J. Mizumura et al., Possibility of partial absorption of nicardipine by routes other than the hepato-portal system after oral administration in rats, J PHARM PHA, 50(7), 1998, pp. 775-781
The systemic availability of nicardipine after different routes of administ
ration has been examined in rats, with particular attention to differentiat
ing oral absorption from intestinal and hepatic metabolism. The quantities
of nicardipine and its metabolite were determined by capillary column gas c
hromatography.
A linear relationship was shown between the hepatic first-pass effect and d
ose after hepato-portal administration of nicardipine; the hepatic first-pa
ss effect was calculated to be approximately 80%. However, the availability
after oral and rectal administration was found to be more than twice that
observed after hepato-portal administration. Partial avoidance of the hepat
ic first-pass effect after oral and rectal administration are estimated to
be 37.3% and 35.2%, respectively, assuming that all absorbed molecules pass
through the liver.
These findings suggest that the absorption of nicardipine after oral admini
stration also occurs by routes other than the hepato-portal system.