Relative bioavailability of lamotrigine chewable dispersible tablets administered rectally.
OBJECTIVE
To determine the relative bioavailability of lamotrigine (LTG) chewable dispersible tablets after rectal administration.


METHODS
Two-period, crossover study with a 2-week washout between dosing periods.


METHODS
Clinical research center.


METHODS
Twelve healthy adult volunteers.


METHODS
One hundred milligrams of a LTG chewable dispersible tablet was administered by oral and rectal routes.


RESULTS
Plasma samples were collected before and up to 120 hours after drug administration. The samples were analyzed for LTG by high-performance liquid chromatography, and the relative bioavailability was determined. Drug concentrations were lower after rectal than after oral administration. The relative bioavailability (F = AUC(rectal)/AUC(oral)) was 0.52 +/- 0.23 (SD).


CONCLUSIONS
Drug prepared from LTG chewable dispersible tablets is absorbed rectally, although not to the same extent as when given orally. Rectal administration of suspension of these tablets can be an acceptable route of administration.
Birnbaum
A K
AK
Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis 55455, USA.
Kriel
R L
RL
Im
Y
Y
Remmel
R P
RP
D000285:Administration, Rectal; D000328:Adult; D000927:Anticonvulsants / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D018592:Cross-Over Studies; D005260:Female; D006801:Humans; D000077213:Lamotrigine; D008297:Male; D014227:Triazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D000927:Anticonvulsants; D014227:Triazines; D000077213:Lamotrigine