Dược Động Học :
▧ Absorption :
Extremely low bioavailability. Less than 2% of an oral dose of acarbose was absorbed as active drug. Peak plasma concentrations of the active drug were achieved 1 hour after dosing. Drug accumulation does not occur with multiple doses.
▧ Metabolism :
Acarbose is only metabolized within the gastrointestinal tract by intestinal bacteria and also digestive enzymes to a lesser extent. 4-methylpyrogallol derivatives (sulfate, methyl, and glucuronide conjugates) are the major metabolites. One metabolite (formed by cleavage of a glucose molecule from acarbose) also has alpha-glucosidase inhibitory activity.
▧ Route of Elimination :
The fraction of acarbose that is absorbed as intact drug is almost completely excreted by the kidneys. A fraction of the metabolites (approximately 34% of the dose) was absorbed and subsequently excreted in the urine. The active metabolite is excreted into the urine and accounts for less than 2% of the total administered dose. When given intravenously, 89% of the dose was excreted into the urine as the active drug. When given orally, less than 2% of the oral dose was recovered into the urine as active (parent compound and active metabolite) drug.
▧ Half Life :
Healthy volunteers = 2 hours