LIU Hai-pei1�� 2�� MENG Fan-hua1�� GUO Ji-fen1*�� SI Duan-yun3�� ZHU Xiao-wei2�� ZHAO Yi-min1
1.Institute of Pharmacology and Toxicology�� Academy of Military Sciences�� Beijing 100850�� China; 2. Tianjin University of Traditional Chinese Medicine�� Tianjin 300193�� China; 3. Tianjin Institute of Pharmaceutical Research�� Tianjin 300193�� China
Abstract��
OBJECTIVE To characterize the pharmacokinetics and excretion of icaritin in rats after oral and intravenous administration. METHODS The concentrations of free icaritin and glucuronide-conjugates in rat plasma�� urine and feces were determined. RESULTS The ��max and AUC0-�� showed dose-dependent increase after oral doses of 20�� 40 and 80 mg��kg-1�� and the bioavailability were 17.29%�� 13.80% and 10.70%�� respectively. The ��max and AUC0-�� after oral dose of 80 mg��kg-1 were 13.26 ng��mL-1�� 495.67 ng��h��mL-1 for free icaritin and 597.50 ng��mL-1�� 12 038 ng��h��mL-1 for total icaritin (free and conjugates). The ��max and AUC0-�� after intravenous dose of 20 mg��kg-1 were 5 896 ng��mL-1�� 2 470 ng��h��mL-1 for free icaritin and 11 598 ng��mL-1�� 23 303 ng��h��mL-1 for total icaritin. The urine�� feces excretion ratios after oral dose of 80 mg��kg-1 during 72 h were 0.04%�� 25.09% for free icaritin and 0.14%�� 32.46% for total icaritin. The urine�� feces excretion ratios after intravenous dose of 20 mg��kg-1 during 72 h were 0.58%�� 8.76% for free icaritin and 2.48%�� 10.82% for total icaritin. CONCLUSION Icaritin was presented mainly as glucuronide conjugates in plasma�� and the bioavailability was low. Main of icaritin excreted from feces.
2010, Vol. 45 
