In order to increase the gastro-intestinal absorption of cephalexin, a new cephalexin phthalidyl ester was synthetized. Comparative studies of cephalexin phthalidyl ester in the gastro-intestinal absorption were conducted after oral administration in rabbits. The amounts of cephalexin in plasma were determined by a fluorometric method. Cephalexin phthalexin phthalidyl ester could not be identified in plasma, but only cephalexin was found by TLC method. In comparison with cephalexin, cephalexin phthalidyl ester produced much higher plasma levels of cephalexin than did cephalexin itself after its oral administration in rabbits.