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

Table 5 Pharmacokinetic parameters of CAP and its metabolites (5'-DFCR, 5'-DFUR and 5-FU) in SW620 cells after CAP administration (500 μM) (Mean ± SD, n = 4)

SW620		T_max (h)	C_max (ng/μg protein)	AUC_0-t (h*ng/μg protein)
Pre-metabolized by HepG2 cells for 0 h	CAP	24 ± 0	1.34 ± 0.23	46.54 ± 2.27
	5'-DFCR	48 ± 0	0.03 ± 0.004	0.65 ± 0.03
	5'-DFUR	48 ± 0	0.02 ± 0.003	0.20 ± 0.05
	5-FU	48 ± 0	0.001 ± 0.0004	0.01 ± 0.004
Pre-metabolized by HepG2 cells for 24 h	CAP	12 ± 0^**	0.001 ± 0.0004	42.93 ± 1.54
	5'-DFCR	24 ± 0^**	0.04 ± 0.001	1.54 ± 0.32^**
	5'-DFUR	48 ± 0	0.03 ± 0.002^*	0.70 ± 0.01^**
	5-FU	48 ± 0	0.007 ± 0.0003^**	0.70 ± 0.02^**
Pre-metabolized by HepG2 cells for 48 h	CAP	48 ± 0^**	1.02 ± 0.23^*	41.45 ± 1.36^*
	5'-DFCR	12 ± 0^**	0.05 ± 0.003^**	1.83 ± 0.44^**
	5'-DFUR	24 ± 0^**	0.04 ± 0.007^**	1.01 ± 0.26^**
	5-FU	48 ± 0	0.05 ± 0.004^**	1.20 ± 0.37^**

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