CA2498267A1 - Method for treating erectile dysfunction and increasing libido in men - Google Patents

Method for treating erectile dysfunction and increasing libido in men

Info

Publication number
CA2498267A1
CA2498267A1 CA002498267A CA2498267A CA2498267A1 CA 2498267 A1 CA2498267 A1 CA 2498267A1 CA 002498267 A CA002498267 A CA 002498267A CA 2498267 A CA2498267 A CA 2498267A CA 2498267 A1 CA2498267 A1 CA 2498267A1
Authority
CA
Canada
Prior art keywords
testosterone
steroid
men
enhancer
isopropyl myristate
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
CA002498267A
Other languages
French (fr)
Other versions
CA2498267C (en
Inventor
Robert E. Dudley
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.)
Unimed Pharmaceuticals LLC
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to CA2498267A priority Critical patent/CA2498267C/en
Priority claimed from CA002420895A external-priority patent/CA2420895C/en
Publication of CA2498267A1 publication Critical patent/CA2498267A1/en
Application granted granted Critical
Publication of CA2498267C publication Critical patent/CA2498267C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants

Landscapes

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

Abstract

The present invention relates to a transdermal hydroalcoholic testosterone gel formulation that overcomes the problems associated with other testosterone delivery mechanisms by providing, among other things, a desirable pharmacokinetic hormone profile with little or no skin irritation. The gel may be used as a method of improving sexual performance, including treating erectile dysfunction, and increasing libido by increasing testosterone levels in men. In addition, the gel may be used in conjunction with pharmaceuticals aimed at treating erectile dysfunction, such as VIAGRA®, to enhance their effectiveness.

Claims (54)

