Title:  Formulations for pulmonary delivery of dopamine agonists

United States Patent:  6,193,954

Assignee:  Abbott Laboratories (Abbott Park, IL)

Filed:  March 21, 1997

The present invention relates to methods and formulations for administering a dopamine agonist to the airways of a patient. The preferred dopamine agonist is selected from (5aR-trans)-4,5,6,7,11b-hexahydro-2-propylbenzo[f]thieno[2,3-c]quinoline- 9,10) -diol, diacetate (ester) hydrochloride. The delivery method relates to certain aerosol formulations and liquid formulations which are administered into the airways to provide effective delivery of the dopamine agonists to the receptor.

SUMMARY OF THE INVENTION

Dopamine agonists such as those described below are effectively absorbed from the airways. After absorption from the lung, the drug bypasses the liver and is distributed to the body. The efficacy of fomulations administered to the lungs is similar to that obtained by injection.

Accordingly, the present invention provides a method of administering a dopamine agonist to a patient comprising administering a therapeutically effective amount of a dopamine agonist to the airways of the patient. This deliver means can occur through nasal or tracheal administration and can be in the form of a formulation or composition comprising a dopamine agonist delivered in the form of a solid, microparticle or powder and may further comprise a pulmonary delivery excipient selected from solids or liquids which are aqueous based or non-aqueous based. Liquid formulations delivered through the airways according to this invention may be prepared in aqueous or non-aqueous vehicles and delivered to the airways by means of drops or sprays. The present invention therefore relates to a composition for pulmonary delivery comprising a dopamnine agonist dispersed in an aqueous or non-aqueous delivery vehicle. The aqueous vehicle is selected from pure water, substantially pure water or water combined with other excipients such as salts, ions or other excipients which are generally used in aqueous based systems. The liquid formulations are in the form of solution based dispersions or solutions in solvents or cosolvents such as alcohols or glycols with water. Non-aqueous solutions include those alchohol or glycol based systems which may have some water but which are not comprised of a majority percentage of water and which are known to those of skill in the art as effective and safe delivery vehicles. Non-aqueous solutions also include those systems containing halogenated hydrocarbons. Administration of liquid formulations in the form of drops or dispersions occurs through the nose and/or trachea to facilitate absorption of the formulation and prodrug and/or active ingredients into the lungs and ultimately delivery to the dopamine receptors where the medicinal effect is achieved to treat, for example, Parkinson's disease or conditions resulting from substance abuse such as self-administration of cocaine. Devices may be utilized to assist in the delivery of the drug(s).

In another embodiment, the present invention provides a pharmaceutical composition for aerosol delivery of a dopamine agonist comprising a dopamine agonist, a propellant, poloxamer and tocopherol.

In another embodiment, the present invention provides a method of administering a dopamine agonist to a patient comprising administering to the patient a therapeutically effective amount of the aerosol composition described above.

In another embodiment, the present invention provides a method of administering a dopamine agonist to a patient comprising administering to the lungs of the patient a therapeutically effective amount of the liquid formulation described above.

Claim 1 of 31 Claims

What is claimed is:

1. A method of administering a dopamine agonist to a patient in need of such treatment comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising a dopamine agonist, a propellant and poloxamer.

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