Pharmaceutical composition and method for treating hypogonadism

• US 9,125,816 B2
• Filed: 08/13/2013
• Issued: 09/08/2015
• Est. Priority Date: 08/30/2000
• Status: Expired due to Fees

• Current Assignee: Unimed Pharmaceuticals LLC (Abbott Laboratories), Besins Healthcare, Inc.
• Original Assignee: Unimed Pharmaceuticals LLC (Abbott Laboratories), Besins Healthcare, Inc.
• Inventors: Dudley, Robert E., Drouin, Dominique
• Primary Examiner(s): MCMILLIAN, KARA RENITA
• Application Number:
  US13/965,499
• Publication Number:
  US 20140011788A1
• Time in Patent Office: 756 Days
• US Class Current: 1/1
• 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 method of administering testosterone to human males for treating hypogonadism, the method comprising the step of:

administering once per day a therapeutically effective dose of a pharmaceutical composition to human males, the pharmaceutical composition consisting of;

(i) 0.1% to 10% (w/w) testosterone;

(ii) 0.10% to 5.0% (w/w) isopropyl myristate;

(iii) 30.0% to 98.0% (w/w) of ethanol, isopropanol or combinations thereof;

(iv) 0.1% to 5.0% of a polyacrylic acid, wherein the polyacrylic acid is neutralized with sodium hydroxide; and

(v) water

wherein the administration is sufficient for the testosterone to reach the bloodstream of the human males to achieve a steady state pharmacokinetic profile similar to the pharmacokinetic profile for a testosterone gel shown in FIG. 5c,

further wherein the administration of the pharmaceutical composition results in continuous transdermal delivery of testosterone for at least 24 hours, and

still further wherein the administration of the pharmaceutical composition is as a gel and not as part of a patch.

2. The method of claim 1, wherein the sodium hydroxide is 0.1 N NaOH.

3. The method of claim 1, wherein the composition consists of testosterone, isopropyl myristate, ethanol, polyacrylic acid neutralized with sodium hydroxide and water.

4. The method of claim 3, wherein the ethanol is 95% (v/v) ethanol.