Patent US3050661A successfully refreshed from Google Patents.
US4900734A
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Novel pharmaceutical composition containing estradiol and progesterone for oral administration
Assignee: Individual
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Filing: 1987-08-27
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Granted: 1990-02-13
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Expires: 2007-08-27
Abstract
Abstract A pharmaceutical composition is provided for oral administration. The composition comprises estradiol dissolved in an oil vehicle containing a suspension of micronized progesterone. The oil vehicle is high in glycerides of polyunsaturated fatty acids. The estradiol and micronized progesterone contained in the oil are more readily absorbable in the blood stream and achieve enhanced estradiol and progesterone blood serum levels. The pharmaceutical composition according to the invention can be readily formulated into capsules and administered for the treatment of menopausal symptoms.
Inventors
- 👤 Wayne S. Maxson
- 👤 Joel T. Hargrove
- 👤 Joe H. Delk
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 19:04
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K31/00; A61K31/56; A61K31/57; A61K9/00; A61K9/48; A61K9/4841; A61K9/4858
Claims Analysis
Total Claims: 40
Claim 1
Independent Claim
83 words
A pharmaceutical composition for treating menopausal symptoms in women which comprises estradiol dissolved in a highly unsaturated edible oil containing a suspension of micronized progesterone particles; said oil comprising glycerides of one or more polyunsaturated fatty acids; said estradiol and progesterone being present in a therapeutically effective amount for treating menopause; and said estradiol and progesterone being present in an amount so that the composition can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 2
Dependent Claim
83 words
A pharmaceutical composition for treating menopausal symptoms in women which comprises estradiol dissolved in a highly unsaturated edible oil containing a suspension of micronized progesterone particles; said oil comprising glycerides of one or more polyunsaturated fatty acids; said estradiol and progesterone being present in a therapeutically effective amount for treating menopause; and said estradiol and progesterone being present in an amount so that the composition can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 3
Dependent Claim
18 words
The composition of claim 1, wherein at least 51% of the glycerides are glycerides of polyunsaturated fatty acids.
Claim 4
Dependent Claim
73 words
The composition of claim 2, wherein said oil has an acid value in the range of 0.4-10, a saponification value in the range of 186-194, an iodine value in the range of 130-150, a thiocyanogen value in the range of 82-87, a R-M value of less than 0.5, an hydroxyl value in the range of 1-12, an unsaponifiable content of less than 1.5 wt.%, and a specific gravity in the range of 0.919-0.924.
Claim 5
Dependent Claim
28 words
The pharmaceutical composition of claim 1, wherein the oil consists essentially of glycerides having 5-10 wt.% saturated fatty acids; 13-22 wt.% oleic acid, and 72-79 wt.% linoleic acid.
Claim 6
Dependent Claim
28 words
The composition of claim 1, wherein the oil is selected from the group consisting of safflower oil, linseed oil, soybean oil, corn oil, sunflower oil, and mixtures thereof.
Claim 7
Dependent Claim
11 words
The composition of claim 4, wherein the oil is safflower oil.
Claim 8
Dependent Claim
123 words
A pharmaceutical composition which comprises estradiol dissolved in a edible glyceride oil and micronized progesterone particles suspended in the oil; said oil having an iodine value of at least 110 and comprising glycerides of one or more polyunsaturated fatty acids; and said progesterone particles being of a particle size wherein at least 99% of the particles are less than 10 microns in diameter and at least 78% of the particles are less than 5 microns in diameter; said estradiol and progesterone being present in a therapeutically effective amount for treating menopause; and said estradiol and progesterone being present in an amount so that the composition can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 9
Dependent Claim
123 words
A pharmaceutical composition which comprises estradiol dissolved in a edible glyceride oil and micronized progesterone particles suspended in the oil; said oil having an iodine value of at least 110 and comprising glycerides of one or more polyunsaturated fatty acids; and said progesterone particles being of a particle size wherein at least 99% of the particles are less than 10 microns in diameter and at least 78% of the particles are less than 5 microns in diameter; said estradiol and progesterone being present in a therapeutically effective amount for treating menopause; and said estradiol and progesterone being present in an amount so that the composition can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 10
Dependent Claim
14 words
The composition of claim 7, wherein the oil has an iodine value of 130-160.
