Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1997-06-03
1999-01-05
Brouillette, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424430, 424422, A61F 1300
Patent
active
058559060
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/IE/00063, filed Dec. 12, 1995.
This invention relates to intravaginal drug delivery devices for the administration of 17.beta.-oestradiol precursors. The term "17.beta.-oestradiol precursor" is intended to embrace certain compounds which can be converted into 17.beta.-oestradiol, which compounds possess physicochemical and clinical properties as defined hereinbelow. In particular, the present invention relates to intravaginal drug delivery devices for the administration of a 17.beta.-oestradiol precursor at a substantially constant rate over a prolonged period for oestrogen-requiring conditions such that either the symptoms associated with hypo-oestrogenism may be alleviated or prevented or, alternatively, fertility is controlled. More particularly, the invention relates to, but is not limited to, an intravaginal drug delivery device for the administration of a 17.beta.-oestradiol precursor for hormone replacement therapy in the human female.
Hypo-oestrogenism in the premenopausal human female may occur due to female, hypo-oestrogenism occurs as a natural consequence of the ageing process. Fertility control involves the administration of sufficient oestrogen to prevent ovulation, in effect, an induced hyper-oestrogenism. The description hereinafter primarily concerns the utility of intravaginal drug delivery devices of the invention for the alleviation or prevention of symptoms associated with hypo-oestrogenism, specifically, hormone replacement therapy, but it will be appreciated that the intravaginal drug delivery devices of the invention may also be used to induce hyper-oestrogenism, specifically, to prevent ovulation and, therefore, to act as a contraceptive.
In the normal, healthy human female, 17.beta.-oestradiol is the principal oestrogen produced by the functioning premenopausal ovary, primarily in 17.beta.-oestradiol levels vary during the monthly cycle in the premenopausal human female, being at their highest during the peri-ovulatory phase (about 1000 pmol per liter). As ageing progresses in the human female, ovulation becomes less frequent and less predictable, resulting in diminished production of 17.beta.-oestradiol. At the menopause, when irreversible failure of ovarian follicular activity occurs, 17.beta.-oestradiol production decreases dramatically to less than 20 .mu.g per day, giving circulating levels of 17.beta.-oestradiol in assuming a molecular weight of 272 for oestradiol)
Non-oral 17.beta.-oestradiol preparations intended for use in hormone replacement therapy typically deliver plasma levels of 17.beta.-oestradiol corresponding to mean levels of the hormone in the premenopausal subject at days 6 to 8 (about 200 pmol per liter) and days 8 to 10 (about 360 pmol per liter) of the cycle. For the transdermal route, which is one non-oral route, these plasma concentrations correspond to a dose of 50 .mu.g per day (low dose) to 100 .mu.g per day (high dose). This is generally accepted as the desirable non-oral dosage range in order to provide efficaceous relief of postmenopausal symptoms whilst minimising potential as: hot flushes, night sweats, insomnia, mood changes, anxiety, irritability, loss of memory and loss of concentration. following: genital tract atrophy, dyspareunia, loss of libido, urethral syndrome. joint aches, paraesthesia, dry skin, dry or brittle hair, brittle nails.
In those cases where the combination of symptoms is sufficiently severe, it is well recognised that oestrogen hormone replacement therapy is indicated. In the postmenopausal human female requiring such therapy, the aim is to restore premenopausal oestrogen balance by delivering the natural oestrogenic hormone, 17.beta.-oestradiol, to the systemic circulation in a pattern that mimics its physiological secretion, that is, recognised by practitioners that hormone replacement therapy, once initiated in the human female, may be necessary for many years extending from the onset of the menopause. A physiologically effective dose of 17.beta.-oestradiol, sufficient to provide effective
REFERENCES:
patent: 3545439 (1970-12-01), Duncan
patent: 4291014 (1981-09-01), Keith
Brouillette D. Gabrielle
Galen (Chemicals) Limited
Maioli Jay H.
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