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Claims for Patent: 6,747,019

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Claims for Patent: 6,747,019

Title: Low dose estrogen interrupted hormone replacement therapy
Abstract:A hormone replacement therapy, comprising a plurality of daily doses of a pharmaceutical preparation, the doses being administered continuously and consecutively in alternating phases of three daily doses, a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol per day, and a relatively dominant progestagenic activity phase of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.
Inventor(s): Casper; Robert F. (Toronto, CA), Shangold; Gary A. (Califon, NJ), Ausmanas; Militza K. (Lake Forest, IL)
Assignee: Jencap Research, Ltd. (Toronto, CA) Ortho-McNeil Pharmaceutical, Inc. (Raritan, NJ)
Application Number:10/134,455
Patent Claims: 1. A pharmaceutical preparation for administration to a female in need of hormone replacement therapy, comprising a plurality of doses for administration in alternating relatively dominant estrogenic activity phases, the relatively dominant estrogenic activity phases consisting of a relatively dominant estrogenic activity relatively dominant estrogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

2. The pharmaceutical preparation as claimed in claim 1 for administration to a female in need of hormone replacement therapy comprising a plurality of daily doses for consecutive administration, the doses being administered in alternating phases, the phases comprising a relatively dominant estrogenic activity phase comprising three consecutive daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily doses of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

3. The pharmaceutical preparation as claimed in claim 2 wherein the substance exhibiting progestogenic activity is selected on the basis that it binds to progestin receptors, demonstrates poor affinity for androgen receptors and has a lack of affinity for sex-hormone-binding globulin.

4. The pharmaceutical preparation as claimed in claim 3 wherein the substance exhibiting estrogenic activity is selected from 17.alpha.-ethinylestradiol, esters and ethers of 17.alpha.-ethinylestradiol, 17.alpha.-ethinylestradiol 3-dimethylamino propionate, 17.alpha.ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17.alpha.-ethinylestradiol 3-methyl ether (mestranol); natural estrogens, estrone, estrone sulfate, estrone sulfate piperazine salt, estradiol and estriol, and their esters, as well as the synthetic estrogens, and the substance exhibiting progestogenic activity is selected from desogestrel, dydrogesterone, medroxyprogesterone acetate, norethynodrel, cyproterone acetate, chlormadinone acetate, magestrol acetate, 17 D-acetyl norgestimate, dienogest, trimegestone, drosperinone and nomagestrel.

5. The pharmaceutical preparation as claimed in claim 1 wherein the doses are in oral form.

6. The pharmaceutical preparation as claimed in claim 5 wherein the oral form is a tablet.

7. A package containing a pharmaceutical preparation for administration to a female in need of hormone replacement therapy, comprising a plurality of doses arranged in alternating phases, the phases consisting of a relatively dominant estrogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

8. The pharmaceutical package as claimed in claim 7 containing a pharmaceutical regimen for administration to a female in need of hormone replacement therapy, the doses being arranged for administration in alternating phases, the phases consisting of a relatively dominant estrogenic activity phase comprising three consecutive daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily doses comprising a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

9. The pharmaceutical package as claimed in claim 8 wherein the substance exhibiting progestogenic activity is selected on the basis that it binds to progestin receptors, it demonstrates poor affinity for androgen receptors and has a lack of affinity for sex-hormone-binding globulin.

10. The pharmaceutical package as claimed in claim 8 wherein the substance exhibiting estrogen activity is selected from 17.alpha.-ethinylestradiol, esters and ethers of 17.alpha.-ethinylestradiol, 17.alpha.-ethinylestradiol 3-dimethylamino propionate, 17.alpha.-ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17.alpha.-ethinylestradiol 3-methyl ether (mestranol); natural estrogens, estrone, estrone sulfate, estrone sulfate piperazine salt, estradiol and estriol, and their esters, as well as the synthetic estrogens, and the substance exhibiting progestogenic activity is selected from desogestrel, dydrogesterone, medroxyprogesterone acetate, norethynodrel, cyproterone acetate, chlormadinone acetate, magestrol acetate, 17 D-acetyl norgestimate, dienogest, trimegestone, drosperinone and nomagestrel.

11. The pharmaceutical package as claimed in claim 7, wherein the doses are in oral form.

12. The pharmaceutical package as claimed in claim 11, wherein the oral form is a tablet.

13. A method of treating a female in need of hormone replacement therapy comprising administering to said female a pharmaceutical regimen comprising a plurality of doses arranged in alternating phases, the phases comprising a relatively dominant estrogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily doses or an equivalent thereof, of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

14. A method of treating a female in need of hormone replacement therapy as claimed in claim 13 comprising administering to said female a pharmaceutical regimen comprising a plurality of doses arranged in alternating phases, the phases comprising a relatively dominant estrogenic activity phase comprising three daily doses of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol, and a relatively dominant progestogenic activity phase comprising three daily doses of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17.beta.-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 .mu.g per day of norgestimate.

15. The method as claimed in claim 14 wherein the substance exhibiting progestogenic activity is selected on the basis that it binds to progestogen receptors, demonstrates poor affinity for androgen receptors and has a lack of affinity for sex-hormone-binding globulin.

16. The method as claimed in claim 14 wherein the substance exhibiting estrogenic activity is selected from 17.alpha.-ethinylestradiol, esters and ethers of 17.alpha.-ethinylestradiol, 17.alpha.-ethinylestradiol 3-dimethyl amino propionate, 17.alpha.-ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17.alpha.-ethinylestradiol 3-methyl ether (mestranol); natural estrogens, estrone, estrone sulfate, estrone sulfate piperazine salt, estradiol and estriol, and their esters, as well as the synthetic estrogens, and the substance exhibiting progestogenic activity is selected from desogestrel, dydrogesterone, medroxyprogesterofle acetate, norethynodrel, cyproterone acetate, chlormadinone acetate, magestrol acetate, 17 D-acetyl norgestimate, dienogest, trimegestone, drosperinone and nomagestrel.

17. The method as claimed in claim 13 wherein the doses are in oral form.

18. The method as claimed in claim 17 wherein the oral form is a tablet.

19. The preparation as claimed in claim 1 in which the daily doses in the relatively dominant estrogenic activity phase comprise about 1 mg per day of 17.beta.-estradiol, and in the relatively dominant progestogenic activity phase comprise about 1 mg per day of 17.beta.-estradiol and about 90 .mu.g per day of norgestimate.

20. The preparation as claimed in claim 19, wherein the doses are in oral form.

21. The preparation as claimed in claim 20 wherein the doses are in tablet form.

22. The package claimed in claim 7 in which the daily doses in the relatively dominant estrogenic activity phase comprise about 1 mg per day of 17.beta.-estradiol and in the relatively dominant progestogenic activity phase comprise about 1 mg per day of 17.beta.-estradiol and about 90 .mu.g per day of norgestimate.

23. The package as claimed in claim 22, wherein the doses are in oral form.

24. The package as claimed in claim 23, wherein the doses are in tablet form.
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