Preparation of particulate compositions by wet milling a sparingly water-soluble drug substance as an aqueous dispersion in a multi-chamber bead mill, where the aqueous dispersion also comprises a soluble carrier, a surfactant and an anti-agglomeration agent

摘要

A process for preparing a particulate composition of a sparingly water-soluble drug substance which comprises: wet milling the drug substance as an aqueous dispersion in a multi-chamber bead mill with circulation of product between the chambers. The aqueous dispersion including a soluble carrier suitable as an excipient for spray drying. A surfactant to maintain the particles in suspension on resuspension. And an anti-agglomeration agent effective after administration of a pharmaceutical formulation to a patient, and spray drying the aqueous dispersion after milling. The drug substance may include a compound of formula I or II.