Minopafant

The injectable formulation of E5880, a novel platelet activating factor (PAF) receptor antagonist, was developed. The physicochemical properties of E5880 micelles in the optimized formulation (0.6 mg/mL of E5880, 0.1% of citric acid, 10% lactose, pH 2.8) were characterized. The critical micelle concentration of E5880 was 0.09 mg/mL, and the structure was spherical. The micelle size was 5.6 nm. The number of molecules per micelle was 46. The micropolarity around the hydrocarbon region in the micelle was similar to that of isobutanol.

E5880, a novel platelet activating factor (PAF) receptor antagonist, was dispersed in water for use in injectable formulation and the physicochemical properties of the preparation were characterized. The critical concentration for formation of micelles was 0.12 mM. Using area per molecule data, the critical packing parameter was calculated, indicating that the structure of the micelles was spherical and that each micelle containing 49 molecules. The diameter of the micelle was 8.1 nm. Attractive interactions occurred between E5880 molecules in the micelle. The hydrocarbon region in the micelle was more rigid and less hydrated than that of other surfactants, stearyltrimethylammonium chloride (STAC) and cetyltrimethylammonium chloride (CTAC).