Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1998-06-05
2000-05-09
Azpuru, Carlos A.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424435, A61F 1302
Patent
active
060600772
DESCRIPTION:
BRIEF SUMMARY
The invention concerns a medicament for local, essentially non systemic, treatment of vaginal dryness.
The problems of vaginal dryness, in particular in the menopausal woman, are known: dyspareunia, urogenital atrophy which can cause problems with the urinary function, and risks of infection due to an insufficiently developed flora.
One aim of the invention is to provide a medicament which is suitable for essentially non systemic treatment, which is thus distinguished from substitutive hormonotherapy treatments where the hormone can be administered per os, transcutaneously or intravaginally.
In contrast, European patent EP-A-0 103 995 and U.S. Pat. No. 5,019,395 describe galenical formulations for general hormonotherapy where the compositions contain high doses of active principle, respectively 4% to 15% by weight and 0.1% to 8% by weight of the medicament.
In particular, the medicament of the invention is distinguished from vaginally administered substitutive hormonotherapy medicaments in the form, for example, of vaginal creams, tablets, or suppositories which contain high doses of estrogens. Such cases simply take advantage of the fact that systemic passage is better when administered vaginally than when administered orally, in particular because of the absence of estrogen metabolization when administered vaginally.
In contrast, the invention seeks to provide a local treatment with minimal or zero systemic passage by direct use of a natural estrogen, in particular 17.beta.-estradiol, to alleviate local problems by avoiding secondary systemic effects which may occur in certain patients, in particular the occurrence of endometrial hyperplasia.
Local treatments of this type have already been proposed, for example in the form of a vaginal ring in the form of a torus comprising an estrogen which diffuses through the porous membrane of the ring, thus enabling continuous release over a long period.
In common with all intravaginal devices, however, such rings have the disadvantage of necessitating the presence of a non degradable foreign body in the organism and of requiring insertion and removal manipulations.
A galenical formulation comprising 17.beta.-estradiol in the form of vaginal tablets which are administered daily has also been proposed for such local treatment. Such tablets contain a matrix comprising an excipient such as a cellulosic polymer which absorbs traces of residual vaginal moisture to impregnate the matrix containing the active principle and gradually release the latter.
However, because of their particular galenical form, the dosage of such tablets must be relatively high to obtain the desired results, typically a dosage of 25 micrograms (.mu.g) of 17.beta.-estradiol per tablet (one tablet corresponds to one unit dose) to provide the desired cytological, histological and clinical improvement in the vaginal mucous membrane. Because of this relatively high dose, endometrial proliferation was noted in certain patients during clinical studies, indicating systemic passage of 17.beta.-estradiol: see in particular C. Fielding et al., "Preoperative Treatment with Estradiol in Women Scheduled for Vaginal Operation for Genital Prolapse. A Randomised, Double-Blind Trial", Maturitas, 1992, 15, 241-249.
One aim of the present invention is to propose a medicament of the above type with a particular galenical formulation which enables the dosage of 17.beta.-estradiol to be reduced so as to avoid systemic passage despite the extreme sensitivity of the vaginal mucous membrane to estrogens, while ensuring satisfactory trophic effectiveness.
According to the invention, this medicament is characterized by a unit galenical formulation comprising a natural estrogen selected from 17.beta.-estradiol and its salts in solution or in suspension in a lipophilic agent, with an estrogen content which corresponds to an equivalent unit dose of at most 15 .mu.g, preferably less than 10 .mu.g, of 17.beta.-estradiol, a hydrophilic gel-forming bioadhesive agent, a gelling agent for the lipophilic agent and a hydrodispersible
REFERENCES:
patent: 5019395 (1991-05-01), Mahjour et al.
Azpuru Carlos A.
Laboratoire Innothera, Societe Anonyme
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