METABOLISM OF ORALLY ADMINISTERED ICARIIN IN RATS

AIM: To evaluate the pharmacological action of icariin in traditional Chinese medicines. METHODS: Icariin was given orally to rats, the major metabolites of icariin in gastric, small intestinal, urine and bile samples were determined and isolated by HPLC and identified by chemical and spectroscopic evidences. RESULTS: Two metabolites, icariside II and icaritin in both small intestine and urine, and two metabolites, icaritin-3-O-α-L-rhamnopyranosyl-7-O-β-D-glucopyranuronoside and icariside II in bile were identified. The major metabolic route of orally administered icariin in rats was also proposed. CONCLUSION: Icariin is metabolized prior to absorption and exists mainly as its metabolites in vivo.