This in vitro investigation was performed to study the adsorption rate cons
tant as well as the adsorption characteristics of fluoxetine (F) to activat
ed charcoal and its commercial formulation Carbomix powder in simulated gas
tric (pH 1.2) fluid environment. Ion-selective electrode (ISE) potentiometr
y, based on the selective, direct and continuous monitoring of F with an F-
ISE constructed in our laboratory was used. The method used in the kinetic
experiments consists of the rapid addition of a slurry containing the charc
oal into the drug solution under stirring and continuous recording of the F
-ISE potential until the establishment of equilibrium. The free ionized dru
g concentration at appropriate time intervals was calculated from the recor
ded adsorption curve and the apparent adsorption rate constant was estimate
d assuming pseudo first order kinetics. Within run R.S.D. of the estimates
ranged from 0.24 to 11.5%, while between run R.S.D. (n=3-4) ranged from 0.9
0 to 13.8%. A linear relationship was found between the apparent adsorption
rate constants and the amount of charcoal used with slopes (+/-S.D.) for a
ctivated charcoal and Carbomix equal to 1.14(+/-0.21) and 0.146(+/-0.009) s
(-1) g(-1), respectively. Successive additions of microvolumes of F solutio
n were made into a charcoal slurry with measurement of the F-ISE potential
at equilibrium. The maximum adsorption capacity values (+/-S.D.) of activat
ed charcoal and Carbomix were 254.8+/-1.8 and 405+/-41 mg/g, respectively w
hile the affinity constant values (+/-S.D.) were 45.6+/-2.2 and 55.5+/-2.91
/g, respectively. The adsorption of F to charcoals was rapid and for amount
s of charcoal 10 times greater than the amount of the drug, 95% of F was ad
sorbed within the first 5 min. Relative to the toxic and lethal doses in ca
ses of F intoxications, both types of charcoals tested adsorbed effectively
F at gastric pH. Carbomix can be considered as appropriate charcoal formul
ation for medical treatment in cases of F poisoning. (C) 2001 Elsevier Scie
nce B.V. All rights reserved.