We have studied the physico-chemical change and pharmacological transformation of traditional herbal medicines with processing. Evodia fruit (EF) has processed for the purpose of detoxification and reduction of its bitter taste. There are various methods of processing EF in Oriental medicinal reference. Among them, we processed EF according to the method of Sang-han theory, the most famous medicinal reference. We processed EF with washing in hot water, and then dried. Processed EFs(PEFs) were prepared according to the above procedure through repetition of 1,3,5 and 7 times respectively. The contents of weight loss, water extract, diluted ethanol extract, ether extract, total ash, acid insoluble ash, alkaloids and limonin in non-processed EF (NPEF) and PEFs were examined. The weight loss, and contents of water extract and dilute ethanol extract in PEF showed decrease in proportion to increase of washing time, while the contents of ether extract, total ash and acid insoluble ash showed little change as compared with those of NPEF. And the content of evodiamine and rutaecarpine was not changed distinctly. However, the content of limonin decreased in the final processed material in proportion to increase of washing times with hot water. And the intense of bitter taste in PEF was also reduced. These results were ascribed to the flowing-out of the water-soluble portion. The biological activities of NPEF and PEF were also investigated. In the test of DPPH scavenging effect, xanthine oxidase inhibition effect and TBA-Rs effect, PEF was more effective than NPEF in vitro. Also, both NPEF and PEF showed potent analgesic and anti-inflammatory effects against in mice. Especially, PEF by 3 times washing with hot water was more effective than other PEFs. From these results, it is considered that PEF should be prepared by 3 times washing with hot water.