DE3341638A1 - Three-phase product for contraception composed of ethinylestradiol and lynestrenol - Google Patents
Three-phase product for contraception composed of ethinylestradiol and lynestrenolInfo
- Publication number
- DE3341638A1 DE3341638A1 DE19833341638 DE3341638A DE3341638A1 DE 3341638 A1 DE3341638 A1 DE 3341638A1 DE 19833341638 DE19833341638 DE 19833341638 DE 3341638 A DE3341638 A DE 3341638A DE 3341638 A1 DE3341638 A1 DE 3341638A1
- Authority
- DE
- Germany
- Prior art keywords
- lynestrenol
- ethinylestradiol
- days
- phase
- contraception
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- YNVGQYHLRCDXFQ-XGXHKTLJSA-N Lynestrenol Chemical compound C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 YNVGQYHLRCDXFQ-XGXHKTLJSA-N 0.000 title claims abstract description 11
- 229960001910 lynestrenol Drugs 0.000 title claims abstract description 11
- 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 title abstract description 11
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 title abstract description 10
- 229960002568 ethinylestradiol Drugs 0.000 title abstract description 10
- 239000003433 contraceptive agent Substances 0.000 claims abstract description 6
- 238000002360 preparation method Methods 0.000 claims description 11
- 239000000583 progesterone congener Substances 0.000 claims description 5
- 229940011871 estrogen Drugs 0.000 claims description 4
- 239000000262 estrogen Substances 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 2
- 230000002254 contraceptive effect Effects 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 4
- 239000006187 pill Substances 0.000 abstract description 4
- 150000003431 steroids Chemical class 0.000 abstract description 4
- 239000000203 mixture Substances 0.000 abstract description 3
- 230000004962 physiological condition Effects 0.000 abstract description 3
- 229940088597 hormone Drugs 0.000 abstract description 2
- 239000005556 hormone Substances 0.000 abstract description 2
- 230000000740 bleeding effect Effects 0.000 abstract 1
- 229960004400 levonorgestrel Drugs 0.000 description 5
- JFRPGRWPRUCLQL-TWYXDQSVSA-N (8r,9s,13s,14s,17r)-3-ethyl-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-17-ol;(8r,9s,10r,13s,14s,17r)-17-ethynyl-13-methyl-2,3,6,7,8,9,10,11,12,14,15,16-dodecahydro-1h-cyclopenta[a]phenanthren-17-ol Chemical compound C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.C1C[C@]2(C)[C@@](C#C)(O)CC[C@H]2[C@@H]2CCC3=CC(CC)=CC=C3[C@H]21 JFRPGRWPRUCLQL-TWYXDQSVSA-N 0.000 description 3
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 description 2
- ORKBYCQJWQBPFG-WOMZHKBXSA-N (8r,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 ORKBYCQJWQBPFG-WOMZHKBXSA-N 0.000 description 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 2
- 230000003054 hormonal effect Effects 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 230000009466 transformation Effects 0.000 description 2
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 206010006313 Breast tenderness Diseases 0.000 description 1
- 208000005189 Embolism Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 206010027514 Metrorrhagia Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 description 1
- 208000001435 Thromboembolism Diseases 0.000 description 1
- 208000021017 Weight Gain Diseases 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 231100000508 hormonal effect Toxicity 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 229960001652 norethindrone acetate Drugs 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
1) Bezeichnung der Erfindung Bin 3)reiphasen-Präparat zur Empfängnisverhüturg aus Ethinylöstradiol und Lynestrenol 2) Technisches Gebiet Hormonale Koiatrazeptiva.1) Description of the invention. Bin 3) three-phase preparation for contraception from ethinyl estradiol and lynestrenol 2) Technical field Hormonal Koiatraceptives.
