Biliary excretion and enterohepatic recycling of proscillaridin a after oral administration to man
Autor: | K. E. Andersson, G. Wettrell, B. Bergdahl |
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Rok vydání: | 1977 |
Předmět: |
Male
medicine.medical_specialty Time Factors Administration Oral Excretion Drug Stability Oral administration Internal medicine Enterohepatic Circulation Blood plasma medicine Bile Humans Pharmacology (medical) Intestinal Mucosa Aged Glucuronidase Pharmacology chemistry.chemical_classification Common bile duct Chemistry Hydrolysis Glycoside General Medicine Metabolism Middle Aged Proscillaridin Bufanolides Endocrinology medicine.anatomical_structure Biliary tract Female Sulfatases medicine.drug |
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 |
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