Title:  Method for enhanced brain delivery of bupropion

United States Patent:  6,150,420

Assignee:  Theramax, Inc. (Lexington, KY)

Filed:  January 22, 1999

This invention provides to a method for enhancement of delivery of bupropion by administration via the nasal route, and methods of treatment comprising intranasal administration of bupropion. The present invention further provides pharmaceutical compositions comprising bupropion and/or pharmaceutically acceptable salts thereof.

SUMMARY OF THE INVENTION

Accordingly, a major object of the present invention is to provide a method for safely and conveniently administering bupropion to a patient in need of such treatment, comprising intranasally administering an effective amount of bupropion to prevent or treat symptoms of withdrawal from nicotine and for the treatment of depression.

The objective of the present inventors is to improve bupropion bioavailability by administering bupropion via the nasal route in order to reduce the dose required for its beneficial effect. This will result in lower plasma concentrations of metabolites of bupropion, and therefore fewer side effects. Intranasal delivery will improve drug bioavailability by direct absorption into the circulation avoiding extensive hepatic first-pass metabolism which significantly lowers the plasma and brain concentrations of bupropion administered orally. Therefore, small doses of bupropion can be administered which will result in fewer side effects, and the drug will be more tolerable and more effective, both in treating patients suffering from depression, and in tobacco smokers engaged in treatment of their smoking addiction. Lipophilic drugs achieve higher brain levels after intranasal administration than after intravenous administration. The nasal route of administration of bupropion may help to enhance the effectiveness of bupropion in the brain (the site of action). Additionally, as bupropion is heavily metabolized by the liver, administration by the nasal route may help to reduce drug interactions with other drugs that are also extensively metabolized by the liver.

Claim 1 of 23 Claims

What is claimed is:

1. A method for delivering bupropion to a patient comprising intranasally administering an effective amount of a pharmaceutical composition comprising bupropion, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier therefor.

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