Claim 11
Dependent Claim
14 words
The composition of claim 8, wherein the oil has an iodine value of 140-150.
Claim 12
Dependent Claim
73 words
The composition of claim 7, wherein the oil has an acid value in the range of 0.4-10, a saponification value in the range of 186-194, an iodone value in the range of 130-150, a thiocyanogen value in the range of 82-87, and R-M value of less than 0.5, a hydroxyl value in the range of 1-12, an unsaponifiable content of less than 1.5 wt.%, and a specific gravity in the range of 0.919-0.924.
Claim 13
Dependent Claim
26 words
The composition of claim 7, wherein the oil consists of glycerides having 5-10 wt.% saturated fatty acids; 13-22 wt.% oleic acid, and 72-79 wt.% linoleic acid.
Claim 14
Dependent Claim
28 words
The composition of claim 7, wherein the oil is selected from the group consisting of safflower oil, linseed oil, soybean oil, corn oil, sunflower oil, and mixtures thereof.
Claim 15
Dependent Claim
11 words
The composition of claim 12, wherein the oil is safflower oil.
Claim 16
Dependent Claim
88 words
A capsule for oral administration of estradiol and progesterone which comprises a pharmaceutically acceptable capsule containing estradiol dissolved in a highly unsaturated edible oil containing a suspension of micronized progesterone particles therein; said oil comprising glycerides of one or more polyunsaturated acids; said capsule containing estradiol and progesterone in a therapeutically effective amount for treating menopause; and said capsule containing estradiol and progesterone in an amount so that the capsules can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 17
Dependent Claim
88 words
A capsule for oral administration of estradiol and progesterone which comprises a pharmaceutically acceptable capsule containing estradiol dissolved in a highly unsaturated edible oil containing a suspension of micronized progesterone particles therein; said oil comprising glycerides of one or more polyunsaturated acids; said capsule containing estradiol and progesterone in a therapeutically effective amount for treating menopause; and said capsule containing estradiol and progesterone in an amount so that the capsules can be orally administered to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 18
Dependent Claim
16 words
The capsule of claim 14, wherein the oil has an iodine value of at least 110.
Claim 19
Dependent Claim
40 words
The capsule of claim 15, wherein the progesterone particles are of a particle size wherein 99% of the particles are less than 10 microns in diameter and at least 78% of the particles are less than 5 microns in diameter.
Claim 20
Dependent Claim
28 words
The capsule of claim 16, wherein the oil is selected from the group consisting of safflower oil, linseed oil, soybean oil, corn oil, sunflower oil, and mixtures thereof.
Claim 21
Dependent Claim
11 words
The capsule of claim 17, wherein the oil is safflower oil.
Claim 22
Dependent Claim
14 words
The capsule of claim 14, which contains 0.2-0.5 mg. estradiol and 50-100 mg. progesterone.
Claim 23
Dependent Claim
14 words
The capsule of claim 14, which contains 0.2-0.5 mg. estradiol and 50-100 mg. progesterone.
Claim 24
Dependent Claim
14 words
The capsule of claim 19, which contains 0.35 mg. estradiol and 100 mg. progesterone.
Claim 25
Independent Claim
91 words
A method for treating menopausal symptoms in women which comprises orally administering to a woman suffering from menopausal symptoms a therapeutically effective amount of a pharmaceutical composition which comprises estradiol dissolved in a highly unsaturated oil containing a suspension of micronized progesterone particles; said oil comprising glycerides of one or more polyunsaturated fatty acids; said composition containing estradiol and progesterone in a therapeutically effective amount for treating menopause; and said composition being orally administered in an amount to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 26
Independent Claim
91 words
A method for treating menopausal symptoms in women which comprises orally administering to a woman suffering from menopausal symptoms a therapeutically effective amount of a pharmaceutical composition which comprises estradiol dissolved in a highly unsaturated oil containing a suspension of micronized progesterone particles; said oil comprising glycerides of one or more polyunsaturated fatty acids; said composition containing estradiol and progesterone in a therapeutically effective amount for treating menopause; and said composition being orally administered in an amount to provide a daily dosage rate of 0.9-1.2 mg. estradiol and 150-300 mg. progesterone.
