Contraceptive transdermal delivery of hormones
Inventors
Rossi, Thomas M. • Foegh, Marie • Kydonieus, Agis
Assignees
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Publication Number
US-9198919-B2
Publication Date
2015-12-01
Expiration Date
Abstract
Dosing regimen for transdermal delivery of hormones comprising a variable treatment cycle and a variable rest interval.
Core Innovation
The invention relates to preventing pregnancy by a method that uses transdermal administration over an eight week treatment cycle. The cycle includes a treatment interval of seven weeks and a rest interval of one week, during which contraceptively effective amounts of a progestin and an estrogen are administered transdermally by successive applications of transdermal hormone delivery devices.
During the rest interval, low dose progestin and low dose estrogen are administered transdermally by application of a transdermal hormone delivery device. The progestin is levonorgestrel and the estrogen is ethinyl estradiol, and the method is configured so that the woman experiences menstruation with attenuated symptoms of menstruation during the rest interval.
The amount of levonorgestrel delivered during the treatment interval results in an average levonorgestrel serum concentration of at least 750 pg/ml, while the average progestin serum concentration during the rest interval is 25% to 75% of the amount delivered during the treatment interval. The amount of ethinyl estradiol delivered during the treatment interval results in an average ethinyl estradiol serum concentration of at least 15 pg/ml, and the average estrogen serum concentration during the rest interval is also limited to 25% to 75% of the amount delivered during the treatment interval.
Claims Coverage
The independent claim covers a contraceptive method with an 8-week cycle structure, including transdermal administration of levonorgestrel and ethinyl estradiol via successive devices and low-dose rest-interval delivery. Across the dependent claims, the regimen is further constrained by serum pharmacokinetic relationships and rest-interval implementation details.
Transdermal progestin and estrogen over a 7-week treatment interval with successive devices
During an eight week treatment cycle having a treatment interval of seven weeks and a rest interval of one week, transdermally administering a contraceptively effective amount of a progestin and an estrogen during the treatment interval by successive applications of transdermal hormone delivery devices.
Low dose transdermal progestin and low dose transdermal estrogen throughout a 1-week rest interval
Transdermally administering low dose progestin and low dose estrogen throughout the rest interval by application of a transdermal hormone delivery device.
Levonorgestrel and ethinyl estradiol serum concentration thresholds
The progestin is levonorgestrel and the amount delivered during the treatment interval results in an average levonorgestrel serum concentration of at least 750 pg/ml; the estrogen is ethinyl estradiol and the amount delivered during the treatment interval results in an average ethinyl estradiol serum concentration of at least 15 pg/ml.
Rest-interval progestin and estrogen fraction limits relative to treatment interval
The amount of the progestin delivered during the rest interval results in an average progestin serum concentration that is 25% to 75% of the amount of the progestin delivered during the treatment interval; the amount of the estrogen delivered during the rest interval results in an average estrogen serum concentration that is 25% to 75% of the amount of the estrogen delivered during the treatment interval.
Menstruation with attenuated symptoms during the rest interval
Whereby the woman experiences menstruation, with attenuated symptoms of menstruation during the rest interval.
Overall claim coverage centers on preventing pregnancy using transdermal levonorgestrel plus ethinyl estradiol in a structured eight week cycle. The inventive concept is constrained by treatment-interval serum thresholds and by rest-interval delivery restricted to 25% to 75% of the treatment-interval delivered amounts, to achieve menstruation with attenuated symptoms during the rest interval.
Stated Advantages
Menstruation with attenuated symptoms of menstruation during the rest interval.
Documented Applications
Contraception: preventing pregnancy in a woman.
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