Biliary excretion and enterohepatic recycling of proscillaridin a after oral administration to man

Autor: K. E. Andersson, G. Wettrell, B. Bergdahl
Rok vydání: 1977
Předmět:
Zdroj: European Journal of Clinical Pharmacology. 11:273-276
ISSN: 1432-1041
0031-6970
DOI: 10.1007/bf00607676
Popis: A single oral dose of proscillaridin A (1.0-1.5 mg) was given to six patients with T-tube drainage of the common bile duct, and simultaneous samples of bile and plasma were collected at various times during the following 24 hours. Glycoside activity was assayed by the 86Rb-uptake inhibition technique. Peak activities in plasma (mean 0.80 ng/ml) were attained after 0.5-2h, and in bile (mean 6.9 ng/ml) after 1-4h. Subsequently, proscillaridin activity in bile was less than 5 ng/ml for the remainder of the sampling period, and 10-100 times higher than that in plasma. Bile samples treated with beta-glucuronidase and sulphatase showed 100-200 fold increase in glycoside activity. Deconjugation was also produced by treatment with enteric contents. The results suggest that conjugation of unchanged proscillaridin is a major metabolic route. After excretion in the bile, the conjugates may be split in the intestine and reabsorbed as active glycoside.
Databáze: OpenAIRE