CA2166121A1 - Hormonal method of acne therapy - Google Patents

Hormonal method of acne therapy

Info

Publication number
CA2166121A1
CA2166121A1 CA002166121A CA2166121A CA2166121A1 CA 2166121 A1 CA2166121 A1 CA 2166121A1 CA 002166121 A CA002166121 A CA 002166121A CA 2166121 A CA2166121 A CA 2166121A CA 2166121 A1 CA2166121 A1 CA 2166121A1
Authority
CA
Canada
Prior art keywords
hormone
constituent
daily
units
hormonal
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
CA002166121A
Other languages
French (fr)
Inventor
Marika Ehrlich
Herbert Kuhl
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=6491735&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2166121(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Individual filed Critical Individual
Publication of CA2166121A1 publication Critical patent/CA2166121A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents

Abstract

A method for controlling acne and a hormonal composition for providing acne therapy are provided. Two hormone constituents are packaged spatially separated in a packaging unit for chronologically sequential, oral admin-istration. Each hormone constituent is provided in the form of a plurality of daily hormone units accommodated spatially separately and individually removable in the packaging unit. A first of the hormone constituents contains essentially only an estrogen preparation as active hormonal substance that effects an increase in the sexual hormone-bonding globulins (SHBG). The second hormone constituent contains in estrogen preparation and an anti-androgen preparation in combination. The total plurality of daily units is equal days in the desired cycle.
Preferably, the first hormone constituent comprises 5 through 14 daily units and the second hormone constituent comprises 23 through 14 daily units so that the plurality of daily units of the first hormone constituent is lower than the plurality of daily units of the second hormone constituent.

Description

'~JCI~ OEH~lEP.T + BI~EH~IE~:T RN: 0~ 23~7~41 13~15. 1~-~l 13: :~7 #~gl~! P. O2~11 PAT~NT
ATTY. REF. P95,3119 n~r. N~T~OD OF ~N~ ~RAP~

~A~K~OUND OF T~ v~ ON
The invention is dlrected to a hormonal me~hod for acne therapy, wherein two hormone ~onstituents are packa~ed ~pa~ially separated in a packaging unit for chronologically sequential, oral adm$~1~tration. ~ach hormonal constituent comprises a plurality of daily hormone units accommoda~ed spatially separately and individuAlly re~ d~le in the packaging unit. The ~irst of ~he hormone constituents contains only ~n estrogen prepa~a~ion as active hormonal substance which effeats an increase in the ~exu~l hormone-bonding globulins (SHBG). Th~ second hormone constituent contains an es~rogen preparation and an anti-androgen preparatlon in combination. The method of the invention comprises controlling acne by administering the hormonal constituents to a hum~n patient ~u~fering from acne.
Hormonal me~n~ for treating acne has ~een known for a long time, this being available as co~bina~ion prepara-tion ~or ~ases of ~eborrhea, acne and alopecia ~ndro-geneti~a as well as for less se~ious cases of hirsutism.
The prior mixed hormone ~onstituent~ contain 2 mg cypro-~eroneacetate as ~nti-~ndrogen preparati~n and 35 ~g ethinyl e~tradiol as ~n es~rogen pr~para~ion. A combina-tion preparation with 2 mg ~hloromadinone~et~te and 50 ~g me~ranol has a similar ~ffe~t.
2~ The ~now~n hormonal regimens for acne therapy, as se~
forth above, ~re a matter of combination prepAra~io~s that are also e~ective as ovulation inhibitors in ~ddition to their e~ficacy in combatting acne. In~of~r as the desire~
cycle duration amounts th 28 days, these hormones are admlnistered for 21 days, whereby ~he hormone ~o~blnations are given in 21 daily ~nits, followed by a seven-d~y pause in which no admin~stration of hormone is given. Thi~ pause VC~ EH~lERT + BOEHMERT P~ 01S1~37~41 1g~57 12-21 13: 37 #~;gl21 F .12~
.. . . .. ., . . . ., .. ., .. , . _ . . _ . . .. . . ..... .. ... . .
2l66l2l . .

