POLYMORPHIC FORM OF ESTEROL AND ITS PRODUCTION
Patent Information
- Application Number
- ARP20250100542
- Authority / Receiving Office
- AR · AR
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-02-28
- Filing Date
- 2025-02-27
- Publication Date
- 2026-09-02
Claims
The present invention relates to a process for producing crystalline estetrol monohydrate, and in particular a certain polymorphic form thereof, comprising the steps of dissolving estetrol in an aqueous mixture comprising an alcohol to obtain a solution; cooling the solution to a cooling temperature 2; optionally, stirring the cooled solution at the cooling temperature 2; further cooling the solution to a cooling temperature 3 to form a suspension; stirring the suspension at the cooling temperature 3; and isolating the crystalline estetrol monohydrate from the suspension.
1. Estetrol monohydrate identified by characteristic XRD peaks at 11.9, 12.2, 12.4, 12.8, 13.4, 19.9, 20.7, 20.8, 21.6, 21.7 and 24.5º (± 0.1º) 2 using CuK radiation.
2. A process for producing estetrol monohydrate, preferably estetrol monohydrate according to claim 1, comprising the steps of: a) dissolving estetrol in a solvent mixture of water and at least one alcohol, preferably at a temperature of 55.0°C to 100.0°C; b) cooling the solution to a cooling temperature 2 to obtain a mixture; c) maintaining the cooled mixture at the cooling temperature 2; d) further cooling the mixture to a cooling temperature 3 to form a suspension; e) maintaining the cooled suspension at the cooling temperature 3; and f) isolating estetrol monohydrate from the suspension.
15. A pharmaceutical composition comprising estetrol monohydrate according to claim 1, or obtained or obtainable by the process according to any one of claims 2 to 14; and at least one pharmaceutically acceptable excipient.