Mit dem Verabreichungsmodus eines Dreiphasen- (Dreistufen-) Kontrazeptivums werden physiologische Verhältnisse naehgeahmt 3) Stand der Technik Im Juni 1961 wurde in der BR1) das erste Pillenpräparat Anovlar zur Empfängnisverhütung eingeführt. Im Laufe der folgenden Jahre stellte sich heraus, daß die anfänglich sehr hohe Dosierung ( 50 Mikrogramm Ethinylöstradiol 4 mg Norethisteronacetat ) für den gewünschten Effekt nicht erforderlich war. Also ging die Entwicklung dahin, die Dosen beider Komponenten der Pille zu vermindern, um Nebenwirkungen zu reduzieren und die Verträglichkeit zu steigern. Heute geht es darum, eine Kombination zu finden, die den Stoffwechsel nur minimal tangiert und eine gute Zyklusstabilität gewährleistet. Die in den letzten Jahren entwickelten Zweiphasen- bzw. Dreiphasenpräparate kommen diesen Forderungen weitgehend entgegen. With the mode of administration of a three-phase (three-stage) contraceptive physiological conditions are mimicked 3) State of the art In June 1961 the first pill preparation Anovlar for contraception was introduced in the BR1). In the course of the following years it turned out that the initially very high dosage (50 micrograms ethinyl estradiol 4 mg norethisterone acetate) for the desired Effect was not required. So the development went there, the doses of both Decrease components of the pill in order to reduce side effects and improve tolerability to increase. Today it's about finding a combination that will boost your metabolism only minimally affected and good cycle stability guaranteed. The ones in the last Years of developed two-phase or three-phase preparations meet these requirements largely contrary.
Marktführer Ovanon (Fa. Nourypharma - München ) - Zweiphasenpräparat (Ethinylöstradiol, Lynestrenol ) - (istrogen Gesamtdosis pro Zyklus 1,10 mg (22 Tbl.) - Gestagen Gesamtdosis pro Zyklus 37.5 mg (22 Tbl.) Kritik - herkömmliche Zweiphasenpräparate sind in der Verordnung häufig schon Mittel der zweiten Wahl - Steroid Gesamtdosis pro Zyklus könnte noch merklich reduziert werden - Verträglichkeit und Zyklusstabilität ließen sich noch steigern Dreistufenpräparat Triquilar (Fa. Schering - Berlin) - erates dreistufenpräparat - Kombinationspräparat aus Ethinylöstradiol und evo -norgestrel Zusammensetzung 6 Tage 30 ug Ethinylöstradiol + 0.050 mg Levonorgestrel 5 Tage 40 ug " + 0.075 mg 10 Tage 30 ug * + 0.125 mg Kritik - Transformationsdisis beträgt für d - Norgestrel 6 mg ( für Lynestrenol 150 mg ) - d Norgestrel ist somit eine potente Substanz es besitzt eine hormonelle Restwirkung; dies führt im Einzelfall zu: a) Gewischtszunahmen b) Ausfall des Kopfhaares o) vermehrte Behaarung im Gesicht, an Armen und Beinen d) Akne e) senkt HDL Spiegel (Schutz gegen Arteriosklerose) 4) Welche Aufgabe soll gelöst werden? Es sollte eine physiologische und Zyklue-gerechte Wirkstoffkombination aus einem synthetischen Östrogen und einem wenig potenten Gestagen gefunden werden. Die Steroid Gesamtdosis pro Zyklus sollte merklich reduziert werden. Market leader Ovanon (Nourypharma - Munich) - two-phase preparation (Ethinyl estradiol, lynestrenol) - (total istrogenic dose per cycle 1.10 mg (22 Tablets) - total progestin dose per cycle 37.5 mg (22 tablets) criticism - Conventional two-phase preparations are often already means of the prescription second choice - total steroid dose per cycle could still be reduced noticeably - Tolerance and cycle stability could be increased three-step preparation Triquilar (Schering - Berlin) - erates three-step preparation - combination preparation from ethinyl estradiol and evo-norgestrel composition, 30 ug ethinyl estradiol for 6 days + 0.050 mg levonorgestrel 5 days 40 ug "+ 0.075 mg 10 days 30 ug * + 0.125 mg review - Transformation disis for d - norgestrel is 6 mg (for lynestrenol 150 mg ) - d Norgestrel is therefore a potent substance; it has a residual hormonal effect; in individual cases this leads to: a) increased weight b) loss of scalp hair o) increased Hair on the face, arms and legs d) Acne e) lowers HDL levels (protection against Arteriosclerosis) 4) Which task should be solved? It should a physiological and cycle-appropriate combination of active ingredients from a synthetic one Estrogen and a little potent progestin can be found. The total steroid dose per cycle should be reduced noticeably.
