Patent ID: 7081253

Claim:
A method of preparing a pharmaceutical formulation of a lipophilic pharmaceutical active agent in the form of an aqueous monodisperse nanodispersion having a Gaussian distribution, which steps consist essentially of (α) mixing the components (a) 0.1 to 30% by weight of a phospholipid, (b) 1 to 50% by weight of a polyoxyethylene coemulsifier selected from the group consisting of polyethoxylated fatty alcohols, polyethoxylated fatty acids, polyethoxylated vitamin E derivatives, polyethoxylated lanolin and derivatives thereof, polyethoxylated fatty acid partial glycerides, polyethoxylated alkylphenols, and salts thereof, polyethoxylated fatty amines and fatty acid amides and polyethoxylated carbohydrates, (c) 0.1 to 80% by weight of a lipophilic component which comprises a natural or synthetic or a partially synthetic C 4 –C 18 triglyceride and a lipophilic pharmaceutical active agent, in which aqueous nanodispersion any pharmaceutically active agent is lipophilic and is always present in component (c), and (d) 0.63 to 14.2% by weight of ethanol, with the proviso that the sum of (a), (b), (c) and (d) is 100% by weight, in conventional stirring apparatus until a homogeneous clear liquid is obtained, and (β) adding the liquid obtained in step (α) to a water phase, wherein (β) is carried out in the absence of high shear or cavitation forces, and wherein the particles in the nanodispersion have an average diameter <50 nm.