Progestogen-anti-progestogen regimens

• US 20010027189A1
• Filed: 01/08/2001
• Published: 10/04/2001
• Est. Priority Date: 06/25/1996
• Status: Active Grant

• Current Assignee: N.V. Organon (Merck & Co., Inc.)
• Original Assignee: Herman Jan Tijmen Coelingh Bennink, Pieter M. Verbost
• Inventors: Verbost, Pieter M., Bennink, Herman Jan Tijmen Coelingh
• Granted Patent: US 6,506,390 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048

Abstract

Disclosed is a contraceptive and/or HRT (hormone replacement therapy) kit comprising sequential daily dosage units each containing as the sole contraceptively effective ingredient of a progestogen, or as effective ingredient for HRT a progestogen with or without an estrogen or an estrogen only, and further two or more dosage units comprising an anti-progestogen. One of the anti-progestogen is administered at the beginning and the others regularly divided throughout the cycle, preferably one only in the middle of the cycle.

Claims

1. A contraceptive and/or HRT (hormone replacement therapy) kit comprising sequential daily dosage units each containing as the sole contraceptively effective ingredient a progestogen, or as effective ingredient for HRT a progestogen with or without an estrogen or an estrogen only, and further two dosage units comprising an anti-progestogen.

2. The contraceptive and/or HRT kit of

claim 1

wherein said kit contains a total of 20 to 32 dosage units.

3. The contraceptive and/or HRT kit of

claim 1

or

2

consisting of four phases, in which the first phase is a single dosage unit containing an anti-progestogen and optionally a progestogen, the second phase containing progestogen, estrogen or a mixture thereof, the third phase containing an anti-progestogen and optionally a progestogen, and the fourth phase containing progestogen, estrogen or a mixture thereof.

4. The contraceptive and/or HRT kit of

claim 1

consisting of four phases, in which the first phase is a single dosage unit containing an anti-progestogen and optionally a progestogen, the second phase consists of 9-15 dosage units containing progestogen, estrogen or a mixture thereof, the third phase is a single dosage unit containing an anti-progestogen and optionally a progestogen, and the fourth phase consists of 9-15 dosage units containing progestogen, estrogen or a mixture thereof.

6. The contraceptive and/or HRT kit of

claim 3

,

4

or 5, further comprising placebo dosage units.

7. The contraceptive and/or HRT kit of any one of

claims 3

to

6

, wherein the dosage of the anti-progestogen in the third phase and, if present, subsequent phases, is lower than the dosage of the anti-progestogen in the first phase.

8. The contraceptive and/or HRT kit of any one of claims 1-7, wherein the progestogen is desogestrel present in a quantity of 75 μ

g per dosage unit and the antiprogestogen is Org 31710 present in a quantity of 25 mg in the first phase and in a quantity of 2.5 to 12.5 mg in the third and subsequent phases.

11. A process of manufacturing a drug delivery system according to any one of claims 1-7 comprising mixing predetermined quantities of a progestogen, and if required estrogen, with predetermined quantities of excipients and converting the mixture into dosage units each comprising the progestogen and optionally the estrogen or the mixture of the progestogen and the estrogen, and mixing predetermined quantities of an anti-progestogen with predetermined quantities of excipients and optionally predetermined quantities of a progestogen and converting the mixture into dosage units each comprising the anti-progestogen, and packaging a plurality of said dosage units into a kit.

5. A contraceptive and/or HRT kit 1 consisting of four to eight phases in which the odd-numbered phases all comprise a single dosage unit containing an anti-progestogen and optionally a progestogen and the even-numbered phases all consist of 8-15 dosage units containing progestogen, estrogen or a mixture thereof.

9. The use of daily dosage units consisting essentially a progestogen, and of an anti-progestogen, in the preparation of a drug delivery system, said drug delivery system characterized by consisting of daily dosage units containing only a progestogenic compound as therapeutically effective ingredient and two to seven dosage units comprising anti-progestogen, one of which is administered at the beginning, and the other or others divided regularly throughout the cycle.

10. The use of oral daily dosage units consisting essentially of an estrogen and a progestogen, and of an anti-progestogen, in the preparation of a drug delivery system, said drug delivery system characterized by consisting of daily dosage units containing progestogen and/or estrogen as therapeutically effective ingredient and two to seven dosage units comprising an anti-progestogen, one of which is administered at the beginning and the other or others divided regularly throughout the cycle.