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US20040243606A1 - Hormonal contraceptive product - Google Patents

Hormonal contraceptive product Download PDF

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Publication number
US20040243606A1
US20040243606A1 US10/867,954 US86795404A US2004243606A1 US 20040243606 A1 US20040243606 A1 US 20040243606A1 US 86795404 A US86795404 A US 86795404A US 2004243606 A1 US2004243606 A1 US 2004243606A1
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United States
Prior art keywords
estrogen
product
hormonal
administration
ethinyl estradiol
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.)
Abandoned
Application number
US10/867,954
Inventor
Rolf-Dieter Hesch
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Wyeth LLC
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Wyeth Pharmaceuticals Inc
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Filing date
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Application filed by Wyeth Pharmaceuticals Inc filed Critical Wyeth Pharmaceuticals Inc
Priority to US10/867,954 priority Critical patent/US20040243606A1/en
Publication of US20040243606A1 publication Critical patent/US20040243606A1/en
Assigned to WYETH reassignment WYETH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: HESCH, PROFESSOR DR. ROLF-DIETER
Assigned to WYETH LLC reassignment WYETH LLC CHANGE OF NAME (SEE DOCUMENT FOR DETAILS). Assignors: WYETH
Abandoned legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones

Definitions

  • the present invention relates to a hormonal contraceptive product with two hormonal components, the use thereof and a hormonal contraception process.
  • the desired cycle time is 28 days
  • administration takes place over 21 days in a constant or varying absolute and/or relative dosage of a combination of an estrogen product and a gestagen product, in which the estrogen product can e.g. be natural estrogen or synthetic ethinyl estradiol and the taking of the aforementioned 21 daily units is followed by a seven-day interval where there is a withdrawal bleeding simulating natural menstruation.
  • the estrogen product can e.g. be natural estrogen or synthetic ethinyl estradiol and the taking of the aforementioned 21 daily units is followed by a seven-day interval where there is a withdrawal bleeding simulating natural menstruation.
  • the sequential products used in substitution therapy are in particular unsuitable for contraception because the natural estradiol does not prevent ovulation in the dosage administered and the phase in which gestagen is administered is too short, being only 11 days.
  • the above-described sequential system guarantees a relatively good cycle control.
  • German patent 43 08 406 discloses a combination contraceptive product, which comprises one or more stages. At least one stage contains the combination of three components, namely a biogenous estrogen, a synthetic estrogen and a gestagen and the further stages in each case comprise a pharmaceutically unobjectionable placebo or a biogenous or synthetic gestagen, or a biogenous or synthetic estrogen, or a combination of two components, namely a biogenous estrogen, a synthetic estrogen and a gestagen or a combination of synthetic estrogen and a gestagen.
  • the problem of the invention is to provide a hormonal contraceptive product, which ensures high contraceptive safety or reliability and prevents intermenstrual bleeding. There is also to be a further reduction in the side effects otherwise observed in hormonal contraceptive products.
  • a hormonal contraceptive product having two hormonal components, the agent comprising for continuous, combined administration a first hormonal component comprising at least one gestagen and a second hormonal component comprising at least one estrogen.
  • a hormonal contraception process in which a product, which comprises at least one first hormonal component, which comprises at least one gestagen, and a second hormonal component comprising at least one estrogen is continuously administered.
  • the product according to the invention is used for inhibiting ovulation.
  • the product according to the invention is used for the treatment and/or prophylaxis of breast tumours.
  • gestagen as the first hormonal component is chosen from the group comprising progesterone, chlormadinone acetate, norethisterone acetate, cyproterone acetate, desogestrel, levonorgestrel, other natural and/or synthetic gestagens, antigestagens and hormonal analogs with gestagen or antigestagen action, as well as hormonal compounds which rapidly split off at least one gestagen following taking.
  • the estrogen as the second hormonal component can be selected from the group comprising synthetic estrogens, biogenous estrogens, antiestrogens and hormonal analogs with estrogen or antiestrogen action.
