Rapid-onset medicament for treatment of sexual dysfunction

• US 20030022912A1
• Filed: 02/07/2002
• Published: 01/30/2003
• Est. Priority Date: 02/08/2001
• Status: Abandoned Application

• Current Assignee: Pharmacia & Upjohn Company (Pfizer Inc.)
• Original Assignee: Pharmacia & Upjohn Company (Pfizer Inc.)
• Inventors: Tyle, Praveen, McCurdy, Vincent E., Wu, Sy-Juen, Pierman, Steven A., Martino, Alice C., Reo, Joseph P.
• Application Number:
  US10/072,368
• Publication Number:
  US 20030022912A1
• Time in Patent Office: Days
• US Class Current: 514/292
• CPC Class Codes: A61K 31/437 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• CPC Class Codes: A61K 31/4745 condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48
• CPC Class Codes: A61K 9/0043 Nose
• 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: A61K 9/0058 Chewing gums non-medicinal aspects, preparing chewing gum A23G4/00; chewing gum for care of the teeth or oral cavity, e.g. with breath freshener A61Q11/00
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• 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

Abstract

A rapid-onset pharmaceutical composition is provided, useful for treatment of sexual dysfunction, stimulation of sexual activity and enhancement of sexual desire, interest and performance in men and women. The composition is a dosage form comprising (a) a therapeutically or sexual-stimulatorily effective amount of a therapeutic agent having a molecular weight, excluding counterions, not greater than 250, and (b) at least one pharmaceutically acceptable excipient; and is adapted for delivery by a route of administration that entails interaction with the organs of taste yet has acceptable organoleptic properties. Illustrative therapeutic agents useful in dosage forms of the invention are compounds having the formula

wherein X is O or S; and pharmaceutically acceptable salts thereof.

Claims

1. A pharmaceutical dosage form comprising (a) at least one agent effective in treatment of sexual dysfunction having a molecular weight, excluding counterions, not greater than 250, in a therapeutically or sexual-stimulatorily effective total amount, and (b) at least one pharmaceutically acceptable excipient;

the dosage form being adapted for delivery by a route of administration that entails interaction with the organs of taste yet having acceptable organoleptic properties.

2. The dosage form of claim 1 wherein the at least one agent has a molecular weight, excluding counterions, not greater than 235.

3. The dosage form of claim 1 wherein the at least one agent has a molecular weight, excluding counterions, not greater than 220.

4. The dosage form of claim 1 wherein the at least one agent has a solubility in water at 20-25°

C. of at least about 10 g/l.

5. The dosage form of claim 1 wherein the at least one agent is a compound having the formula

6. The dosage form of claim 1 wherein the total amount of the at least one agent per dose is lower than an amount causing significant side-effects.

7. The dosage form of claim 1 wherein the therapeutic agent is sumanirole or a salt thereof and is present in an amount of about 0.05 mg to about 5 mg per dose.

8. The dosage form of claim 1 wherein the therapeutic agent is (R)-5,6-dihydro-5-(methylamino)-4H-imidazo[4,5-ij]-quinoline-2(1H)-thione or a salt thereof and is present in an amount of about 0.05 mg to about 5 mg per dose.

9. The dosage form of claim 8 wherein the therapeutic agent is present in an amount of about 0.1 to about 3 mg per dose.

10. The dosage form of claim 1 that is adapted for a route of administration selected from oral, buccal, sublingual, nasal and tracheal routes.

11. The dosage form of claim 1 that is selected from

(a) buccal and sublingual tablets;

(b) mucoadhesive films;

(c) oral strips;

(d) chewable tablets;

(e) rapidly disintegrating oral dosage forms;

(f) lozenges and pastilles;

(g) breath-fresheners;

(h) chewing gums;

(i) lollipops and popsicles;

(j) food adjuncts;

(k) candies and chocolates;

(l) periodontal gels;

(m) mouthwashes;

(n) oral and nasal drops and sprays;

(o) dosage forms adapted for inhalation as an aerosol or vapor;

(p) elixirs, solutions, suspensions and other orally administered liquid dosage forms;

(q) powders, granules and tablets for dissolution or dispersion in water prior to oral administration; and

(r) effervescent tablets and granules.