is followed by a wlthd~awal ~leeding that simulates ~he natural menstru~l ble~dlng.
The prior hormonal ther~pies have definitely pro~en them~elves; however, a further improvement in the ability to ~e able ~o ~ombat acne is 3till desired.
German ~ett~rs Paten~ ~1 04 3B5 dis~lose~ an ovulation-inhibitlng means for hormonal contracep~ion having two hormone con~tituents packaged ~patially separa~ed in a packagin~ unit ~or chronologically sequen-tial, oral admini~tration, each hormone constituent beingre~pectively composed of a plurality o~ ~ily hormone units accom~odated ~patially sep~ratel~ ~nd individually ~e~v-able in thq packaging unit, whereby a first ~f the hormone constituents çontain~ essentially only ~n estrogen prepara-tion as act~ve horm~nal subætan~e that effe~ts a disturb-ance of the follicle stimulation and the second hormon~
constituent contains a combination of an es~rogen prepara-tion and a ~estagen preparation in a dose at least adequate to inhibit ovulati~n, whe~by the ~o~al nu~ber of daily hor~ne units is equal to the total number of days in the desired cy~le, ~he El~st hormone constituent compriseæ 5 through 14 d~lly unt,t~ and the second hormone con6tituent ~omp~ises 23 throug!- 14 dally uni~s, where~y the plurality ~f ~aily units of the first hormone constituent is lower ~5 than the pl~rality of daily units o~ the second hormone ~onstituent.
In this kn~wn ovul~ti~n-inhiblting method, the estrogen preparation can, for ex~ple, comprise ethinyl estradiol and the g6stagen or anti-androgen prep2r~tion can ~ompxi~e cyproteroneacetate or chloromadinoneacet~te.
It is ~:h2~ra~eristi~ o~ the a.bov~-de~cri}~ed ovula~ion-inhi~iting me~ns th~t the adminis~ra~ion ensues without pAuse wi~h a constant estrogen dose, as a result whereof a uniform e8trogen level is maintained.

IJC~ EH~ERT + E~ EH~EF~T R~ 01~161;~337~41 l~lg5. 1~ 37 #~ )4~

SUMMARY OF THE INVENTIO~
The object of the lnvention is to develop an imp~oved hormonal method for tre~tlng ~cne such that an improved a~ne ~her~py i~ enabled.
This o~ject i~ invPnti~ely achieved in th~t the total plurality of daily unit~ is equal ~o ~he t~tal plurality of d~y~ in the desired cycle, in that the first hormon~ constituent comprises 5 ~hrough 14 daily units and ~he ~econd hormone ~onstituent ~omprises ~3 through 14 daily units; and in th~t the plurality of daily uni~5 of the first hormone constituent i5 lower than the plurali~y of daily units of th~ ~econd hormone ~ons~ituent.
It can thereby ~e provided that at least one of the e~trogen preparatlon~ aomprises at least one component from the group encompassing ethinyl e~tradiol, mestranol, o~her syntheti~ es~rogens as well as hormon~l eompounds that ~uickly ~plit off ~t l~ast one of the aforementione~
ho~mone aomponents after ingestion.
The inven~ion also provides that the e~rogen preparations of the first and of the se~ond hormone con~tituen~ ~re identical in terms of their type and/or their effe~tive ~ose.
It c~n ~lso be inven~vely provided that the first and the second hormone con~tituents comprise ethinyl ~S estradiol wi~h ~ concentration of 15 - 35 ~g per dally unit as estrogen preparation.
The in~ention also proposes that the an~i-androgen preparation comprise~ cyproteroneacetate.
It Gan al~o be provided ac~ording to ~he inven~ion th~t the anti-androgen prepar~tlon cont~in~ abou~ mg cyproteroneacet~te per d~ily unit.
A further embodiment of the invention is ~h~ac-teri~ed in that the anti-androgen prep~ration comprises chlorodinoneacetate.