I claim:
1. A method of improving the sexual performance in a male subject, comprising:
percutaneously delivering a pharmaceutically effective amount of a steroid in the testosterone synthetic pathway to the subject via a pharmaceutical composition comprising the steroid, at least one of a C1-C4 alcohol, and a penetration enhancer.
2, The method in claim 1 wherein the penetration enhancer comprises at least one of a C8-C22 fatty acid.
3. The method in claim 1 wherein the fatty acid comprises an alkyl chain length of at least 12 carbon atoms.
4. The method in claim 1 wherein the lower alcohol comprises at least one of ethanol, 2-propanol, n-propanol, and mixtures thereof.
5. The method in claim 1 wherein the the steroid is testosterone and the enhancer is isopropyl myristate.
6. The method of claim 5 wherein the composition comprises about 1.0 g w/w of testosterone.
7. The method of claim 5 wherein the enhancer comprises about 0.5 g w/w of isopropyl myristate.
8. The method of claim 5 wherein the thickener is CARBOPOL.
9. The method of claim 1 where the steroid comprises about 0.5 g to about 5.0 g testosterone, the thickener comprises about 0.10 g to about 2 g of CARBOPOL, the enhancer comprises about 0.1 g to about 2 g of isopropyl myristate, the C1 -C4 alcohol comprises about 40.0 g to about 90 g of ethanol.
10. The method in claim 1 wherein the men are hypogonadal.
57 17. The method in claim 10 wherein the men suffer from primary hypogonadism.,
12. The method in claim 1 wherein the delivering occurs daily.
13. The method in claim 12 wherein the delivery comprises administering the composition to the right/left upper arms/shoulders and to the right/left sides of the abdomen once per day on alternate days.
14. The method in claim 1 wherein the pharmaceutically effective amount of steroid comprises 75 mg of testosterone per day.
15. The method in claim 14 wherein the men achieve hormonal steady state levels of testosterone.
16. The method in claim 1 wherein the improving sexual performance comprises treating impotence in the men.
17. A method of increasing the libido of men comprising:
delivering a pharmaceutically effective amount of a steroid in the testosterone synthetic pathway to the men percutaneously in a composition comprised of a C1-alcohol, a penetration enhancer, a thickener, testosterone, and water.
18. The method in claim 17 wherein the penetration enhancer comprises at least one of a C8-C22 fatty acid.
19. The method in claim 17 wherein the fatty acid comprises an alkyl chain length of at least 12 carbon atoms.
20. The method in claim 17 wherein the lower alcohol comprises at least one of ethanol, 2-propanol, n-propanol, and mixture thereof.
21. The method in claim 17 wherein the steroid is testosterone and the enhancer is isopropyl myristate.
22. The method of claim 21 wherein the composition comprises about 1.0 g w/w of testosterone.
23. The method of claim 21 wherein the enhancer comprises about 0.5 g w/w of isopropyl myristate.
24. The method of claim 21 wherein the thickener is CARBOPOL.
25. The method of claim 17 where the steroid comprises about 0.5 g to about 5.0 g testosterone, the thickener comprises about 0.10 g to about 2 g of CARBOPOL, the enhancer comprises about 0.1 g to about 2 g of isopropyl myristate, the C1-C4 alcohol comprises about 40.0 g to about 90 g of ethanol.
26. The method in claim 17 wherein the men are hypogonadal.
27. The method in claim 17 wherein the men suffer from primary hypogonadism.
28. The method in claim 17 wherein the delivering occurs daily.
29. The method in claim 28 wherein the delivery comprises administering the composition to the right/left upper arms/shoulders and to the right/left sides of the abdomen once per day on alternate days.
30. The method in claim 17 wherein the pharmaceutically effective amount of a steroid in the testosterone synthetic pathway comprises 75 mg of testosterone per day.
31. The method in claim 17 wherein the men achieve hormonal steady state levels of testosterone.
32. A method for improving the efficacy of a pharmaceutical useful for treating erectile dysfunction in a male subject, comprising:
percutaneously delivering a pharmaceutically effective amount of a steroid in the testosterone synthetic pathway to the subject in a composition comprising at least one of a C1-C4 alcohol, the steroid, and a penetration enhancer; and administering the pharmaceutical to the subject.
33. The method in claim 32 wherein the subject is eugonadal.
34. The method of claim 32 wherein the pharmaceutical is a phosphodiesterase type 5 inhibitor.
35. The method in claim 32 wherein the pharmaceutical is at least one of sildenafil citrate, pentoxifylline, yohimbine, apomorphine, alprostadil, papavaerine, phentolamine, and combinations, salts, derivatives and enantiomers of thereof
34. The method in claim 32 wherein the pharmaceuticals are selected from the group consisting of VIAGRA, UPRIMA, TRENTAL or ACTIBINE.
35. ~The method in claim 32 wherein the penetration enhancer comprises at least one of a C8-C22 fatty acid.
36. The method in claim 32 wherein the fatty acid comprises an alkyl chain length of at least 12 carbon atoms.
37. The method in claim 32 wherein the lower alcohol comprises at least one of ethanol, 2-propanol, n-propanol, and mixtures thereof.
38. The method in claim 32 wherein the the steroid is testosterone and the enhancer is isopropyl myristate.
39. The method of claim 38 wherein the composition comprises about 1.0 g w/w of testosterone.
40. ~The method of claim 38 wherein the enhancer comprises about 0.5 g w/w of isopropyl myristate.
41. The method of claim 38 wherein the thickener is CARBOPOL.
42. The method of claim 32 where the steroid comprises about 0.5 g to about 5.0 g testosterone, the thickener comprises about 0.10 g to about 2 g of CARBOPOL, the enhancer comprises about 0.1 g to about 2 g of isopropyl myristate, the C1-C4 alcohol comprises about 40.0 g to about 90 g of ethanol.
43. The method in claim 32 wherein the men are hypogonadal.
44. The method in claim 32 wherein the men suffer from primary hypogonadism.
45. The method in claim 32 wherein the delivering occurs daily.
46. The method in claim 32 wherein the delivery comprises administering the composition to the right/left upper arms/shoulders and to the right/left sides of the abdomen once per day on alternate days.
47. The method in claim 32 wherein the pharmaceutically effective amount steroid comprises 75 mg of testosterone per day.
48. The method in claim 32 wherein the men achieve hormonal steady state levels of testosterone.
49. A kit comprised of a pharmaceutical useful for treating erectile dysfunction in a man and a transdermal testosterone gel.
50. The kit of claim 49 wherein the pharmaceutical is a phosphodiesterase type inhibitor
51. The kit in claim 49 wherein the pharmaceutical is at least one of sildenafil citrate, pentoxifylline, yohimbine, apomorphine, alprostadil, papavaerine, phentolamine, and combinations, salts, derivatives and enantiomers of thereof
52. The kit in claim 49 wherein the pharmaceuticals are selected from the group consisting of VIAGRA, UPRIMA, TRENTAL or ACTIBINE.
53. The kit of claim 49 wherein the testosterone gel comprises about 0.5 g to about 5.0 g testosterone, a thickener, an enhancer, and a C1-C4 alcohol.
54. The kit of claim 53 wherein the thickener comprises about 0.10 g to about 2 g of CARBOPOL, the enhancer comprises about 0.1 g to about 2 g of isopropyl myristate, the C1-C4 alcohol comprises about 40.0 g to about 90 g of ethanol.
CA2498267A 2001-08-29 2001-08-29 Method for treating erectile dysfunction and increasing libido in men Expired - Lifetime CA2498267C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2498267A CA2498267C (en) 2001-08-29 2001-08-29 Method for treating erectile dysfunction and increasing libido in men

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CA2498267A CA2498267C (en) 2001-08-29 2001-08-29 Method for treating erectile dysfunction and increasing libido in men
CA002420895A CA2420895C (en) 2000-08-30 2001-08-29 Method for treating erectile dysfunction and increasing libido in men

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CA002420895A Division CA2420895C (en) 2000-08-30 2001-08-29 Method for treating erectile dysfunction and increasing libido in men

Publications (2)

Publication Number Publication Date
CA2498267A1 true CA2498267A1 (en) 2002-03-07
CA2498267C CA2498267C (en) 2010-10-26

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ID=34427647

Family Applications (1)

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CA2498267A Expired - Lifetime CA2498267C (en) 2001-08-29 2001-08-29 Method for treating erectile dysfunction and increasing libido in men

Country Status (1)

Country Link
CA (1) CA2498267C (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006061689A1 (en) * 2004-12-10 2006-06-15 Alan Drizen Topical drug delivery system

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006061689A1 (en) * 2004-12-10 2006-06-15 Alan Drizen Topical drug delivery system

Also Published As

Publication number Publication date
CA2498267C (en) 2010-10-26

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Effective date: 20210830