  • the synthetic estrogen is selected from the group comprising ethinyl estradiol, mestranol and the like, as well as hormonal compounds rapidly splitting off at least one synthetic estrogen following taking.
  • the synthetic estrogen is ethinyl estradiol.
  • the daily administered ethinyl estradiol quantity is 1 to 20 ⁇ g. In particularly preferred manner, the daily administered ethinyl estradiol quantity is 5 to 10 ⁇ g.
  • the biogenous estrogen is selected from the group comprising estradiol, estriol, estrone, estrane, etc., as well as hormonal compounds rapidly splitting off at least one biogenous estrogen after taking.
  • the estradiol comprises 17- ⁇ -estradiol and/or 17- ⁇ -estradiol.
  • the daily administered biogenous estrogen quantity in the case of estradiol, particularly ⁇ and ⁇ -estradiol, is 0.1 to 2 mg and in the case of conjugate estrogens 0.05 to 0.5 mg.
  • the product according to the invention can be administered orally.
  • the product according to the invention can be administered transdermally.
  • the product according to the invention can be administered intravaginally.
  • the product according to the invention can be in depot injection form.
  • the product according to the invention can be administered as a hormonal implant.
  • the daily units in each case comprising both hormonal components, are placed in spatially separated and individually removable manner in a packaging unit.
  • the first hormonal component can be administered in combination with the second hormonal component.
  • the invention is based on the surprising finding that as a result of the continuous, combined administration of a product comprising two hormonal components, namely a first hormonal component comprising at least one gestagen and a second hormonal component comprising at least one estrogen, a high contraceptive reliability can be achieved.
  • estrogens are not understood to cover steroid molecules, which preferably evolve their action in that they in different ways exert a biological effect at different cell locations in different organs.
  • Estrogens can act (1) on the cellular membrane, (2) intracellular, cytoplasmic proteins and (3) specific nuclear receptors. It has recently become known that besides the standard estrogen receptor type 1 there is a second estrogen receptor type 2, whose organ distribution is different from that of the estrogen receptor type 1.
  • biogenous estrogens are steroid molecules, which evolve an estrogen-like action on the membrane, cytoplasmic proteins and nuclear receptors for hydrophobic ring substances and consequently trigger biological effects corresponding to a hydrophobic steroid ring structure able to initiate an estrogen-like action in cells, organs and the complete organism.
  • biogenous estrogens also covers those estrogens which are produced by the human body and consequently include endogenic estrogens.
  • the biogenous estrogens used in specific embodiments of the product according to the invention are typically those which are chemically synthesized. However, it is fundamentally also possible to use compounds isolated from an organism.
  • Biogenous estrogens also cover conjugate, biogenous estrogens such as e.g. estradiol valerate and estrone sulphate.
  • antiestrogens is here understood to mean hydrophobic ring structure substances and other substances able to specifically and selectively counteract the above-described estrogen action on cells, organs or the overall organism.
  • Continuous administration is here understood to mean an administration uninterrupted over the use period, in which there are no hormonal component taking-free intervals. This means that there is no interruption of the administration of the product by administering placebos in place of the hormonal product. Thus, over the administration period typically lasting several months to years there are no changes to the fundamental composition of the hormonal components. Instead over the entire administration period the hormonal components forming the hormonal product according to the invention are administered uninterrupted and unchanged with no modification to the concentration.
  • concentration of estrogen understood in the full breadth of the concept defined here
  • gestagen also understood in the full breadth of the term defined here, can be changed for older women compared with younger women.
  • the hormonal product according to the invention is particularly suitable for women aged more than 40, where the risk of circulatory disturbances is known to increase with increasing age. There is also a reduction in the thrombosis risk, which has of late acquired considerable significance in contraceptive therapy.
  • the low dosages of the two hormonal components and in particular the estrogen component is made possible by the additive action of the two hormonal components, without there being any limitation to the action of the product according to the invention with respect to its contraceptive and ovulation-inhibition properties.
  • the ovulation inhibition and menstrual cycle suppression reliably ensured by the product according to the invention is of great significance for certain patients, such as e.g. for top sports women, dancers and business women, who wish to exclude any reduction in their physical, intellectual and emotional efficiency as a result of the menstrual cycle.
