中空坐剤の製剤学的評価(第3報)IndomethacinのウサギにおけるBioavailabilityに対するMacrogol300の影響

概要

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In the previous report, it was proved that the hollow type suppository contained indomethacin (IDM) with macrogol 300 (M-300) solution had the largest area under the plasma concentration-time curve (AUC) after the rectal administration to rabbits. In this report, the effect of M-300 on bioavailability of hollow type suppositories made of Witepsol H-15,including IDM in their hollow cavities was estimated by changing the amount of M-300 in rabbits. When the content of IDM in suppository was changed to 50 mg, 25 mg and then 12.5 mg while M-300 was being kept at the same amount of 0.5 ml, each of the AUC/dose parameter was similar in value, and no dependency on dose could be seen. Next, when IDM was kept at 25 mg and M-300 increased, AUC augmented depending on the increase of M-300 amount (16.6±3.1 h・μg/ml→29.9±4.8 h・μg/ml), but when M-300 increased more than 0.5 ml, AUC was not enhanced anymore. It was suggested that there is a suitable quantity in using M-300.
1985-03-25