United States Patent:  6,080,762

Assignee:  Eli Lilly and Company (Indianapolis, IN)

Filed:  April 8, 1999

The present invention relates to formulations and methods for pulmonary and nasal administration of raloxifene.

SUMMARY OF THE INVENTION

The present invention relates to a method for pulmonary delivery of raloxifene to a patient which comprises:

having the patient inhale an aerosolized amount of raloxifene through the patient's mouth into the lungs; and

optionally repeating the inhalation step a sufficient number of times until an effective amount of raloxifene is delivered to the patient.

In addition, the present invention relates to a method for the nasal delivery of raloxifene to a patient which comprises:

having the patient inhale an aerosolized amount of raloxifene through and into the patient's nose; and

optionally repeating the inhalation step a sufficient number of times until an effective amount of raloxifene is delivered to the patient.

Furthermore, the present invention relates to a pharmaceutical formulation comprising raloxifene dissolved or suspended in a pharmaceutical solvent at a concentration between 1 mg/mL and 100 mg/mL, optionally in the presence of one or more preservatives, surfactants or gases, said formulation suitable for nebulization or spraying.

Moreover, the present invention relates to a pharmaceutical formulation comprising raloxifene present as a dry powder, with a mass median equivalent aerodynamic diameter between 0.5 .mu.m and 100 .mu.m, in an aerosol propellant, optionally in the presence of ethanol, said formulation suitable for use in a metered dose inhaler.

The methods of the present invention provide for an unexpected high level of bioavailability of raloxifene which results from delivery of raloxifene via the nose and/or lung.

Claim 1 of 30 Claims

1. A method for pulmonary delivery of raloxifene to a patient which comprises:

having the patient inhale an aerosolized amount of raloxifene through the patient's mouth into the lungs; and

optionally repeating the inhalation step a sufficient number of times until an effective amount of raloxifene is delivered to the patient.

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