Testosterone gel and method of use

• US 8,466,138 B2
• Filed: 10/05/2011
• Issued: 06/18/2013
• Est. Priority Date: 10/12/2005
• Status: Active Grant

• Current Assignee: Besins Healthcare Luxemborg SARL (Besins Healthcare, Inc.)
• Original Assignee: Unimed Pharmaceuticals LLC (Abbott Laboratories Incorporated), Laboratories Besins International SAS
• Inventors: Malladi, Ramana, Miller, Jodi
• Primary Examiner(s): Padmanabhan, Sreeni
• Assistant Examiner(s): McMillian, Kara R
• Application Number:
  US13/253,848
• Publication Number:
  US 20120028946A1
• Time in Patent Office: 622 Days
• Field of Search: 514/177, 514/178, 552/638, 568/369
• US Class Current: 514/177
• 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 47/32 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 5/26 Androgens

Abstract

The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Claims

1. A method of treating hypogonadism in a human male in need thereof comprising the step of:

applying a therapeutically effective dose of a hydroalcoholic gel to an area of skin of a human male, the hydroalcoholic gel consisting of;

i) 1.62% (w/w) testosterone;

ii) 1.0% (w/w) isopropyl myristate;

iii) 73.5% (w/w) ethanol;

iv) 1.0% (w/w) of a polyacrylic acid;

v) 7.0% (w/w) of 0.1 N sodium hydroxide; and

vi) water.

2. The method of claim 1, wherein the ethanol is 95% (v/v) ethanol.

3. The method of claim 1, wherein the polyacrylic acid is has been neutralized by combining the polyacrylic acid with the 7.0% (w/w) 0.1 N sodium hydroxide.

4. The method of claim 1, wherein after the applying of the hydroalcoholic gel, the hydroalcoholic gel provides sufficient testosterone to achieve a circulating blood serum testosterone concentration in the human male of between about 298 and about 1043 ng testosterone per dl serum.

5. The method of claim 1, wherein after the applying application of the hydroalcoholic gel, the serum testosterone concentration in the human male is maintained between about 300 and about 1050 ng testosterone per dl serum.

6. The method of claim 1, wherein the polyacrylic acid is a carbomer.

7. The method of claim 3, wherein the polyacylic acid is a carbomer.

8. The method of claim 1, wherein the therapeutically effective dose of the hydroalcoholic gel is 2.5 grams.

9. The method of claim 8, wherein the dose of the testosterone administered to the human male by the applying is 40.5 milligrams.