Treatment of female sexual dysfunction

• US 5,945,117 A
• Filed: 01/30/1998
• Issued: 08/31/1999
• Est. Priority Date: 01/30/1998
• Status: Expired due to Fees

• Current Assignee: Pentech Pharmaceuticals Incorporated
• Original Assignee: Pentech Pharmaceuticals Incorporated
• Inventors: El-Rashidy, Ragab, Ronsen, Bruce
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HOWARD, SHARON LEE
• Application Number:
  US09/016,252
• Time in Patent Office: 578 Days
• Field of Search: 424/430, 424/435, 424/464, 514/772.6
• US Class Current: 424/430
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 15/12 for climacteric disorders

Abstract

Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms. Administration of apomorphine increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow for enhanced clitoral erection and vaginal engorgement in a female. A plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter is preferably maintained.

Claims

1. A method of ameliorating sexual dysfunction in a human female which comprises administering to said human female apomorphine or a pharmaceutically acceptable acid addition salt thereof as a sublingual dosage form and in an amount sufficient to increase intraclitoral blood flow and vaginal wall blood flow on stimulation of said human female but less than the amount that induces substantial nausea.

2. The method in accordance with claim 1 wherein the sublingual dosage form contains about 2 milligrams to about 12 milligrams of apomorphine.

3. The method in accordance with claim 1 wherein the amount of apomorphine administered is in the range of about 25 to about 80 micrograms per kilogram of body weight.

4. The method in accordance with claim 1 wherein the apomorphine is administered as the hydrochloride salt.

5. The method in accordance with claim 1 wherein the apomorphine is administered together with a β

-cyclodextrin.

6. The method in accordance with claim 1 wherein the β

-cyclodextrin is hydroxypropyl-β

-cyclodextrin.

7. A method of stimulating dopamine receptors in the mid-brain region of a human female to cause clitoral erectogenesis and vaginal engorgement which comprises administering to the human female apomorphine in a sublingual dose containing about 25 to about 80 micrograms of apomorphine per kilogram of body weight and at a rate so as to maintain a plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter during sexual activity.

8. The method in accordance with claim 7 wherein the plasma concentration of apomorphine is maintained in the range of about 0.3 to about 4 nanograms per milliliter during sexual activity.

9. The method in accordance with claim 7 wherein the plasma concentration of apomorphine is maintained in the range of about 1 to about 2 nanograms per milliliter during sexual activity.

10. A method of ameliorating sexual dysfunction in a human female which comprises administering to said human female apomorphine or a pharmaceutically acceptable acid addition salt thereof sublingually prior to sexual activity, and in an amount sufficient to stimulation induce clitoral erectogenesis and vaginal engorgement and to maintain a plasma concentration of apomorphine at a level of no more than about 5.5 nanograms per milliliter.

11. The method in accordance with claim 10 wherein the plasma concentration of apomorphine is maintained at a level of about 0.3 to about 4 nanograms per milliliter.

12. The method in accordance with claim 10 wherein the plasma concentration of apomorphine is maintained at a level of about 1 to about 2 nanograms per milliliter.

13. The method in accordance with claim 10 wherein the amount of apomorphine administered is in the range of about 2 milligrams to about 12 milligrams.

14. The method in accordance with claim 10 wherein the amount of apomorphine administered is in the range of about 25 to about 80 micrograms per kilogram of body weight.

15. The method in accordance with claim 10 wherein apomorphine is administered as the hydrochloride salt.