AIM: To explore the biotransformation of compound 7-(4-chlorbenzyl)-7,8,13, 13a-tetrahydroberberine in the rabbit. METHODS: Analyze the rabbit bile sample with HPLC, LC/MS and LC/NMR. RESULTS: A metabolite and unchanged 7-(4-chlorbenzyl)-7,8,13,13a-tetrahydroberberine were found in the rabit bile, the metabolite was characterized and its structure was elucidated. CONCLUSION: Compound 7-(4-chlorbenzyl)-7,8,13,13a-tetrahydroberberine is metabolized by demethylation at 10-OCH3 position.