In‐vitro Interaction of a Novel Immunosuppressant, FK 506, and Antacids

Abstract— The effect of selected antacids on the amount of FK 506 in solution in simulated gastric juice has been studied. FK 506 (2–5 mg) was incubated in 100 mL simulated gastric fluid (SGF) with the equivalent of 500 mg of various antacids. The addition of Mylanta and Turns resulted in 14 and 30% loss of FK 506, respectively, in 24 h; 98% loss was observed in 12 h in the presence of Mag‐Ox; 100% loss was observed in the presence of magnesium oxide powder in 2 h. The loss of FK 506 from these solutions appears to be due to a pH mediated degradation of FK 506. The addition of aluminium hydroxide gel USP (Roxane) to the FK 506 solution resulted in a 35% loss within 2 min but no further loss was noted for 24 h, indicative of adsorption of FK 506. These results suggest that until additional in‐vivo studies are carried out, it is prudent not to dose FK 506 and antacids at the same time to avoid potential interactions. 1991 Royal Pharmaceutical Society of Great Britain