抄録
Erlotinib, a reversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, is orally available and used for the treatment of non-small cell lung cancer (NSCLC). The simple suspension method is recognized as being useful in patients with dysphagia. In this study, we aimed to clarify the solubility and stability of erlotinib tablets against the temperature and pH of the solvent used for the simple suspension method. In addition, we evaluated the pharmacokinetic profile of erlotinib in three NSCLC patients who received erlotinib by this method. Erlotinib tablets were suspended in water at three different temperatures (25, 55 and 80℃) or beverages with three different pHs (3.62, 6.97 and 8.96) at 55℃. Concentrations of erlotinib in suspension samples, which were collected at 1, 2, 5, 10, 30 and 60 minutes after the start of suspending, were determined using a high performance liquid chromatography method. The concentrations of erlotinib were not significantly affected by the temperature and pH at 10 minutes and after the start of suspending, and erlotinib was stable, at least, for 60 minutes in each water solution examined. The plasma concentration time-courses of erlotinib at a steady-state in the three patients who received erlotinib by the simple suspension method were similar to those in the phase 1 study. These findings suggest that the simple suspension method for erlotinib is a treatment option for NSCLC patients with dysphagia.
