Influence of antacids on the bioavailability of glibenclamide.
A single oral dose of glibenclamide (2.5 mg) was given to eight healthy volunteers in a randomized cross-over study after a standardized fasting and breakfast (374 kcal), with or without a concomitant intake of 10 ml of antacid suspension. Serum glibenclamide levels were determined by means of a specific radioimmunoassay method. The areas under the blood concentration-time curves (AUC0-infinity), with or without antacid, were 408.17 +/- 168.25 and 307.9 +/- 84.13 ng/ml (p less than 0.05), respectively. The peak concentrations of 96.88 +/- 49.9 and 66.19 +/- 32.35 ng/ml/h (p less than 0.05) with or without antacid, were reached in 4.13 and 3.81 h, respectively. Values of tmax, Vd and t1/2 were not affected by the presence of the antacid. A 33% increase in bioavailability of glibenclamide emerged, as seen from the respective AUC values, but no clinically remarkable effect was observed in the subjects.
Zuccaro
P
P
Clinical Biochemistry Department, Istituto Superiore di Sanità, Rome, Italy.
Pacifici
R
R
Pichini
S
S
Avico
U
U
Federzoni
G
G
Pini
L A
LA
Sternieri
E
E
D000328:Adult; D000863:Antacids / Q000494:pharmacology*; D001682:Biological Availability; D001786:Blood Glucose / Q000378:metabolism; D002096:C-Peptide / Q000097:blood; D003124:Colorimetry; D005260:Female; D005905:Glyburide / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D007328:Insulin / Q000097:blood; D008297:Male
D000863:Antacids; D001786:Blood Glucose; D002096:C-Peptide; D007328:Insulin; D005905:Glyburide