The absorption rate of lysino-methylene-ampicillin from the rat small intestine, compared with ampicillin, was determined in vitro and in situ to establish the biopharmaceutical properties of lysino-methylene-ampicillin which is one of the new penicillinase-resistance antibiotics. The half of administered dose was absorbed rapidly within thirty minutes. The water-oil distribution coefficient of lysino-methylene-ampicillin was 0.03 in chloroform versus buffer system with $Na_{2}HPO_{4}-citric$ acid of pH5.2 at $37^{circ}C$, and its dissolution rate reached the plateau in an hour and then represented 0.6 percent of equilibrium solubility