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PLASMA AND BILIARY DISPOSITION OF PIRENZEPINE IN MAN

1. The binding of pirenzepine, a selective muscarinic receptor antagonist to plasma and bile, was studied in vitro and in vivo. Plasma and hepatic bile were incubated with 14C‐pirenzepine and the bound fraction of 14C‐pirenzepine determined by equilibrium dialysis. The bound fractions were 12.6% (s.e.m. = 1.5) and 12.1% (s.e.m.= 1.6) in plasma and bile samples, respectively. After in vitro incubation, the radioactivity in both plasma and bile was removed by exhaustive dialysis against water for up to 94 h, suggesting that the binding was a noncovalent association.