  • the two hormonal components of the product according to the invention it is possible to administer the same either orally, transdermally, intravaginally, by depot injections or hormone implants.
  • the advantages observed for the particular administration forms are obtained.
  • Possible oral administration forms are all the forms known from the prior art such as e.g. tablets, dragees, pills or capsules, which are produced using conventional adjuvants and carrier substances.
  • the two hormonal component forming the product can e.g. be applied to a plaster or also can be applied by transdermal, therapeutic systems and are consequently supplied to the organism.
  • a plaster or also can be applied by transdermal, therapeutic systems and are consequently supplied to the organism.
  • an already prepared combination of the two hormonal components or the latter individually can be introduced into such a system, which is based on ionotherapy or diffusion or optionally a combination of these effects.
  • Mutations on the second allele particularly frequently occur in given phases of the cell cycle, namely in the GI phase. Every four weeks the menstrual cycle drives the breast cell in a cell cycle, “opens” the genome for mutations, which are either repaired or apoptotically “removed”. Under the conditions of the conventional combined or sequential contraception treatment a woman can have 500 to 700 cycles over her life span, whereas under natural conditions a women has a maximum of 20 to 30 cycles. Thus, in an unusually frequently number of cell cycles over in each case 8 days a considerable mutation risk is introduced into the stimulated breast tissue.
  • the breast cells are brought into a “rest phase” and it is scientifically ensured that in the rest phase less cancerogenic mutations are introduced into a tissue than in a stimulated tissue. This reduces by a multiple mutagenesis, i.e. the breast cancer risk.
  • the quantity of administered gestagens and estrogens substantially corresponds to the quantity of comparable prior art products.
  • the examples provide further information concerning the quantities to be administered daily of the different compounds forming the first and/or second hormonal components.
  • estriol can be used in a concentration range of 0.5 to 3 mg and chlormadinone acetate in a concentration range of 0.75 to 5 mg.
  • the product was administered for 12 months without any taking interval.
  • the mode of action corresponded to that of example 1.
  • estradiol valerate can be used in a concentration range of 0.5 to 5 mg and lynestrenol in a concentration range of 0.5 to 4.5 mg.
  • the product was administered for 12 months without any taking interval.
  • the mode of action corresponded to that of example 1.
  • tamoxifen For contraceptive treatment use was made of a product containing per daily unit in tablet form 20 mg of tamoxifen 2 mg of lutenyl. It is noteworthy that tamoxifen can be used in a concentration range of 10 to 50 mg and lutenyl in a concentration range of 1 to 5 mg. This product is preferably suitable for contraception in women with a family breast cancer risk. The product was administered for 12 months without any taking interval and the mode of action corresponded to that of example 1.
  • raloxifen can be used in a concentration range of 30 to 100 mg and medroxyprogesterone acetate in a concentration range of 2 to 10 mg.
  • MPA medroxyprogesterone acetate
  • This combination is preferably suitable for women with a family breast cancer risk and young women who have suffered breast cancer.
  • the product was administered for 12 months without any taking interval and the mode of action corresponded to that of example 1.

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention relates to a hormonal contraceptive product having two hormonal components, an estrogen and a gestagen, and a method for the continuous suppression of the menstrual cycle by uninterrupted administration of the product of the invention.

