Hormonal contraceptive product

Abstract

The present invention relates to a hormonal contraceptive product having two hormonal components, an estrogen and a gestagen, and a method for the continuous suppression of the menstrual cycle by uninterrupted administration of the product of the invention.

Description

[0001] The application is a continuation of U.S. application Ser. No. 09 / 508,648, filed Jun. 5, 2000, which is the U.S. National Phase under 35 U.S.C. .sctn.371 of International Application PCT / DE98 / 02636, filed Sep. 11, 1998, which claims priority to German Application No. DE 19739916.9, filed Sep. 11, 1997.BACKGROUND OF THE INVENTION 1. Field of the Invention[0002] The present invention relates to a hormonal contraceptive product with two hormonal components, the use thereof and a hormonal contraception process.[0003] 2. Description of the Related Art[0004] Since hormonal contraceptives became available in the 1960's, a number of hormonal components have been investigated with regards to their suitability in the most varied administration diagrams. A fundamental subdivision into combination and sequential products is possible.[0005] For example, if the desired cycle time is 28 days, in the case of the known combination products administration takes place over 21 days in a constant...

AI Technical Summary

Benefits of technology

[0031] The invention is based on the surprising finding that as a result of the continuous, combined administration of a product comprising two hormonal components, namely a first hormonal component comprising at least one gestagen and a second hormonal component comprising at least one estrogen, a high contraceptive reliability can be achieved.

[0040] As a result of the estrogen component, respectively by specific action of hydrophobic ring substances with an estrogen-like action, there can be a suppression of gonadotropins. This is desirable. The resulting suppression of the ovarial function is compensated by an adequate substitution of estrogen action. This prevents the development of osteoporosis, the favourable vascular effects of estrogens are maintained and there is no unfavourable influence to the lipid metabolism. By interrupting the cycle-dependent instability in the hormone system, the premenstrual syndrome can be favourably influenced. In addition, the physiological equilibrium of the coagulation system is not disturbed, because the unstable equilibrium in which the coagulation system occurs is not activated and deactivated by the up and down of hormone fluctuations. Thus, the hormonal product according to the invention is particularly suitable for women aged more than 40, where the risk of circulatory disturbances is known to increase with increasing age. There is also a reduction in the thrombosis risk, which has of late acquired considerable significance in contraceptive therapy.

[0041] It has surprisingly also been found that on administering the product according to the invention there is a reliable continuous suppression of the menstrual cycle and menstruation in the case of a very low dosage. Without wishing to be bound by this explanation, the combination of the two indicated hormonal components and in particular the low estrogen dosage would appear to be suitable for eliminating the otherwise conventional side effects of ethinyl estradiol and to drop below the administrations of more than 15 .mu.g of ethinyl estradiol otherwise considered typically necessary in prior art contraceptives.

[0048] Mutations on the second allele particularly frequently occur in given phases of the cell cycle, namely in the GI phase. Every four weeks the menstrual cycle drives the breast cell in a cell cycle, "opens" the genome for mutations, which are either repaired or apoptotically "removed". Under the conditions of the conventional combined or sequential contraception treatment a woman can have 500 to 700 cycles over her life span, whereas under natural conditions a women has a maximum of 20 to 30 cycles. Thus, in an unusually frequently number of cell cycles over in each case 8 days a considerable mutation risk is introduced into the stimulated breast tissue. If the menstrual cycle is suppressed, as is possible with the product according to the invention, the breast cells are brought into a "rest phase" and it is scientifically ensured that in the rest phase less cancerogenic mutations are introduced into a tissue than in a stimulated tissue. This reduces by a multiple mutagenesis, i.e. the breast cancer risk.

Problems solved by technology

Only in the case of substitution products in the menopause of older women have hormones been administered throughout the cycle, e.g. in the sequence 10 days estrogen product, 11 days combination of estrogen and gestagen product, 7 days estrogen product, 7 days estrogen product in a particularly low dosage, but said substitution products are unsuitable for ovulation inhibition.

The sequential products used in substitution therapy are in particular unsuitable for contraception because the natural estradiol does not prevent ovulation in the dosage administered and the phase in which gestagen is administered is too short, being only 11 days.

If a further mutation occurs in a specific organ cell on the second allele, then uncontrolled, malignant growth can occur.

Thus, in an unusually frequently number of cell cycles over in each case 8 days a considerable mutation risk is introduced into the stimulated breast tissue.