A robotic homogenized tissue sample transferring method has been developed by using a Packard MultiProbe II 8-tip system. It enables robotically transferring homogenized tissue samples from individual test tubes into a 96-well format plate for further sample purification and analysis. Extensive validation has been made to establish the accuracy and variability of this method. This automatic tissue sample transferring approach combined with automatic tissue homogenization, has significantly increased the throughput of tissue sample preparation in screening of drug candidates using liquid chromatography coupled with highly sensitive and selective tandem mass spectrometry (LC-MS/MS).