Combination preparation for contraception based on natural estrogens
View Patent ↗The combination preparation for contraception includes from 2 to 4 first stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient, from 16 to 22 second stage daily dosage portions each including an effective amount of a combination of at least one natural estrogen and at least one natural or synthetic gestogen as active ingredient; from 2 to 4 third stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient; and from 2 to 4 final stage daily dosage portions containing a pharmaceutically acceptable placebo. The estrogen may be estradiol, an estradiol compound that is metabolized to estradiol when taken into the body, a conjugated equine estrogen or a phytoestrogen. The natural or synthetic gestogen can be natural progesterone or a synthetic gestogens, such as medroxyprogesterone acetate.
1. A combination preparation for contraception comprising
a first stage consisting of two daily dosage portions, each consisting of an effective amount of estradiol valerate;
a second stage consisting of a first group and a second group of daily dosage portions of a combination of said estradiol valerate and dienogest;
a third stage consisting of two daily dosage portions, each consisting of an effective amount of said estradiol valerate, wherein said effective amount of said estradiol valerate in each of said two daily dosage portions in said third stage is the same, but smaller than said effective amount of said estradiol valerate in each of said two daily dosage portions in said first stage; and
an additional stage consisting of two daily dosage portions, each consisting of a pharmaceutically acceptable placebo;
wherein said first group of said daily dosage portions of said second stage consists of five of said daily dosage portions of said combination and wherein said second group of said daily dosage portions of said second stage consists of seventeen of said daily dosage portions of said combination; and
wherein respective amounts of said estradiol valerate in each of said daily dosage portions of said second stage are equal and respective amounts of said dienogest in said daily dosage portions of said second group of said second stage are equal to 1.5 to 3 times corresponding amounts of said dienogest in said daily dosage portions of said first group of said second stage.
2. The combination preparation as defined in claim 1 , wherein said effective amount of said estradiol valerate in each of said daily dosage portions during said first stage is from 3 to 4 mg/day and said corresponding amounts of said dienogest in said daily dosage portions in said first group of said second stage are minimum amounts necessary for effective contraceptive activity.
3. A combination preparation for contraception consists of
a first stage consisting of three daily dosage portions, each consisting of an effective amount of estradiol valerate;
a second stage consisting of a first group and a second group of daily dosage portions of a combination of said estradiol valerate and dienoest;
a third stage consisting of two daily dosage portions, each consisting of an effective amount of said estradiol valerate, wherein said effective amount of said estradiol valerate in each of said two daily dosage portions in said third stage is the same, but smaller than said effective amount of said estradiol valerate in each of said two daily dosage portions in said first stage; and
an additional stage consisting of three daily dosage portions, each consisting of a pharmaceutically acceptable placebo;
wherein said first group of said daily dosage portions of said second stage consists of four of said daily dosage portions of said combination and wherein said second group of said daily dosage portions of said second stage consists of sixteen of said daily dosage portions of said combination; and
wherein respective amounts of said estradiol valerate in each of said daily dosage portions of said second stage are equal and respective amount of said dienogest in said daily dosage portions of said second group of said second stage are equal to 1.5 to 3 times corresponding amounts of said dienogest in said daily dosage portions of said first group of said second stage.
4. The combination preparation as defined in claim 3 , wherein said effective amount of said estradiol valerate in each of said daily dosage portions during said first stage is from 3 to 4 mg/day and said respective amounts of said dienogest in said daily dosage portions in said first group of said second stage is a minimum amount necessary for effective contraceptive activity.
5. The combination preparation as defined in claim 3 or 4 , wherein 1 mg of said dienogest is present in each of said daily dosage portions in said first group of said second stage.