The effect of new alpha-glucosidase inhibitors (BAY m 1099 and BAY o 1248) on meal-stimulated increases in glucose and insulin levels in man.
To confirm findings obtained from animal experiments demonstrating the metabolic effect of two new glucosidase inhibitors, 7 single blind cross-over studies with 42 healthy male volunteers were performed. In each group 6 subjects received 25, 50, 100 and 200 mg BAY m 1099 and 10, 20, and 40 mg BAY o 1248 or placebo with a standardized breakfast. Blood glucose and serum insulin were measured in venous blood before and 30, 60, 90, 120 and 180 min after each of 3 meals. ECG, blood pressure, body weight, monitor ECG and haematological and clinico-chemical parameters were also examined. The postprandial increase in blood glucose and serum insulin after breakfast were significantly and dose-dependently reduced by BAY m 1099. 10 and 20 mg BAY o 1248 not only reduced the increases in blood glucose and serum insulin after breakfast, but also after lunch (10 mg). 40 mg BAY o 1248 prevented the postprandial increase in both metabolic parameters after breakfast (p less than 0.05), an effect which was sustained after lunch. Intestinal problems occurred (flatulence, meteorism, diarrhoea) in 25 of 42 volunteers. Objective tolerability was good. The results of these first clinical pharmacological studies with two new glucosidase inhibitors justify studies on patients with diabetes mellitus.
D017485:1-Deoxynojirimycin / Q000031:analogs & derivatives; D000328:Adult; D001786:Blood Glucose / Q000378:metabolism*; D002986:Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D005944:Glucosamine / Q000031:analogs & derivatives / Q000494:pharmacology; D005959:Glucosidases / Q000037:antagonists & inhibitors*; D065089:Glycoside Hydrolase Inhibitors; D006801:Humans; D050112:Imino Pyranoses; D007328:Insulin / Q000097:blood*; D008297:Male; D008875:Middle Aged; D011897:Random Allocation
D001786:Blood Glucose; D065089:Glycoside Hydrolase Inhibitors; D050112:Imino Pyranoses; D007328:Insulin; C045621:miglitol; D017485:1-Deoxynojirimycin; D005959:Glucosidases; D005944:Glucosamine; C045622:emiglitate