GB2109231A - Medicament containing progesterone - Google Patents

Medicament containing progesterone Download PDF

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Publication number
GB2109231A
GB2109231A GB08229804A GB8229804A GB2109231A GB 2109231 A GB2109231 A GB 2109231A GB 08229804 A GB08229804 A GB 08229804A GB 8229804 A GB8229804 A GB 8229804A GB 2109231 A GB2109231 A GB 2109231A
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United Kingdom
Prior art keywords
progesterone
group
mammary
percutaneous
medicament
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GB08229804A
Inventor
Jean Louis Abel Besins
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Individual
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Individual
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    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

A medicament, for the treatment of mammary disorders such as mastodynias and mastopathias, is in the form of a gel containing progesterone and is administered percutaneously.

Description

SPECIFICATION Medicament based on progesterone The present invention relates to a medicament based on progesterone for the treatment of mammary disorders such as mastodynias and mastopathias.
This medicament is characterized in that the progesterone is in the form of gel applied by the percutaneous route.
In fact, it has been discovered, according to the invention, that progesterone, among the hormonal steroids, presents the particular feature of being metabolized in the skin into derivatives whose hormonal activity appears to be virtually zero. This results in that, when a solution of progesterone is administered by the percutaneous route, 80% of the steroids are metabolized in the skin and only 20% are capable of passing the cutaneous barrier. The percutaneous administration of progesterone therefore offers a particular advantage in mammary pathology, since it allows administration and concentration within the mammary receptor itself of a large quantity of progesterone.On the other hand, a concentration just sufficient for a therapeutic effect at mammary level is often obtained, by the oral or injectable route, only at the cost of excessive activity at uterus level, sometimes causing an atrophy of the tunica mucosa uteri, or even a metrorhagia. The percutaneous route therefore enables the disparity of the respective concentrations to be reversed and the desired effect on the mammary gland to be obtained, without undesirable repercussions on the uterus.
According to the invention, the progesterone is therefore applied by the percutaneous route in the form of a dilute alcoholic gel having a concentration of 1%. In other words, for 100 grams of composition, the progesterone is present at the rate of 1 gram and the excipient is constituted by a carboxypolyvinyl polymer, triethanolamine, 95" alcohol and purified water. The progesterone, at breast level, opposed the increase in the capillary permeability provoked by the oestrogens, it participates in the growth and differentiation of the galactophori and acini and it blocks the cycle of the rapid epithelial mitoses provoked by the oestrogens.
The administration of pure progesterone by the percutaneous route makes it possible to treat and prevent the vascular and cellular effects of a local deficit of progesterone at breast level. It may be employed in all cases of benign mammary pathology, such as mastodynias, mastopathias, prevention of recurrences (cysts, adeno-fibromas). Therapeutical tests have been made on a group of 52 women, in two ways namely: In a first group, only the progesterone was administered by the percutaneous route in 26 patients whilst, in the second group of 26 patients, the progesterone was administered by the percutaneous route in association with a synthetic luteomimetic, an oestroprogestative or other hormonal medication.
In each of the two groups of 26 paitents, the following had been observed: essential mastodynias, i.e. painful phenoma of congestion without any morphological substratum on physical examination (four times in group 1, six times in group 2); a mastopathia in the form of an isolated cystic dystrophy or of multiple microcysts without mastodynias (five times in group 1,fourtimes in group 2); a mammary dystrophy associated with a mastodynia (thirteen times in group 1, eight times in group 2); the existance of organised benign mammaryforma- tions associated or not with a mastodynia and/or with a cystic dystrophy (four times in group 1, eigth times in group 2).
In the 52 patients referred to above, the progesterone was administrated by the percutaneous route in the form of dilute alcoholic gel at a concentration of 1%. A dose of 5 grams was applied to the two breasts each day, from the beginning ofthe cycle and during menstruation for one month, then in the second part of the cycle during the following two months.
In group 1, the results were excellent in eight cases and good in seven cases. The results were considered as being excellent when an improvement or disappearance of the mastodynia, a regression of the mammary swelling with disappearance of the local phenomena of cutaneous hypervascularisation and, when associated with a mastopathia, an involution of the latter, were observed in the patients. The results were considered good when the mastodynia disappeared and the mastosic element persisted, and mediocre when there was persistence of the disorders, although they were attenuated. In group 1, only seven mediocre cases and three failures were obtained.
With the patients of group 2, the results varied depending on the therapeutic association of the percutaneous progesterone and, the luteomimetics of synthetic oestroprogestatives by the oral route. In virtually all types of association, a majority of cases with excellent or good results was always encountered. General tolerance was excellent in all cases.
No repercussions of the percutaneous therapy by progesterone was observed on the menstrual cycle, nor on the digestive, particularly hepatic, function, nor did the patients put on weight, as may be the case when luteomimetics or oestroprogestatives are taken orally. No local cutaneous intolerance was observed during application, nor allergic phenomenon nor cutaneous pigmentation.
1. Medicament based on progesterone for the treatment of mamxary disorders such as mastodynias and mastopathias, wherein it is presented in the form of gel for application by the percutaneous route.
2. The medicament of claim 1, wherein it is constituted by a dilute alcoholic gel.
3. The medicament of claim 2, wherein it comprises 1% of pure progesterone.
4. The medicament of claim 3, wherein the excipient is constituted by a carboxypolyvinyl polymer, triethanolamine, 95% alcohol and purified
**WARNING** end of DESC field may overlap start of CLMS **.

