In vitro co-culture systems of hepatic and intestinal cells for cellular pharmacokinetic and pharmacodynamic studies of capecitabine against colorectal cancer

Table 3 Pharmacokinetic parameters of CAP and its metabolites (5'-DFCR, 5'-DFUR and 5-FU) in HCT-8 cells after CAP administration (500 μM) (Mean ± SD, n = 4)

HCT-8		T_max (h)	C_max (ng/μg protein)	AUC_0-t (h*ng/μg protein)
Pre-metabolized by HepG2 cells for 0 h	CAP	48 ± 0	1.09 ± 0.18	44.88 ± 5.61
	5'-DFCR	24 ± 0	0.03 ± 0.01	0.91 ± 0.05
	5'-DFUR	24 ± 0	0.03 ± 0.009	1.14 ± 0.73
	5-FU	48 ± 0	0.02 ± 0.002	0.31 ± 0.01
Pre-metabolized by HepG2 cells for 24 h	CAP	24 ± 0^**	0.91 ± 0.05	40.10 ± 3.41
	5'-DFCR	12 ± 0^**	0.05 ± 0.006^**	1.71 ± 0.78^**
	5'-DFUR	12 ± 0^**	0.11 ± 0.07^**	3.32 ± 0.44^**
	5-FU	48 ± 0	0.043 ± 0.003^**	1.25 ± 0.77^**
Pre-metabolized by HepG2 cells for 48 h	CAP	12 ± 0^**	0.87 ± 0.09^*	33.94 ± 6.12^**
	5'-DFCR	12 ± 0^**	0.062 ± 0.002^**	1.90 ± 0.34^**
	5'-DFUR	6 ± 0^**	0.12 ± 0.07^**	3.12 ± 0.17^**
	5-FU	48 ± 0	0.06 ± 0.005^**	2.07 ± 0.22^**

T_max time to peak concentration; C_max peak concentration; AUC_0-t area under the concentration–time curve from zero to the time of last measurable concentration
^*P < 0.05
^**P < 0.01 compared with the group of pre-metabolized by HepG2 cells for 0 h

ISSN: 1475-2867