Apomorphine and sildenafil composition

• US 6,087,362 A
• Filed: 03/16/1999
• Issued: 07/11/2000
• Est. Priority Date: 03/16/1999
• Status: Expired due to Fees

• Current Assignee: Pentech Pharmaceuticals Incorporated
• Original Assignee: Pentech Pharmaceuticals Incorporated
• Inventors: El-Rashidy, Ragab
• Primary Examiner(s): HENLEY III, RAYMOND J
• Application Number:
  US09/270,035
• Time in Patent Office: 483 Days
• Field of Search: 514/284, 514/253
• US Class Current: 514/252.16
• 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 31/47 Quinolines; Isoquinolines
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The treatment of sexual dysfunction in human patients by an oral therapy regimen of administration of apomorphine and sildenafil is disclosed. This treatment optimizes the efficacy of each drug and substantially minimizes the undesirable side effects associated individually therewith. Apomorphine and sildenafil can be co-administered with a combination dosage unit or administered sequentially in separate dosage units, substantially prior to sexual activity. Other erectogenic agents can be administered along with apomorphine and sildenafil.

Claims

1. A method suitable for treating erectile dysfunction in a human patient which comprises administering to said patient prior to sexual activity apomorphine or a pharmaceutically acceptable acid addition salt thereof and sildenafil or a pharmaceutically acceptable acid addition salt thereof each being administered in an amount sufficient to induce and maintain an erection adequate for sustaining satisfaction during sexual activity but less than an amount that induces substantial nausea.

2. The method in accordance with claim 1 wherein the apomorphine and sildenafil are co-administered in a single dosage unit comprising about 1 to about 6 mg apomorphine and about 10 to about 75 mg sildenafil.

3. The method in accordance with claim 2 wherein the single dosage unit comprises about 2 to about 5 mg apomorphine and about 15 to about 50 mg sildenafil.

4. The method in accordance with claim 1 wherein the sildenafil and apomorphine is sequentially administered by first administering a dosage unit comprising sildenafil in an amount in the range of about 10 to about 75 mg and then a dosage unit comprising apomorphine in an amount in the range of about 1 to about 6 mg.

5. The method in accordance with claim 4 wherein the amount of administered apomorphine is in a range of about 2 to 5 mg.

6. The method in accordance with claim 4 wherein the amount of administered sildenafil is in a range of about 15 to about 50 mg.

7. The method in accordance with claim 4 wherein the amount of administered apomorphine is in a range of about 2 to about 5 mg and the amount of administered sildenafil is in a range of about 15 to about 50 mg.

8. The method in accordance with claim 4 wherein the sildenafil is administered within about 30-60 minutes of apomorphine administration.

9. The method in accordance with claim 1 wherein the administration is by sublingual route or combinations thereof.

10. A pharmaceutical composition comprising sildenafil and apomorphine in a pharmaceutically acceptable vehicle.

11. The composition of claim 10 wherein the amount of sildenafil is in the range of about 10 to about 25 mg.

12. The composition of claim 10 wherein the amount of apomorphine is in the range of about 1 to about 6 mg.

13. The composition of claim 10 in sublingual or buccal tablet form.

17. The composition of claim 10 further including erectogenic agents selected from adrenal steroids, alpha receptor blockers, or peripheral vasodilators added at a concentration in the range of about 50 to about 100 percent by weight of the weight of apomorphine.

18. The composition of claim 17 wherein the erectogenic agent is an adrenal steroid selected from the group consisting of testosterone and dehydroepiandrosterone.

19. The composition of claim 17 wherein the erectogenic agent is an alpha receptor blocker selected from the group consisting of phentolamine, yohimbine, prazosin, doxazosin, terazosin, and trimazosin.

20. The composition of claim 17 wherein the erectogenic agent is prostaglandin E₁.

14. A pharmaceutical composition comprising sildenafil and a cyclodextrin in a pharmaceutically acceptable vehicle.

15. The composition of claim 14 wherein the cyclodextrin is hydroxypropyl-beta-cyclodextrin.

16. The composition of claim 15 wherein the amount of sildenafil is about 20 mg and the amount of hydroxypropyl-beta-cyclodextrin is about 1 to about 10% by weight of the total composition.