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The sera of diabetic patients showed an inverse correlation (r = -0.67, n = 57) between free gliclazide (oral hypoglycemic drug) level and the fructosamine value. The binding capacity of the primary binding site for gliclazide in the albumin molecule was increased from 4.5 x 10(-4) to 8.0 x 10(-4) M-1 by glycation of albumin, but not that of the secondary binding site (1.2 x 10(-4) M-1). This suggests that the glycation of albumin increases its total binding capacity for gliclazide, resulting in a low free gliclazide level. Therefore, a low hypoglycemic activity of the drug is observed when it is administered to diabetic patients with hyperglycemia.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Influence of Blood Proteins on Biomedical Analysis. XII. Effects of Glycation on Gliclazide (Oral Hypoglycemic Drug)-Binding with Serum Albumin in Diabetics.