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.