Apomorphine-containing dosage forms for ameliorating male erectile dysfunction

• US 6,306,437 B1
• Filed: 06/29/2000
• Issued: 10/23/2001
• 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:
  US09/606,919
• Time in Patent Office: 481 Days
• Field of Search: 514/284, 514/224.2, 514/224.5, 514/224.8, 514/646, 514/617, 424/464, 424/468
• US Class Current: 424/464
• 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 layered tablet composition for sublingual administration to treat erectile dysfunction, comprising an apomorphine core portion having a first T₅₀ value and an outer layer portion comprising an antiemetic agent having a second T₅₀ value, wherein the first T₅₀ is greater than the second T₅₀, said composition further comprising an osmotic agent, and a swellable hydrophilic carrier.

2. The composition in accordance with claim 1 wherein apomorphine is present as apomorphine hydrochloride.

3. The composition in accordance with claim 1 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 acid addition salts thereof.

4. The composition in accordance with claim 3 wherein the antiemetic agent is a phenothiazine.

5. The composition in accordance with claim 4 wherein the phenothiazine is prochlorperazine.

6. The composition in accordance with claim 3 wherein the antiemetic agent is a benzamide.

7. The composition in accordance with claim 6 wherein the benzamide is metoclopramide hydrochloride.

8. An antiemetic-apomorphine tablet composition suitable for sublingual delivery to treat erectile dysfunction, comprising:

a core comprising an apomorphine component having a first T₅₀ value; and

an outer layer comprising an antiemetic agent having a second T₅₀ value, wherein said first T₅₀ is greater than said second T₅₀ value.

9. The composition of claim 8 further comprising an osmotic agent.

10. The composition of claim 8 further comprising a swellable hydrophilic carrier.

11. The composition of claim 8 further comprising an osmotic agent and a swellable hydrophilic carrier.

12. The composition of claim 11, wherein said antiemetic agent is selected from the group consisting of prochlorperazine, nicotine, and acid addition salts thereof.

13. The composition of claim 12, wherein said first T₅₀ is at least eight times greater than said second T₅₀.

14. The composition of claim 12, wherein said first T₅₀ is at least six times greater than said second T₅₀.

15. The composition of claim 12, wherein said first T₅₀ is at least two times greater than said second T₅₀.

16. The composition of claim 8, wherein said antiemetic agent is selected from the group consisting of the phenothiazines, the benzamides, the meclizines, the serotonin antagonists, hydroxyzine, lobeline sulfate, dimenhydrinate, scopolamine, metopimazine, diphenidol hydrochloride, nicotine, and acid addition salts thereof.

17. The composition of claim 8, wherein said first T₅₀ is at least two times greater than said second T₅₀.