Hormonal medicaments and their use for the correction of oestrog

Details Hormonal medicaments and their use for the correction of oestrog Hormonal medicaments and their use for the correction of oestrog

1997-04-24

1999-04-06

Spivack, Phyllis G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

A61K 3156

Patent

active

058918671

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to the field of chemotherapy.
More precisely, it relates to new pharmaceutical compositions formed from an estro-progestogenic combination for correction of estrogen deficiencies during natural or artificial menopauses.
It particularly relates to a trisequential estro-progestogenic combination, characterized in that it is made up of dosage units comprising only an oestrogen, dosage units comprising a combination of an estrogen and a progestogen and dosage units comprising only an excipient
This combination is intended for administration by the oral route, and by using a particular formulation, it has been possible to be able to use estradiol, that is to say natural estrogen, by this route.
The progestogen used is a pure progestogen, such as nomegestrol acetate. As a result, it has been found that in such a combination, nomegestrol acetate does not cancel the natural effects of estradiol, while allowing an artificial cycle of very good quality to be obtained in the menopausal woman.
It specifically relates to a new estro-progestogenic medicament for correction of estrogen deficiencies, characterized in that it is formed from three different types of dosage units, which are intended for use in successive sequences, that is to say 17.beta.-estradiol tablets, tablets comprising both 17.beta.-estradiol and nomegestrol acetate, and placebo tablets comprising only excipient.
These administration units are intended for administration in accordance with the following sequences: for fourteen consecutive days
Consequently, the 17.beta.-estradiol tablets will be administered from day D1 to day D10, the tablets of the combination of 17.beta.-estradiol and nomegestrol acetate will be administered from day D11 to day D24, and the placebo tablets will be administered from day D25 to day D30.
According to a particular embodiment, the dosage units of oestradiol comprise an amount of active principle ranging from 1 to 3 mg, the dosage units containing the combination of 17.beta.-estradiol and nomegestrol acetate comprise an amount of 17.beta.-estradiol ranging from 1 to 3 mg and an amount of nomegestrol acetate ranging from 1.5 to 6 mg. Preferably, the dosage units of estradiol comprise 1 to 2 mg of 17.beta.-estradiol and the dosage units of the estro-progestogenic combination comprise 1 to 2 mg of 17.beta.-estradiol and 2.5 to 5 mg of nomegestrol acetate. Specifically, the optimum formulations comprise 1.5 mg of 17.beta.-estradiol or a combination of 1.5 mg of 17.beta.-estradiol and 3.75 mg of nomegestrol acetate.
This sequential mode of administration is intended to compensate functional disorders caused by hypoestrogenia associated with menopause or with premenopause. In particular, it is aimed at re-establishing an endometrial cycle in menopausal women, in particular those treated with 1 or 2 mg of 17.beta.-estradiol.
35 menopausal patients were studied in order to specify the best dose of nomegestrol acetate (N) to be associated with estradiol to obtain menstrual cycles of quality with good luteal impregnation of the endometrium.
These patients were monitored in 6 different centres and received: initially, in an open trial, 17.beta.-estradiol by itself (in an amount of 1 or 2 mg/day, the gynecologist having to adjust the dosages as a function of the clinical response) for 2 months; subsequently, under blind conditions, one of the following combinations for 4 months (estradiol for 10 days, combination for the following 14 days, pause of 7 days).


______________________________________ .circle-solid. group A: O2 2mg - N5 mg (n = 6) .circle-solid. group B: O2 2mg - N2.5 mg (n = 8) .circle-solid. group C: O2 2mg - N5 mg (n = 9) .circle-solid. group D: O2 2mg - N2.5 mg (n = 7) .circle-solid. group E: O2 2mg - N1.25 mg (n = 5) ______________________________________ (O2: 17estradiol N: nomegestrol acetate)
In 6 cases, the estradiol dosage was adjusted and differed between the two treatment phases.
Two histological approaches were realized, the traditional one comprised semi-quant

REFERENCES:
Remington's Pharmaceutical Sciences (15th ed.) 1975 p. 914-915.

Affiliated with

Also associated with

Rating

Hormonal medicaments and their use for the correction of oestrog does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Hormonal medicaments and their use for the correction of oestrog, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Hormonal medicaments and their use for the correction of oestrog will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1371497