PROCESSES FOR PREPARING CRYSTALLINE AND AMORPHOUS MUPIROCIN CALCIUM

• Main Author: ERZSEBET MESZAROS SOS
• Format: Patent
• Language: English; Spanish
• Published: 04.10.2004
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate. A highly pure composition of amorphous mupirocin calcium is provided, and processes for its preparation by solvent removal, lyophilization and precipitation with use of anti-solvent. Pharmaceutical compositions of amorphous form, and methods of using them to treat infections are also provided. Also provided are combined processes for preparing mupirocin clacium dihydrate and amorphous, by producing amorphous form first, followed by conversion of amorphous form into the dihydrate through crystallization from an aqueous solution. Also provided are processes for removing the water of crystallization of the dihydrate to obtain mupirocin calcium anhydrate. Se proveen procesos para preparar calcio de mupirocina desde acido pseudomonico en un sistema de dos fases utilizando un carboxilato organico. Se provee una composicion altamente pura de calcio de mupirocina y procesos para su preparacion mediante la remocion del solvente, la liofilizacion y la precipitacion utilizando un antisolvente. Tambien se proveen composiciones farmaceuticas de la forma amorfa, y metodos para su utilizacion para tratar infecciones. Tambien se proveen procesos combinados para prepara calcio de mupirocina dihidratado y amorfa, produciendo la forma amorfa primero, seguido por la conversion de la forma amorfa en el dihidrato a traves de la cristalizacion desde una solucion acuosa. Tambien se proveen procesos para remover el agua de la cristalizacion del dihidrato para obtener calcio de mupirocina anhidratado.