'JCI~I:BClEHMEF:T + E:OEH~`1EF~T I~lN:OE~ 337g41 1~ 1 13:37 #6~1~! p.lZ15~11 _, _ _ _ _ .... . . . . . . . . . .. . . .. . . . . . .. . . . .. . . ... . .

T~e invention also prop~6e~ that the anti-androgen preparation ao~prises approximately 1-3 mg chloro~inone-acetate per d~ily uni~.
The invent~on thereby also propose~ that the anti-andrcgen preparation oo~p~ises dieneogest.
It ~an also be pr~vi~ed that the anti-androgen preparation compri~es approxi~ately 1-3 mg dieneogest per daily unit.
I~ ¢an also be ~nventively provided that thç total numbe~ o~ daily uni~s amounts to Z8.
The ~n~ention also preferably p~ovide~ that the first hormone consti~Uent comprises at mos~ 10 d~ily ~nlts.
In a pre~erred embodimen~ of the method, the firs~
hormone constituent comprises 7 daily units and the sec~n~
hormone constituent comprise~ 21 daily units.
Finally, th~ in~ention also teach~s the employment of the hormonal means of the invention fo~ Acne ~herapy.
The invention is ~ased on ~he surp~i6ing perception that one succeeds in ena~ing an improved acne ~her~py when, in conformi~y with the ovulation-inhibiting means of Ge~man ~etters Patent 41 ~4 385, any ~nd all pau~e in administration i~ foregone and a uniform estrogen level, particularly on the basis of ethinyl estradiol, is main-tained oVer the entire cycle of, ~or exa~ple, 2a days. As a res~lt ~hereof, an es~entially constantly elevated concentration of SHBG is effect4d tha~ int~epts the free t~sto~terone, the acne being f~vo~bl~ influenced as a result ther~of.
0~ course, an ovula~l~n-inhi~i~lng ef~ect corres-ponding to the ovulation-inhibiting means of German Pub-lis~ed Application 41 04 38S al~o oc:curs given the mean6 of the invention, which ~an be po~entially desirablç. The other advantages of maintaining a uniform estrogen level as des~ribed in German Let~ers Patent 41 04 385, this being achieve~ ~y avoidlng any and all pause in ad~ini~tration~

E~CIEHI~IERT l E0EH~IERT RN:0001513~337g41 1~15. 12-21 13:38 #680 F.0C;/ll . .... .. .... . ... ... . .. ... ... ............ . .. . .. . ..... ... .. .. .

are also ~eneficially achie~ed in the administration of the means of the invention.
Further features of the invention derive ~rom the ~ollowing de~cription wherein exemplary embodiments are S explained.

ECIEHMEPT + E:OEHI~IE~T F~ ;l32337~4l 1~5,1~-21 13:~ #6~ P.07/11 ............... . .. .. ~ .. . . .. .. .. ... ..... ....... ........ .... ... .... .... ... ..

2 ~ 66 1 2 1 DE~ATT.P.n DESCRIPTION OF THE INVENTION
Exam~le 1:
A oo~ination prepar~tion that c~ntained 7 d~ily unit6 of respectively 20 ~g ethinyl e~tra~iol each as well 5 as ~1 dai}y units o~ re~pe~tiv~ly ZO ~g eth$nyl estradiol and 2 mg ~yproteroneac~ta~e w~ employed for aone therapy.
The ~ormonal regimen was administerçd to a human patien~
s~f~ering from acne for a year and exhibited a very good a~ne-co~batting effect.
ExamPle. ~:
A combination preparatlon that comprised 7 daily units of respe~tl~ely 20 ~g ethinyl ectradiol each and 21 daily units o~ respe~tively 2~ ~g e~hinyl est~adiol and mg chloromadinoneacetate was employed for acne the~py.
Th~ eff$c~y ~orrespon~ed to that of Example 1.
ExamDle 3 A ~om~ination preparation that comprised 7 daily uni~s of respectively 20 ~ ethinyl ectradiol each and 21 daLly unitæ of respectively 20 ~g ethinyl estradiol and 2 mg dieneogest each was employed ~s preparation $or a¢ne therapy. ~he ~iaaay corresponded to that o~ Example 1 and Example 2.
Both individually a~ well as in arbitrary ~ombina-tion, the featureæ of the invention disclosed in the above 25 spe~ifi~ation and in the claims can be critical for reallzing the various e~odi~ents of the invention~