Claims (5)

**WARNING** start of CLMS field may overlap end of DESC **. SPECIFICATION Medicament based on progesterone The present invention relates to a medicament based on progesterone for the treatment of mammary disorders such as mastodynias and mastopathias. This medicament is characterized in that the progesterone is in the form of gel applied by the percutaneous route. In fact, it has been discovered, according to the invention, that progesterone, among the hormonal steroids, presents the particular feature of being metabolized in the skin into derivatives whose hormonal activity appears to be virtually zero. This results in that, when a solution of progesterone is administered by the percutaneous route, 80% of the steroids are metabolized in the skin and only 20% are capable of passing the cutaneous barrier. The percutaneous administration of progesterone therefore offers a particular advantage in mammary pathology, since it allows administration and concentration within the mammary receptor itself of a large quantity of progesterone.On the other hand, a concentration just sufficient for a therapeutic effect at mammary level is often obtained, by the oral or injectable route, only at the cost of excessive activity at uterus level, sometimes causing an atrophy of the tunica mucosa uteri, or even a metrorhagia. The percutaneous route therefore enables the disparity of the respective concentrations to be reversed and the desired effect on the mammary gland to be obtained, without undesirable repercussions on the uterus. According to the invention, the progesterone is therefore applied by the percutaneous route in the form of a dilute alcoholic gel having a concentration of 1%. In other words, for 100 grams of composition, the progesterone is present at the rate of 1 gram and the excipient is constituted by a carboxypolyvinyl polymer, triethanolamine, 95" alcohol and purified water. The progesterone, at breast level, opposed the increase in the capillary permeability provoked by the oestrogens, it participates in the growth and differentiation of the galactophori and acini and it blocks the cycle of the rapid epithelial mitoses provoked by the oestrogens. The administration of pure progesterone by the percutaneous route makes it possible to treat and prevent the vascular and cellular effects of a local deficit of progesterone at breast level. It may be employed in all cases of benign mammary pathology, such as mastodynias, mastopathias, prevention of recurrences (cysts, adeno-fibromas). Therapeutical tests have been made on a group of 52 women, in two ways namely: In a first group, only the progesterone was administered by the percutaneous route in 26 patients whilst, in the second group of 26 patients, the progesterone was administered by the percutaneous route in association with a synthetic luteomimetic, an oestroprogestative or other hormonal medication. In each of the two groups of 26 paitents, the following had been observed: essential mastodynias, i.e. painful phenoma of congestion without any morphological substratum on physical examination (four times in group 1, six times in group 2); a mastopathia in the form of an isolated cystic dystrophy or of multiple microcysts without mastodynias (five times in group 1,fourtimes in group 2); a mammary dystrophy associated with a mastodynia (thirteen times in group 1, eight times in group 2); the existance of organised benign mammaryforma- tions associated or not with a mastodynia and/or with a cystic dystrophy (four times in group 1, eigth times in group 2). In the 52 patients referred to above, the progesterone was administrated by the percutaneous route in the form of dilute alcoholic gel at a