GB2314771A - Topical preparation for relief of erectile dysfunction - Google Patents

Topical preparation for relief of erectile dysfunction Download PDF

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Publication number
GB2314771A
GB2314771A GB9613860A GB9613860A GB2314771A GB 2314771 A GB2314771 A GB 2314771A GB 9613860 A GB9613860 A GB 9613860A GB 9613860 A GB9613860 A GB 9613860A GB 2314771 A GB2314771 A GB 2314771A
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GB
United Kingdom
Prior art keywords
preparation
preparation according
component
relief
erectile dysfunction
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.)
Granted
Application number
GB9613860A
Other versions
GB9613860D0 (en
GB2314771B (en
Inventor
Michael Euan Carruthers
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.)
Multimed Ltd
Original Assignee
Multimed 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 Multimed Ltd filed Critical Multimed Ltd
Priority to GB9613860A priority Critical patent/GB2314771B/en
Publication of GB9613860D0 publication Critical patent/GB9613860D0/en
Publication of GB2314771A publication Critical patent/GB2314771A/en
Application granted granted Critical
Publication of GB2314771B publication Critical patent/GB2314771B/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • 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

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

Abstract

This invention relates to a topical preparation for the relief of erectile dysfunction containing a aminophylline; b co-dergocrine mesylate; c isosorbide dinitrate; Id at least one compound capable of releasing and/or donating and/or carrying nitric oxide; e.g. L-arginine and optionally e testosterone.

Description

TOPICAL PREPARATION FOR RELIEF OF ERECTILE DYSFUNCTION The present invention relates to pharmaceutical preparations for the relief of erectile dysfunction.
The use of mechanical and/or pharmaceutical preparations for the treatment of impotence in men is well known. However these methods have often been clumsy and mechanical or cold blooded and anxiety producing. The present invention concerns a preparation that is applied directly to the penis.
According to the present invention a topical preparation for the relief of erectile dysfunction contains [a] aminophylline; [b] co-dergocrine mesylate; [c] isosorbide dinitrate; [d] at least one compound capable of releasing and/or donating and/or carrying nitric oxide; and optionally [e] testosterone.
According to the present invention the topical preparation can be supplied in the form of a cream, gel or spray for application to the penis before sexual activity.
Thus the mentioned active components can be carried in a water-based cream or jelly such as KY jelly.
A preferred embodiment of the invention is a medicated condom, in which a preparation according to the invention is contained within a prophylactic sheath, e.g. as an internal coating. When the condom is worn the active ingredients of the preparation are held in contact with the penis all the time; other benefits are the retention of blood within the penis due to the condom and the prevention of rubbing off of the preparation on the sexual partner.
The preparation according to the invention can generate high concentrations of NO in the genital tract of both men and women, and this can have both spermicidal and bacteriocidal (and even virocidal) effects to make for safer sex.
A preferred component [d) for use in the invention is L-arginine, which is the natural substrate for all three forms of the NOS (Nitric Oxide Synthase) enzyme in the body; it also has the advantages that it is a natural product which is often taken in large amounts by mouth, and is easily and cheaply available.
Other compounds suitable for component [d] include sodium nitrite, amyl nitrite, glyceryl trinitrate, sodium nitroprusside, 3- morpholinosydonimine (SIN-1), S-nitroso-N acetyl-D, L-penicillamine (SNAP), S-nitrosoglutathione (SNOG), and the nitroxyl releaser N-acetyl-N-acetoxy-4chlorobenzenesulphonamide (NANAC).
The above compounds for use as or in component [d] may be present singly or in any combination of two or more.
A suitable concentration of component [d] in the preparation is 0.01-5* w/v, e.g. about 1% w/v. All percentages herein are calculated as weight in grams per 100 mQ of the total preparation.
In preparations according to the invention any form of testosterone as component [e] (when present) may be used.
A preferred example contains dihydrotestosterone (DHT).
Testosterone, and especially DHT, has a local effect, sensitising the penis and aiding NO generation, and in higher concentrations is absorbed systemically, contributing to the general actions of testosterone given by other routes. These general actions include enhancement of libido and potency.
A suitable concentration of component [e), when present, is up to 0.5 or 5% w/v (g/100 mQ).
Compound [c], isosorbide dinitrate, is absorbed topically and will general nitric oxide;; it is suitably present in a proportion of 0.1 to 1%, e.g. about 0.25%, g/100 mQ. Components [a) and [b] can improve blood supply to the penis to facilitate erection. Component [a) is suitably present in a concentration of 0.5 to 5%, e.g. about 3%, g/100 me. Component [b] is suitably present in a concentration of 0.1 to 2%, e.g. about 0.05%, g/100 mQ.
One preferred preparation according to the invention has the composition (A) component [d) 1% Aminophylline 3% Mesylated co-dergocrine 0.05% Isosorbide dinitrate 0.25% KY jelly (excipient) balance Another preferred preparation according to the invention has the above composition (A) with up to 0.5g/100 mQ of testosterone (e.g. DHT) also included.

