Evaluation of Several Surface-Active Agents on Digoxin Rectal Absorption

概要

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Rectal suppositories of digoxin were made with cacao butter containing 5% of polysorbate 60, SFAE-11, SFAE-15, SML, GMS, and PGMS. Physical properties, melting point, dissolution time, and hardness of these suppositories were measured. Blood levels of digoxin in rabbits after rectal administration (0.3 mg/kg) were determined by a radioimmunoassay method. Bioavailability was estimated by measuring the relative area under the concentration-time curve for digoxin suppositories. Plasma digoxin concentrations of suppositories containing SML, GMS, and PGMS were poor. The relative AUC for digoxin suppositories containing SFAE-15, SFAE-11, SML, GMS, and PGMS were 0.90, 1.02, 0.23, 0.27, and 0.23 respectively when a suppository containing polysorbate 60 was used as the standard. The ratio between 1.5-hour value and 0.5-hour value of plasma digoxin concentration after rectal administration for suppositories containing SFAE-15, and SFAE-11 were 0.56 and 0.65. The highest plasma digoxin concentration was obtained with suppository containing SFAE-15 and plasma digoxin level was kept for along time with suppository containing SFAE-11.
日本医療薬学会の論文
1981-12-20