Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1998-06-03
2000-02-22
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
514170, 514843, A61K 920, A61K 3156
Patent
active
060277491
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The present invention relates to a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days, and relates also to a corresponding pack (contraceptive kit) containing that combined preparation, and to a contraceptive method that uses the above contraceptive preparation.
Oral contraceptives in the form of combined preparations have been known since 1960 as so-called monophase preparations. Those preparations consist of 21 unit doses that comprise active ingredient and 7 tablets or dragees that are active ingredient-free. The daily unit dose is composed of an oestrogen and gestagen. In monophase preparations the dose of active ingredient to be administered daily is the same in each unit dose. If the dose that is to be administered daily of the active components in the individual unit doses is different in individual sections over the administration cycle, then the preparation is referred to as a so-called multi-phase preparation. Triquilar.RTM. may be mentioned as an especially well-known example (DE-AS 23 65 103).
As a result of the development of new, more active gestagens than those contained in the first oral contraceptives, a continuous reduction of the daily dose of gestagen has been possible. It has also been possible for the daily dose of oestrogen to be reduced although, as before, the oestrogen contained in hormonal contraceptives is usually ethynyloestradiol. In the development of new, improved oral contraceptives, the following three factors have been (and are) dominant: bleeding and component. The daily dosage amount of that component corresponds at least to the threshold dose considered necessary for the gestagen in question to inhibit ovulation. The ethynyloestradiol usually used as the oestrogen in combined preparations should increase the ovulation-inhibiting effect of the gestagen and in particular ensure stability of the cycle. In the case of administration of ethynyloestradiol alone, the daily dose that has to be used in order to inhibit ovulation is 100 .mu.g.
Combined preparations with the most recent generation of gestagens are, for example, the monophase preparations Femovan (DE-PS 2 546 062) and Marvelon (DE-OS 2 361 120). Milvane.RTM. may be mentioned as an example of a multi-phase preparation in which the unit doses contain a gestagen of the most recent generation, namely gestodene (EP-0 148 724). In those three-phase preparations, usually 4-6 dragees are administered in the first phase, each dragee comprising a low dose of oestrogen and a low dose of gestagen. In the second phase of 4-6 dragees, each unit dose comprises an oestrogen in the same dose or a dose that is slightly increased (up to a maximum of twice) and a gestagen in the same dose or a in a dose that is slightly increased (up to a maximum of 1.5 times). In a third phase of 9-11 units, each dragee comprises an oestrogen in the same dose or a dose that is slightly reduced, at most reduced to the initial amount, and a gestagen in a dose that is further increased, to a maximum of 3 times the initial amount. 7 pill-free days then follow.
Recently, multi-phase combined preparations have been proposed that may provide an extended administration of active ingredient-containing unit doses, that is to say of up to 24 days in the 28-day cycle. In those preparations the daily dose of gestagen either increases f
REFERENCES:
patent: 5756490 (1998-05-01), Lachnit et al.
Klemann Walter
Schmidt-Gollwitzer Karin
Schering AG
Spear James M.
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