Description

    RELATED APPLICATIONS
  • The application is a continuation of U.S. application Ser. No. 09/508,648, filed Jun. 5, 2000, which is the U.S. National Phase under 35 U.S.C. §371 of International Application PCT/DE98/02636, filed Sep. 11, 1998, which claims priority to German Application No. DE 19739916.9, filed Sep. 11, 1997.[0001]
  • BACKGROUND OF THE INVENTION
  • 1. Field of the Invention [0002]
  • The present invention relates to a hormonal contraceptive product with two hormonal components, the use thereof and a hormonal contraception process. [0003]
  • 2. Description of the Related Art [0004]
  • Since hormonal contraceptives became available in the 1960's, a number of hormonal components have been investigated with regards to their suitability in the most varied administration diagrams. A fundamental subdivision into combination and sequential products is possible. [0005]
  • For example, if the desired cycle time is 28 days, in the case of the known combination products administration takes place over 21 days in a constant or varying absolute and/or relative dosage of a combination of an estrogen product and a gestagen product, in which the estrogen product can e.g. be natural estrogen or synthetic ethinyl estradiol and the taking of the aforementioned 21 daily units is followed by a seven-day interval where there is a withdrawal bleeding simulating natural menstruation. [0006]
  • In the known sequential products, once again for a desired cycle time of 28 days, administration takes place for 7 days of a pure estrogen product and then for 15 days of a combination of an estrogen product and a gestagen product and here again there is then a taking-free period of e.g. 6 days when withdrawal bleeding occurs. It is admittedly already known to bridge the inherent taking intervals of combination and sequential products in the interest of greater taking security by administering within the days in question placebos. However, it has hitherto always been assumed that during the roughly one-week taking interval no hormones of the present type should be administered, in order to ensure a reliable withdrawal bleeding. Only in the case of substitution products in the menopause of older women have hormones been administered throughout the cycle, e.g. in the sequence 10 days estrogen product, 11 days combination of estrogen and gestagen product, 7 days estrogen product, 7 days estrogen product in a particularly low dosage, but said substitution products are unsuitable for ovulation inhibition. [0007]
  • The sequential products used in substitution therapy are in particular unsuitable for contraception because the natural estradiol does not prevent ovulation in the dosage administered and the phase in which gestagen is administered is too short, being only 11 days. However, in the case of the substitution products, the above-described sequential system guarantees a relatively good cycle control. [0008]
  • German patent 43 08 406 discloses a combination contraceptive product, which comprises one or more stages. At least one stage contains the combination of three components, namely a biogenous estrogen, a synthetic estrogen and a gestagen and the further stages in each case comprise a pharmaceutically unobjectionable placebo or a biogenous or synthetic gestagen, or a biogenous or synthetic estrogen, or a combination of two components, namely a biogenous estrogen, a synthetic estrogen and a gestagen or a combination of synthetic estrogen and a gestagen. [0009]
  • The description of the above document makes it clear that in the stage concept described therein there is typically a change of state over the period of time. Such a state change can take place in that the composition of the phases forming the stage is modified with respect to the components used and in that only the concentrations of the components used in the phases forming the stage undergo changes. [0010]
  • The problem of the invention is to provide a hormonal contraceptive product, which ensures high contraceptive safety or reliability and prevents intermenstrual bleeding. There is also to be a further reduction in the side effects otherwise observed in hormonal contraceptive products. [0011]
  • SUMMARY OF THE INVENTION
  • According to the invention this problem is solved by a hormonal contraceptive product having two hormonal components, the agent comprising for continuous, combined administration a first hormonal component comprising at least one gestagen and a second hormonal component comprising at least one estrogen. [0012]
  • The problem is also solved by a hormonal contraception process, in which a product, which comprises at least one first hormonal component, which comprises at least one gestagen, and a second hormonal component comprising at least one estrogen is continuously administered. [0013]
  • According to another aspect of the invention the product according to the invention is used for inhibiting ovulation. [0014]
  • According to a further aspect of the invention the product according to the invention is used for the treatment and/or prophylaxis of breast tumours. [0015]