Claims (8)

CLAIMS:
1. A topical preparation for the relief of erectile dysfunction containing [a] aminophylline; [b] co-dergocrine mesylate; [c] isosorbide dinitrate; [d] at least one compound capable of releasing and/or donating and/or carrying nitric oxide; and optionally [e] testosterone.
2. A preparation according to claim 1 containing the testosterone component comprising dihydrotestosterone (DHT).
3. A preparation according to claim 1 or 2 wherein component [d] comprises L-arginine.
4. A preparation according to claim 1 or 2 wherein component [d] is selected from L-arginine, sodium nitrite, amyl nitrite, glyceryl trinitrate, sodium nitroprusside, 3morpholinosydonimine (SIN-1), S-nitroso-N-acetyl-D, Lpenicillamine (SNAP), S-nitrosoglutathione (SNOG) and the nitroxyl releaser N-acetyl-N-acetoxy-4chlorobenzenesulphonamide (NANAC).
5. A preparation according to any preceding claim containing 0.5-5 of [a], 0.01-0.2% of [b], 0.1-1W of [c], 0.01-5% of [d], and 0 to 0.5t of [e], all percentages being calculated as weight g/100 mS of the preparation.
6. A preparation according to any preceding claim containing 3% of [a], 0.05% of [b], 0.25% of [c] and 1% of [d], all percentages being calculated as weight g/100mP of the preparation.
7. A preparation according to any preceding claim in the form of a cream, gel or spray.
8. A preparation according to any preceding claim carried within a condom or prophylactic sheath.
GB9613860A 1996-07-02 1996-07-02 Topical preparation for relief of erectile dysfunction Expired - Fee Related GB2314771B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
GB9613860A GB2314771B (en) 1996-07-02 1996-07-02 Topical preparation for relief of erectile dysfunction

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB9613860A GB2314771B (en) 1996-07-02 1996-07-02 Topical preparation for relief of erectile dysfunction

Publications (3)

Publication Number Publication Date
GB9613860D0 GB9613860D0 (en) 1996-09-04
GB2314771A true GB2314771A (en) 1998-01-14
GB2314771B GB2314771B (en) 2000-09-06

Family

ID=10796216

Family Applications (1)

Application Number Title Priority Date Filing Date
GB9613860A Expired - Fee Related GB2314771B (en) 1996-07-02 1996-07-02 Topical preparation for relief of erectile dysfunction

Country Status (1)

Country Link
GB (1) GB2314771B (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0879599A2 (en) * 1997-05-18 1998-11-25 Adel Prof. Dr. Abdel-Wadood Gomaa A topical preparation for treatment of erectile dysfunction comprising theophylline or aminophylline, isosorbide dinitrate and co-dergocrine mesylate
JP2002505676A (en) * 1997-06-23 2002-02-19 クイーンズ ユニバーシティー アット キングストン Microdose therapy
JP2006515359A (en) * 2003-01-13 2006-05-25 ホーファー リサーチ マネージメント エスエイ Improvement of sexual function and genital vasculature by proanthocyanidins

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Dialog File 149, Full Text Acc. No. 01620717 & Brit. Med. J.Vol. 312, No. 7045, June 96, pp 1512-15 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0879599A2 (en) * 1997-05-18 1998-11-25 Adel Prof. Dr. Abdel-Wadood Gomaa A topical preparation for treatment of erectile dysfunction comprising theophylline or aminophylline, isosorbide dinitrate and co-dergocrine mesylate
EP0879599A3 (en) * 1997-05-18 2000-11-02 Adel Prof. Dr. Abdel-Wadood Gomaa A topical preparation for treatment of erectile dysfunction comprising theophylline or aminophylline, isosorbide dinitrate and co-dergocrine mesylate
JP2002505676A (en) * 1997-06-23 2002-02-19 クイーンズ ユニバーシティー アット キングストン Microdose therapy
JP2006515359A (en) * 2003-01-13 2006-05-25 ホーファー リサーチ マネージメント エスエイ Improvement of sexual function and genital vasculature by proanthocyanidins
JP2012006948A (en) * 2003-01-13 2012-01-12 Horphag Research Ip (Pre) Ltd Attaining sexual wellness and health of sexual vascular system with proanthocyanidin

Also Published As

Publication number Publication date
GB9613860D0 (en) 1996-09-04
GB2314771B (en) 2000-09-06

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PCNP Patent ceased through non-payment of renewal fee

Effective date: 20060702