Nasal pharmaceutical formulations and methods of using the same
AssigneeMerck Patent GmbH
InventorImtiaz Chaudry
Life of this patent
Estimating the term…
Abstract
Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is beclomethasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is beclomethasone dipropionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.
Claims30
A nasal pharmaceutical formulation comprising a therapeutically effective amount of beclomethasone, wherein the formulation comprises about 0.005% to about 5% by weight beclomethasone having the following particle size distribution profile:
- (i) about 10% of the beclomethasone particles have a particle size of less than 0.75 microns;
- (ii) about 25% of the beclomethasone particles have a particle size of less than 1.5 microns;
- (iii) about 50% of the beclomethasone particles have a particle size of less than 2.0 microns;
- (iv) about 75% of the beclomethasone particles have a particle size of less than 3.5 microns;
- and
- (v) about 90% of the beclomethasone particles have a particle size of less than 5.0 microns, and wherein the beclomethasone is suitable for administration to an individual via intranasally.
A nasal spray formulation comprising:
- an aqueous suspension having about 0.005% to about 5% by weight beclomethasone and having the following particle size distribution profile:
- (i) about 10% of the beclomethasone particles have a particle size of less than 0.40 microns;
- (ii) about 25% of the beclomethasone particles have a particle size of less than 0.70 microns;
- (iii) about 50% of the beclomethasone particles have a particle size of less than 1.30 microns;
- (iv) about 75% of the beclomethasone particles have a particle size of less than 2.0 microns;
- and
- (v) about 90% of the beclomethasone particles have a particle size of less than 3.0 microns.
A method of treating one or more symptoms of rhinitis in an individual, said method comprising the steps of applying to the individual's nasal mucosa a formulation comprising about 0.005% to about 5% by weight beclomethasone having the following particle size distribution profile:
- (i) about 10% of the beclomethasone particles have a particle size of less than 0.75 microns;
- (ii) about 25% of the beclomethasone particles have a particle size of less than 1.5 microns;
- (iii) about 50% of the beclomethasone particles have a particle size of less than 2.0 microns;
- (iv) about 75% of the beclomethasone particles have a particle size of less than 3.5 microns;
- and
- (v) about 90% of the beclomethasone particles have a particle size of less than 5.0 microns, and wherein the beclomethasone is suitable for administration to an individual via intranasally.
Dependencies are inferred from the claim text.