  • According to another embodiment the invention proposes that gestagen as the first hormonal component is chosen from the group comprising progesterone, chlormadinone acetate, norethisterone acetate, cyproterone acetate, desogestrel, levonorgestrel, other natural and/or synthetic gestagens, antigestagens and hormonal analogs with gestagen or antigestagen action, as well as hormonal compounds which rapidly split off at least one gestagen following taking. [0016]
  • In the product according to the invention, the estrogen as the second hormonal component can be selected from the group comprising synthetic estrogens, biogenous estrogens, antiestrogens and hormonal analogs with estrogen or antiestrogen action. [0017]
  • In a preferred embodiment the synthetic estrogen is selected from the group comprising ethinyl estradiol, mestranol and the like, as well as hormonal compounds rapidly splitting off at least one synthetic estrogen following taking. [0018]
  • In particularly preferred manner the synthetic estrogen is ethinyl estradiol. [0019]
  • In preferred embodiments the daily administered ethinyl estradiol quantity is 1 to 20 μg. In particularly preferred manner, the daily administered ethinyl estradiol quantity is 5 to 10 μg. [0020]
  • According to the invention the biogenous estrogen is selected from the group comprising estradiol, estriol, estrone, estrane, etc., as well as hormonal compounds rapidly splitting off at least one biogenous estrogen after taking. [0021]
  • According to an embodiment the estradiol comprises 17-α-estradiol and/or 17-β-estradiol. [0022]
  • According to another embodiment the daily administered biogenous estrogen quantity in the case of estradiol, particularly α and β-estradiol, is 0.1 to 2 mg and in the case of conjugate estrogens 0.05 to 0.5 mg. [0023]
  • In an embodiment the product according to the invention can be administered orally. [0024]
  • In an alternative embodiment the product according to the invention can be administered transdermally. [0025]
  • In a second alternative embodiment the product according to the invention can be administered intravaginally. [0026]
  • In a third alternative embodiment the product according to the invention can be in depot injection form. [0027]
  • In a fourth alternative embodiment the product according to the invention can be administered as a hormonal implant. [0028]
  • Finally, the daily units in each case comprising both hormonal components, are placed in spatially separated and individually removable manner in a packaging unit. [0029]
  • In an embodiment of the process according to the invention the first hormonal component can be administered in combination with the second hormonal component. [0030]
  • In another embodiment of the process according to the invention the product according to the invention is administered.[0031]
  • DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT
  • The invention is based on the surprising finding that as a result of the continuous, combined administration of a product comprising two hormonal components, namely a first hormonal component comprising at least one gestagen and a second hormonal component comprising at least one estrogen, a high contraceptive reliability can be achieved. [0032]
  • In accordance with modern opinion, estrogens are not understood to cover steroid molecules, which preferably evolve their action in that they in different ways exert a biological effect at different cell locations in different organs. Estrogens can act (1) on the cellular membrane, (2) intracellular, cytoplasmic proteins and (3) specific nuclear receptors. It has recently become known that besides the standard estrogen receptor type 1 there is a second estrogen receptor type 2, whose organ distribution is different from that of the estrogen receptor type 1. [0033]
  • Thus, the above definition also covers the compounds known as “designer hormones,” which have the aforementioned characteristics. [0034]
  • Thus, biogenous estrogens are steroid molecules, which evolve an estrogen-like action on the membrane, cytoplasmic proteins and nuclear receptors for hydrophobic ring substances and consequently trigger biological effects corresponding to a hydrophobic steroid ring structure able to initiate an estrogen-like action in cells, organs and the complete organism. [0035]
  • The term biogenous estrogens also covers those estrogens which are produced by the human body and consequently include endogenic estrogens. The biogenous estrogens used in specific embodiments of the product according to the invention are typically those which are chemically synthesized. However, it is fundamentally also possible to use compounds isolated from an organism. [0036]
  • Biogenous estrogens also cover conjugate, biogenous estrogens such as e.g. estradiol valerate and estrone sulphate. [0037]
  • The term antiestrogens is here understood to mean hydrophobic ring structure substances and other substances able to specifically and selectively counteract the above-described estrogen action on cells, organs or the overall organism. [0038]
