Inhibition of disaccharide digestion in rat intestine by the alpha-glucosidase inhibitor acarbose (BAY g 5421).
Administration of the alpha-glucosidase inhibitor, acarbose (BAY g 5421), to rats together with a sucrose load results in a marked retardation of sucrose digestion. The carbohydrate content of the small intestine is dose dependently increased; the time needed for the absorption is doubled. In the large intestine significant amounts of carbohydrate can be found only after administration of high doses of acarbose (2-4 mg/kg p.o.). In oral sucrose and maltose loading tests the blood glucose increase is dose dependently reduced by acarbose (ED50, 1 or 12 mg/kg, respectively). In perfused jejunal loops of rats, acarbose inhibits the absorption of sucrose (4 g/l) and maltose (1 and 2 g/l), the IC50 values being 3.2, 36, and 57 micrograms/ml, respectively. The data indicate that acarbose effectively inhibits sucrose digestion. It is 10-20 times less effective with maltose as a substrate. Slight malabsorption is induced by acarbose only in doses higher than the ED50.
D020909:Acarbose; D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D004063:Digestion / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005959:Glucosidases / Q000037:antagonists & inhibitors*; D065089:Glycoside Hydrolase Inhibitors; D007408:Intestinal Absorption / Q000187:drug effects*; D007420:Intestine, Large / Q000032:analysis; D007421:Intestine, Small / Q000187:drug effects / Q000201:enzymology; D007583:Jejunum / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008320:Maltose / Q000378:metabolism*; D009844:Oligosaccharides / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013395:Sucrose / Q000378:metabolism*; D014312:Trisaccharides / Q000008:administration & dosage / Q000494:pharmacology*
D001786:Blood Glucose; D065089:Glycoside Hydrolase Inhibitors; D009844:Oligosaccharides; D014312:Trisaccharides; D013395:Sucrose; D008320:Maltose; D005959:Glucosidases; D020909:Acarbose