Davison C, Banks W, Fritz A
Arch Int Pharmacodyn Ther. 1976 Jun;221(2):294-310.
The metabolism of danazol has been investigated in the rat, the monkey and in human volunteers using 14C-isoxazolo-, 14C-ethynyl, 6,7-tritiated and unlabelled compound. The drug was well absorbed, and rapidly metabolized; approximately 60 endproducts were seen in monkey urine. Four compounds have been unequivocally identified in monkey fecal extracts by physico-chemical methods; several others have been tentatively identified by chromatographic means. Very little unchanged danazol was found in monkey urine or feces at physiological dosages; the major identified urinary and fecal end-products were 2-hydroxymethylethisterone, delta1-2-hydroxymethylethisterone and ethisterone. In the rat the major portion of the radioactivity was excreted in the fecal matter, while in the monkey about equal portions were eliminated in urine and feces. Tissue distribution studies in monkeys and rats showed concentrations greater than the plasma levels only in the liver, adrenal glands and kidneys.
已使用14C-异恶唑、14C-乙炔基、6,7-氚化和未标记的化合物在大鼠、猴子和人类志愿者中研究了达那唑的代谢情况。该药物吸收良好，且迅速代谢；在猴子尿液中可见约60种终产物。通过物理化学方法在猴子粪便提取物中明确鉴定出了四种化合物；其他几种则通过色谱法初步鉴定。在生理剂量下，在猴子尿液或粪便中发现的未变化的达那唑极少；已鉴定出的主要尿液和粪便终产物为2-羟甲基炔诺酮、δ1-2-羟甲基炔诺酮和炔诺酮。在大鼠中，大部分放射性物质经粪便排出，而在猴子中，经尿液和粪便排出的量大致相等。在猴子和大鼠中进行的组织分布研究表明，仅在肝脏、肾上腺和肾脏中的浓度高于血浆水平。
