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WO2001008659A1 - Preparations pharmaceutiques pour application directe destinees au traitement de la dyserection - Google Patents

Preparations pharmaceutiques pour application directe destinees au traitement de la dyserection Download PDF

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Publication number
WO2001008659A1
WO2001008659A1 PCT/CA2000/000799 CA0000799W WO0108659A1 WO 2001008659 A1 WO2001008659 A1 WO 2001008659A1 CA 0000799 W CA0000799 W CA 0000799W WO 0108659 A1 WO0108659 A1 WO 0108659A1
Authority
WO
WIPO (PCT)
Prior art keywords
prostaglandin
phentolamine
pharmaceutical composition
papaverine
providing
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CA2000/000799
Other languages
English (en)
Inventor
J. Simon Mcgrail
Ara G. Keresteci
Barry Kasman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LAKEFIELD MINERALS Ltd
Original Assignee
LAKEFIELD MINERALS Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by LAKEFIELD MINERALS Ltd filed Critical LAKEFIELD MINERALS Ltd
Priority to AU59576/00A priority Critical patent/AU5957600A/en
Publication of WO2001008659A1 publication Critical patent/WO2001008659A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence

Definitions

  • the invention relates to pharmaceutical preparations for treating erectile dysfunction.
  • 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.
  • ViagraTM 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
  • urethral suppository 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, papavenne, 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
  • Penile injection therapy Another drawback of penile injection therapy is p ⁇ apism 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 papavenne, phentolamine and prostaglandin E1 that can both be absorbed through the skin into the bloodstream while effectively carrying the drugs into the bloodstream
  • drugs such as papavenne, phentolamine and prostaglandin E1 that can both be absorbed through the skin into the bloodstream while effectively carrying the drugs into the bloodstream
  • 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.
  • composition for topical application to treat erectile dysfunction.
  • the composition includes at least one of the following compounds:
  • a suitable penetrant carrier to enhance absorption of at least one of these compounds is also provided.
  • a pharmaceutical composition for topical application to treat erectile dysfunction 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).
  • a method of making a pharmaceutical composition for topical application to treat erectile dysfunction 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.
  • a method for making a pharmaceutical composition for topical application to treat erectile dysfunction 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.
  • a method of making a pharmaceutical composition for topical application to treat erectile dysfunction 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.
  • 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.
  • composition for topical application to treat erectile dysfunction.
  • the composition includes at least one of the following compounds:
  • a pharmaceutical composition has at least one pharmaceutical that enlarges blood vessels.
  • the pharmaceutical is dissolved in DMSO.
  • 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.
  • DMSO dimethyl sulfoxide
  • 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.
  • 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.
  • 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.
  • Example 1 Preparation of water/DMSQ formulation.
  • solution A 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.
  • 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.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une composition pharmaceutique pour application directe destinée au traitement de la dysérection. Cette composition comprend au moins un des composés suivants: la paparévine, la phentolamine et la prostaglandine E1. Les composés sont mélangés avec du diméthylsulfoxyde (DMSO) qui agit comme support pénétrant approprié pour améliorer l'absorption des composés. Cette composition pharmaceutique appliquée directement est efficace pour favoriser des érections de durée normale
PCT/CA2000/000799 1999-07-30 2000-07-05 Preparations pharmaceutiques pour application directe destinees au traitement de la dyserection Ceased WO2001008659A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU59576/00A AU5957600A (en) 1999-07-30 2000-07-05 Pharmaceutical compositions for topical application to treat erectile dysfunction

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36504899A 1999-07-30 1999-07-30
US09/365,048 1999-07-30

Publications (1)

Publication Number Publication Date
WO2001008659A1 true WO2001008659A1 (fr) 2001-02-08

Family

ID=23437266

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA2000/000799 Ceased WO2001008659A1 (fr) 1999-07-30 2000-07-05 Preparations pharmaceutiques pour application directe destinees au traitement de la dyserection

Country Status (2)

