The effect of oral phenformin on the active transport of glucose by everted sacs of rat intestine was investigated. Pretreatment of the animals with a single dose of the drug resulted in an inhibition of active transport. A log-dose relationship was found in the range studied (5 to 150 mg./kg.). These findings could explain the observation that phenformin increases the tolerance to orally administered glucose but has no effect on intravenous glucose tolerance in humans.

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