Transdermal compositions and methods for treatment of fibromyalgia and chronic fatigue syndrome

• US 7,799,769 B2
• Filed: 12/16/2005
• Issued: 09/21/2010
• Est. Priority Date: 06/18/2003
• Status: Active Grant

• Current Assignee: Thomas D. Robinson
• Original Assignee: White Mountain Pharma, Inc.
• Inventors: Gyurik, Robert, White, Hillary D.
• Primary Examiner(s): HUI, SAN MING R
• Application Number:
  US11/303,813
• Publication Number:
  US 20060100186A1
• Time in Patent Office: 1,740 Days
• Field of Search: 514/170, 514/180
• US Class Current: 514/170
• 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 31/568 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 38/27 Growth hormone [GH], i.e. somatotropin
• 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: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/12 for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
• CPC Class Codes: A61P 5/26 Androgens

Abstract

Compositions and methods for alleviating the symptoms associated with chronic fatigue syndrome and fibromyalgia syndrome are provided. The compositions are based on use of a transdermal gel formulation delivery system for androgens, either alone or in combination with other hormones.

Claims

1. A pharmaceutical composition formulated for administering a therapeutic female-appropriate amount of an androgen compound to a female human patient who has a condition which is associated with deficient serum androgen levels, said pharmaceutical composition comprising a safe female-appropriate unit dose of said androgen, in a pharmaceutically acceptable carrier formulated for daily topical administration to said female human patient as a gel, the safe female-appropriate unit dose of said androgen being in an amount which is both effective for alleviating the female patient'"'"'s condition associated with androgen deficiency and for consistently raising the female patients'"'"' serum androgen levels only within limits approximating the reference range for normal premenopausal women, wherein the composition contains a daily unit dose of about 7.5 mg of testosterone and is formulated to provide steady state total testosterone serum levels within a range of between about 0.9 ng/mL to about 1.4 ng/mL for at least 24 hours after each daily administration without raising free testosterone serum levels or twenty-four hour free testosterone AUC above the levels required for therapeutic efficacy and safety.

2. The composition according to claim 1 wherein the concentration of androgen is present in an amount of about 1% on a weight basis.

3. The composition according to claim 1 wherein the androgen is selected from the group consisting of testosterone, danazol, fluoxymesterone, oxandrolone, nandrolone decanoate, nandrolone phenpropionate, oxymethalone, stanozolol, methandrostenolone, testolactone, pregnenolone dehydroepiandrosterone, and testosterone derivatives.

4. The composition according to claim 1 wherein the androgen is selected from the group consisting of testosterone, dihydrotestosterone, androstenedione, methyltestosterone, and testosterone esters.

5. The composition according to claim 4 wherein the testosterone ester is selected from the group consisting of testosterone enanthate and testosterone cypionate.

6. A composition according to claim 3 in which the condition which is associated with deficient serum androgen levels is selected from the group consisting of fibromyalgia, chronic fatigue syndrome, and decreased sexual desire and the safe female effective unit dose is an amount which will raise the female human patient'"'"'s steady state serum androgen level without causing androgenic side effects.

7. The composition of claim 1, wherein the composition formulated to provide steady state total testosterone serum levels within a range of between about 0.9 ng/mL to about 1.4 ng/mL for at least 24 hours after each daily administration without raising free testosterone serum levels above about 4.69 pg/mL or twenty-four hour free testosterone AUC above about 71.38 pg-h/mL.

8. A method of alleviating the symptoms of a condition which is associated with deficient serum androgen levels in a female human patient comprising administering daily to said patient suffering from deficient serum androgen levels a safe and effective amount of the composition of claim 1 which is both effective for alleviating the female patient'"'"'s condition associated with androgen deficiency and for consistently raising the female patients'"'"' serum androgen levels only within limits approximating the reference range for normal premenopausal women, wherein the composition contains a daily unit dose of about 7.5 mg of testosterone and is formulated to provide steady state total testosterone serum levels within a range of between about 0.9 ng/mL to about 1.4 ng/mL for at least 24 hours after each daily administration without raising free testosterone serum levels or twenty-four hour free testosterone AUC above the levels required for therapeutic efficacy and safety.

9. The method of claim 8 wherein the concentration of androgen is present in an amount of about 1% on a weight basis.

10. The method of claim 8 wherein the androgen is selected from the group consisting of testosterone, danazol, fluoxymesterone, oxandrolone, nandrolone decanoate, nandrolone phenpropionate, oxymethalone, stanozolol, methandrostenolone, testolactone, pregnenolone dehydroepiandrosterone, and testosterone derivatives.

11. The method of claim 8 wherein the androgen is selected from the group consisting of testosterone, dihydrotestosterone, androstenedione, methyltestosterone, and testosterone esters.

12. The method of claim 11 wherein the testosterone ester is selected from the group consisting of testosterone enanthate and testosterone cypionate.

13. The method of claim 10 wherein the condition which is associated with deficient serum androgen levels is selected from the group consisting of fibromyalgia, chronic fatigue syndrome, and decreased sexual desire and the safe female effective unit dose is an amount which will raise the female human patient'"'"'s steady state serum androgen level without causing androgenic side effects.

14. The method of claim 8 wherein the composition is formulated to provide steady state total testosterone serum levels within a range of between about 0.9 ng/mL to about 1.4 ng/mL for at least 24 hours after each daily administration without raising free testosterone serum levels above about 4.69 pg/mL or twenty-four hour free testosterone AUC above about 71.38 pg-h/mL.