Contraceptive transdermal delivery of hormones
Inventors
Rossi, Thomas M. • Foegh, Marie • Kydonieus, Agis
Assignees
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Publication Number
US-9198920-B2
Publication Date
2015-12-01
Expiration Date
Abstract
Dosing regimen for transdermal delivery of hormones comprising a 28 day treatment cycle with a fixed treatment interval and a fixed rest interval.
Core Innovation
The invention relates to transdermal administration for preventing pregnancy using a five week treatment cycle with a treatment interval of four weeks and a rest interval of one week. During the treatment interval, contraceptively effective amounts of a progestin and an estrogen are transdermally administered by successive applications of transdermal hormone delivery devices, and during the rest interval, low dose progestin and low dose estrogen are transdermally administered throughout the rest interval by application of a transdermal hormone delivery device.
The progestin is levonorgestrel and the estrogen is ethinyl estradiol. The amount of levonorgestrel delivered during the treatment interval results in an average levonorgestrel serum concentration of at least 750 pg/ml, and the amount delivered during the rest interval results in an average levonorgestrel serum concentration that is 25% to 75% of the amount delivered during the treatment interval.
Similarly, 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 amount delivered during the rest interval results in an average ethinyl estradiol serum concentration that is 25% to 75% of the amount delivered during the treatment interval. The method is characterized by menstruation with attenuated symptoms of menstruation during the rest interval, and is implemented with transdermal hormone delivery devices in a manner consistent with the five week cycle, including administration throughout the rest interval.
Claims Coverage
The claim coverage includes 7 inventive features across a transdermal contraceptive method with a four week treatment interval and a one week rest interval, using levonorgestrel and ethinyl estradiol with specified serum concentration thresholds and rest-interval dose relationships. Dependent claims further refine serum concentration behavior, rest device sizing, fractional hormone delivery during rest, and wear duration.
Five week transdermal contraceptive cycle with treatment and rest intervals
A method of preventing pregnancy in a woman using a five week treatment cycle having a treatment interval of four weeks and a rest interval of 1 week, wherein transdermally administering contraceptively effective progestin and estrogen during the treatment interval by successive applications of transdermal hormone delivery devices, and transdermally administering low dose progestin and low dose estrogen throughout the rest interval by application of a transdermal hormone delivery device.
Lev-onorgestrel and ethinyl estradiol with defined average serum thresholds and 25% to 75% rest-interval dosing
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, while the rest interval average levonorgestrel serum concentration is 25% to 75% of the treatment interval amount; 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, while the rest interval average ethinyl estradiol serum concentration is 25% to 75% of the treatment interval amount.
Attenuated menstruation symptoms during the rest interval
The method whereby the woman experiences menstruation with attenuated symptoms of menstruation during the rest interval.
Peak-to-trough serum concentration relationship during treatment interval dosing
During the treatment interval each worn device delivers serum hormone levels that peak after patch application and reach trough levels when the patch is removed, with peak levels at least about 1.25 times the trough levels.
Rest interval device sizing relative to treatment interval device
The rest interval device uses the same hormone concentrations as the treatment interval device but is smaller (a fraction of its size).
Rest interval hormone delivery as fractions of treatment interval amounts
The method includes delivering levonorgestrel and ethinyl estradiol during a rest interval at fractions (¼, ⅓, ½, ¾, or 5/6) of the amounts delivered during treatment intervals.
Entire rest interval wear of the rest interval device
The rest interval device is worn for the entire rest interval.
Overall, the claim set covers a transdermal contraceptive regimen that applies successive transdermal hormone delivery devices during a four-week treatment interval and a low-dose transdermal hormone delivery device throughout a one-week rest interval, using levonorgestrel and ethinyl estradiol with specified average serum concentration thresholds and 25% to 75% rest-interval dose relationships, and aiming for menstruation with attenuated symptoms. Dependent claims further constrain peak-to-trough serum behavior, rest device sizing, fractional hormone dose relationships during rest, and wear duration across the full rest interval.
Stated Advantages
Menstruation with attenuated symptoms of menstruation during the rest interval.
Documented Applications
Transdermal contraceptive methods for preventing pregnancy in a woman using a five week treatment cycle with a treatment interval of four weeks and a rest interval of 1 week.
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