Apomorphine-containing dosage forms for ameliorating male erectile dysfunction

• US 6,121,276 A
• Filed: 06/22/1998
• Issued: 09/19/2000
• Est. Priority Date: 04/22/1994
• Status: Expired due to Fees

• Current Assignee: Pentech Pharmaceuticals Incorporated
• Original Assignee: Pentech Pharmaceuticals Incorporated
• Inventors: El-Rashidy, Ragab, Ronsen, Bruce
• Primary Examiner(s): Jones, Dwayne C.
• Assistant Examiner(s): DELACROIX MUIRHEI, CYBILLE
• Application Number:
  US09/102,406
• Time in Patent Office: 820 Days
• Field of Search: 514/284, 424/449, 424/464, 424/468, 424/474
• US Class Current: 514/284
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/473 ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 49/0004 Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61P 15/10 for impotence

Abstract

Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.

Claims

1. A method suitable for treating erectile dysfunction in a male patient which comprises orally administering to the patient prior to sexual activity:

an oral dosage of an antiemetic agent in an amount sufficient to substantially reduce nausea associated with use of apomorphine; and

an oral dosage of apomorphine or a pharmaceutically acceptable acid addition salt thereof in an amount sufficient to induce and maintain an erection adequate for vaginal penetration.

2. The method in accordance with claim 1 wherein the antiemetic agent is a phenothiazine.

3. The method in accordance with claim 2 wherein the antiemetic agent is prochlorperazine.

4. The method in accordance with claim 1 wherein the antiemetic agent is a benzamide.

5. The method in accordance with claim 1 wherein the antiemetic agent is a meclizine.

6. The method in accordance with claim 1 wherein the antiemetic agent is a serotonin antagonist.

7. The method in accordance with claim 1 wherein the antiemetic agent is a member of the group consisting of hydroxyzine, dimenhydrinate, scopolamine, metopimazine, and diphenidol hydrochloride.

8. The method in accordance with claim 1 wherein the antiemetic agent is a ganglionic stimulating alkaloid and the apomorphine is administered to the patient as the hydrochloride salt.

9. The method in accordance with claim 8 wherein the antiemetic agent is nicotine sulfate and the weight ratio of apomorphine hydrochloride to nicotine sulfate administered to the patient is in the range of about 10 to about 1.

10. The method in accordance with claim 8 wherein the apomorphine and the antiemetic agent are co-administered to the patient in a single dosage unit comprising about 1 to about 10 milligrams apomorphine and about 0.5 to about 2 milligrams nicotine sulfate.

11. The method in accordance with claim 1 wherein the antiemetic agent is prochlorperazine hydrochloride.

12. The method in accordance with claim 11 wherein the weight ratio of apomorphine hydrochloride to prochlorperazine hydrochloride administered to the patient is in the range of about 5 to about 0.25.

13. The method in accordance with claim 11 wherein the amount of prochlorperazine hydrochloride administered to the patient is in the range of about 5 to about 150 micrograms per kilogram of patient'"'"'s body weight.

14. The method in accordance with claim 1 wherein the apomorphine and the antiemetic agent are administered to the patient substantially concurrently.

15. The method in accordance with claim 1 wherein the apomorphine and the antiemetic agent are administered to the patient sequentially by first administering a composition comprising an antiemetic agent and thereafter a composition comprising apomorphine.

16. The method in accordance with claim 1 wherein the apomorphine and the antiemetic agent are co-administered to the patient as a sublingual tablet.

17. The method in accordance with claim 1 wherein the apomorphine is administered as a sublingual tablet and the antiemetic agent is administered as a buccal patch.

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

19. An oral dosage unit comprising an antiemetic agent as a relatively faster release component and apomorphine as a component released after release of the antiemetic agent has begun.

20. The dosage unit of claim 19 in the form of a layered tablet.

21. The dosage unit of claim 19 wherein the antiemetic agent is a member of the group consisting of the phenothiazines, the benzamides, the meclizines, the serotonin antagonists, hydroxyzine, lobeline sulfate, dimenhydrinate, scopolamine, metopimazine, diphenidol hydrochloride, nicotine, and the acid addition salts thereof.

22. The dosage unit of claim 19 wherein the antiemetic agent is a prochlorperazine.

23. The dosage unit of claim 19 wherein the antiemetic agent is metoclopramide hydrochloride.

24. The dosage unit of claim 19 in the form of a tablet having a core portion containing the apomorphine and an outer layer portion containing the antiemetic agent.

25. The dosage unit of claim 19 having a time to 90 percent release of apomorphine in the range of about 25 minutes to about 300 minutes.