DE3341638A1 - Three-phase product for contraception composed of ethinylestradiol and lynestrenol - Google Patents

Three-phase product for contraception composed of ethinylestradiol and lynestrenol

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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
Application number
DE19833341638
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German (de)
Inventor
Hermann Dr.rer.nat. 8000 München Heßlinger
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Individual
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Individual
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Publication date
Application filed by Individual filed Critical Individual
Priority to DE19833341638 priority Critical patent/DE3341638A1/en
Publication of DE3341638A1 publication Critical patent/DE3341638A1/en
Ceased legal-status Critical Current

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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

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  • 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

The mode of administration of a three-phase contraceptive of this type ideally simulates physiological conditions. The marked reduction in the total steroid dose per cycle ensures a low risk of side effects and thus makes the "pill" even better tolerated. Despite low hormone doses, a stable sequence of cycles is set up (less intracyclic bleeding). Three-phase contraceptive according to Dr. H. Hesslinger Composition: 6 days 30 mu g ethinylestradiol + 0.75 mg lynestrenol 5 days 40 mu g ethinylestradiol + 1.0 mg lynestrenol 11 days 30 mu g ethinylestradiol + 1.5 mg lynestrenol

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: 6 Tage 30 µg Ethinylöstradiol 0.75 mg Lynestrenol 5 Tage 40 µg " 1.0 mg " 11 Tage 30 µg " 1.5 mg " 6) Vorteilhafte Wirkungen (Bezugnahme auf den bisherigen Stand der Technik ) - erstes Dreiphasen-Kontrazeptivum mit Lynestrenol - Transformationsdosis für Lynestrenol 150 ing (d-Norgestrel in Triquilar 6 mg) - Steroid Gesamtdosis pro Zyklus deutlich reduziert 0.68 mg Ostrogen / 26 mg Gestagen ( Ovanon: 1.10 mg Östrogen / 37.5 mg gestagen ) - die Pille wird somit noch verträglicher ( also ein noch geringeres Risiko für; Übelkeit, Kopfschmerzen, Brustspannen, Thromboembolien Gewichtszunahmen, Depressionen) - trotz geringer Hormongaben ein stabiler Zyklusablauf ( weniger Zwischenblutungen ) - mit dem Verabreichungsmodus eines Dreiphasen-Kontrazeptivums werden physiologische Verhältnisse ideal nachgeahmt (Vorteil gegenüber einem Zweistufenpräparatwie Ovanon )5) Three-phase preparation according to Dr. H. Heßlinger Composition: 6 days 30 µg ethinyl estradiol 0.75 mg lynestrenol 5 days 40 µg "1.0 mg" 11 days 30 µg "1.5 mg" 6) Advantageous effects (referring to the prior art) - first three-phase contraceptive with lynestrenol - transformation dose for lynestrenol 150 ing (d-norgestrel in triquilar 6 mg) - total steroid dose per cycle significantly reduced 0.68 mg estrogen / 26 mg gestagen ( Ovanon: 1.10 mg estrogen / 37.5 mg gestagen) - the pill is therefore even more tolerable (i.e. an even lower risk of; nausea, headache, breast tenderness, thromboembolism, weight gain, depression) - despite the small dose of hormones, a stable cycle (less intermenstrual bleeding) - with the Administration mode of a three-phase contraceptive ideally mimics physiological conditions (advantage over a two-stage preparation such as Ovanon)

Claims (2)

Patentansprüche (# 35 Abs.1 Satz 3 Nr. Patent claims (# 35, Paragraph 1, Sentence 3, No. 2 PatG) Oberbegriff Ovulationshemmer - ein Dreiphasen-Präparat mit dem Gestagen Lynestrenol Kennzeichnender Teil optimale Zyklus - gerechte Wirkstoffkombination aus einem synthetischen östrogen und einem Ges tagen2 PatG) generic term ovulation inhibitor - a three-phase preparation with the gestagen lynestrenol characterizing part optimal Cycle-appropriate combination of active ingredients from a synthetic estrogen and a Days
DE19833341638 1983-11-17 1983-11-17 Three-phase product for contraception composed of ethinylestradiol and lynestrenol Ceased DE3341638A1 (en)

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

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DE19833341638 Ceased DE3341638A1 (en) 1983-11-17 1983-11-17 Three-phase product for contraception composed of ethinylestradiol and lynestrenol

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DE (1) DE3341638A1 (en)

Cited By (8)

* Cited by examiner, † Cited by third party
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

Cited By (12)

* Cited by examiner, † Cited by third party
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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