12. The dosage form of claim 1 that is adapted for discreet self-administration.

13. The dosage form of claim 1 that is adapted for nasal administration.

14. The dosage form of claim 13 that is formulated as a nasal spray solution.

15. The dosage form of claim 1 that is adapted for oral, buccal or sublingual administration.

16. The dosage form of claim 15 that dissolves in the mouth without need for drinking water or other fluid.

17. The dosage form of claim 15 that is a breath-freshening pastille.

18. The dosage form of claim 15 that is a chewing gum.

19. The dosage form of claim 15 that is a sublingual tablet.

20. The dosage form of claim 15 that is a mucoadhesive film.

21. The dosage form of claim 15 that is an oral strip.

22. The dosage form of claim 15 that is an oral fast-melt tablet.

39. A method of treating sexual dysfunction in a subject comprising intraoral administration of a dosage form of claim 1 to the subject, less than about 1 hour prior to sexual activity.

41. A method of enhancing sexual desire, interest or performance in a subject comprising intraoral administration of a dosage form of claim 1 to the subject, less than about 1 hour prior to sexual activity.

23. A pharmaceutical dosage form comprising (a) a therapeutically or sexual-stimulatorily effective amount of about 0.1 mg to about 10 mg per dose of a therapeutic agent that comprises at least one compound of formula

24. The dosage form of claim 23 wherein the water-soluble compound or salt thereof has a solubility in water at 20-25°

C. of at least about 10 g/l.

25. The dosage form of claim 23 wherein the water-soluble compound or salt thereof is disclosed generically or specifically in U.S. Pat. No. 5,273,975.

26. The dosage form of claim 23 that is adapted for a route of administration selected from oral, buccal, sublingual, nasal and tracheal routes.

27. The dosage form of claim 23 that is selected from

(a) buccal and sublingual tablets;

(b) mucoadhesive films;

(c) oral strips;

(d) chewable tablets;

(e) rapidly disintegrating oral dosage forms;

(f) lozenges and pastilles;

(g) breath-fresheners;

(h) chewing gums;

(i) lollipops and popsicles;

(j) food adjuncts;

(k) candies and chocolates;

(l) periodontal gels;

(m) mouthwashes;

(n) oral and nasal drops and sprays;

(o) dosage forms adapted for inhalation as an aerosol or vapor;

(p) elixirs, solutions, suspensions and other orally administered liquid dosage forms;

(q) powders, granules and tablets for dissolution or dispersion in water prior to oral administration; and

(r) effervescent tablets and granules.

28. The dosage form of claim 23 that is adapted for discreet self-administration.

29. The dosage form of claim 23 that is adapted for nasal administration.

30. The dosage form of claim 29 that is formulated as a nasal spray solution.

31. The dosage form of claim 23 that is adapted for oral, buccal or sublingual administration.

32. The dosage form of claim 31 that dissolves in the mouth without need for drinking water or other fluid.

33. The dosage form of claim 31 that is a breath-freshening pastille.

34. The dosage form of claim 31 that is a chewing gum.

35. The dosage form of claim 31 that is a sublingual tablet.

36. The dosage form of claim 31 that is a mucoadhesive film.

37. The dosage form of claim 31 that is an oral strip.

38. The dosage form of claim 31 that is an oral fast-melt tablet.

40. A method of treating sexual dysfunction in a subject comprising intraoral administration of a dosage form of claim 23 to the subject, less than about 1 hour prior to sexual activity.

42. A method of enhancing sexual desire, interest or performance in a subject comprising intraoral administration of a dosage form of claim 23 to the subject, less than about 1 hour prior to sexual activity.