PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING HYPOGONADISM

• US 20110201586A1
• Filed: 03/24/2011
• Published: 08/18/2011
• Est. Priority Date: 08/30/2000
• Status: Abandoned Application

• Current Assignee: Dominique Drouin, Robert E. Dudley
• Original Assignee: Dominique Drouin, Robert E. Dudley
• Inventors: Drouin, Dominique, Dudley, Robert E.
• Application Number:
  US13/071,264
• Publication Number:
  US 20110201586A1
• Time in Patent Office: Days
• US Class Current: 514/178
• 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 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/475 having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine vincamine A61K31/4375
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 31/557 Eicosanoids, e.g. leukotrienes or prostaglandins
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• 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 31/5685 having an oxo group in position 17, e.g. androsterone
• 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 47/12 Carboxylic acids; Salts or anhydrides thereof
• 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 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• 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 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/26 Androgens

Abstract

A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition.

Claims

1. A hydroalcoholic gel pharmaceutical composition, comprising:

a. from about 0.5% to about 10% testosterone;

b. from about 30% to about 98% alcohol selected from the group consisting of ethanol and isopropanol;

c. from about 0.1% to about 5% of a thickening agent;

d. from about 0.25% to about 2.5% of at least one penetration enhancer selected from the group consisting of isostearic acid, octanoic acid, lauryl alcohol, isopropyl myristate, butyl stearate, methyl laurate, diisopropyl adipate, glyceryl monolaurate, tetrahydrofurfuryl alcohol polyethylene glycol ether, polyethylene glycol, propylene glycol, 2-(2-ethoxyethoxy)ethanol, diethylene glycol monomethyl ether, dimethyl sulfoxide, glycerol, ethyl acetate, acetoacetic ester, N-alkylpyrrolidone, derivatives thereof, and combinations thereof; and

e. water in an amount sufficient to make the composition 100%,

wherein the percentages of components are weight to weight of the composition.

2. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the testosterone is present in a concentration of from about 0.5% to about 5% (w/w) of the composition.

3. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the alcohol is ethanol.

4. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the thickening agent is an anionic polymer.

5. The hydroalcoholic gel pharmaceutical composition of claim 4, wherein the anionic polymer is selected from the group consisting of polyacrylic acid, carboxymethyl cellulose, and combinations thereof.

6. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the composition further comprises 0.1N sodium hydroxide.

7. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises isostearic acid.

8. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises octanoic acid.

9. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises lauryl alcohol.

10. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises isopropyl myristate.

11. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises butyl stearate.

12. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises methyl laurate.

13. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises diisopropyl adipate.

14. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises glyceryl monolaurate.

15. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises tetrahydrofurfuryl alcohol polyethylene glycol ether.

16. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises polyethylene glycol.

17. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises propylene glycol.

18. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises 2-(2-ethoxyethoxy)ethanol.

19. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises diethylene glycol monomethyl ether.

20. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises dimethyl sulfoxide.

21. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises glycerol.

22. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises ethyl acetate.

23. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises acetoacetic ester.

24. The hydroalcoholic gel pharmaceutical composition of claim 1, wherein the penetration enhancer comprises N-alkylpyrrolidone.