Compositions containing alkali metal sulfate salts of conjugated estrogens and antioxidants as stabilizers
First Claim
1. A stabilized therapeutic preparation exhibiting no oxidation and less than about 5% hydrolysis up to at least 24 months, said preparation adapted for treatment of menopausal syndrome, female hypogonadism, amenorrhea, female castration, primary ovarian failure, abnormal uterine bleeding due to hormonal imbalance, and senile vaginitis, consisting essentially of:
- at least one alkali metal sulfate salt of a synthetic conjugated estrogen selected from the group consisting of estrone, equilin, 17α
-dihydroequilin, 17β
-hydroequilin, 17β
-estradiol, 17α
-estradiol, equilenin, and 17β
-dihydroequilenin in estrogenically effective proportions, andan antioxidant effective amount of at least one suitable antioxidant for said alkali metal sulfate salt of said synthetic conjugated estrogen selected from the group consisting of sodium sulfite, potassium sulfite, sodium metabisulfite, potassium metabisulfite, sodium bisulfite, potassium bisulfite, sodium thiosulfate, potassium thiosulfate, thioglycerol, thiosorbitol, cysteine hydrochloride, and α
-tocopherol, wherein the preparation is maintained at an alkalinity corresponding to a pH of not less than about 7.0.
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Abstract
A new and remarkably stable synthesized conjugated estrogen composition comprising one or more selected alkali metal synthetic conjugated estrogen sulfate salts and an effective amount of one or more suitable antioxidants has been found for use in novel and stable therapeutic preparations of a pH of not less than about 7 which are adapted to relieve, inter alia, complaints occurring in the menopausal syndrome and other female complaints. Preferably, the steroids are selected from the sodium and potassium salts of the group consisting of estrone, equilin, 17α-dihydroequilin, and mixtures or conjugates thereof. Most preferably, the preparations are so formulated so that sodium estrone sulfate, sodium equilin sulphate, and 17α-dihydroequilin sodium sulphate as conjugated estrogens are present in a weight ratio of about 6:3:1, respectively and administered in tablets containing 0.625 mg, 1.25 mg, or 2.5 mg of total conjugated estrogens.
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Citations
10 Claims
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1. A stabilized therapeutic preparation exhibiting no oxidation and less than about 5% hydrolysis up to at least 24 months, said preparation adapted for treatment of menopausal syndrome, female hypogonadism, amenorrhea, female castration, primary ovarian failure, abnormal uterine bleeding due to hormonal imbalance, and senile vaginitis, consisting essentially of:
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at least one alkali metal sulfate salt of a synthetic conjugated estrogen selected from the group consisting of estrone, equilin, 17α
-dihydroequilin, 17β
-hydroequilin, 17β
-estradiol, 17α
-estradiol, equilenin, and 17β
-dihydroequilenin in estrogenically effective proportions, andan antioxidant effective amount of at least one suitable antioxidant for said alkali metal sulfate salt of said synthetic conjugated estrogen selected from the group consisting of sodium sulfite, potassium sulfite, sodium metabisulfite, potassium metabisulfite, sodium bisulfite, potassium bisulfite, sodium thiosulfate, potassium thiosulfate, thioglycerol, thiosorbitol, cysteine hydrochloride, and α
-tocopherol, wherein the preparation is maintained at an alkalinity corresponding to a pH of not less than about 7.0. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
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10. A method for stabilizing therapeutic compositions that are adapted for treatment of menopausal syndrome, female hypogonadism, amenorrhea, female castration, primary ovarian failure, abnormal uterine bleeding due to hormonal imbalance, and senile vaginitis, and exhibiting no oxidation and less than about 5% hydrolysis for times greater up to at least 24 months, which compositions consist essentially of at least one alkali metal sulfate salt of a synthetic conjugated estrogen selected from the group consisting of estrone, equilin, 17α
- -dihydroequilin, 17β
-hydroequilin, 17β
-estradiol, 17α
-estradiol, equilinen, and 17β
-dihydroequilenin in estrogenically effective proportions, said method comprising;adding an antioxidant effective amount of at least one suitable antioxidant for said alkali metal sulfate salt of said synthetic confugated estrogen selected from the group consisting of sodium sulfite, potassium sulfite, sodium metabisulfite, potassium metabisulfite, sodium bisulfite, potassium bisulfite, sodium thiosulfate, potassium thiosulfate, thioglycerol, thiosorbitol, cysteine hydrochloride, and α
-tocopherol, wherein the preparation is maintained at an alkalinity corresponding to a pH of not less than about 7.0.
- -dihydroequilin, 17β
Specification