Compositions and methods for amelioration of human female sexual dysfunction

• US 6,486,207 B2
• Filed: 12/10/1998
• Issued: 11/26/2002
• Est. Priority Date: 12/10/1998
• Status: Expired due to Term

• Current Assignee: Nexmed Holdings
• Original Assignee: Nexmed Holdings
• Inventors: Buyuktimkin, Servet, Buyuktimkin, Nadir, Yeager, James L.
• Primary Examiner(s): Dees, Jose′ G.
• Assistant Examiner(s): CHOI, FRANK I
• Application Number:
  US09/208,965
• Publication Number:
  US 20020028846A1
• Time in Patent Office: 1,447 Days
• Field of Search: 514/573, 514/529, 514/530, 514/675, 514/724, 514/729, 514/396, 514/579, 514/646, 514/656, 514/658, 514/731, 514/736, 514/772, 514/772.1, 514/772.3, 514/777, 514/780, 514/785, 514/929, 514/975, 514/772.6, 514/782, 514/946, 514/947, 514/967
• US Class Current: 514/573
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications

Abstract

The invention provides a composition suitable for topical application comprising: an effective amount of a prostaglandin, a polymer thickener, a lipophilic component, and a buffer system. In another embodiment, the invention provides a composition suitable for topical application comprising: an effective amount of a vasoactive agent, a polymer thickener, a lipophilic component, and a buffer system. The invention also provides methods of ameliorating female sexual dysfunction. Also provided are methods of increasing female sexual arousal and methods of enhancing female sexual response.

Claims

1. A method for ameliorating female sexual arousal disorder, comprising the step of administering a composition to the genitalia of a human female in need of treatment, the composition comprising:

an amount of a vasoactive agent chosen from the group consisting of prostaglandin E₁, pharmaceutically acceptable prostaglandin E₁ salts, prostaglandin E₁ alkyl esters, and mixutres thereof effective to produce an increase in sexual arousal, a polymer thickener, a lipophilic component, a penetration enhancer chosen from the group consisting of alkyl-2-(N,N-disubstituted amino) alkanoates, (N,N-disubstituted amino) alkanol alkanoates and mixtures thereof and a buffer system wherein the pH of the composition is about 3.0 to about 6.0, wherein treatment increases subjective sexual arousal thereby alleviating symptoms of female sexual arousal disorder, wherein female sexual disorder is the persistant or recurrent inability to attain, or to maintain, sufficient sexual excitment, which causes personal distress.

2. The method of claim 1 wherein the composition is administered less than one hour before intercourse.

3. The method of claim 1 wherein the composition is administered to the labia of the human female.

4. The method of claim 1 wherein the composition is administered to the clitoris of the human female.

5. The method of claim 1 wherein the composition is administered to the vagina of the human female.

6. The method of claim 1 further comprising the step of determining a diagnosis of female sexual arousal disorder.

7. The method of claim 1 wherein the method further comprises the step of measuring the increase in sexual arousal by self-report by a suitable quantitative questionnaire.

8. The method of claim 1 wherein the polymer thickener is a polyacrylic acid polymer.

10. The method of claim 1 wherein the polymer thickener is about 0.5 to about 5 weight percent polysaccharide gum.

11. The method of claim 10 wherein the polysaccharide gum is chosen from the group consisting of galactomannan gums and galactomannan gum derivatives.

12. The method of claim 1 wherein the vasoactive agent is prostaglandin E₁ present in the composition from about 0.05 to about 0.4 percent by weight of the total composition.

13. The method of claim 1 wherein the lipophilic component is a mixture of ethanol and ethyl laurate present in the composition from about 0.5 to about 15 percent weight of the total composition.

14. The method of claim 1 wherein the vasoactive agent is prostaglandin E₁ present in the composition from about 0.05 to about 0.4 percent weight of the total composition, the polymer thickener is polyacrylic acid polymer present in the composition from about 0.5 to about 5 percent weight of the total composition, and the lipophilic component is a mixutre of ethanol and ethyl laurate present in the composition from about 0.5 to about 15 percent weight of the total composition.

15. The method of claim 1 wherein the vasoactive agent is prostaglandin E₁ present in the composition from about 0.05 to about 0.4 percent weight of the total composition, the polymer thickener is a polysaccharide gum chosen from the group consisting of galactomannan gum and gallactomannan gum derivatives present in the composition from about 0.5 to about 5 percent weight of the total composition, and the lipophilic component is a mixture of ethanol and ethyl laurate present in the composition from about 0.5 to about 15 percent weight of the total composition.

16. The method of claim 1 wherein the penetration enhancer comprises dodecyl N,N-dimethylamino isopropionate (DDAIP).

9. The method of calim 8 wherein the polymer thickener is about 0.5 to about 5 weight percent polyacrylic acid polymer.

17. A method for treating female sexual arousal disorder, comprising the step of administering to the genitalia of a human female in need of treatment a composition suitable for topical application comprising an amount effective to produce an increase in subjective sexual arousal of the vasoactive agent prostaglandin E₁ present in the composition from about 0.07 to about 0.4 percent weight of the total composition;

the polymer thickener polyacrylic acid polymer present in the composition from about 0.5 to about 5 percent weight of the total composition;

a lipophilic component that is a mixture of ethanol and ethyl laurate present in the composition from about 0.5 to about 15 percent of the total composition;

a penetration enhancer chosen from the group consisting of alkyl-2-(N,N-disubstituted amino) alkanoates, (N,N-disubstituted amino) alkanol alkanoates and mixtures thereof and a buffer system wherein the pH of the composition is about 3.0 to 6.0, wherein the treatment increases subjective sexual arousal thereby alleviating symptoms of female arousal disorder, wherein female sexual arousal disorder is the persistant or recurrent inability to attain, or to maintain, sufficient sexual excitement, which causes personal distress.

18. The method of claim 17 wherein the composition is administered less than one hour before intercourse.