Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1998-12-23
2001-05-01
MacMillan, Keith D. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S170000, C514S178000, C514S182000, C514S859000, C514S864000
Reexamination Certificate
active
06225299
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a hormonal agent or composition for skin treatment, especially seborrhea,
Acne vulgaris
, androgenically conditioned alopecia and androgenic symptoms of women.
In central Europe the incidence of hormonally conditioned skin diseases, such as acne, seborrhea and hirsutism, is estimated at 35 to 50%. These illnesses appear primarily in young men and women after puberty who are exposed to considerable suffering because of them (H. Hagen, et al, Klinische Erfassumg antiandrogener Effekte von Dienogest {Clinical Determination of antiandrogenic effects of dienogest}, pp. 223-230 in “Dienogest-Präklinik und Klinik eines neuen Gestagens”, A. Teichmann, ed, Walter de Gruyter Verlag, Berlin, N.Y., 1995).
The sebaceous gland activity is considerably influenced by hormones. Testosterone and dihydrotestosterones are responsible for the sebocyte proliferation and sebogenesis and provide, as a result, the driving force for sebogenesis. An interaction with androgen receptors, which are localized in human skin (acne areas, such as the face, upper breast portions, the V-shaped region of the back and the outer sides of the upper arms), especially the sebaceous gland and sebaceous gland follicle, is, among other things, a prerequisite for this(R. Choudhry, et al, “Localization of androgen receptors in human skin by immunohistochemistry: implications for the hormonal regulation of hair growth, sebaceous gland and sweat glands”, in J. Endocr. 133, pp. 467-475(1992); M. E. Sawaya, “Purification of androgen receptors in human sebocytes and hair”, in J. Invest. Dermat. 98, pp. 92-96(1992).
Continuous sebum production increases in acne patients depending on the androgen secretions and the peripheral response of the end organs and reaches its highest value in
Acne conglobata.
A hormonal agent or composition which is described in German Patent DE-PS 43 21 957 is used for acne therapy. This hormonal agent is a composition which is taken orally. Because of its systemic action undesirable effects and material accumulation occur in acne patients. Besides the hormonal treatment of acne it is also known to stimulate hair growth. In German Patent Document DE 36 15 396 a combination preparation comprising a hair tonic including cyproteron acetate in hair tonic is used as a combined preparation for treating the scalp skin and for promotion of hair growth.
The action of cyproteron acetate and chlormadinon acetate during therapeutic application is based on a centrally mediated antigonadotropic effect. Because of that an acne therapy and/or treatment of alopecia in humans is not possible with these active ingredients. Furthermore cyproteronic acetate and chlormadinon acetate causes a peripheral competitive androgen receptor blockage in acne of women (Ch. Luderschmidt, “Die Akne der Frau{The Acne of Women}” in Gynäkol. Prax., 19, pp. 479-488, 1995).
SUMMARY OF THE INVENTION
It is an object of the present invention to provide a pharmaceutical composition, especially for the treatment of acne, seborrhea or alopecia, in which the systemic effect of the hormonal agent acting as active ingredient is prevented and a direct peripheral effect is produced at the place of occurrence on the skin (seborrhea, acne areas, alopecia, androgenic symptoms of women) and which may be used in both women as well as men.
It is another object of the invention to still further limit and/or to hinder the permeation of the active ingredient through the skin by suitable galenic measures. Because of these measures the penetration of the skin by the active ingredient is promoted instead of hindered. However the permeation by the substances is controlled by the formulation so that the active material is not available or only slightly available systemically in order to avoid or minimize undesirable effects in the organism.
It is an additional object of the invention to provide a manufacturing or production process for the pharmaceutical composition in which the active ingredient is stable and prepared thermodynamically active so that, after it is applied to the skin, it penetrates the skin very rapidly and to a great extent, however slightly or only in a very much reduced extent by the most diverse penetration paths, e.g. transfollicularly, transglandularly and transepidermally. This process should further guarantee that the active ingredient does not come into contact with water, reactive solvents or surfactants or light for a long period of time.
Particularly it is an object of the present invention to include defatting or deoiling substances, like those described in German Patent Document DE 42 29 820, which promote the penetration of hormonal active ingredients in the skin, for a local, but nonsystemically effective, application. The use of defatting or deoiling substances should prevent or hinder the stimulation of the skin to overproduce oil or fat because of oil or fat removal.
The method of applying the pharmaceutical composition topically after it is prepared by the preparative methods according to the invention releases the active ingredient as fast as possible and as completely as possible, promotes its passage into the skin tissue while avoiding absorption and thus introduces no undesirable reciprocal action (interactions) with the biological tissue, as are known, for example, for certain solvents and surfactants.
According to the invention these objects are attained by a method of topical treatment of
Acne vulgaris
, seborrhea, androgonically conditioned alopecia and androgenic symptoms of women comprising the step of applying locally on the skin a pharmaceutical composition containing the antiandrogenically acting gestogen, dienogest, or a combination of dienogest and an estrogen, especially 17&agr;-estradiol or estriol.
REFERENCES:
patent: 4720489 (1988-01-01), Shander
patent: 5055456 (1991-10-01), Harris et al.
patent: 5633242 (1997-05-01), Oettel et al.
patent: 2840144 (1980-03-01), None
Neumann et al., Androgen antagonists, Gynakologe, vol. 12(4), pp. 228-242, 1979.*
Erdmann et al., Ovarian suppression using diane 30/50.rtm., Geburtshilfe und Frauenheilkunde, vol. 54(11) pp. 627-633, 1994.*
Grob et al., The genuine article (r) number., Helvetica Chimica Acta, vol. 80 (2) pp. 566-585, 1997.*
Nolting, Dermatologic therapy unit anti-androgens, Fortschritte Der Medizin, vol. 95(12) pp. 825-828, 1977.*
M. Faure, E. Drapier-Faure: “Bilan Hormonal Chez Une Femme Presentant Une Acne Ou Une Alopecie”, in Rev. Fr. Gynecol. Obstet. 1992, 87, 6, pp. 331-334.
“Haarasufall, Neuere Therapieansaetze Bei Androgenetischer Alopezie”, by Wolf Nuernberg, in Deutsche Apotheker Zeitung, 132, Nr. 10, Mar. 5, 1992, pp. 457-461.
Dittgen Michael
Golbs Siegfried
Graser Thomas
Luderschmidt Christoph
Oettel Michael
JENAPHARM GmbH & Co. KG
Kim V
MacMillan Keith D.
Striker Michael J.
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