Graduated estrogen contraceptive

• US 8,124,595 B2
• Filed: 11/12/2004
• Issued: 02/28/2012
• Est. Priority Date: 11/14/2003
• Status: Active Grant

• Current Assignee: Allergan Therapeutics LLC (Abbvie Incorporated)
• Original Assignee: Warner Chilcott Company LLC (Abbvie Incorporated)
• Inventors: Boissonneault, Roger M.
• Primary Examiner(s): Richter, Johann
• Assistant Examiner(s): CHUI, MEI PING
• Application Number:
  US10/987,653
• Publication Number:
  US 20050107351A1
• Time in Patent Office: 2,664 Days
• Field of Search: 514/169, 514/170, 514/171, 514/177, 514/182, 514/841, 514/843
• US Class Current: 514/169
• 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 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 7/06 Antianaemics

Abstract

A multiphasic estrogenic/progestogenic contraceptive regimen that provides for the reduction or elimination of estrogen in the initial phase is disclosed. Also described is a contraceptive kit that may be used to practice the method of the invention.

Claims

1. A method of contraception comprising the steps of sequentially administering to a female of child bearing age:

(a) a composition I containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 0.5 to about 5 mcg of ethinyl estradiol for about 5 to about 9 days;

(b) a composition II containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 10 to about 50 mcg of ethinyl estradiol for about 5 to about 9 days;

(c) a composition III containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 25 to about 50 mcg of ethinyl estradiol for about 8 to about 12 days; and

(d) a composition IV which contains ferrous fumarate or is a placebo for 1 to 4 days, wherein the sequential administration of compositions I, II, III and IV is repeated upon the completion of the administration of composition IV and the daily administration of compositions I, II, III and IV is for a 28 day period and wherein the amount of estrogen in composition III is greater than the amount of estrogen in composition II by at least an amount equivalent to 5 mcg of ethinyl estradiol.

2. The method according to claim 1, wherein the progestogen in each composition is norethindrone acetate.

3. The method according to claim 1, wherein the estrogen in each composition is ethinyl estradiol.

4. The method according to claim 3, wherein composition I contains an amount of ethinyl estradiol from about 0.5 to about 5 mcg.

5. The method according to claim 4, wherein composition I contains about 5 mcg of ethinyl estradiol.

6. The method according to claim 1, wherein each of compositions I, II and III contain a progestogen in an amount equivalent to about 0.5 to about 1.5 mg of norethindrone acetate.

7. The method according to claim 1, wherein composition I contains about 1.0 mg of norethindrone acetate and is administered for about 7 days, composition II contains about 1.0 mg of norethindrone acetate and is administered for about 7 days, composition III contains about 1.0 mg of norethindrone acetate and is administered for about 10 days, and composition IV contains about 75 mg of ferrous fumarate and is administered for 4 days.

8. The method according to claim 7, wherein composition I contains about 5 mcg of ethinyl estradiol, composition II contains about 30 mcg of ethinyl estradiol and composition III contains about 35 mcg of ethinyl estradiol.

9. A method of contraception comprising the steps of sequentially administering to a female of child bearing age:

(a) a composition I containing about 0.3 to about 1.5 mg norethindrone acetate and about 0.5 to about 5 mcg of ethinyl estradiol for about 5 to about 9 days;

(b) a composition II containing about 0.3 to about 1.5 mg norethindrone acetate and about 10 to 50 mcg ethinyl estradiol for about 5 to about 9 days;

(c) a composition III containing about 0.3 to about 1.5 mg norethindrone acetate and about 25 to 50 mcg ethinyl estradiol for about 8 to about 12 days; and

(d) a composition IV that contains ferrous fumurate or is a placebo for 1 to 4 days,

wherein the sequential administration of compositions I, II, III and IV is repeated and the daily administration of compositions I, II, III and IV is for a 28 day period, wherein composition III contains at least 5 mcg of ethinyl estradiol more than composition II.

10. The method according to claim 9, wherein each of compositions I, II and III contain about 0.5 to about 1.5 mg of norethindrone acetate.

11. A method of contraception comprising the steps of sequentially administering to a female of child bearing age:

(a) a composition I containing about 1 mg norethindrone acetate and about 5 mcg of ethinyl estradiol for 7 days;

(b) a composition II containing about 1 mg of norethindrone acetate and about 10 mcg of ethinyl estradiol for 7 days;

(c) a composition III containing about 1 mg of norethindrone acetate and about 25 mcg of ethinyl estradiol for 10 days; and

(d) a composition IV which contains ferrous fumarate or is a placebo for 4 days, wherein the sequential administration of compositions I, II, III and IV is repeated upon the completion of the administration of composition IV.