the subject with a metered dose of epinephrine equivalent to mg of epinephrine administered intramuscularly (i.m.). A kit for intranasal administration of epinephrine, the kit comprising:
a. at least one dosage unit comprising a pharmaceutical composition according to any one of claims 13 to 15 for intranasal administration; and
b. Kit, including instructions for use. for use in the treatment of anaphylactic shock in patients in need of
A therapeutically effective amount of a composition according to any one of claims 1 to 12, or at least one dosage unit form according to claim 16 . Therapeutic effectiveness of an epinephrine composition according to any one of claims 13 to 15, or at least one dosage unit form according to claims 17 or 18, for use in the treatment of anaphylactic shock in a patient in need thereof. amount .