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

Table 1 Pharmacokinetic parameters of CAP and its metabolites (5'-DFCR, 5'-DFUR and 5-FU) in SW480 cells after CAP administration (500 μM) (Mean ± SD, n = 4)

SW480		T_max (h)	C_max (ng/μg protein)	AUC_0-t (h*ng/μg protein)
Pre-metabolized by HepG2 cells for 0 h	CAP	16.00 ± 6.93	1.27 ± 0.27	43.77 ± 2.18
	5'-DFCR	6.00 ± 0	0.03 ± 0.002	0.81 ± 0.07
	5'-DFUR	48 ± 0	0.03 ± 0.001	1.03 ± 0.09
	5-FU	48 ± 0	0.0008 ± 0.00005	0.009 ± 0.0003
Pre-metabolized by HepG2 cells for 24 h	CAP	12 ± 0^**	1.04 ± 0.08	39.05 ± 3.36
	5'-DFCR	12 ± 0^**	0.08 ± 0.003^	2.27 ± 0.17^**
	5'-DFUR	24 ± 0^**	0.06 ± 0.005^**	1.98 ± 0.06^**
	5-FU	48 ± 0	0.02 ± 0.002^**	0.72 ± 0.05^**
Pre-metabolized by HepG2 cells for 48 h	CAP	12 ± 0^**	0.95 ± 0.08^**	35.74 ± 5.89^**
	5'-DFCR	6 ± 0	0.11 ± 0.05^**	2.97 ± 0.66^**
	5'-DFUR	48 ± 0	0.07 ± 0.004^**	2.84 ± 0.51^**
	5-FU	48 ± 0	0.06 ± 0.007^**	2.34 ± 0.44^**

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