CO5200771A1 - A PHARMACEUTICAL COMPOSITION TO BE USED AS AN CONTRACEPTIVE AGENT - Google Patents
A PHARMACEUTICAL COMPOSITION TO BE USED AS AN CONTRACEPTIVE AGENTInfo
- Publication number
- CO5200771A1 CO5200771A1 CO00065489A CO00065489A CO5200771A1 CO 5200771 A1 CO5200771 A1 CO 5200771A1 CO 00065489 A CO00065489 A CO 00065489A CO 00065489 A CO00065489 A CO 00065489A CO 5200771 A1 CO5200771 A1 CO 5200771A1
- Authority
- CO
- Colombia
- Prior art keywords
- amount
- drospirenone
- dosage units
- daily dosage
- mammal
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000003433 contraceptive agent Substances 0.000 title 1
- 229940124558 contraceptive agent Drugs 0.000 title 1
- METQSPRSQINEEU-UHFFFAOYSA-N dihydrospirorenone Natural products CC12CCC(C3(CCC(=O)C=C3C3CC33)C)C3C1C1CC1C21CCC(=O)O1 METQSPRSQINEEU-UHFFFAOYSA-N 0.000 abstract 7
- METQSPRSQINEEU-HXCATZOESA-N drospirenone Chemical compound C([C@]12[C@H]3C[C@H]3[C@H]3[C@H]4[C@@H]([C@]5(CCC(=O)C=C5[C@@H]5C[C@@H]54)C)CC[C@@]31C)CC(=O)O2 METQSPRSQINEEU-HXCATZOESA-N 0.000 abstract 7
- 229960004845 drospirenone Drugs 0.000 abstract 7
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 abstract 6
- 229960002568 ethinylestradiol Drugs 0.000 abstract 5
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 abstract 4
- 241000124008 Mammalia Species 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 239000013543 active substance Substances 0.000 abstract 2
- 238000004090 dissolution Methods 0.000 abstract 2
- 239000002552 dosage form Substances 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 230000016087 ovulation Effects 0.000 abstract 2
- 238000004806 packaging method and process Methods 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000002245 particle Substances 0.000 abstract 1
- 230000001737 promoting effect Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
Landscapes
- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Una composición farmacéutica, caracterizada por comprender, como un primer agente activo, 6b, 7b; 15b, 16b-dimetilen-3-oxo-17a-pregn-4-en-21, 17 -carbolactona (drospirenona) en una cantidad correspondiente a una dosis diaria, a ser administrada con la composición, de desde aproximadamente 2 mg a aproximadamente 4 mg, y, como un segundo agente activo, 17a-etinilestradiol (etinilestradiol) en una cantidad correspondiente a una dosis diaria de desde aproximadamente 0,01 mg a aproximadamente 0,05 mg, conjuntamente con uno o más soportes o excipientes farmacéuticamente aceptables.Una preparación farmacéutica, caracterizada por consistir de un número de unidades de dosificación diaria colocadas en una unidad de empaque, empaquetadas separadamente y separables individualmente, y provistas para la administración oral durante un periodo de 21 días consecutivos, comprendiendo dichas unidades de dosificación diaria una combinación de drospirenona en una cantidad de desde aproximadamente 2 mg a aproximadamente 4 mg y etinilestradiol en una cantidad de desde aproximadamente 0,01 a aproximadamente 0,05 mg.Una preparación farmacéutica caracterizada por consistir de un número de unidades de dosificación diaria colocadas en una unidad de empaque, empaquetadas separadamente y separables individualmente y provistas para la administración oral durante un período de al menos 28 días consecutivos, en donde al menos 21 de dichas unidades de dosificación diaria comprenden una combinación da drospirenona en una cantidad de desde aproximadamente 2 mg a aproximadamente 4 mg y etinilestradiol en una cantidad de desde aproximadamente 0,01 a aproximadamente 0,05 mg, y en donde 7 ó menos de dichas unidades de dosificación diaria contienen sólo etinilestradiol en una cantidad de desde aproximadamente 0,01 a aproximadamente 0,05 mg.Un método para inhibir ovulación en un mamífero, en particular en un humano, caracterizado por comprender administrar, a dicho mamífero, drospirenona en una cantidad en la gama de desde aproximadamente 2 mg a aproximadamente 4 mg por día, conjuntamente con etinilestradiol en una cantidad de desde aproximadamente 0,01 mg a aproximadamente 0,05 mg por día, siendo dichas cantidades efectivas para inhibir ovulación en dicho mamífero.Un método para promover una disolución rápida de