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

Table 2 Pharmacokinetic parameters of CAP and its metabolites (5'-DFCR, 5'-DFUR and 5-FU) in LoVo cells after CAP administration (500 μM) (Mean ± SD, n = 4)

LoVo		T_max (h)	C_max (ng/μg protein)	AUC_0-t (h*ng/μg protein)
Pre-metabolized by HepG2 cells for 0 h	CAP	12 ± 0	1.83 ± 0.39	66.33 ± 5.55
	5'-DFCR	24 ± 0	0.41 ± 0.11	1.57 ± 0.42
	5'-DFUR	48 ± 0	0.01 ± 0.003	0.27 ± 0.01
	5-FU	48 ± 0	0.007 ± 0.0002	0.23 ± 0.03
Pre-metabolized by HepG2 cells for 24 h	CAP	24 ± 0^**	1.52 ± 0.76^*	55.24 ± 6.64^**
	5'-DFCR	24 ± 0	0.14 ± 0.04^**	4.89 ± 0.88^**
	5'-DFUR	24 ± 0^**	0.02 ± 0.001^**	0.52 ± 0.09^**
	5-FU	24 ± 0^**	0.01 ± 0.003^*	0.43 ± 0.02^**
Pre-metabolized by HepG2 cells for 48 h	CAP	24 ± 0^**	1.54 ± 0.35^*	57.96 ± 0.74^*
	5'-DFCR	24 ± 0	0.24 ± 0.03^**	8.37 ± 0.53^**
	5'-DFUR	24 ± 0^**	0.04 ± 0.002^**	1.24 ± 0.24^**
	5-FU	48 ± 0	0.03 ± 0.009^**	1.00 ± 0.09^**

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