TABLE 4

Passive permeability (CL_perm) and in vitro CL_int from intestinal S9, HLM, and recombinant P450 and the scaled gut clearances (CL_int,g) from HLM and rCYP

Compound	CL_perm	Human Intestinal S9 CL_int	HLM CL_int (n = 2)	HLM CL_int,g (n = 2)	rCYP CL_int (n = 2)			rCYP CL_int,g (n = 2)
Compound	CL_perm	Human Intestinal S9 CL_int	HLM CL_int (n = 2)	HLM CL_int,g (n = 2)	Enzyme	Mean	S.D.	Enzyme	Mean	SD
	l/h	μl/min per mg protein	μl/min per mg protein	l/h	μl/min per pmol			μl/min per mg protein
Alprazolam	4.03	0.1 ± 0.01 (n = 2)	ND	ND	1A2	ND	ND	1A2	ND	ND
					2C9	ND	ND	2C9	ND	ND
					2C19	ND	ND	2C19	ND	ND
					2C8	ND	ND	2C8	ND	ND
					2D6	ND	ND	2D6	ND	ND
					3A4	0.091	0.000146	3A4	1.34	0.0022
Buspirone	7.9	4.52 ± 1.54 (n = 5)^{^a}	163.8 ± 8.7	4.47 ± 0.23	1A2	0.13	0.04	1A2	0	0
					2C9	0.063	0.08	2C9	0.05	0.06
					2C19	0.087	0.0023	2C19	0.02	0.00046
					2C8	0.073	0.018	2C8	0	0
					2D6	0.91	0.086	2D6	0.068	0.006
					3A4	4.77	0.27	3A4	70.36	3.98
Cyclosporine A	1.99	2.31 ± 1.54 (n = 3)	32.4 ± 3.8	0.88 ± 0.10	1A2	ND	ND	1A2	ND	ND
					2C9	0.36	0.0074	2C9	0.272	0.0056
					2C19	0.37	0.019	2C19	0.074	0.0038
					2C8	0.40	0.062	2C8	0	0
					2D6	0.33	0.11	2D6	0.025	0.008
					3A4	0.66	0.025	3A4	9.735	0.368
Erythromycin	3.25	2.48 ± 1.08 (n = 3)	9.2 ± 2.9	0.25 ± 0.07	1A2	ND	ND	1A2	ND	ND
					2C9	ND	ND	2C9	ND	ND
					2C19	ND	ND	2C19	ND	ND
					2C8	ND	ND	2C8	ND	ND
					2D6	ND	ND	2D6	ND	ND
					3A4	0.15	0.01	3A4	0.14	0.01
Felodipine	10.62	13.71 ± 5.29 (n = 4)	178.5 ± 6.7	4.87 ± 0.18	1A2	0.034	0.043	1A2	0	0
					2C9	0.075	0.049	2C9	0.0567	0.037
					2C19	1.07	0.095	2C19	0.214	0.019
					2C8	1.14	0.033	2C8	0	0
					2D6	0.017	0.010	2D6	0.0013	0.0008
					3A4	17.9	0.090	3A4	264.02	1.327
Indinavir	2.5	11.70 ± 9.49 (n = 4)^{^a}	NA	NA	ND			ND
Midazolam	10.5	13.55 ± 3.25 (n = 12)	290.5 ± 0.39	7.93 ± 0.011	1A2	ND	ND	1A2	ND	ND
					2C9	ND	ND	2C9	ND	ND
					2C19	0.074	0.0096	2C19	0.0148	0.00192
					2C8	ND	ND	2C8	ND	ND
					2D6	0.008	0.005	2D6	0.0006	0.0004
					3A4	3.421	0.040	3A4	50.46	0.59
Nifedipine	4.02	7.12 ± 3.34 (n = 4)^{^a}	191.9 ± 3.1	5.23 ± 0.086	1A2	0.20	0.06	1A2	0	0
					2C9	0.17	0.07	2C9	0.128	0.0529
					2C19	1.18	0.02	2C19	0.236	0.004
					2C8	0.38	0.04	2C8	0	0
					2D6	0.06	0.11	2D6	0.0045	0.0083
					3A4	10.53	0.47	3A4	155.31	6.932
Paracetamol	4.88	NA (n = 2)	NA	NA	NA			NA
Saquinavir	0.67	57.63 ± 27 (n = 4)^{^a}	NA	NA	NA			NA
Sildenafil	3.43	4.35 ± 0.51 (n = 4)	74.8 ± 1.66	2.04 ± 0.045	1A2	0.024	0.021	1A2	0	0
					2C9	0.184	0.019	2C9	0.139	0.0144
					2C19	0.004	0.002	2C19	0.0008	0.0004
					2C8	0.055	0.034	2C8	0	0
					2D6	0.104	0.016	2D6	0.0078	0.0012
					3A4	1.10	0.048	3A4	16.225	0.708
Tacrolimus	1.78	10.36 ± 0.14 (n = 3)	233.7 ± 25.3	6.38 ± 0.70	1A2	0.30	0.17	1A2	0	0
					2C9	0.15	0.01	2C9	0.1134	0.0076
					2C19	0.10	0.06	2C19	0.02	0.012
					2C8	0.19	0.05	2C8	0	0
					2D6	1.05	0.09	2D6	0.0788	0.0068
					3A4	2.86	0.10	3A4	42.185	1.475
Terfenadine	NA	49.5	163.80 ± 19.6	4.47 ± 0.53	ND			ND
Triazolam	11.8	1.1 ± 0.54 (n = 4)^{^a}	28.1 ± 3.3	0.77 ± 0.089	1A2	0.01	0.000	1A2	0	0
					2C9	0.02	0.029	2C9	0.0151	0.0219
					2C19	ND	ND	2C19	ND	ND
					2C8	0.02	0.005	2C8	0	0
					2D6	ND	ND	2D6	ND	ND
					3A4	0.42	0.023	3A4	6.195	0.339
Verapamil	13.51	3.8 ± 0.15 (n = 4)	85.2 ± 14.8	2.32 ± 0.40	1A2	ND	ND	1A2	ND	ND
					2C9	ND	ND	2C9	ND	ND
					2C19	ND	ND	2C19	ND	ND
					2C8	0.39	0.018	2C8	0	0
					2D6	0.24	0.024	2D6	0.018	0.0018
					3A4	2.13	0.085	3A4	31.41	1.254

NA, not available; ND, no metabolism detected.
↵^a Means from different individuals are significantly different (P < 0.05) statistically determined by one-way analysis of variance.