Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1994-08-31
1997-03-25
Phelan, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
514969, A61F 1300
Patent
active
056142137
DESCRIPTION:
BRIEF SUMMARY
The invention relates to the use of estriol as sole active ingredient for the production of a transdermal medicament, which continuously releases the active ingredient, for the treatment of climacteric osteoporosis.
BACKGROUND OF THE INVENTION
The loss of the female sex hormone--estrogen--in the climacteric can lead to phenomena which require therapy. Estrogens are steroid hormones which are derived from the tetracyclic C.sub.18 steroid estrane. Among the natural estrogens, one differentiates between estrone (E.sub.1), estradiol (E.sub.2) and estriol (E.sub.3), estrone and estriol being the physiologically most important. Hormone replacement with both these estrogens quickly leads to an improvement in psychological consciousness and in the long term to a favourable influence on the bone and lipoid metabolism. The last-mentioned factors represent effective prevention of diseases of the skeletal system and of illnesses of the heart circulation system. It has been proved without any doubt that E.sub.1 and E.sub.2 can prevent advancing osteoporosis in the climacteric and can slow the advance of arteriosclerotic vascular changes.
Against the said favourable effects there stands a risk, which is considered tolerable, from possible stimulating effects of the estrogens on the growth of hormone-dependent tumours of the genital tract (endometrium) and of the mammary gland. The known combination of estrogens with gestagens has the aim of minimizing the corresponding risks through the anti-proliferative action of gestagens in the uterus.
Examples of therapies with natural estrogens are: TTS), the urine of gravid mares and are a mixture of different estrogens and atrophy of the genital mucous membranes.
As explained above, a disadvantage of therapy with such types of estrogens is their ability to cause uterine cancer (endometrium carcinoma) or breast cancer.
It has been proved that, by combining the aforementioned estrogens with a gestagen, the risk to those concerned of suffering an endometrium carcinoma is reduced to 1/6th of the risk to women treated only with estrogen. Examples of such combination therapies are described in DE-A-39 10 578, DE-A-39 08 130, DE 38 36 826 and EP 0 474 374.
However, a favourable effect on mortality from mastocarcinomas is not to be expected from a corresponding estrogen-gestagen combination. (L. A. Brinton "Menopause and . . . " New York, Academy of Sciences, 592, 357-362, (1990); R. A. Lobo, "Estrogen and Cardiovascular Disease" in "Multidisciplinary Perspectives on Menopause", published by M. Flint, F. Kronenberg and W. Utian, Annals of the N.Y. Acad. of Sciences, 592, pages 286-294 (1990)).
Breast cancer is the most frequent symptom of cancer in women over all. The theory is generally accepted that the mitogenic effect of the sum of the quantities of estrogen acting upon the mammary gland during life is a decisive (risk) factor for the occurrence of a cancerous disease of this organ (cf. B. E. Henderson, R. Ross and L. Bernstein "Estrogens as a cause of human cancer", The Richard and Hinda Rosenthal Foundation Award Lecture, Cancer Res., 48, 246-253, (1988); R. Clarke, R. B. Dickson and M. E. Lippman "The role of steroid hormones and growth factors in the control of normal and malignant breast" in "Nuclear Hormone Receptors", published by M. G. Parker, Academic Press, London, pages 297-319 (1991)).
The danger of the risk increase as regards illness from breast cancer is therefore a central factor in the assessment of the benefits and risks of hormone replacement therapy (HRT-Hormon Replacement Therapy; L. A. Brinton "Menopause and the risk of breast cancer", in Multidisciplinary Perspectives on Menopause. Ann, N.Y. Academy of Sciences, published by M. Flint, F. Kronenberg and W. Utian, 592, pages 357-362 (1990) review). In the case of longer-lasting therapy, various epidemiological studies suggested an increase in the relative risk by a factor of 1.5 to 3.1, the latter being in the cases where HRT had lasted more than 10 years (Table 3, page 359 of the aforementioned paper).
The s
REFERENCES:
patent: 4738957 (1988-04-01), Laurent
patent: 5108995 (1992-04-01), Casper
patent: 5116828 (1992-05-01), Miura
Rudel et al; Oral Contraceptives: Human fertility studies and side effects, in Int. Encycl. Pharmacol of the Endocrine System CH, 34, London, Pergamon Press, 1972.
Lemon; Antimammary Cancerogenic Activity of 17.alpha.-ethinyl-estriol, Cancer, 60 2873-2881, 1987.
Follingstad; J. of the American Medical Assoc., 239, 29/30, 1978.
Blum et al; Clin. Exp. Obstet. Gynecol., 12 --1/2 1985.
Lindsay et al; Bone loss during oestriol therapy in postmenopausal women, in Maturitas 1, 279-285, 1979.
Brinton; "Menopause and . . . " N.Y. Acad. of Science, 592, pp 357-362, 1990.
Loboi; "Estrogen and Cardiovascular Disease" in Multidisciplinary Perspectives on Menopause, Annals of N.Y. Acad. of Science, 592 pp. 286-294, 1990.
Henderson, et al.; Richard and Hinda Rosenthal Fndtn Award Lecture, Cancer Research, 48, 246-253, 1988.
Clarke et al; "The role of steroid hormones . . . ", Nucl. Hormone Receptors, London Acad. Press, pp. 297-319-1991.
JP910116731 Abstract (1991).
Drugs vol. 39, No. 2, 1990 pp. 205-217 Sitruk-Ware "Estrogen Therapy During Menopause . . . Recommendations".
Maturitas, 12 (1990) 199-214 Lauritzen "clinical Use of oestrogens and progestogens".
Dittgen Michael
Elger Walter
Ernst Michael
Hubler Doris
Oettel Michael
EnTec Gesellschaft fuer Endokrinologische Technologie m.b.H.
Phelan D. Gabrielle
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