Bio-availability of three formulations of glibenclamide.
Eighteen healthy men participated in a double-blind, randomised, crossover study to compare the bio-availability of three 5 mg formulations of glibenclamide. The products compared were Daonil (Hoechst), Glycomin (Lennon) and Melix (Lagamed). Volunteers received a continuous intravenous infusion of glucose at a rate of 0.25 g/kg/h for 10 hours. Two hours after commencement of this infusion medication was given orally with 200 ml of a 10% (m/v) glucose solution. The subjects also drank 200 ml of the glucose solution hourly for 5 hours after medication. Blood samples were taken up to 22 hours after medication for radio-immunoassay of glibenclamide as well as for measurement of glucose concentrations. The following kinetic variables were calculated; maximum concentration, time to maximum concentration, terminal half-life, areas under the serum concentration-time curves, relative total clearance, total mean time and relative volume of distribution. Daonil and Glycomin were bio-equivalent, but important differences were demonstrated between these two formulations and Melix. This study method necessitates close surveillance of volunteers in order to detect and treat hypoglycaemia.
Meyer
B H
BH
Department of Pharmacology, University of the Orange Free State, Bloemfontein.
Müller
F O
FO
Luus
H G
HG
Eckert
H G
HG
D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D002986:Clinical Trials as Topic; D004311:Double-Blind Method; D004339:Drug Compounding; D005905:Glyburide / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D011897:Random Allocation; D013997:Time Factors
D005905:Glyburide