Classifications

• • 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
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
• • 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
  • A61K31/565—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
  • A61K31/567—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 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• • 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
  • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/18—Feminine contraceptives

Definitions

• the present invention relates to a method for hormonal contraception in which a pharmaceutical preparation containing at least one progestagen is transdermally administered, if necessary and once before an expected sexual intercourse.
• Hormonal contraception with daily low oral doses of synthetic estrogens and progestins is currently the most effective reversible method of contraception.
• preparations which contain only progestins.
• hormonal contraceptives is usually oral.
• administration of gestagens as depot preparation is also possible. These include so-called injection preparations, intrauterine devices and implants.
• transdermal administration of an estrogen / gestagen combination released from a patch is also on the market.
• the "postcoital pill” is available in European countries, also for the prevention of an unwanted pregnancy. This contains a high-dose combination of ethinyl estradiol and progestins.
• the invention has for its object to provide a method for hormonal contraception, which ensures a higher contraceptive safety compared to hormonal postcoital methods, is under the control of women and does not induce abortion. Furthermore, a higher compatibility than other hormonal contraceptive agents should be achieved. According to the invention, this object is achieved by a method for hormonal contraception, in which a pharmaceutical preparation containing at least one progestagen is administered transdermally, if necessary, once before an expected sexual intercourse. The higher tolerance is achieved by the - compared to oral application - lower dosage of the transdermally administered gestagen.
• Progesterone which is formed in the second half of the cycle by the ovary, and its synthetic function in terms of its biological function with regard to ovulation inhibition and pregnancy maintenance are referred to as progestins.
• the invention is based on the surprising finding that a high contraceptive safety can be achieved by the precautionary administration of the pharmaceutical composition. If it is not for intercourse, the patch is easy to remove. When intercourse has been carried out, administration of the progestogen over two or three days in very small doses has the following advantages:
• the method according to the invention for hormonal contraception is of great importance for women with irregular and / or rare traffic, that is, for example, from two to three times a month. On the one hand, it allows the active decision for contraception by the woman or the couple. On the other hand, when compared to emergency contraception significantly reduced dose, prolonged use and more stable levels of effective ovulation is reliably inhibited. The endometrium is reduced by this treatment in its receptivity. This is a consequence of the approx. 48-hour application and thus active advantage of the precoital versus the postcoital procedure. The frequency of use should be limited as much as possible to two to three times per cycle, since it can lead to cycle disorders with more frequent use.
• single administration means sticking once a suitably sized patch with a defined release of gestagen for two or three days. If the sexual intercourse does not take place, the plaster is removed and within a short time the progestin is eliminated from the organism. After about 8 hours, a sufficient effective level of the progestin is achieved and remains at glued plaster for at least 48 hours in the same level. This achieves high reliability of the contraceptive method.
• progestins particularly suitable for the practice of the invention are progestins, desogestrel, etonorgestrel, gestodene, levonorgestrel or trimegestone.
• progestin praecoitalen amount is unique for example, 50 - 100 ug gestodene release within 24 h of a 10 to 30 cm 2 patch or a more equivalent amount of another gestagen.
• Quantities of another gestagen which are equivalent to the given transdermal dose of gestagen can be calculated on the basis of the oral gestagen quantities required for ovulation inhibition, taking into account the oral compared to the transdermal bioavailability of the progestogens.
• the progestin may be incorporated into a patch and thus delivered directly to the bloodstream.
• the patch size is about 10 to 30 cm 2 , preferably 10 to 20 cm 2 .
• an estrogen component into the precoital patch is also possible.
• an additional use of an estrogen in the Patch is preferably ethinyl estradiol in a dose sufficient for a daily release of 10 to 30 micrograms ethinylestradiol used.
• the invention also relates to the praecoitale patch as such, for carrying out the method according to the invention.
• the claimed praecoital patch contains as active ingredient only one or more gestagens, preferably gestodene. From this patch of a size of 10 to 30 cm 2 , preferably 10 to 20 cm 2 , daily 50 to 100 micrograms of gestodene - or an amount of another progestogen equivalent to this amount of gestodene - is released.
• a pharmaceutical kit which comprises at least one transdermal patch containing as active ingredient either only a gestagen or a combination of active ingredients of progestogen and estrogen, preferably gestodene and ethinyl estradiol, as well as product information or instructions for use according to the method of the invention.
• Example 1 Preparation of a plaster to be used according to the invention The precoital plaster is produced as follows:
• the resulting plaster (10 cm 2 ) has the following composition:
• the resulting plaster has the following composition:
• Step Example! 3 Determination of the daily release rate
• the preparation of the patches is carried out as described in Example 1 or 2.
• the formulation is tested on the in-vitro mouse skin permeation test.
• the test is performed using nude mouse skin preparations (HsdCpb: NMRI-nu) from Harlan Bioservice for Science GmbH, Walsrode, Germany.
• the formulation is applied to the outside of the skin sample. Both are placed in a permeation measuring cell so that the skin inside comes into contact with the receptor medium.
• the receptor medium used is a HEPES buffer.
• Sodium azide is added to prevent germ growth and the receptor solution is maintained at 32 ° C.
• samples of the receptor solution are taken and the concentration of gestodene determined by HPLC.
• the release rate is then determined as the amount of active ingredient released per unit area and time [ ⁇ g / cm 2 • 24 h] using the calculated amounts of active substance.
• One patch according to Example 1 or 2 was applied to female subjects on the upper arm and the concentration of gestodene in the serum was monitored.

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• Health & Medical Sciences (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)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Dermatology (AREA)
• Gynecology & Obstetrics (AREA)
• Endocrinology (AREA)
• Reproductive Health (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Steroid Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

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• 2005
  • 2005-10-19 DE DE102005050729A patent/DE102005050729A1/de not_active Withdrawn
• 2006
  • 2006-10-19 WO PCT/EP2006/010273 patent/WO2007045513A1/de active Application Filing
  • 2006-10-19 CA CA2626567A patent/CA2626567C/en not_active Expired - Fee Related
  • 2006-10-19 CN CNA2006800480426A patent/CN101340915A/zh active Pending
  • 2006-10-19 EP EP06828860A patent/EP1937275A1/de not_active Withdrawn
  • 2006-10-19 JP JP2008535989A patent/JP2009512658A/ja not_active Withdrawn
  • 2006-10-19 US US12/090,719 patent/US20080311180A1/en not_active Abandoned
  • 2006-10-19 BR BRPI0617683-6A patent/BRPI0617683A2/pt not_active IP Right Cessation
  • 2006-10-19 KR KR1020087011824A patent/KR20080056774A/ko not_active Application Discontinuation
  • 2006-10-19 US US11/583,143 patent/US20070111976A1/en not_active Abandoned
• 2008
  • 2008-04-18 GT GT200800038A patent/GT200800038A/es unknown
  • 2008-04-21 HN HN2008000621A patent/HN2008000621A/es unknown
  • 2008-04-21 EC EC2008008390A patent/ECSP088390A/es unknown
  • 2008-04-21 CR CR9908A patent/CR9908A/es not_active Application Discontinuation
• 2012
  • 2012-05-29 US US13/482,023 patent/US20130089574A1/en not_active Abandoned
• 2013
  • 2013-09-24 JP JP2013197047A patent/JP2014001239A/ja not_active Withdrawn

Non-Patent Citations (1)

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