TABLE 3

Pharmacokinetic parameters for 11 UGT substrates

Drug	CL_tot	R_b	CL_r	F	F_aF_g			Reference
Drug	CL_tot	R_b	CL_r	F	17.1	20.7	25.5	Reference
	ml · min⁻¹ · kg⁻¹		ml · min⁻¹ · kg⁻¹		Q_h (ml · min⁻¹ · kg⁻¹)
Quercetin	11	1.0	0	0.001^{^a}	0.004	0.003	0.002	Cubitt et al., 2009
Raloxifene	14.7^{^b}	1.0	0	0.02	0.143	0.069	0.047	Thummel et al., 2005
Bazedoxifene	6.7^{^c}	0.55	0	0.06	0.145	0.117	0.101	Patat et al., 2003; Chandrasekaran et al., 2009
Bazedoxifene	6.7^{^c}	0.55	0	0.06	0.145	0.117	0.101	Chandrasekaran et al., 2003
Diclofenac	3.5	0.63	0	0.54	0.800	0.738	0.690	Willis et al., 1979
Diclofenac	3.5	0.63	0	0.54	0.800	0.738	0.690	Obach et al., 2008
Tolfenamic acid	2.2	0.66	0	0.60	0.745	0.715	0.690	Pentikäinen et al., 1981
Tolcapone	1.9	0.61	0	0.60	0.734	0.706	0.683	Jorga et al., 1998
Tolcapone	1.9	0.61	0	0.60	0.734	0.706	0.683	Obach et al., 2008
Entacapone	12	0.59	0	0.25	1.00^{^e}	1.00^{^f}	1.00^{^f}	Heikkinen et al., 2001
Entacapone	12	0.59	0	0.25	1.00^{^e}	1.00^{^f}	1.00^{^f}	Obach et al., 2008
Telmisartan	8.4	0.67	0	0.43	1.00^{^e, ^f}	1.00^{^f}	0.846^{^f}	Obach et al., 2008
Telmisartan	8.4	0.67	0	0.43	1.00^{^e, ^f}	1.00^{^f}	0.846^{^f}	Stangier et al., 2000
Gemfibrozil	1.7	0.58	0	0.98	1.00^{^f}	1.00^{^f}	1.00^{^f}	Thummel et al., 2005
Etodolac	0.66^{^d}	0.55	0	0.80	0.859	0.848	0.839
Indomethacin	1.4	0.55^{^g}	0.21	1.0	1.00^{^f}	1.00^{^f}	1.00^{^f}	Thummel et al., 2005

↵a Calculated from CL_tot (11 ml · min⁻¹ · kg⁻¹) and oral clearance (8333 ml · min⁻¹ · kg⁻¹) (Cubitt et al., 2009).
↵b Calculated from oral clearance data (735 ml · min⁻¹ · kg⁻¹) and reported bioavailability of 2% (Thummel et al., 2005).
↵c Calculated from oral clearance data (86.7 ml · min⁻¹ · kg⁻¹) and reported bioavailability of 6.2% (Patat et al., 2003; Chandrasekaran et al., 2009).
↵d Calculated from oral clearance data (0.82 ml · min⁻¹ · kg⁻¹) and reported bioavailability of 80%. Etodolac (Lodine) U.S. Food and Drug Administration drug approval package (http://www.accessdata.fda.gov/drugsatfda_docs/label/2006/018922s022,020584s009lbl.pdf).
↵e Calculated F_aF_g was < 0, because CL_tot/R_b/Q_h was > 1. Therefore, CL_tot/R_b was assumed to 90% of Q_h.
↵f When calculated F_aF_g was > 1, it was treated as 1.0.
↵g Assumed to be 0.55 because indomethacin and etodolac are acidic drugs (Cubitt et al., 2011).