血友病B治療薬の経口化に関する研究

抄録

For the oral administration of factor IX, (1) the stability of factor IX, (2) the encapsulation of factor IX in liposome preparations, (3) the transformation of prothrombin (factor II) into thrombin, and (4) the absorption of factor II, VII, IX and X from the intestine were studied. The following results were obtained : factor IX was stable from 4°C to 25°C and in a mild alkaline solution. Factor IX was the most effectively encapsulated in liposome preparations with stearylamine or Ca²⁺. The transformation of prothrombin into thrombin was inhibited by adding lecithin or aprotinine. Oral administration of factor IX entrapped in liposomes tended to shorten clotting time in beagle dogs.