  • Continuous administration is here understood to mean an administration uninterrupted over the use period, in which there are no hormonal component taking-free intervals. This means that there is no interruption of the administration of the product by administering placebos in place of the hormonal product. Thus, over the administration period typically lasting several months to years there are no changes to the fundamental composition of the hormonal components. Instead over the entire administration period the hormonal components forming the hormonal product according to the invention are administered uninterrupted and unchanged with no modification to the concentration. However, it is conceivable for the concentration of estrogen, understood in the full breadth of the concept defined here, and gestagen, also understood in the full breadth of the term defined here, can be changed for older women compared with younger women. This can also take place in such a way that over the continuous administration period initially there is a start with a specific composition and this is then adapted over a period of weeks, months and years to the changed biological needs of the women through the administration of a subsequent product, but which also comprises a product according to the present invention. [0039]
  • As a result of the continuous administration of said hormonal components it is ensured that the natural hormonal processes taking place in the female organism do not interrupt the contraceptive security. [0040]
  • As a result of the estrogen component, respectively by specific action of hydrophobic ring substances with an estrogen-like action, there can be a suppression of gonadotropins. This is desirable. The resulting suppression of the ovarial function is compensated by an adequate substitution of estrogen action. This prevents the development of osteoporosis, the favourable vascular effects of estrogens are maintained and there is no unfavourable influence to the lipid metabolism. By interrupting the cycle-dependent instability in the hormone system, the premenstrual syndrome can be favourably influenced. In addition, the physiological equilibrium of the coagulation system is not disturbed, because the unstable equilibrium in which the coagulation system occurs is not activated and deactivated by the up and down of hormone fluctuations. Thus, the hormonal product according to the invention is particularly suitable for women aged more than 40, where the risk of circulatory disturbances is known to increase with increasing age. There is also a reduction in the thrombosis risk, which has of late acquired considerable significance in contraceptive therapy. [0041]
  • It has surprisingly also been found that on administering the product according to the invention there is a reliable continuous suppression of the menstrual cycle and menstruation in the case of a very low dosage. Without wishing to be bound by this explanation, the combination of the two indicated hormonal components and in particular the low estrogen dosage would appear to be suitable for eliminating the otherwise conventional side effects of ethinyl estradiol and to drop below the administrations of more than 15 μg of ethinyl estradiol otherwise considered typically necessary in prior art contraceptives. [0042]
  • The low dosages of the two hormonal components and in particular the estrogen component is made possible by the additive action of the two hormonal components, without there being any limitation to the action of the product according to the invention with respect to its contraceptive and ovulation-inhibition properties. [0043]
  • The ovulation inhibition and menstrual cycle suppression reliably ensured by the product according to the invention is of great significance for certain patients, such as e.g. for top sports women, dancers and business women, who wish to exclude any reduction in their physical, intellectual and emotional efficiency as a result of the menstrual cycle. As a result of the combined, continuous administration of the two hormonal components of the product according to the invention it is possible to administer the same either orally, transdermally, intravaginally, by depot injections or hormone implants. Here again the advantages observed for the particular administration forms are obtained. [0044]
  • Possible oral administration forms are all the forms known from the prior art such as e.g. tablets, dragees, pills or capsules, which are produced using conventional adjuvants and carrier substances. [0045]
  • In the transdermal administration of the product according to the invention the two hormonal component forming the product can e.g. be applied to a plaster or also can be applied by transdermal, therapeutic systems and are consequently supplied to the organism. For example an already prepared combination of the two hormonal components or the latter individually can be introduced into such a system, which is based on ionotherapy or diffusion or optionally a combination of these effects. [0046]