Claim 27
Dependent Claim
40 words
The method of claim 21, wherein the progesterone particles are of a particle size wherein 99% of the particles are less than 10 microns in diameter and at least 78% of the particles are less than 5 microns in diameter.
Claim 28
Dependent Claim
14 words
The method of claim 23, wherein the composition is contained in a digestible capsule.
Claim 29
Dependent Claim
25 words
The method of claim 23, wherein the daily dosage rate is adminstered in the form of capsules containing 0.2-0.5 mg. estradiol and 50-100 mg. progesterone.
Claim 30
Dependent Claim
28 words
The capsule of claim 25, wherein the oil is selected from the group consisting of safflower oil, linseed oil, soybean oil, corn oil, sunflower oil, and mixtures thereof.
Claim 31
Dependent Claim
16 words
The method of claim 26, wherein the capsule contains 0.35 mg. estradiol and 100 mg. progesterone.
Claim 32
Dependent Claim
11 words
The method of claim 27, wherein the oil is safflower oil.
Claim 33
Independent Claim
45 words
The method of increasing blood serum estradiol and progesterone levels in humans which comprises orally administering to humans to composition comprising estradiol dissolved in an edible oil containing a suspension of micronized progesterone particles, said oil comprising glycerides of one or more polyunsaturated fatty acids.
Claim 34
Independent Claim
45 words
The method of increasing blood serum estradiol and progesterone levels in humans which comprises orally administering to humans to composition comprising estradiol dissolved in an edible oil containing a suspension of micronized progesterone particles, said oil comprising glycerides of one or more polyunsaturated fatty acids.
Claim 35
Dependent Claim
51 words
The method of claim 29, wherein the oil has an iodine value of at least 110 and the progesterone particles are of a particle size wherein 99% of the particles are less than 10 microns in diameter and at least 78% of the particles are less than 5 microns in diameter.
Claim 36
Dependent Claim
28 words
The method of claim 30, wherein the oil is selected from the group consisting of safflower oil, linseed oil, soybean oil, corn oil, sunflower oil, and mixtures thereof.
Claim 37
Dependent Claim
25 words
The method of claim 31, wherein the oil is safflower oil and the estradiol, progesterone and oil containing composition is contained in a digestible capsule.
Claim 38
Independent Claim
81 words
A method for preparing an orally active pharmaceutical composition comprising estradiol, progesterone and a glyceride oil of one or more polyunsaturated acids, which method comprises the steps of: heating a quantity of the oil; dissolving a quantity of estradiol in the oil to form a solution; cooling the solution to room temperature; stirring and mixing micronized progesterone into the solution, whereby a composition is formed containing estradiol dissolved in the oil which contains suspended micronized particles of progesterone and solubilized progesterone.
Claim 39
Independent Claim
81 words
A method for preparing an orally active pharmaceutical composition comprising estradiol, progesterone and a glyceride oil of one or more polyunsaturated acids, which method comprises the steps of: heating a quantity of the oil; dissolving a quantity of estradiol in the oil to form a solution; cooling the solution to room temperature; stirring and mixing micronized progesterone into the solution, whereby a composition is formed containing estradiol dissolved in the oil which contains suspended micronized particles of progesterone and solubilized progesterone.
Claim 40
Dependent Claim
20 words
The method of claim 33, wherein the mixture formed in claim 33 is further diluted with additional quantities of oil.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1993-02-12 | 1993-08-14 | 1994-02-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-02-12 | 1997-08-14 | 1998-02-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-02-12 | 2001-08-14 | 2002-02-13 | $7700.00 | Window Closed / Lapsed |