Note: Descriptions are shown in the official language in which they were submitted.
'~JCI~ OEH~lEP.T + BI~EH~IE~:T RN: 0~ 23~7~41 13~15. 1~-~l 13: :~7 #~gl~! P. O2~11
66121
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
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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~
21 66 121
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.
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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~
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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.
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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~