Claims for Patent: 12,427,114

Summary for Patent: 12,427,114

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; and75-99.9 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:	US18/621,501
Patent Claims:	1. Dry estetrol-containing granules comprising: 70-95 wt. % of one or more granulation excipients; and 5-30 wt. % of estetrol particles having a volume median diameter of 2 μm to 50 μm and containing at least 90 wt. % of an estetrol component. 2. The dry estetrol-containing granules of claim 1, obtained by a process comprising: mixing the estetrol particles estetrol particles having a volume median diameter of 2 μm to 50 μm and containing at least 90 wt. % of the estetrol component with the one or more granulation excipients to produce a granulation mixture; mixing the granulation mixture with a granulation liquid comprising at least 60 wt. % of a liquid solvent to produce estetrol-containing granules; and removing liquid solvent from the estetrol-containing granules to produce said dry estetrol-containing granules. 3. The dry estetrol-containing granules of claim 1, wherein the estetrol component is estetrol monohydrate. 4. A solid pharmaceutical dosage form comprising the dry estetrol-containing granules of claim 1, wherein the solid pharmaceutical dosage form releases at least 50% of the estetrol component after 5 minutes in an aqueous dissolution medium. 5. The solid pharmaceutical dosage form of claim 4, comprising from 1 mg to 20 mg of the estetrol component. 6. The solid pharmaceutical dosage form of claim 4, comprising 20 mg of the estetrol component. 7. The solid pharmaceutical dosage form of claim 4, further comprising a further pharmaceutically acceptable ingredient selected from progesterone, desogestrel, etonogestrel, gestodene, dienogest, levonorgestrel, norgestimate, norethisterone, norethisteron-acetate (NETA), nomegestrol, nomegestrol-acetate (NOMAC), drospirenone, trimegestone, nestorone, and dydrogesterone. 8. The solid pharmaceutical dosage form of claim 5, further comprising 0.05-10 mg of drospirenone. 9. The solid pharmaceutical dosage form of claim 4, wherein the dosage form is an orodispersible dosage form. 10. The solid pharmaceutical dosage form of claim 4, wherein the estetrol particles are present in the dosage form in an amount of 0.5-25 wt. %. 11. The solid pharmaceutical dosage form of claim 4, wherein the dosage form comprises a water-soluble carbohydrate selected from maltose, fructose, sucrose, lactose, glucose, galactose, trehalose, xylitol, sorbitol, erythritol, maltitol, mannitol, isomalt, and combinations thereof. 12. The solid pharmaceutical dosage form according to claim 4, wherein the dosage form comprises 0.1-20 wt. % of a disintegrating agent selected from modified starches, crosslinked polyvinylpyrrolidone, crosslinked carmellose, and combinations thereof. 13. A female hormone replacement therapy method, comprising administering dry estetrol-containing granules of claim 1 to a subject in need thereof. 14. The method of claim 13, comprising once daily administration of the granules during a period of at least 1 week. 15. A female contraception method, comprising administering dry estetrol-containing granules of claim 1 to a subject in need thereof.