concentration of 1%. A dose of 5 grams was applied to the two breasts each day, from the beginning ofthe cycle and during menstruation for one month, then in the second part of the cycle during the following two months. In group 1, the results were excellent in eight cases and good in seven cases. The results were considered as being excellent when an improvement or disappearance of the mastodynia, a regression of the mammary swelling with disappearance of the local phenomena of cutaneous hypervascularisation and, when associated with a mastopathia, an involution of the latter, were observed in the patients. The results were considered good when the mastodynia disappeared and the mastosic element persisted, and mediocre when there was persistence of the disorders, although they were attenuated. In group 1, only seven mediocre cases and three failures were obtained. With the patients of group 2, the results varied depending on the therapeutic association of the percutaneous progesterone and, the luteomimetics of synthetic oestroprogestatives by the oral route. In virtually all types of association, a majority of cases with excellent or good results was always encountered. General tolerance was excellent in all cases. No repercussions of the percutaneous therapy by progesterone was observed on the menstrual cycle, nor on the digestive, particularly hepatic, function, nor did the patients put on weight, as may be the case when luteomimetics or oestroprogestatives are taken orally. No local cutaneous intolerance was observed during application, nor allergic phenomenon nor cutaneous pigmentation. CLAIMS
1. Medicament based on progesterone for the treatment of mamxary disorders such as mastodynias and mastopathias, wherein it is presented in the form of gel for application by the percutaneous route.
2. The medicament of claim 1, wherein it is constituted by a dilute alcoholic gel.
3. The medicament of claim 2, wherein it comprises 1% of pure progesterone.
4. The medicament of claim 3, wherein the excipient is constituted by a carboxypolyvinyl polymer, triethanolamine, 95% alcohol and purified water.
5. Medicament substantially as hereinbefore described.
GB08229804A 1981-10-26 1982-10-19 Medicament containing progesterone Withdrawn GB2109231A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR8120034A FR2515041A1 (en) 1981-10-26 1981-10-26 PROGESTERONE-BASED DRUG FOR THE TREATMENT OF MAMMARY DISEASES

Publications (1)

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GB2109231A true GB2109231A (en) 1983-06-02

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GB08229804A Withdrawn GB2109231A (en) 1981-10-26 1982-10-19 Medicament containing progesterone

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DE (1) DE3238984A1 (en)
FR (1) FR2515041A1 (en)
GB (1) GB2109231A (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6503894B1 (en) 2000-08-30 2003-01-07 Unimed Pharmaceuticals, Inc. Pharmaceutical composition and method for treating hypogonadism
US6670350B1 (en) * 1999-02-18 2003-12-30 Jenapharm Gmbh & Co. Kg Method of administering dienogest in high dosages to reduce the body of the breast and pharmaceutical composition for same
US6696433B2 (en) 1996-07-22 2004-02-24 Renovo Limited Use of sex steroids function modulators to treat wounds and fibrotic disorders
DE102008064534A1 (en) * 2008-12-29 2010-07-15 Reimers, Simon External frame for connection with two-wheeled electric car, for perpendicular locomotion of paralyzed/handicapped persons, has bar provided in hip height on driving body, where passenger body is fixed in frame and connected with car
US8466137B2 (en) 2005-10-12 2013-06-18 Unimed Pharmaceuticals, Llc Testosterone gel and method of use

