Intestinal Absorption of β-Adrenergic Blocking Agent Nadolol. I. : Comparison of Absorption Behaivor of Nadolol with Those of Other β-Blocking Agents in Rats

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Intestinal absorption of nadolol, a new long-acting β-adrenergic blocking agent, was compared with those of six other β-blocking agents by the in situ ligated loop method in rats. It was found that nadolol was well absorbed from the duodenum, jejunum, ileum and colon, but not the stomach. The in situ intestinal absorption of β-blocking agents including nadolol was consistent with pH-partiton theory. The absorption of nadolol was, however, strongly inhibited by trihydroxy bile salts, sodium cholate and its taurine and glycine conjugates, but not by dihydroxy bile salts such as sodium chenodeoxycholate and sodium deoxycholate. An inhibitory effect on the absorption of nadolol was also found in vivo in rats with bile duct ligation. No inhibition of the absorption of other β-blocking agents by sodium cholate was observed. The results suggest a specific interaction between nadolol and trihydroxy bile salts, especially sodium cholate.
公益社団法人日本薬学会の論文
1986-08-25