Effects of food on the bioavailability of sustained-release pinacidil in humans.
The effects of a standard breakfast meal on the bioavailability of a sustained-release tablet formulation of pinacidil [(+/-)-2-cyano-1- (4-pyridyl)-3-(1,2,2-trimethylpropyl)guanidine monohydrate) were investigated in eight healthy volunteers. Concomitant food intake resulted in significantly increased maximum measured serum pinacidil concentrations, Cmax, (172 +/- 21 versus 102 +/- 49 ng/mL, p less than 0.05), and relative bioavailability, measured as AUCo-infinity (904 +/- 189 versus 697 +/- 279 ng.h/mL, p less than 0.05). The time to maximum serum concentration (tmax) was not affected by food (2.3 +/- 1.3 versus 3.3 +/- 1.2 h, p greater than 0.05), and the terminal elimination half-life, (t1/2z) was significantly decreased (4.7 +/- 2.2 versus 2.3 +/- 0.4 h, p less than 0.05).
McBurney
A
A
Department of Clinical Pharmacology, Glenfield General Hospital, Leicester, UK.
Farrow
P R
PR
Ward
J W
JW
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D005260:Female; D005502:Food; D006146:Guanidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D020110:Pinacidil; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D006146:Guanidines; D014665:Vasodilator Agents; D020110:Pinacidil