アテノロールの直腸吸収におよぼす坐剤基剤の影響

概要

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The effects of suppository bases on the release of atenolol (AT) and its rectal absorption in rat and rabbit were studied. The release profiles of AT from various suppository bases were different by dialysis tubing method. The release of AT from Pharmasol B115 was markedly rapid and after 40 min reached 100%. The order of the release rate was Pharmasol B115>T115>macrogol 4000. The plasma concentrations of AT after rectal administration of various bases were measured for 5hr. In rats, Cmax for Pharmasol T115 was higher than those of the other bases, and AUC for Pharmasol B115 was the largest value among the bases tested. Relative AUC for Pharmasol B115, T115, and macrogol 4000 as compared to AUC value of intravenous administration were 34%, 25%, and 9%, respectively. In rabbits, Cmax and AUC for Pharmasol T115 was larger than those of the other bases. Relative AUC of AT for macrogol 4000 was below 10% in both rat and rabbit. The plasma level of AT for Pharmasol B115 containing sodium n-caprate considerably increased as compared with that of the base alone for 2hr.
日本医療薬学会の論文
1989-06-20