Claims for Patent: 11,964,055

Summary for Patent: 11,964,055

Title:	Orodispersible dosage unit containing an estetrol component
Abstract:	The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 μg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 μm to 50 μm. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.
Inventor(s):	Séverine Francine Isabelle JASPART, Johannes Jan Platteeuw, Denny Johan Marijn Van Den Heuvel
Assignee:	Estetra SRL
Application Number:	US17/504,087
Patent Claims:	1. A solid pharmaceutical dosage unit having a weight of 30 to 1,000 mg, the dosage unit consisting of: 0.1-30 wt. % of estetrol particles having a volume median diameter of 2 μm to 50 μm, containing at least 90 wt. % of an estetrol component selected from estetrol, estetrol esters, and combinations thereof, and being present in the dosage unit as a component of dry estetrol-containing granules that further comprise one or more granulation excipients; and 70-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 μg of the estetrol component. 2. The solid pharmaceutical dosage unit according to claim 1, wherein the dosage unit comprises the estetrol component in an amount of at least 1 wt. %. 3. The solid pharmaceutical dosage unit according to claim 1, wherein the estetrol particles have a volume median diameter of 3 μm to 35 μm. 4. The solid pharmaceutical dosage unit according to claim 1, wherein the estetrol-containing granules comprise the one or more granulation excipients in an amount of 70-95 wt. % and the estetrol component in an amount of 5-30 wt. % of the estetrol component. 5. The solid pharmaceutical dosage unit according to claim 1, wherein the dosage unit is an orodispersible solid pharmaceutical dosage unit. 6. The solid pharmaceutical dosage unit according to claim 5, wherein the dosage unit has a disintegration time in water of less than 5 minutes. 7. The solid pharmaceutical dosage unit according to claim 6, wherein the dosage unit has a disintegration time in water of less than 2 minutes. 8. The solid pharmaceutical dosage unit according to claim 6, wherein the disintegration time is determined by a disintegration test according to Ph. Eur. 2.9.1. or USP<701>. 9. The solid pharmaceutical dosage unit according to claim 1, wherein the estetrol component is estetrol or an ester thereof. 10. The solid pharmaceutical dosage unit according to claim 1, wherein the dosage unit is a tablet, dragée, lozenge, or film. 11. The solid pharmaceutical dosage unit according to claim 10, wherein the dosage unit is a tablet. 12. The solid pharmaceutical dosage unit according to claim 1, wherein the pharmaceutically acceptable ingredient comprises a progestin selected from the group consisting of: progesterone, desogestrel, etonogestrel, gestodene, dienogest, levonorgestrel, norgestimate, norethisterone, norethisteron-acetate (NETA), nomegestrol, nomegestrol-acetate (NOMAC), drospirenone, trimegestone, nestorone, and dydrogesterone. 13. The solid pharmaceutical dosage unit according to claim 12, wherein the progestin is 0.05-10 mg of drospirenone. 14. The solid pharmaceutical dosage unit according to claim 1, wherein the dosage unit is formed by a process comprising direct compression or compression moulding. 15. The solid pharmaceutical dosage unit according to claim 1, wherein the dosage unit releases at least 70% of the estetrol component after 5 minutes in an aqueous dissolution medium. 16. The solid pharmaceutical dosage unit according to claim 15, wherein the dosage unit releases at least 80% of the estetrol component after 5 minutes in an aqueous dissolution medium. 17. A method of providing female hormone replacement therapy to a subject in need thereof, comprising administering a solid dosage unit according to claim 1 by sublingual, buccal or sublabial administration. 18. The method of claim 17, wherein the administering is by once daily administration during a period of at least 1 week. 19. A method of providing female contraception to a subject in need thereof, comprising administering a solid dosage unit according to claim 1 by sublingual, buccal or sublabial administration. 20. The method of claim 19, wherein the administering is by once daily administration during a period of at least 1 week.