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Concomitant food intake can increase the bioavailability of propranolol by transient inhibition of its presystemic primary conjugation
Author(s) -
Liedholm H,
Melander A
Publication year - 1986
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1986.135
Subject(s) - propranolol , bioavailability , concomitant , chemistry , pharmacology , pharmacokinetics , steady state (chemistry) , medicine , endocrinology
The influence of concomitant food intake on the bioavailability and presystemic primary conjugation of propranolol (80 mg) was studied in 11 healthy women. Food increased the maximum serum concentration and serum AUC of propranolol (P < 0.05) and reduced those of conjugated propranolol (P < 0.05). The mean AUC ratio of conjugated/unchanged propranolol was 13:1 in the fasting state but only about 6:1 in the nonfasting state (P < 0.001). The time to maximum serum concentration and the t ½ were not affected by food. There was no influence of food on any kinetic parameter of propranolol or conjugated propranolol when a slow‐release formulation was used. We conclude that concomitant food intake can evoke a short‐lasting, delivery rate—dependent inhibition of the presystemic primary conjugation of propranolol. This is one, but not the sole, mechanism by which food can enhance propranolol bioavailability. Clinical Pharmacology and Therapeutics (1986) 40, 29–36; doi: 10.1038/clpt.1986.135