Table 2

Estimation of CL_{int,in vivo} from in vivo pharmacokinetic data for model compounds in rats and humans

Compounds	Species	CL_oral or CL_tot	F_a	f_p	R_B	CL_{int,in vivo}		E_H	Metabolic Pathway	Reference
Compounds	Species	CL_oral or CL_tot	F_a	f_p	R_B	Well stirred	Dispersion	E_H	Metabolic Pathway	Reference
		ml/min/kg body weight				ml/min/kg body weight
FK1052	Rat	875^2-a	0.95	0.03	1.21	27,700	7,950	0.93	Oxidation	In house data
	Human	26.4^2-a		0.016	0.78	1,570	1,070	0.61
FK480	Rat	81.1^2-a	0.70	0.01	0.626	5,680	3,820	0.62	Oxidation	In house data
	Human	2.4^2-a		0.005	0.6	336	321	0.12
Diazepam	Rat	103.8^2-a	1.00	0.137	1.04	758	496	0.64	Oxidation	Diaz-Garcia et al. (1992), Luurila et al. (1996),
	Human	0.7^2-a		0.032	1.04	21.9	21.5	0.03		Navia and Chaturvedi (1996), Sawada et al. (1985), Klotz et al. (1976)
Diltiazem	Rat	300.2^2-a	1.00	0.184	0.93	1,630	685	0.85	Oxidation	Tsui et al. (1994), Kölle et al. (1983)
	Human	64.2^2-a		0.22	1.0	292	160	0.76		Levet-Trafit et al. (1996), Lee et al. (1992), Piepho et al. (1982)
Quinotolast	Rat	27.9^2-b	1.00	0.033	0.65	574	489	0.35	Oxidation, glucuronidation	Katashima et al. (1993a,b)
	Human	1.23^2-a		0.0191	0.59	64.4	62.2	0.09		Nakashima et al. (1993), in house data
Troglitazone	Rat	21.5^2-b	0.718	0.000921	0.594	67,800	43,700	0.66	Glucuronidation, sulfation	Izumi et al. (1996)
	Human	13.1^2-a		0.000941	0.548	10,000	7,910	0.45
FK079	Rat	1.64^2-b	1.00	0.060	0.63	28.8	28.3	0.05	Oxidation, hydrolysis	Tokuda et al. (1997)
	Human	10.82^2-a		0.017	0.59	636	497	0.22
Zidovudine	Rat	40.67^2-b	1.00	0.786	1.0	20.2	18.4	0.22	Glucuronidation, oxidation	Mays et al., (1991), de Miranda et al., (1990)
	Human	39.12^2-a		0.8	0.98	42.1	28.4	0.62		Yazdanian et al. (1998), Blum et al., (1988), Collins and Unadkat, (1989), Hedaya et al., (1990)
Acetaminophen	Rat	23.8^2-b	1.00	0.82	1.0	51.0	41.0	0.43	Glucuronidation, sulfation	Hjelle and Klaassen, (1984), Koss et al., (1970)
	Human	4.65^2-b		0.79	1.0	6.71	6.17	0.20		Gazzard et al. (1973), Chiou and Barve (1998), Sonne et al. (1988), Lin and Levy (1986)

↵2-a Cl_oral.
↵2-b Cl_tot.