  • In the case of oral administration it has proved appropriate to place the daily units, which in case comprise a combination of the two hormonal components, in a spatially separated and individually removable manner in a packaging unit, so that it is easy to check whether the typically daily taken, oral administration form has in fact been taken. It is important to ensure that there are no taking-free days. Depot injections can be administered at 1 to 6 months or longer intervals. Hormonal implants contain both hormonal components and deliver the same over a period of preferably 3 to 6 months. [0047]
  • When using the product according to the invention it has surprisingly been found that the treatment and/or prophylaxis of breast tumours is possible. The latest breast cancer risk research has revealed that mutations, which can be hereditary or acquired, occur in certain risk genes. Modern cancer therapy assumes that a cancerogenic mutation is present on one of the two alleles of a gene which is initially controlled by the other, healthy allele. If a further mutation occurs in a specific organ cell on the second allele, then uncontrolled, malignant growth can occur. [0048]
  • Mutations on the second allele particularly frequently occur in given phases of the cell cycle, namely in the GI phase. Every four weeks the menstrual cycle drives the breast cell in a cell cycle, “opens” the genome for mutations, which are either repaired or apoptotically “removed”. Under the conditions of the conventional combined or sequential contraception treatment a woman can have 500 to 700 cycles over her life span, whereas under natural conditions a women has a maximum of 20 to 30 cycles. Thus, in an unusually frequently number of cell cycles over in each case 8 days a considerable mutation risk is introduced into the stimulated breast tissue. If the menstrual cycle is suppressed, as is possible with the product according to the invention, the breast cells are brought into a “rest phase” and it is scientifically ensured that in the rest phase less cancerogenic mutations are introduced into a tissue than in a stimulated tissue. This reduces by a multiple mutagenesis, i.e. the breast cancer risk. [0049]
  • The aforementioned use of the product according to the invention for the treatment and/or prophylaxis of breast cancers is in particular associated with special advantages if the users of the product are high-risk subjects, such as e.g. those with a high family breast cancer risk. [0050]
  • The quantity of administered gestagens and estrogens substantially corresponds to the quantity of comparable prior art products. The examples provide further information concerning the quantities to be administered daily of the different compounds forming the first and/or second hormonal components. [0051]
  • The invention is explained in greater detail hereinafter relative to examples revealing further features, advantages and embodiments of the present invention. [0052]
  • EXAMPLE 1
  • For contraceptive treatment use was made of a product which per daily unit in table form contained 5 μg of ethinyl estradiol and 2 mg of norethisterone acetate. It is noteworthy that norethisterone acetate can be used in a concentration range of 0.5 to 5 mg. The product was administered for 9 months and revealed a very good contraceptive reliability whilst completely suppressing the menstrual cycle with no side effects. Within the framework of the present investigation it was ensured that the test persons took the product daily, i.e. without any taking interval, over the entire aforementioned time period. [0053]
  • EXAMPLE 2
  • For contraceptive treatment use was made of a product which per daily unit in table form contains 0.5 mg of estriol and 2 mg of chlormadinone acetate. It is noteworthy that estriol can be used in a concentration range of 0.5 to 3 mg and chlormadinone acetate in a concentration range of 0.75 to 5 mg. The product was administered for 12 months without any taking interval. The mode of action corresponded to that of example 1. [0054]
  • EXAMPLE 3
  • For contraceptive treatment use was made of a product which in each daily unit in tablet form contained 0.5 mg of estradiol valerate and 2 mg of lynestrenol. It is noteworthy that estradiol valerate can be used in a concentration range of 0.5 to 5 mg and lynestrenol in a concentration range of 0.5 to 4.5 mg. The product was administered for 12 months without any taking interval. The mode of action corresponded to that of example 1. [0055]
  • EXAMPLE 4
  • For contraceptive treatment use was made of a product containing per daily unit in tablet form 7.5 μg of ethinyl estradiol and 75 μg of desogestrel. It is noteworthy that desogestrel can be used in a concentration range of 50 to 200 μg. The product was administered for 12 months without any taking interval. The mode of action corresponded to that of example 1. [0056]
  • EXAMPLE 5
  • For contraceptive treatment use was made of a product containing per daily unit in tablet form 20 mg of tamoxifen 2 mg of lutenyl. It is noteworthy that tamoxifen can be used in a concentration range of 10 to 50 mg and lutenyl in a concentration range of 1 to 5 mg. This product is preferably suitable for contraception in women with a family breast cancer risk. The product was administered for 12 months without any taking interval and the mode of action corresponded to that of example 1. [0057]