Claims (14)

WE CLAIM:
.
1. A method for controlling acne comprising:
administering to a human patient suffering from acne two hormone constituents packaged in a packaging unit intended for chronological sequential oral administration, said constituents each comprising a plurality of daily hormone units accommodated specially separate in and individually removable from the packaging unit, wherein a first hormone constituent comprises an estrogen preparation as the sole active hormonal substance which effects an increase in sexual hormone-binding globulins of the patient and a second hormone constituent comprising a combination of an estrogen preparation and an anti-androgen prepara-tion, wherein the total of the daily units is equal to a total number of days in a cycle and the total daily units of the first hormonal constituent is less than the total daily units of the second hormonal constituent.
2. A method as defined in Claim 1, wherein the total number of days in the cycle is 28 and the packaging unit contains 5 to 14 daily units of the first hormone constituent and 23 to 14 daily units of the second hormonal constituent.
3. A method as defined in Claim 1, wherein at least one of the estrogen preparations comprises a com-ponent selected from the group consisting of ethinyl estradiol, mestranol, synthetic, androgens, and hormonal compounds which release ethinyl estradiol, mestranol or synthetic estrogen after ingestion.
4. A method as defined in Claim 1, wherein the estrogen preparation of the first hormone constituent and the second hormone constituent are the same.
5. A method as defined in Claim 1, wherein the estrogen preparation of the first and the second hormone constituents is ethinyl estradiol provided in a concen-tration of from about 15 to about 35 µg per daily unit.
6. A method as defined in Claim 1, wherein in the second hormone constituent the anti-androgen preparation comprises cyproteroneacetate.
7. A method as defined in Claim 1, wherein the anti-androgen preparation comprises from about 1 to about 2 mg cyproteroneacetate per daily unit.
8. A method as defined in Claim 1, wherein the anti-androgen preparation comprises chlorodinoacetate.
9. A method according to Claim 1, wherein the anti-androgen preparation comprises from about 1 to about 3 mg chlorodinoneacetate per daily unit.
10. A method according to Claim 1, wherein the anti-androgen preparation comprises dieneogest.
11. A method according to Claim 1, wherein the anti-androgen preparation comprises from about 1 to about 3 mg dioneogest per daily unit.
12. A method according to Claim 1, wherein the total number of days in the cycle is 28 and the number of daily units of the first hormone constituent is at most 10 daily units.
13. A method as defined in Claim 1, wherein the total number of days in the cycle is 28 and the packaging units contains about 7 daily units of the first hormone constituent and about 21 daily units of the second hormone constituent.
14. A packaged hormonal composition for use in controlling acne comprising:
packaging unit subdivided into separate compartments, each compartment adapted to individually, removably receive a daily dosage unit of a hormone constituent, a plurality of daily dosage units of a first hormone constituent disposed in some of the compartments and a plurality of daily dosage units of a second hormone constituent disposed in others of said compartment, the total number of compartments and daily dosage units being equal to a total number of days in a cycle, the first hormone constituent comprising an estrogen preparation as the sole active hormonal substance which is effective to provide an increase in sexual hormone-binding globulins, the second hormone constituent comprising a combination of an estrogen preparation and an anti-androgen preparation, and wherein the total daily dosage units of the first hormonal constituent is less than the total of the daily dosage units of the second hormonal constituent.
CA002166121A 1993-07-01 1994-06-03 Hormonal method of acne therapy Abandoned CA2166121A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DEP4321957.8-41 1993-07-01
DE4321957A DE4321957C2 (en) 1993-07-01 1993-07-01 Use of a hormonal agent to treat acne
PCT/DE1994/000629 WO1995001180A1 (en) 1993-07-01 1994-06-03 Hormonal agent for the treatment of acne and its use

