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Title:
PHARMACEUTICAL COMPOSITIONS FOR TOPICAL APPLICATION TO TREAT ERECTILE DYSFUNCTION
Document Type and Number:
WIPO Patent Application WO/2001/008659
Kind Code:
A1
Abstract:
A pharmaceutical composition for topical application to treat erectile dysfunction is provided. The composition includes at least one of the following compounds: paparevine, phentolamine and prostaglandin E1. The compounds are mixed with dimethyl sulfoxide (DMSO) which acts as a suitable penetrant carrier to enhance absorption of the compounds. The pharmaceutical composition is effective for creating erections of normal duration through topical application.

Inventors:
MCGRAIL J SIMON
KERESTECI ARA G
KASMAN BARRY
Application Number:
PCT/CA2000/000799
Publication Date:
February 08, 2001
Filing Date:
July 05, 2000
Export Citation:
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Assignee:
LAKEFIELD MINERALS LTD (CA)
International Classes:
A61K9/00; A61K47/20; A61P15/10; (IPC1-7): A61K9/00; A61K47/20; A61P15/10
Domestic Patent References:
WO1998043614A11998-10-08
WO1998052569A11998-11-26
Foreign References:
US4801587A1989-01-31
US6031002A2000-02-29
EP0346297A11989-12-13
US5741511A1998-04-21
US5942545A1999-08-24
DE19728103A11999-01-07
Attorney, Agent or Firm:
DONAHUE ERNST & YOUNG LLP (Suite 1800 P.O. Box 197 T.D. Centre Toronto, Ontario M5K 1H6, CA)
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Claims:
Claims We claim:
1. A pharmaceutical composition for topical application to treat erectile dysfunction, the composition including at least one of the following compounds: * Papaverine <BR> <BR> Phentolamine<BR> Prostaglandin E1, and a suitable penetrant carrier to enhance absorption of said at least one compound.
2. A pharmaceutical composition according to claim 1 wherein the penetrant carrier is dimethyl sulfoxide (DMSO).
3. A pharmaceutical composition according to claim 2 wherein the composition includes papaverine and prostaglandin E1.
4. A pharmaceutical composition according to claim 2 wherein the composition includes papaverine and phentolamine.
5. A pharmaceutical composition according to claim 2 wherein the composition includes prostaglandin E1 and phentolamine.
6. A pharmaceutical composition according to claim 2 wherein the composition includes papaverine, phentolamine and prostaglandin E1.
7. A pharmaceutical composition for topical application to treat erectile dysfunction, the composition including at least one compound that is effective for producing an erection upon entry into the bloodstream of the penis, dissolved in dimethyl sulfoxide (DMSO).
8. A pharmaceutical composition according to claim 7 wherein the at least one compound is selected from the group comprising papaverine, phentolamine and prostaglandin E1.
9. A pharmaceutical composition according to claim 7 wherein the at least one compound includes papaverine and prostaglandin E1.
10. A pharmaceutical composition according to claim 7 wherein the at least one pharmaceutical includes papaverine and phentolamine.
11. A pharmaceutical according to claim 7 wherein the at least one pharmaceutical includes phentolamine and prostaglandin E1.
12. A pharmaceutical composition according to claim 7 wherein the at least one compound includes papaverine, phentolamine and prostaglandin E1.
13. A method of making a pharmaceutical composition for topical application to treat erectile dysfunction comprising the steps of: providing a quantity of at least one compound that is effective for producing an erection upon entry into the bloodstream of the penis; mixing said at least one compound in a volume of water; providing a volume of DMSO; and mixing the compound/water mixture in said DMSO.
14. A method according to claim 13 wherein the at least the compound includes papaverine, phentolamine and prostaglandin E1.
15. A method of making a pharmaceutical composition for topical application to treat erectile dysfunction comprising the steps of: Providing a quantity of papaverine; Providing a quantity of phentolamine; Providing a quantity of prostaglandin E1; * Mixing the papaverine, phentolamine and prostaglandin E1 in a quantity of water; Providing a quantity of a suitable penetrant carrier to enhance absorption of said papaverine, phentolamine and prostaglandin E1; and * Mixing the solution in said suitable penetrant carrier.
16. A method according to claim 16 wherein the suitable penetrant carrier is DMSO.
17. A method of making a pharmaceutical composition for topical application to treat erectile dysfunction comprising the steps of: Providing a quantity of papaverine; * Providing a quantity of phentolamine; Providing a quantity of prostaglandin E1; Mixing the papaverine, phentolamine and prostaglandin E1 in a quantity of water to create a solution; Providing a quantity of DMSO; and Mixing the solution in said DMSO.
18. A method of making a pharmaceutical composition for topical application to treat erectile dysfunction comprising the steps of: * Providing a quantity of papaverine; Providing a quantity of phentolamine; Providing a quantity of prostaglandin E1; Providing a quantity of DMSO; and * Mixing the papaverine, phentolamine and prostaglandin E1 in said DMSO.
19. Use of the pharmaceutical composition of claim 1 to topically treat erectile dysfunction.
20. Use of the pharmaceutical composition of claim 7 to topically treat erectile dysfunction.
Description:
Pharmaceutical Compositions for Topical Application to Treat Erectile Dvsfunction Field of the Invention The invention relates to pharmaceutical preparations for treating erectile dysfunction.

