Original Articles

Absorption, distribution, excretion and metabolites of [14C]armillarisin A in rats

He-sheng Shao, Shou-ren Zhang, Shang-ren Pan, Xi-nan Jing, Lan-qin Ying, Hai-yan Zhu, Chong-hua Gu


The 14C labeled at the 5-hydroxymethyl group of armillarisin A(2.86 Ci/mg).The drug was given to rats po 10mg/kg,iv 5.59 mg/kg,and im 3.45 mg/kg.The drug was absorbed and excreted rapidly. The biological half-life was 2.6 min for t1/2alpha and 33min for t1/2beta.
The radioactivities were the highest in kidneys in 24 h. It was excreted 89% in urine and only 8% in feces within 48 h. Four metabolites could be spotted on paper chromatography and autoradiography of the urine.Since the excretion was so rapid, it is advised to prescribe larger doses or shorter intervals between administrations.

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