Publications (1)

Publication Number Publication Date
CA2166121A1 true CA2166121A1 (en) 1995-01-12

Family

ID=6491735

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002166121A Abandoned CA2166121A1 (en) 1993-07-01 1994-06-03 Hormonal method of acne therapy

Country Status (14)

Country Link
EP (1) EP0710111B1 (en)
JP (1) JPH09500112A (en)
AT (1) ATE205716T1 (en)
AU (1) AU695894B2 (en)
BR (1) BR9407340A (en)
CA (1) CA2166121A1 (en)
DE (2) DE4321957C2 (en)
DK (1) DK0710111T3 (en)
ES (1) ES2164103T3 (en)
HU (1) HUT73234A (en)
NO (1) NO308586B1 (en)
PT (1) PT710111E (en)
UA (1) UA43337C2 (en)
WO (1) WO1995001180A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19534209A1 (en) * 1995-09-15 1997-03-20 Jenapharm Gmbh Hormonal agent for the treatment of the skin
EP1048673A4 (en) * 1997-12-26 2002-10-25 Mochida Pharm Co Ltd Neovascularization inhibitor containing dienogest as the active ingredient
DE102004026670A1 (en) 2004-05-28 2005-12-15 Grünenthal GmbH Hormonal contraceptive containing a combination of ethinylestradiol and chlormadinone acetate
DE102004026671A1 (en) 2004-05-28 2005-12-15 Grünenthal GmbH Dosage form for hormonal contraception
DE102004026679A1 (en) * 2004-05-28 2005-12-15 Grünenthal GmbH Hormonal contraceptive containing a combination of ethinylestradiol and chlormadinone acetate
DE102006003508A1 (en) * 2006-01-24 2007-07-26 Grünenthal GmbH Use of hormone combination of estrogen from ethinyl estradiol and metabolites of chlormadinone acetate, with chlormadione acetate as gestagen components, for producing medicament e.g. for preventing menstruation cycle-dependent mood
DE102006003509A1 (en) * 2006-01-24 2007-07-26 Grünenthal GmbH Drug delivery system, for hormonal contraception, comprises hormone-containing daily unit, which exhibits estrogen from ethinyl estradiol and estradiol and from metabolite of the chlormadinone acetate optionally with gestagen component

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GR79447B (en) * 1982-12-31 1984-10-30 Mortimer Christopher H Dr
DE3442857A1 (en) * 1984-11-22 1986-05-22 Schering AG, 1000 Berlin und 4709 Bergkamen Composition for the treatment of androgenisation symptoms in women
DE3916112A1 (en) * 1989-05-16 1990-11-22 Schering Ag DIHYDROSPIRORENONE AS AN ANTIANDROGEN
DE4104385C1 (en) * 1991-02-09 1992-08-13 Marika Dr.Med. 6509 Framersheim De Ehrlich

Also Published As

Publication number Publication date
ATE205716T1 (en) 2001-10-15
EP0710111B1 (en) 2001-09-19
AU695894B2 (en) 1998-08-27
EP0710111A1 (en) 1996-05-08
JPH09500112A (en) 1997-01-07
DE59409869D1 (en) 2001-10-25
BR9407340A (en) 1996-10-08
NO308586B1 (en) 2000-10-02
WO1995001180A1 (en) 1995-01-12
ES2164103T3 (en) 2002-02-16
UA43337C2 (en) 2001-12-17
DE4321957A1 (en) 1995-01-12
PT710111E (en) 2002-02-28
HUT73234A (en) 1996-07-29
HU9503770D0 (en) 1996-02-28
AU6840894A (en) 1995-01-24
DE4321957C2 (en) 1995-09-28
DK0710111T3 (en) 2001-12-10
NO955347L (en) 1995-12-29
NO955347D0 (en) 1995-12-29

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Legal Events

Date Code Title Description
FZDE Discontinued