excretion in urine and bile
cannulated bile duct
Springer Online Journal Archives 1860-2000
Chemistry and Pharmacology
Summary 3H-16-acetyl-16α-gitoxin or3H-pentacetyl-16α-gitoxin were injected iv or administered po to 15 volunteers and 3 patients. The elimination half-life and excretion in urine within 4 days were estimated as a percentage of the administered radioactivity, and metabolic studies on the fate of the administered glycosides were performed. In volunteers the following results were obtained:3H-16-acetyl-16α-gitoxin 1 mg iv.: 50±11 h, 28.3±4.1%;3H-16-acetyl-16α-gitoxin 1mg po: 48±8 h, 25.4±2.8%;3H-penta-acetyl-16α-gitoxin 2 mg po: 51±12 h, 20.7±3.2%, respectively. In 3 patients with a cannulated bile duct 9.9% (mean) of the administered3H-16-acetyl-16α-gitoxin was excreted. By comparison of the radioactivity excreted in urine following the 2 routes of 16-acetate administration, the percentage absorption was calculated to be 88.5%. In serum and urine 16-acetyl-16α-gitoxin and 16α-gitoxin were found as possible metabolites of both glycosides, in the ratio of 75–85: 15–25, and both metabolites were also found in bile. Within 16 h after penta-acetate administration, two additional metabolites (bis-acetylderivatives of 16α-gitoxin) were detected in serum and urine within 16 h after administration of pentaacetate.
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