Lack of Pharmacokinetic Interaction of Sucralfate and Erlotinib following Co-administration in Rats

The objective of this work was to investigate the effect of orally administered sucralfate on the pharmacokinetics of erlotinib and its active metabolite OSI-420 in rats. Twelve healthy male Sprague-Dawley rats were randomly divided into two groups: the control group (received normal saline for 7 days) and the test group (administered with 100 mg/kg sucralfate for 7 days). After the last administration, the rat in each group was given a single dose of 15 mg/kg erlotinib. The plasma concentration of erlotinib and OSI-420 were estimated by ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) and different pharmacokinetic parameters were calculated using DAS 2.0 software. Compared to the control group, the pharmacokinetic parameters (t(1/2), T-max, CLZ/F, C-max and AUC((0-infinity))) of erlotinib and OSI-420 in test group were not significantly changed. This study demonstrated that sucralfate had a possible negative effect on the absorption of erlotinib. Further prospective investigation is warranted.