drospirenona de una forma de dosificación unitaria para administración oral, estando el método caracterizado por comprender proveer drospirenona, en dicha forma de dosificación unitaria, en forma micronizada, o pulverizada desde una solución sobre las partículas de un soporte inerte mezclado con uno o más excipientes farmacéuticamente aceptables que promueven la disolución de la drospirenona.A pharmaceutical composition, characterized by comprising, as a first active agent, 6b, 7b; 15b, 16b-dimethylene-3-oxo-17a-pregn-4-en-21, 17 -carbolactone (drospirenone) in an amount corresponding to a daily dose, to be administered with the composition, from about 2 mg to about 4 mg, and, as a second active agent, 17a-ethynyl estradiol (ethynyl estradiol) in an amount corresponding to a daily dose of from about 0.01 mg to about 0.05 mg, together with one or more pharmaceutically acceptable carriers or excipients. pharmaceutical preparation, characterized in that it consists of a number of daily dosage units placed in a packaging unit, packaged separately and individually separable, and provided for oral administration for a period of 21 consecutive days, said daily dosage units comprising a combination of drospirenone in an amount from about 2 mg to about 4 mg and ethinyl estradiol in an amount from about 0.01 to ap approximately 0.05 mg. A pharmaceutical preparation characterized by consisting of a number of daily dosage units placed in a packaging unit, packaged separately and individually separable and provided for oral administration for a period of at least 28 consecutive days, wherein at least 21 of said daily dosage units comprise a combination of drospirenone in an amount of from about 2 mg to about 4 mg and ethinyl estradiol in an amount of from about 0.01 to about 0.05 mg, and wherein 7 or less of said daily dosage units contain only ethinylestradiol in an amount of from about 0.01 to about 0.05 mg. A method for inhibiting ovulation in a mammal, in particular in a human, characterized by comprising administering, to said mammal, drospirenone. in an amount in the range of from about 2 mg to about 4 mg per day, together with ethinyl estradiol in an amount of from about 0.01 mg to about 0.05 mg per day, said amounts being effective in inhibiting ovulation in said mammal, a method of promoting a rapid dissolution of drospirenone from a unit dosage form for administration. orally, the method being characterized by comprising providing drospirenone, in said unit dosage form, in micronized form, or sprayed from a solution on the particles of an inert support mixed with one or more pharmaceutically acceptable excipients that promote the dissolution of drospirenone.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99202826 | 1999-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5200771A1 true CO5200771A1 (en) | 2002-09-27 |
Family
ID=8240592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO00065489A CO5200771A1 (en) | 1999-08-31 | 2000-08-31 | A PHARMACEUTICAL COMPOSITION TO BE USED AS AN CONTRACEPTIVE AGENT |
Country Status (6)
| Country | Link |
|---|---|
| CN (1) | CN1879632A (en) |
| AR (2) | AR025443A1 (en) |
| CO (1) | CO5200771A1 (en) |
| EC (1) | ECSP003721A (en) |
| PE (1) | PE20010665A1 (en) |
| ZA (2) | ZA200201668B (en) |
-
2000
- 2000-08-30 AR ARP000104515A patent/AR025443A1/en not_active Application Discontinuation
- 2000-08-31 PE PE2000000895A patent/PE20010665A1/en not_active IP Right Cessation
- 2000-08-31 CO CO00065489A patent/CO5200771A1/en not_active Application Discontinuation
- 2000-08-31 CN CNA2005100992135A patent/CN1879632A/en active Pending
- 2000-10-18 EC EC2000003721A patent/ECSP003721A/en unknown
-
2002
- 2002-02-27 ZA ZA200201668A patent/ZA200201668B/en unknown
-
2004
- 2004-03-05 AR ARP040100696A patent/AR043470A2/en not_active Application Discontinuation
-
2005
- 2005-05-25 ZA ZA200404083A patent/ZA200404083B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AR025443A1 (en) | 2002-11-27 |
| ZA200201668B (en) | 2004-06-24 |
| ECSP003721A (en) | 2002-05-23 |
| AR043470A2 (en) | 2005-07-27 |
| PE20010665A1 (en) | 2001-06-19 |
| CN1879632A (en) | 2006-12-20 |
| ZA200404083B (en) | 2006-02-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |