Absorption of sodium γ﹉ydroxybutyrate and its Prodrug γ‐butyrolactone: Relationship between in vitro transport and in Vivo absorption

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摘要：

A qualitative relationship between in vitro transport and in vivo absorption of sodium -hydroxybutyrate and -butyrolactone was demonstrated. As with other short-chain acids, sodium -hydroxybutyrate showed capacity-limited transport in vitro , consistent with the previous observation that this drug exhibited slower in vivo absorption with increasing dose. The prodrug lactone, on the other hand, showed a higher intestinal flux than the acid in the everted gut, and in vivo absorption also was more rapid. Capacity-limited transport and absorption of the lactone appeared less evident. Thus, the increased oral hypnotic activity of the lactone over that of the acid most likely is a result of its more favorable intestinal transport characteristics.

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关键词：

Sodium -hydroxybutyrate - relationship between in vitro transport and in vivo absorption -Butyrolactone - prodrug for sodium -hydroxybutyrate, relationship between in vitro transport and in vivo absorption Hypnotic agents - sodium -hydroxybutyrate and -butyrolactone, relationship between in vitro transport and in vivo absorption

DOI：

10.1002/jps.2600690331

被引量：

513

年份：

1980