Acarbose (O-4,6-dideoxy-4-[[1S,4R,5S,6S)-4,5,6-trihydroxy-3- (hydroxymethyl)-2-cyclohexen-1-yl]amino]-alpha-D-glucopyranosyl- (1----4)-O-alpha-D-glucopyranosyl-(1----4)-D-glucopyranose, Bay g 5421) labelled with 14C was administered to male rats, pregnant and lactating rats as well as to female dogs with single intravenous or oral doses (2 or 4 mg.kg-1) and with repeated oral doses of 2 mg.kg-1 to male rats for 3 weeks. The distribution of radioactivity to organs and tissues, the placental transfer and the secretion into milk was studied using whole-body autoradiographic methods and/or quantitative determination of total radioactivity after autopsy. Unchanged [14C]acarbose was distributed predominantly in the extracellular space, as observed after intravenous dosing to rats. According to the main excretion route, high concentrations were found in kidneys and urine and additionally in blood, lung, and connective tissue or interstitial space. The permeability of the blood/brain barrier for [14C]acarbose and/or its metabolites was very low. No indication was found for distinct differences in the distribution patterns in rats and dogs after intravenous and also in dogs after oral administration. In contrast, in rats after oral dosing the distribution pattern of radioactivity was different with relatively high concentrations in liver, kidney, adrenal gland, spleen, and intestinal mucosa. Due to the slow absorption of the microbial degradation products of [14C]acarbose from the intestine maximum concentrations in the different tissues were reached 8-24 h after dosing.(ABSTRACT TRUNCATED AT 250 WORDS)