Title:  Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation

United States Patent:  6,403,597

Assignee:  Vivus, Inc. (Mountain View, CA)

Filed:  June 21, 2001

A method is provided for treatment of premature ejaculation by administration of a phosphodiesterase inhibitor, e.g., an inhibitor of a Type III, Type IV, or Type V phosphodiesterase. In a preferred embodiment, administration is on as "as needed" basis, i.e., the drug is administered immediately or several hours prior to sexual activity. Pharmaceutical formulations and packaged kits are also provided.

SUMMARY OF THE INVENTION

It is a primary object of the invention to address the above-described need in the art by providing a novel method for the treatment of premature ejaculation by administering an effective amount of a phosphodiesterase inhibitor to an individual in need of such therapy, wherein the term "phosphodiesterase inhibitor" includes phosphodiesterase inhibitors per se as well as pharmaceutically acceptable (and pharmacologically active) salts, esters, amides, prodrugs, active metabolites and other derivatives thereof.

It is another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is administered orally.

It is another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is administered transmucosally, e.g., via the sublingual, buccal, nasal, transurethral or rectal routes, or via inhalation.

It is another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is administered topically, transdermally, parenterally, or by other routes.

It is still another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is a Type III inhibitor, a Type IV inhibitor, a Type V inhibitor, or a nonspecific phosphodiesterase inhibitor.

It is yet another object of the invention to provide such a method wherein the phosphodiesterase inhibitor is a Type V inhibitor.

It is a further object of the invention to provide such a method wherein drug administration is on an as-needed basis.

It is still a further object of the invention to provide such a method wherein the active agent is administered in a controlled release formulation.

It is yet a further object of the invention to provide such a method wherein the controlled release formulation is a sustained release formulation and/or a delayed release formulation.

It is an additional object of the invention to provide such a method wherein the controlled release formulation is a sustained release formulation that provides drug release over a time period in the range of about 4 to about 48 hours.

It is still an additional object of the invention to provide a composition containing an amount of a phosphodiesterase inhibitor effective for the treatment of premature ejaculation.

It is another object of the invention to provide a packaged kit comprised of a container housing a phosphodiesterase inhibitor formulation as provided herein and instructions for administering the formulation in a manner effective to treat premature ejaculation.

Additional objects, advantages and novel features of the invention will be set forth in part in the description which follows, and in part will become apparent to those skilled in the art upon examination of the following, or may be learned by practice of the invention.

In a first aspect of the invention, a method is provided for the treatment of an individual prone to or suffering from premature ejaculation, the method comprising administering to an individual in need of such treatment a pharmaceutical formulation containing a therapeutically effective amount of an active agent selected from the group consisting of phosphodiesterase inhibitors and pharmaceutically acceptable, pharmacologically active salts, esters, amides, prodrugs, active metabolites, and other derivatives thereof. Administration of the pharmaceutical formulation may be on an "as-needed" basis or within the context of an ongoing dosage regimen. By "as-needed" dosing, also known as pro re nata dosing, is meant the administration of a single dose of the active agent at some time prior to anticipated sexual activity. Administration can be immediately prior to sexual activity, or up to about 2 or 3 hours prior to anticipated sexual activity, although with sustained release dosage forms, a single dose can provide therapeutic efficacy over an extended time period in the range of about 4 to 48 hours, depending on the formulation. Drug delivery may be accomplished through any mode of administration, including, but not limited to, the oral and transmucosal routes.

In a further aspect of the invention, pharmaceutical formulations are provided for carrying out the method of the invention. The pharmaceutical formulations comprise a therapeutically effective amount of an active agent as provided herein, a pharmacologically acceptable carrier or vehicle, generally a carrier or vehicle suitable for transmucosal drug administration, and, optionally, an enhancer. Other types of components may be incorporated into the formulation as well, e.g., excipients, surfactants, preservatives (e.g., antioxidants), stabilizers, chelating agents, and the like, as will be appreciated by those skilled in the art of pharmaceutical formulation preparation and drug delivery.

In another aspect of the invention, a packaged kit is provided for a patient to use in the treatment of premature ejaculation. The kit includes a pharmaceutical formulation of a phosphodiesterase inhibitor, a container housing the pharmaceutical formulation during storage and prior to administration, and instructions, e.g., written instructions on a package insert or label, for carrying out drug administration in a manner effective to treat premature ejaculation. The pharmaceutical formulation may be any formulation described herein, e.g., an oral dosage form containing a unit dosage of the phosphodiesterase inhibitor, the unit dosage being a therapeutically effective dosage for treatment of premature ejaculation.

Claim 1 of 94 Claims

We claim:

1. A method for treating premature ejaculation, which comprises administering to a male individual in need of such treatment a therapeutically effective amount of an active agent selected from the group consisting of phosphodiesterase inhibitors and pharmaceutically acceptable salts, esters, amides, prodrugs, and active metabolites thereof.

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