5) Dreiphasen - Präparat nach Dr. H.Heßlinger Zusammensetzung:
Claims (2)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19833341638 DE3341638A1 (en) | 1983-11-17 | 1983-11-17 | Three-phase product for contraception composed of ethinylestradiol and lynestrenol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19833341638 DE3341638A1 (en) | 1983-11-17 | 1983-11-17 | Three-phase product for contraception composed of ethinylestradiol and lynestrenol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE3341638A1 true DE3341638A1 (en) | 1984-05-03 |
Family
ID=6214592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19833341638 Ceased DE3341638A1 (en) | 1983-11-17 | 1983-11-17 | Three-phase product for contraception composed of ethinylestradiol and lynestrenol |
Country Status (1)
| Country | Link |
|---|---|
| DE (1) | DE3341638A1 (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0148724A1 (en) * | 1983-12-22 | 1985-07-17 | Schering Aktiengesellschaft | Sequential combined multiphase preparation and its use for oral contraception |
| US6660726B2 (en) | 2000-03-10 | 2003-12-09 | Endeavor Pharmaceuticals | Estrogenic compounds, pharmaceutical compositions thereof, and methods of using same |
| US6855703B1 (en) | 2000-03-10 | 2005-02-15 | Endeavor Pharmaceuticals | Pharmaceutical compositions of conjugated estrogens and methods of analyzing mixtures containing estrogenic compounds |
| US7459445B2 (en) | 2000-03-10 | 2008-12-02 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds and topical pharmaceutical formulations of the same |
| US7989436B2 (en) | 2003-07-23 | 2011-08-02 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds and pharmaceutical formulations comprising the same |
| US8071577B2 (en) | 2004-04-20 | 2011-12-06 | Bayer Pharma Aktiengesellschaft | Multi-phase contraceptive preparation based on a natural estrogen |
| US8153616B2 (en) | 2005-10-17 | 2012-04-10 | Bayer Pharma Aktiengesellschaft | Combination preparation for oral contraception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same |
| US8349820B2 (en) | 2006-10-20 | 2013-01-08 | Bayer Pharma Aktiengesellschaft | Use of estradiol valerate or 17β-estradiol in combination with dienogest for oral therapy to maintain and/or increase feminine libido |
-
1983
- 1983-11-17 DE DE19833341638 patent/DE3341638A1/en not_active Ceased
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0148724A1 (en) * | 1983-12-22 | 1985-07-17 | Schering Aktiengesellschaft | Sequential combined multiphase preparation and its use for oral contraception |
| US6660726B2 (en) | 2000-03-10 | 2003-12-09 | Endeavor Pharmaceuticals | Estrogenic compounds, pharmaceutical compositions thereof, and methods of using same |
| US6844334B2 (en) | 2000-03-10 | 2005-01-18 | Endeavor Pharmaceuticals | (3) and (6) substitued estrogenic compounds |
| US6855703B1 (en) | 2000-03-10 | 2005-02-15 | Endeavor Pharmaceuticals | Pharmaceutical compositions of conjugated estrogens and methods of analyzing mixtures containing estrogenic compounds |
| US7179799B2 (en) | 2000-03-10 | 2007-02-20 | Barr Laboratories, Inc. | (3) and (6) substituted estrogenic compounds |
| US7459445B2 (en) | 2000-03-10 | 2008-12-02 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds and topical pharmaceutical formulations of the same |
| US7749989B2 (en) | 2000-03-10 | 2010-07-06 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds, methods of using and methods of administering the same |
| US8227454B2 (en) | 2000-03-10 | 2012-07-24 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds, pharmaceutical compositions and formulations comprising the same |
| US7989436B2 (en) | 2003-07-23 | 2011-08-02 | Duramed Pharmaceuticals, Inc. | Estrogenic compounds and pharmaceutical formulations comprising the same |
| US8071577B2 (en) | 2004-04-20 | 2011-12-06 | Bayer Pharma Aktiengesellschaft | Multi-phase contraceptive preparation based on a natural estrogen |
| US8153616B2 (en) | 2005-10-17 | 2012-04-10 | Bayer Pharma Aktiengesellschaft | Combination preparation for oral contraception and oral therapy of dysfunctional uterine bleeding containing estradiol valerate and dienogest and method of using same |
| US8349820B2 (en) | 2006-10-20 | 2013-01-08 | Bayer Pharma Aktiengesellschaft | Use of estradiol valerate or 17β-estradiol in combination with dienogest for oral therapy to maintain and/or increase feminine libido |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| OAV | Applicant agreed to the publication of the unexamined application as to paragraph 31 lit. 2 z1 | ||
| OP8 | Request for examination as to paragraph 44 patent law | ||
| 8131 | Rejection |