PROCESS FOR PRODUCING A PHARMACEUTICAL FORMULATION COMPRISING CRYSTALLINE AND AMORPHOUS FRACTIONS OF AN ACTIVE SUBSTANCE

• Main Authors: OSTENDORF, Michael, HOHEISEL, Werner, NUEBOLDT, Christoph
• Format: Patent
• Language: English
• Published: 03.11.2022
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A process for producing a pharmaceutical formulation comprising the steps of: A) providing particles of a polymer, wherein particles of a pharmaceutical active substance are additionally at least partially embedded in the particles of the polymer; B) heating the particles of the polymer to a predetermined temperature for a predetermined time and C) cooling the particles of the polymer after the predetermined time to a temperature of 18° C. to 24° C., wherein the polymer is at least partially soluble in water and the active substance is at least partially soluble in the polymer.The particulate pharmaceutical active substance is present in the form of particles having a d90 value in the particle size distribution of ≤1 μm. The predetermined temperature is within a range from 10 K below the glass transition temperature (determined by DSC in accordance with DIN EN ISO 11357-2 at a heating rate of 10 K/min) of the polymer to the melting temperature of the active substance. The total proportion of the active substance in the polymer is greater than the amount of active substance soluble in the polymer at the predetermined temperature.The invention further relates to a pharmaceutical formulation comprising a particulate pharmaceutical active substance coated with an at least partially water-soluble polymer, to a process for producing a suspension of a pharmaceutical formulation and to a suspension of a pharmaceutical active substance.