Acarbose acts locally in the gastrointestinal tract on the surface of enterocytes. Only 2% of an oral acarbose dose is systemically absorbed, with a plasma half-life of 2 h. Acarbose is metabolized by the intestinal microbial flora and digestive enzymes and excreted in the stool.

Miglitol requires systemic absorption to achieve its therapeutic effect. Oral absorption is rapid and nearly complete, but saturable; nearly all of a 25-mg dose is absorbed systemically, whereas only 50-70% of a 100-mg dose is absorbed. Miglitol is not metabolized in vivo and is renally excreted. In individuals with severe renal dysfunction, plasma levels of both acarbose and miglitol may rise.

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