Pharmaceutical evaluation of carbamazepine suppositories in rats.
The absorption of carbamazepine (CBZ) after rectal administration in the form of a suppository was studied in rats. CBZ suppositories were prepared with Witepsol H-15 (H-15), Witepsol S-55 (S-55) or polyethylene glycol 6000 (PEG) bases by moulding procedure. An in vitro investigation was undertaken using a dissolution apparatus. The in vitro dissolution rate of CBZ showed marked differences among the bases in the order PEG > H-15 > S-55. An in vivo study demonstrated marked differences in the time required to reach peak plasma concentration (Tmax) of CBZ after rectal and oral administration: the absorption of CBZ from PEG base was the most prolonged among these bases (in the order PEG > H-15 > S-55 > ORAL). Comparison of the area under the plasma concentration-time curve (AUC) of CBZ after rectal administration of the three different suppositories with those after intravenous and oral administration showed no significant differences in the AUC among the five preparations. These results suggest the possibility that CBZ suppositories can replace oral treatment for epilepsy.
Shinoda
M
M
Department of Hospital Pharmacy, Nagoya University Branch Hospital, Japan.
Akita
M
M
Hasegawa
M
M
Nadai
M
M
Hasegawa
T
T
Nabeshima
T
T
D000818:Animals; D000927:Anticonvulsants / Q000493:pharmacokinetics*; D001682:Biological Availability; D002220:Carbamazepine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013488:Suppositories
D000927:Anticonvulsants; D013488:Suppositories; D002220:Carbamazepine