BIOPHAMACEUTICAL CHARACTERISTICS OF A SUPPOSITORY BASE CONTAINING POLY (OXYETHYLENE)-POLY (OXYPROPYLENE) COPOLYMER, UNILUBE. I. EFFECTS OF A SUPPOSITORY BASE CONTAINING UNILUBE 70DP-950B ON RELEASE AND RECTAL ABSORPTION OF AMINOPYRINE IN RABBIT

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The rectal absorption of aminopyrine (AP) from a three-component-system suppository base (TCS), which is a mixture of oleaginous base, water-soluble base and the poly-(oxyethylene) poly-(oxypropylene) block copolymer, Unilube^[○!R], was investigated. Albino rabbits were used as the animal model. The bioavailability of oleaginous base and watersoluble base (polyethylene glycol 4000) were 44.3% and 82.6%, respectively. The time to reach maximum plasma concentration (T_<max>) of the oleaginous and the water-soluble bases were 21.0±8.2 min and 33.0±16.4 min, respectively. When TCS was used, its T_<max> was 30 min and inceasing the amount of Unilube in the base from 5% (w/w) to 20% (w/w) decreased the bioavailability from 100.4% to 47.2%. The softening temperature of TCS was 55-57℃. Collectively, TCS containing 5% of Unilube gave significantly higher bioavailability than the other bases without softening until 57℃. Also, the results of the two different release tests were compared with the results of an animal experiment in this paper.
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