Country Link
AU (1) AU5957600A (fr)
WO (1) WO2001008659A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6677335B1 (en) 1999-10-11 2004-01-13 Pfizer Inc Pharmaceutically active compounds
WO2004011029A3 (fr) * 2002-07-26 2004-05-21 Kenneth W Adams Elargissement du penis
US8374577B2 (en) 2002-06-18 2013-02-12 Telefonaktiebolaget Lm Ericsson (Publ) Parallel coordinated operations in private domains
EP4232002A4 (fr) * 2020-10-22 2024-10-23 Madera Pharmaceuticals, Inc. Traitement transdermique pour le dysfonctionnement érectile

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4801587A (en) * 1987-03-02 1989-01-31 Gene Voss Impotence ointment
EP0346297A1 (fr) * 1988-06-08 1989-12-13 CENTRO MEDICO HARVEY S.r.l. Préparation pour emploi topique dans le traitement thérapeutique d'impotentia coeundi
US5741511A (en) * 1995-04-12 1998-04-21 Sam Yang Co., Ltd. Transdermal drug delivery device for treating erectile dysfunction
WO1998043614A1 (fr) * 1997-03-28 1998-10-08 Lam Pharmaceuticals, Llc Preparations medicamenteuses pour le traitement de dysfonctions sexuelles
WO1998052569A1 (fr) * 1997-05-19 1998-11-26 Zonagen, Inc. Therapie combinatoire permettant de moduler la reponse sexuelle chez un patient
DE19728103A1 (de) * 1997-07-02 1999-01-07 Winfried Dr Med Heinicke Pharmazeutisches Präparat zur Behandlung erektiler Dysfunktion sowie Injektionshilfe zur Injektion des Präparats
US5942545A (en) * 1998-06-15 1999-08-24 Macrochem Corporation Composition and method for treating penile erectile dysfunction
US6031002A (en) * 1998-05-01 2000-02-29 Michael Ebert Method for enhancing female sexual response and a composition therefor

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4801587A (en) * 1987-03-02 1989-01-31 Gene Voss Impotence ointment
EP0346297A1 (fr) * 1988-06-08 1989-12-13 CENTRO MEDICO HARVEY S.r.l. Préparation pour emploi topique dans le traitement thérapeutique d'impotentia coeundi
US5741511A (en) * 1995-04-12 1998-04-21 Sam Yang Co., Ltd. Transdermal drug delivery device for treating erectile dysfunction
WO1998043614A1 (fr) * 1997-03-28 1998-10-08 Lam Pharmaceuticals, Llc Preparations medicamenteuses pour le traitement de dysfonctions sexuelles
WO1998052569A1 (fr) * 1997-05-19 1998-11-26 Zonagen, Inc. Therapie combinatoire permettant de moduler la reponse sexuelle chez un patient
DE19728103A1 (de) * 1997-07-02 1999-01-07 Winfried Dr Med Heinicke Pharmazeutisches Präparat zur Behandlung erektiler Dysfunktion sowie Injektionshilfe zur Injektion des Präparats
US6031002A (en) * 1998-05-01 2000-02-29 Michael Ebert Method for enhancing female sexual response and a composition therefor
US5942545A (en) * 1998-06-15 1999-08-24 Macrochem Corporation Composition and method for treating penile erectile dysfunction

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6677335B1 (en) 1999-10-11 2004-01-13 Pfizer Inc Pharmaceutically active compounds
US7176311B2 (en) 1999-10-11 2007-02-13 Pfizer Inc. Process for preparing pharmaceutically active compounds
US8374577B2 (en) 2002-06-18 2013-02-12 Telefonaktiebolaget Lm Ericsson (Publ) Parallel coordinated operations in private domains
WO2004011029A3 (fr) * 2002-07-26 2004-05-21 Kenneth W Adams Elargissement du penis
US7671091B2 (en) 2002-07-26 2010-03-02 Adams Kenneth W Penis enlargement
EP4232002A4 (fr) * 2020-10-22 2024-10-23 Madera Pharmaceuticals, Inc. Traitement transdermique pour le dysfonctionnement érectile

Also Published As

Publication number Publication date
AU5957600A (en) 2001-02-19

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