ノート
新規抗PAF剤E5880注射剤の開発
2002 年 62 巻 3 号 p. 124-131
詳細
2002 年 62 巻 3 号 p. 124-131
An injectable formulation of E5880, a novel platelet activating factor receptor antagonist, was designated from the study of pH-stability, the selection of excipient, and the relationship between moisture and stability. The physicochemical properties of E5880 micelles in the optimized formulation (0.6 mg/ml of E5880, 0.1% citric acid, 10% lactose, pH 2.8) were characterized. The critical micelle concentration of E5880 in the formulation was 0.09 mg/ml, and the structure was spherical. The micellar size was approximately 5 nm and did not change before or after lyophilization and storage. The number of molecules per micelle was 40. The micropolarity around the hydrocarbon region of the micelle was similar to that of butanol.
