US2010063019A1PendingUtilityA1

Low Dose Estrogen Interrupted Hormone Replacement Therapy

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Assignee: DURAMED PHARMACEUTICALS INCPriority: Mar 30, 1999Filed: Sep 8, 2009Published: Mar 11, 2010
Est. expiryMar 30, 2019(expired)· nominal 20-yr term from priority
Inventors:Robert CasperGary A. ShangoldMilitza K. Ausmanas
A61P 9/00A61P 5/24A61P 5/30A61P 43/00A61P 25/28A61P 19/10A61P 15/12A61K 31/565
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Claims

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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg per day of norgestimate.

Claims

exact text as granted — not AI-modified
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 17β-estradiol, and a relatively dominant progestogenic activity phase comprising three consecutive daily closes or an equivalent thereof, of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17α-ethinylestradiol, esters and ethers of 17α-ethinylestradiol, 17α-ethinylestradiol 3-dimethylamino propionate, 17α ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17α-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, 17D-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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17α-ethinylestradiol, esters and ethers of 17α-ethinylestradiol, 17α-ethinylestradiol 3-dimethylamino propionate, 17α-ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17α-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, 17D-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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg 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 17α-ethinylestradiol, esters and ethers of 17α-ethinylestradiol, 17α-ethinylestradiol 3-dimethyl amino propionate, 17α-ethinylestradiol 3-cyclopentyl ether (quienestrol) and 17α-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, 17D-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 . A use of estrogenically active substance and a progestogenically active substance in the preparation of a medicament, characterized in that the medicament is for hormone replacement therapy for administration to a female in need of such therapy, the medicament comprising a plurality of doses for consecutive administration in alternating phases, which phases consist 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 17β-estradiol, and a relatively dominant progestogenic activity phase comprising three daily doses or an equivalent thereof, of a combination of a substance exhibiting estrogenic activity equivalent to about 1 mg per day of 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg per day of norgestimate. 
   
   
       20 . The use as claimed in  claim 19  wherein the medicament comprises a plurality of doses for consecutive administration in alternating phases, which phases consist 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 17β-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 17β-estradiol and a substance exhibiting progestogenic activity equivalent to about 90 μg per day of norgestimate. 
   
   
       21 . The use as claimed in  claim 20  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.   
   
   
       22 . The use as claimed in  claim 20  wherein the substance exhibiting estrogenic
 activity is selected from 17α-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, 17D-acteyl norgestimate, dienogest, trimegestone, dropserinone and nomagestrel.   
   
   
       23 . 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 17β-estradiol, and in the relatively dominant progestogenic activity phase comprise about 1 mg per day of 17β-estradiol and about 90 μg per day of norgestimate. 
   
   
       24 . The preparation as claimed in  claim 23  wherein the doses are in oral form. 
   
   
       25 . The preparation as claimed in  claim 24  wherein the doses are in tablet form. 
   
   
       26 . 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 17β-estradiol and in the relatively dominant progestogenic activity phase comprise about 1 mg per day of 17β-estradiol and about 90 μg per day of norgestimate. 
   
   
       27 . The package as claimed in  claim 26  wherein the doses are in oral form. 
   
   
       28 . The package as claimed in  claim 27  wherein the doses are in tablet form. 
   
   
       29 . The method as claimed in  claim 14  in which the daily doses in the relatively dominant estrogenic activity phase comprise about 1 mg per day of 17β-estradiol, and in the relatively dominant progestogenic activity phase comprise about 1 mg per day of 17β-estradiol and about 90 μg per day of norgestimate. 
   
   
       30 . The method as claimed in  claim 29  wherein the doses are in oral form. 
   
   
       31 . The method as claimed in  claim 30  wherein the doses are in tablet form. 
   
   
       32 . The use as claimed in  claim 20  in which the daily doses in the relatively dominant estrogenic activity phase comprises about 1 mg per day of 17β-estradiol, and in the relatively dominant progestogenic activity phase comprises about 1 mg per day of 17β-estradiol and about 90 μg per day of norgestimate. 
   
   
       33 . The use as claimed in  claim 32  wherein the doses are in oral form. 
   
   
       34 . The use as claimed in  claim 33  wherein the doses are in tablet form.

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