Topical testosterone formulations and associated methods

• US 6,743,448 B2
• Filed: 12/11/2001
• Issued: 06/01/2004
• Est. Priority Date: 12/11/2000
• Status: Active Grant

• Current Assignee: Abraham H. Kryger
• Original Assignee: Abraham H. Kryger
• Inventors: Kryger, Abraham H.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): DI NOLA BARON, LILIANA
• Application Number:
  US10/021,564
• Publication Number:
  US 20020150625A1
• Time in Patent Office: 903 Days
• Field of Search: 424/484, 424/486, 424/489, 424/501, 514/772.1
• US Class Current: 424/489
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/568 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/183 Amino acids, e.g. glycine, EDTA or aspartame
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system

Abstract

A topical testosterone formulation is disclosed. In one aspect, the formulation may include a therapeutically effective amount of micronized testosterone, an arginine ingredient, and a tocopherol ingredient admixed with a poloxamer lecithin organogel. Additional ingredients may be included, such as melatonin, oxytocin, DHEA, and progesterone.

Claims

1. A method of minimizing aromatic conversion of testosterone to an estrogen during testosterone supplementation therapy a patient in need thereof comprising the steps of:

coadministering to the skin of a subject from a topical formulation, a therapeutically effective amount of testosterone, and an amount of tocopherol that is sufficient to minimize aromatization of the testosterone to an estrogen.

2. The method of claim 1, wherein the topical formulation includes a modified poloxamer lecithin organogel as a carrier.

3. The method of claim 1, further comprising coadministering a therapeutically effective amount of an arginine ingredient from the topical formulation.

4. The method of claim 1, wherein the testosterone is micronized.

5. The method of claim 1, wherein the amount of testosterone is from about 0.5% w/w to about 25% w/w of the topical formulation.

6. The method of claim 5, wherein the amount of testosterone is from about 5% w/w to about 10% w/w of the topical formulation.

7. The method of claim 3, wherein the arginine ingredient is in a salt form.

8. The method of claim 3, wherein the arginine ingredient is L-arginine monochloride.

9. The method of claim 3, wherein the amount of arginine ingredient is from about 5% w/w to about 10% w/w of the topical formulation.

10. The method of claim 1, wherein the tocopherol comprises alpha tocopherol.

11. The method of claim 1, wherein the tocopherol comprises gamma tocopherol.

12. The method of claim 1, wherein the amount of tocopherol is from about 5% w/w to about 10% w/w of the topical formulation.

13. The method of claim 3, further comprising coadministering an effective amount of dehydroepiandrosterone (DHEA) from the topical formulation.

14. The method of claim 1, wherein the DHEA comprises dehydroepiandrosterone sulfate (DHEAS).

15. The method of claim 14, wherein the amount of DHEA is about from about 1% w/w to about 20% w/w of the topical formulation.

16. The method of claims 3, further comprising coadministering an effective amount of melatonin from the topical formulation.

17. The method of claim 16, wherein the amount of melatonin is from about 1% w/w to about 20% w/w of the topical formulation.

18. The method of claim 3, further comprising coadministering an effective amount of progesterone from the topical formulation.

19. The method of claim 18, wherein in the amount of progesterone is from about 1% w/w to about 20% w/w of the topical formulation.

20. The method of claim 3, further comprising coadministering an effective amount of oxytocin from the topical formulation.

21. The method of claim 20, wherein the amount of oxytocin is from about 1% w/w to about 20% w/w of the topical formulation.

22. The method of claim 3, wherein the amount of testosterone is from about 5% w/w to about 10% w/w, the amount of tocopherol is from about 5% w/w to about 10% w/w, and the amount of arginine is from about 5-10% of the topical formulation.