Boyer A W, Somani S M
Arch Int Pharmacodyn Ther. 1985 Dec;278(2):180-92.
The biliary excretion of Phy and its metabolites was studied in the rat after i.v. administration of 3H-Phy (100 micrograms/kg). About 60% of the radioactivity was excreted in three hours. The unchanged drug was excreted to the extent of about 23% of the dose and the metabolites were excreted as 37% of the dose. The half-life of Phy was found to be 21.6 +/- 1.8 min (mean +/- S.E.) as determined in bile, 52.1 +/- 9.1 min as determined from serum, and the systemic clearance of Phy was .63 +/- 2.6 ml/min. The mean Kel was found to be .012 min-1. The biliary excretion rate constant was determined to be .014 +/- .001 min-1 for total radioactivity and .008 +/- .002 min-1 for Phy. Biliary clearance of Phy was .18 ml/min. The serum to bile ratio of Phy at 15-30 min was 5.11, indicating rapid concentration of Phy in the bile. Phy may stimulate bile flow in the rat, particularly at early times. The mass spectrum of extracted Phy from bile at m/e 275, 218, 175, 161 and 160 confirmed its identify. From these studies it appears that bile is a significant route of excretion of Phy in the rat.
静脉注射3H-菲（100微克/千克）后，在大鼠体内研究了菲及其代谢产物的胆汁排泄情况。约60%的放射性在三小时内排出。原形药物的排泄量约为给药剂量的23%，代谢产物的排泄量为给药剂量的37%。在胆汁中测定的菲的半衰期为21.6±1.8分钟（平均值±标准误），从血清中测定的半衰期为52.1±9.1分钟，菲的全身清除率为0.63±2.6毫升/分钟。平均消除速率常数为0.012分钟-1。总放射性的胆汁排泄速率常数测定为0.014±0.001分钟-1，菲的胆汁排泄速率常数为0.008±0.002分钟-1。菲的胆汁清除率为0.18毫升/分钟。15至30分钟时菲的血清与胆汁比值为5.11，表明菲在胆汁中迅速浓缩。菲可能刺激大鼠的胆汁分泌，尤其是在早期。从胆汁中提取的菲在m/e 275、218、175、161和160处的质谱证实了其身份。从这些研究看来，胆汁是大鼠体内菲排泄的重要途径。