  • EXAMPLE 6
  • For contraceptive treatment use was made of a product containing per daily unit in tablet form 50 mg of raloxifen and 2.5 mg of medroxyprogesterone acetate (MPA). It is noteworthy that raloxifen can be used in a concentration range of 30 to 100 mg and medroxyprogesterone acetate in a concentration range of 2 to 10 mg. This combination is preferably suitable for women with a family breast cancer risk and young women who have suffered breast cancer. The product was administered for 12 months without any taking interval and the mode of action corresponded to that of example 1. [0058]
  • EXAMPLE 7
  • For contraceptive treatment use was made of an agent containing per daily unit in tablet form 10 μg of ethinyl estradiol and tibolone in a daily concentration of 2 mg. It is noteworthy that tibolone can be used with a concentration of 1 to 10 mg. The product was administered without any taking interval for 12 months and the mode of action corresponded to that of example 1. [0059]
  • EXAMPLE 8
  • For contraceptive treatment use was made of a product containing per daily unit in table form 10 μg of ethinyl estradiol and as the antiestrogen substance Ro486 in a concentration of 2.5 mg. It is noteworthy that R0486 can be used in a concentration range of 1 to 7.5 mg. The product was administered without any taking interval over a period of 12 months and the mode of action correspond to that of example 1. [0060]
  • The features of the invention described in the description and claims can be essential individually and in random combination for the implementation of the different embodiments of the invention. [0061]

Claims (15)

What is claimed is:
1. A method for hormonal contraception, comprising administering orally, transdermally or via depot to a mammal in need thereof, for a continuous and uninterrupted administration period, a contraceptive product comprising levonorgestrel and ethinyl estradiol, wherein said levonorgestrel and ethinyl estradiol are present in said contraceptive product at unchanged dosages throughout the administration period.
2. The method of claim 1, wherein said ethinyl estradiol is present at a dosage of 1-20 μg per day.
3. The method of claim 2, wherein the administration is oral.
4. The method of claim 3, wherein the administration period is 9 months.
5. The method of claim 3, wherein the administration period is 12 months.
6. A method for continuous suppression of the menstrual cycle in a woman, comprising administering orally, transdermally or via depot to the woman in need thereof, for a continuous and uninterrupted administration period, a contraceptive product comprising levonorgestrel and ethinyl estradiol, wherein said levonorgestrel and ethinyl estradiol are present in said contraceptive product at unchanged dosages throughout the administration period.
7. The method of claim 6, wherein said ethinyl estradiol is present at a dosage of 1-20 μg per day.
8. The method of claim 7, wherein the administration is oral.
9. The method of claim 8, wherein the administration period is 9 months.
10. The method of claim 8, wherein the administration period is 12 months.
11. A method for treating or inhibiting premenstrual syndrome, which comprises administering orally, transdermally, or via depot, to a mammal in need thereof, for a continuous and uninterupted administration period, an effective amount of a gestagen and an estrogen, wherein said gestagen and estrogen are present in unchanged dosages throughout the administration period.
12. The method of claim 11, wherein said gestagen is selected from the group consisting of progesterone, chlormadinone acetate, northisterone acetate, cyprotherone acetate, desogestrel, and levonorgestrel; and
said estrogen is selected from the group consisting of ethinyl estradiol, mestranol, estradiol, estriol, estrone, and estrane.
13. The method of claim 12, wherein said estrogen is ethinyl estradiol, which is present at a dosage of 1-20 μg per day.
14. The method of claim 13, wherein said gestagen is levonorgesterel.
15. The method of claim 14, wherein the administration is oral.
US10/867,954 1997-09-11 2004-06-15 Hormonal contraceptive product Abandoned US20040243606A1 (en)

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DE19739916A DE19739916C2 (en) 1997-09-11 1997-09-11 Use of a combination of a progestogen and an estrogen for the continuous inhibition of ovulation and possibly simultaneous treatment and / or prophylaxis of tumors of the mammary glands
US09/508,648 US6500814B1 (en) 1997-09-11 1998-09-03 Hormonal contraceptive
US10/299,628 US20030073673A1 (en) 1997-09-11 2002-11-19 Hormonal contraceptive product
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US10/841,278 Abandoned US20050004088A1 (en) 1997-09-11 2004-05-07 Hormonal contraceptive product
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US20050004088A1 (en) 2005-01-06
US20030073673A1 (en) 2003-04-17
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EP1011682B1 (en) 2003-05-28

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