Chewable oral contraceptive

• US 6,667,050 B1
• Filed: 06/12/2001
• Issued: 12/23/2003
• Est. Priority Date: 04/06/1999
• Status: Expired due to Term

• Current Assignee: Allergan Pharmaceuticals International Ltd. (Abbvie Incorporated)
• Original Assignee: Galen (Chemicals) Ltd. (Abbvie Incorporated)
• Inventors: Boissonneault, Roger M., deVries, Tina M.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): EVANS, CHARESSE L
• Application Number:
  US09/879,028
• Time in Patent Office: 924 Days
• Field of Search: 424/400, 424/439, 424/440, 424/441, 424/464, 424/484, 424/489, 514/841, 514/843
• US Class Current: 424/439
• 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 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• 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

Abstract

The present invention relates to a chewable, palatable oral contraceptive tablet, comprising an oral contraceptive agent, a chewable carrier suitable for human consumption, and not comprising a ferrocene compound, as well as use of these tablets in a method of human female oral contraception, and in a method of enhancing compliance with a human female oral contraceptive regimen.

Claims

1. A chewable, palatable oral contraceptive tablet, comprising an oral contraceptive agent, a chewable carrier suitable for human consumption, wherein the contraceptive tablet is chewable and palatable and does not contain a ferrocene compound.

2. The tablet of claim 1, wherein the oral contraceptive agent is selected from the group consisting of an estrogen, a progestin, and a combination thereof.

3. The tablet of claim 2, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

4. The tablet of claim 1, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

5. The tablet of claim 1, wherein the oral contraceptive agent comprises an estrogen.

6. The tablet of claim 5, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate.

7. The tablet of claim 6, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

8. The tablet of claim 1, wherein the oral contraceptive agent comprises a progestin.

9. The tablet of claim 8, wherein the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

10. The tablet of claim 9, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

11. The tablet of claim 1, wherein the oral contraceptive agent comprises an estrogen and a progestin.

12. The tablet of claim 11, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate, and the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

13. The tablet of claim 12, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

14. The tablet of claim 13, further comprising at least one of a flavor agent, a sweetener, and a color agent.

15. The tablet of claim 1, wherein the tablet weighs about 50 milligrams to about 300 milligrams.

16. The tablet of claim 1, wherein the tablet has a hardness sufficient for blister packaging.

17. The tablet of claim 1, wherein the tablet has a hardness of about 5 kiloponds to about 15 kiloponds.

18. The tablet of claim 1, wherein the oral contraceptive agent comprises norethindrone and ethinyl estradiol, the carrier comprises dicalcium phosphate, lactose monohydrate, and maltodextrin, and the tablet further comprises sucralose, a flavor agent, sodium starch glycolate, povidone, and magnesium stearate.

19. A method of human female oral contraception, the method comprising providing a chewable, palatable oral contraceptive tablet comprising a contraceptively effective amount of an oral contraceptive agent, and a chewable carrier suitable for human consumption, and does not contain a ferrocene compound, and administering the tablet to a human female.

20. The method of claim 19, wherein the oral contraceptive agent is selected from the group consisting of an estrogen, a progestin, and a combination thereof.

21. The method of claim 20, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

22. The method of claim 19, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

23. The method of claim 19, wherein the oral contraceptive agent comprises an estrogen.

24. The method of claim 23, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate.

25. The method of claim 24, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

26. The method of claim 19, wherein the oral contraceptive agent comprises a progestin.

27. The method of claim 26, wherein the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

28. The method of claim 27, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

29. The method of claim 19, wherein the oral contraceptive agent comprises an estrogen and a progestin.

30. The method of claim 29, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate, and the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

31. The method of claim 30, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

32. The method of claim 31, wherein the tablet further comprises at least one of a flavor agent, a sweetener, and a color agent.

33. The method of claim 19, wherein the tablet weighs about 50 milligrams to about 300 milligrams.

34. The method of claim 19, wherein the tablet has a hardness sufficient for blister packaging.

35. The method of claim 19, wherein the tablet has a hardness of about 5 kiloponds to about 15 kiloponds.

36. The method of claim 19, wherein the oral contraceptive agent comprises norethindrone and ethinyl estradiol, the carrier comprises dicalcium phosphate, lactose monohydrate, and maltodextrin, and the tablet further comprises sucralose, a flavor agent, sodium starch glycolate, povidone, and magnesium stearate.

37. A method of enhancing compliance with a human female oral contraceptive regimen involving oral contraceptive tablets, the method comprising providing chewable, palatable oral contraceptive tablets comprising a contraceptively effective amount of an oral contraceptive agent, and a chewable carrier suitable for human consumption, and not comprising a ferrocene compound, and administering the tablets to the human female in accordance with the contraceptive regimen.

38. The method of claim 37, wherein the oral contraceptive agent is selected from the group consisting of an estrogen, a progestin, and a combination thereof.

39. The method of claim 38, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

40. The method of claim 37, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

41. The method of claim 37, wherein the oral contraceptive agent comprises an estrogen.

42. The method of claim 41, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate.

43. The method of claim 42, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

44. The method of claim 37, wherein the oral contraceptive agent comprises a progestin.

45. The method of claim 44, wherein the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

46. The method of claim 45, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

47. The method of claim 37, wherein the oral contraceptive agent comprises an estrogen and a progestin.

48. The method of claim 47, wherein the estrogen is selected from the group consisting of ethinyl estradiol, estradiol, estradiol valerate, and estradiol acetate, and the progestin is selected from the group consisting of norethindrone, norethindrone acetate, desogestrel, levonorgestrel, ethynodiol diacetate, norgestrel, norgestimate, gestodene, drospirenone, trimegestone, levodesogestrel, gestodyne, and nesterone.

49. The method of claim 48, wherein the carrier is selected from the group consisting of dicalcium phosphate, lactose, corn starch, microcrystalline cellulose, maltodextrin, dextrose, mannitol, sorbitol, xylitol, fructose, sucrose, and calcium carbonate.

50. The method of claim 49, wherein the tablets further comprise at least one of a flavor agent, a sweetener, and a color agent.

51. The method of claim 37, wherein each tablet weighs about 50 milligrams to about 300 milligrams.

52. The method of claim 37, wherein the tablets have a hardness sufficient for blister packaging.

53. The method of claim 37, wherein the tablet has a hardness of about 5 kiloponds to about 15 kiloponds.

54. The method of claim 37, wherein the oral contraceptive agent comprises norethindrone and ethinyl estradiol, the carrier comprises dicalcium phosphate, lactose monohydrate, and maltodextrin, and the tablet further comprises sucralose, a flavor agent, sodium starch glycolate, povidone, and magnesium stearate.

55. The method of claim 37, wherein each tablet comprises a daily dosage of the oral contraceptive agent.

56. The method of claim 55, wherein the regimen comprises providing about 21 to about 25 tablets comprising the oral contraceptive agent.

57. The method of claim 56, wherein the regimen further comprises about 3 to about 7 tablets comprising a placebo.

58. The method of claim 56, wherein the regimen is a uniphasic regimen wherein the oral contraceptive agent is present in the same amount in the tablets.

59. The method of claim 56, wherein the regimen is a multiphasic regimen wherein the oral contraceptive agent is present in differing amounts in the tablets.

60. The method of claim 37, wherein the tablets are provided in a blister package.