Background Male impotency or erectile dysfunction is a problem affecting millions of men across North America and the rest of the world. Up to thirty million men are affected by male impotency in the United States alone. The problem is especially common in aging men. There are several treatments available for this condition.

External vacuum therapies are available for treating all types of impotence.

This is often used as a first step treatment for erectile dysfunction. Generally, this therapy involves the creation of negative pressure in a plastic cylinder through the use of a pump. The user inserts his penis into the cylinder. The vacuum causes blood to enter the penis in a way similar to a natural erection. Despite the fact that this therapy has a ninety percent success rate, it is an awkward and uncomfortable treatment. Because of these drawbacks, men are often reluctant to use this treatment.

Erectile dysfunction can also be treated through oral prescription medication.

The best known is Sildenafil Citrate (Viagra). Viagra received FDA approval on

March 27,1998 and has received much publicity since being introduced into the marketplace. ViagraTM can be taken orally in a pill form. This treatment has had a good success rate in treating impotent men.

However, many men are reluctant to try this treatment. The consistent use of a pill is considered to be undesirable by many men since the drug enters the user's entire system. The drug is therefore circulated through the user's entire body and is not concentrated in the affected region. This is a concern because it is still unknown what the long-ter effects of Viagra may be on other organs and organ systems of the body.

Hormone therapy is used to treat impotence caused by a testosterone deficiency. Raising the level of testosterone in men having a deficiency has proved to be effective for treating impotency in many cases. This treatment has the drawback of having serious side effects.

Another method for treating erectile dysfunction is the use of a urethral suppository. This procedure involves the insertion of an applicator tip into the urethra for delivery of a suppository. Absorption occurs through the urethral wall. This treatment is quite awkward, uncomfortable, and often painful.

More radical treatments for erectile dysfunction include penile implant surgery and vascular surgery. This is a last resort because of the inherent risks of undertaking any surgical procedure.

it has been known since the early nineteen eighties that penile injection therapy is effective for creating erections. Three drugs, papaverine, phentolamine and prostaglandin E1 have been used successfully to create erections through this technique.

The patient must inject a solution containing one or more of these drugs directly into the penis. Hand pressure must be applied afterwards for a few minutes to prevent bleeding.

Despite the fact that impotent men have enjoyed a high success rate through this treatment, the method has several obvious drawbacks. The prospect of injecting a needle into the penis is quite daunting to many men. The puncture of the needle can also cause a great deal of pain. As a result, few choose this method when presented with other alternatives.

Another drawback of penile injection therapy is priapism. This is an unwanted prolonged erection that results from injecting more of the drug than is required for an erection of normal duration. Penile injection therapy also has a drawback of being extremely costly. Injections normally cost about twenty to twenty-five dollars.

A pharmaceutical preparation that can be applied topically to the penis would avoid the drawbacks of the current treatments for erectile dysfunction. A topical treatment has not been previously developed because there has previously not been a known carrier for drugs such as papaverine, phentolamine and prostaglandin E1 that can both be absorbed through the skin into the bloodstream while effectively carrying the drugs into the bloodstream.

There is therefore a need for a pharmaceutical preparation that is effective for creating an erection in impotent men through topical application to the penis.

Summarv of the Invention The invention comprises a pharmaceutical composition that is effective for treating erectile dysfunction through topical application to the penis. The pharmaceutical composition includes at least one compound that is effective for creating an erection when entering the bloodstream of the penis and a suitable penetrant carrier to enhance absorption of the compound.

According to one aspect of the invention a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The composition includes at least one of the following compounds: 'Papaverine <BR> Phentolamine<BR> Prostaglandin E1.