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2558373B1 (en) * 1984-01-20 1987-07-03 Mauvais Jarvis Pierre ANTI-ESTROGEN MEDICINAL PRODUCT BASED ON 4-HYDROXYTAMOXIFENE FOR PERCUTANEOUS ADMINISTRATION
US5744463A (en) * 1996-06-03 1998-04-28 Bair; Glenn O. Treatment of side effects of progestins and progesterone analogues used for birth control
US6056972A (en) * 1997-02-26 2000-05-02 Dimera, Llc Method for reducing coronary artery reactivity
US7968532B2 (en) 2003-12-15 2011-06-28 Besins Healthcare Luxembourg Treatment of gynecomastia with 4-hydroxy tamoxifen
DE602005005986T2 (en) * 2004-03-22 2009-06-04 Laboratoires Besins International 4-HYDROXYTAMOXIFES FOR THE TREATMENT AND PROPHYLAXIS OF BENIGNEN BREAST DISEASES
US7507769B2 (en) 2004-03-22 2009-03-24 Laboratoires Besins International Treatment and prevention of benign breast disease with 4-hydroxy tamoxifen
EP1579856A1 (en) * 2004-03-22 2005-09-28 Laboratoires Besins International Treatment and prevention of benign breast disease with 4-hydroxy tamoxifen

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1047518A (en) * 1963-06-11 1966-11-02 Glaxo Lab Ltd 17ª‡-monoesters of 11,17,21-trihydroxy steroid compounds
US4136173A (en) * 1977-01-31 1979-01-23 American Home Products Corp. Mixed xanthan gum and locust beam gum therapeutic compositions
EP0020794B1 (en) * 1979-06-08 1983-01-12 Toko Yakuhin Kogyo Kabushiki Kaisha Creamy preparation containing steroid and process for the preparation thereof

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6696433B2 (en) 1996-07-22 2004-02-24 Renovo Limited Use of sex steroids function modulators to treat wounds and fibrotic disorders
US6670350B1 (en) * 1999-02-18 2003-12-30 Jenapharm Gmbh & Co. Kg Method of administering dienogest in high dosages to reduce the body of the breast and pharmaceutical composition for same
US6503894B1 (en) 2000-08-30 2003-01-07 Unimed Pharmaceuticals, Inc. Pharmaceutical composition and method for treating hypogonadism
US9132089B2 (en) 2000-08-30 2015-09-15 Besins Healthcare Inc. Pharmaceutical composition and method for treating hypogonadism
US9125816B2 (en) 2000-08-30 2015-09-08 Besins Healthcare Inc. Pharmaceutical composition and method for treating hypogonadism
US8741881B2 (en) 2005-10-12 2014-06-03 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8466138B2 (en) 2005-10-12 2013-06-18 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8486925B2 (en) 2005-10-12 2013-07-16 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8729057B2 (en) 2005-10-12 2014-05-20 Unimed Pharmaeuticals, LLC Testosterone gel and method of use
US8466136B2 (en) 2005-10-12 2013-06-18 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8754070B2 (en) 2005-10-12 2014-06-17 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8759329B2 (en) 2005-10-12 2014-06-24 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
US8466137B2 (en) 2005-10-12 2013-06-18 Unimed Pharmaceuticals, Llc Testosterone gel and method of use
DE102008064534A1 (en) * 2008-12-29 2010-07-15 Reimers, Simon External frame for connection with two-wheeled electric car, for perpendicular locomotion of paralyzed/handicapped persons, has bar provided in hip height on driving body, where passenger body is fixed in frame and connected with car

Also Published As

Publication number Publication date
FR2515041B3 (en) 1984-06-15
FR2515041A1 (en) 1983-04-29
DE3238984A1 (en) 1983-05-05
DE3238984C2 (en) 1991-12-19

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