Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1994-11-07
1996-11-26
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514182, A61K 3156
Patent
active
055785883
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/DE93/00397 filed Apr. 30, 1993. The invention relates to a medicament for increasing the testosterone level in humans.
The main action of the steroid hormone testosterone is the intensifying of the primary and secondary sex characters of man, as well as the maintaining of the functions associated therewith. Apart from this main effect testosterone has a number of secondary effects, which are of great importance for the stressability and performance characteristics of the human organism. These include the maintaining of an anabolic metabolic situation, the restoration of the performance of man following exhausting exercise and increasing the psychophysiological stressability and stress resistance.
The action mechanisms of testosterone have been investigated in detail. The secondary effects on the psychophysiological state have, according to the latest research, been attributed to the presence of testosterone receptors in the central nervous system.
Over 90% of the testosterone in the blood is bound to protein and the biologically active component is free testosterone representing 4 to 8% of the total concentration in the blood. The testosterone concentration in the blood is subject to a physiological daily cycle (maximum concentration in the morning) a seasonal cycle (lowest concentration in May) and influences by living circumstances and ageing processes.
The overall testosterone concentration in the blood is individually very stable under normal conditions. High physical effort, long-lasting stress situations and unfavourable diet lower the blood level. With increasing age and in particular from about 35 in man there is a reduction of the free testosterone concentration. These changes lead to a reduced, general performance, to higher time requirements for restoring the organism after exhaustive exercise and to a reduction of the psychophysiological stressability and stress resistance. Research on physically and cyclically highly stressed persons have revealed that a rise in the testosterone level in the upper part of the individual physiological fluctuation range leads to a cancelling out of this negative situation and to an increase in the general performance characteristics. However, a concentration rise above the individual, upper standard limit leads to no better therapeutic effect and instead causes side effects.
The increase in the testosterone level in humans in the sense of a substitution has consequently become part of preventative and therapeutic concepts in old-age medicine, particularly for man. The supply conventionally takes place perorally or in an oily solution in intramuscular form and in part as a depot preparation.
However, the following disadvantages are associated with these administration forms: into account for the medication; circulatory system liver--bile--intestine--liver ("first-pass effect"); doses with the resulting higher stressing of the metabolism; concentration, which via the physiological control mechanism reduces the endogenic testosterone production.
The problem of the present invention is therefore to provide a medicament for raising the testosterone level in humans, whose application is equivalent in its effect to the intramuscular supply of testosterone, which avoids the aforementioned disadvantages, requires a much lower dose and permits a stressing of the secondary action on the central nervous system.
According to the invention this problem is solved by a medicament having a content of at least one precursor of testosterone and which is preferably androstendione, progesterone or 17-.alpha.-hydroxy progesterone.
A particularly advantageous embodiment of the invention is characterized by a galenic preparation, which allows the supply by per nasal application using a dosing spray and having a preferred content of 3.5 to 15 mg of active substance per pump thrust.
Alternatively thereto the medicament according to the invention can also be in the form of a sustained release drag ee, depot form or buccal tablet for peroral administration.
REFERENCES:
patent: 3284303 (1966-08-01), Meli
patent: 4877774 (1989-10-01), Pitha et al.
patent: 5053403 (1991-10-01), Orentreich et al.
Vander et al., Human Physiology, 4th Ed., 1985.
H acker R udiger
Mattern Claudia
Arrowdean Ltd.
Jordan Kimberly
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