A suitable penetrant carrier to enhance absorption of at least one of these compounds is also provided.

According to another aspect of the invention a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The composition includes at least one compound that is effective in creating erections in impotent men upon

entering the bloodstream of the penis. The compound is dissolved in dimethyl sulfoxide (DMSO).

According to another aspect of the invention a method of making a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The method comprises the steps of providing a quantity of at least one compound that creates an erection upon entering the bloodstream of the penis, mixing at least one compound in a volume of water, providing a volume of DMSO and mixing the compound/water mixture in the DMSO.

According to yet another aspect of the present invention, a method for making a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The method comprises the steps of providing a quantity of papaverine, providing a quantity of phentolamine, providing a quantity of prostaglandin E1, mixing the papaverine, phentolamine and prostaglandin E1 in a quantity of water to create a solution, providing a quantity of a suitable penetrant carrier to enhance absorption of the papaverine, phentolamine and prostaglandin E1 and mixing the solution in the suitable penetrant carrier.

According to another aspect of the present invention, a method of making a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The method comprises the steps of providing a quantity of papaverine, providing a quantity of phentolamine, providing a quantity of prostaglandin E1, mixing the papaverine, phentolamine and prostaglandin E1 in a quantity of water to create a solution, providing a quantity of DMSO and mixing the solution in the DMSO.

According to another aspect of the present invention, a method of making a pharmaceutical composition for topical application to treat erectile dysfunction is provided. The method comprises the steps of providing a quantity of papaverine, providing a quantity of phentolamine, providing a quantity of prostaglandin E1, providing a quantity of DMSO and mixing the papaverine, phentolamine and prostaglandin E1 in the DMSO.

According to another aspect of the present invention, use is made of the pharmaceutical composition for topical application to treat erectile dysfunction. The composition includes at least one of the following compounds: 'Papaverine <BR> Phentolamine<BR> Prostaglandin E 1, and a suitable penetrant carrier to enhance absorption of said at least one compound.

According to yet another aspect of the present invention, use is made of a pharmaceutical preparation to topically treat male impotency. A pharmaceutical composition has at least one pharmaceutical that enlarges blood vessels. The pharmaceutical is dissolved in DMSO.

Description The pharmaceutical composition of the present invention is prepared by mixing an effective amount of papaverine, phentolamine and prostaglandin E1 into a quantity of water sufficient to dissolve these compounds. The solution is then mixed with preferably an equal volume of dimethyl sulfoxide (DMSO). It is not strictly necessary that the volume should be equal but this is preferred for ease of preparation. The resulting mixture is then applied directly onto the penis. The DMSO acts as a carrier for the papaverine, phentolomine and prostaglandin E1 as the DMSO is absorbed through the skin of the penis into the blood vessels of the penis. Once these compounds reach the blood vessels of the penis, an erection is achieved rapidly by the user.

It is also possible two prepare a pharmaceutical composition that is effective for creating an erection in this manner, that includes only one or two of the three drugs mentioned above.

An effective topical preparation may also be prepared by dissolving papaverine, phentolomine and prostaglandin E1 directly into DMSO. The solution is then applied directly to the penis resulting in rapid erection.

It is preferred to mix all three drugs together with DMSO. However, it is also possible to prepare a composition containing either one or two of the three drugs mixed with DMSO. Positive results are achieved with these formulations but the best results are achieved when all three drugs are mixed together.

Compositions containing one or more of papaverine, phentolamine or prostaglandin E1 mixed with an effective penetrant carrier other than DMSO such as a cream are within the scope of the present invention.

The following examples illustrate the invention: Example 1: Preparation of water/DMSO formulation.

Papaverine: 300 milligrams Phentolamine: 15 milligrams Prostaglandin E1: 100 micrograms The compounds above are mixed into approximately 4 milliliters of water to produce solution A. Solution A is then mixed into approximately four milliliters of DMSO to produce solution B. The resulting solution B is appropriate and effective for a single topical application to create an erection.

Example 2: Preparation of pure DMSO mixture.

Papaverine: 300 milligrams Phentolamine: 15 milligrams Prostaglandin E1: 100 micrograms, The compounds above are mixed into 4 milliliters of DMSO. The resulting mixture is appropriate and effective for a single topical application to create erection.

The mixtures of example 1 and example 2 are effective for rapidly producing high quality erections of normal duration.

Although the invention has been described with preferred embodiments, it is to be understood that modifications may be resorted to as will be apparent to those skilled in the art. Such modifications and variations are to be considered within the purview and scope of the present invention.