TABLE 2

CL_int values (microliters per minute per milligram protein or 10⁶ cells) of 32 test compounds using intestinal microsomes, permeabilized enterocytes, and intestinal mucosa and their respective observed in vivo f_g value

CL_int values were measured in at least three independent experiments, and results are presented as the mean ± S.E.

	Observed Human f_g Value	Intestinal Microsomes	Permeabilized Enterocytes	Intestinal Mucosa
Compound	Range 0–1	μl/Min per Milligram Protein		μl/Min per 10⁶ Cells
Dabigatran etexilate	0.05	69.5 ± 3.7	669.4 ± 15.4	585.2 ± 8.5
Raloxifene	0.05	338.0 ± 22.7	114.2 ± 19.6	203.0 ± 20.6
Testosterone	0.05	95.3 ± 7.7	545.7 ± 130.2	612.7 ± 37.9
Lovastatin	0.07	83.8 ± 23.2	186.5 ± 10.8	243.4 ± 14.7
Nisoldipine	0.11	78.1 ± 7.9	131.8 ± 19.5	199.3 ± 13.6
Buspirone	0.18	5.1 ± 2.5	7.8 ± 1.9	19.8 ± 2.8
Rifabutin	0.21	2.9 ± 1.0	16.2 ± 4.0	2.7 ± 1.5
Saquinavir	0.28	140.4 ± 7.0	357.0 ± 46.2	60.6 ± 3.3
Simvastatin	0.29	ND^{^a}	6.8 ± 3.3	7.9 ± 11.1
Atorvastatin	0.40	1.9 ± 1.4	3.0 ± 1.4	ND^{^a}
Terfenadine	0.40	9.0 ± 3.1	55.5 ± 10.1	57.1 ± 1
Felodipine	0.42	14.5 ± 2.1	64.8 ± 10.6	85.7 ± 2.6
Cyclosporin	0.48	10.4 ± 2.6	18.3 ± 8.6	56.5 ± 0.0
Midazolam	0.55	10.8 ± 1.1	9.2 ± 1.3	16.9 ± 3
Cisapride	0.57	4.6 ± 1.5	19.2 ± 3.3	27.0 ± 4.1
Ramipril	0.59	1.4 ± 0.0	ND^{^a}	ND^{^a}
Verapamil	0.60	2.1 ± 1.0	33.6 ± 4.5	73.6 ± 11.1
Sildenafil	0.62	4.7 ± 1.6	2.2 ± 2.2	5.0 ± 7.2
Nifedipine	0.71	2.9 ± 2.2	11.1 ± 2.8	5.9 ± 1.2
Diclofenac	0.78	27.7 ± 3.2	9.9 ± 3.2	10.4 ± 0.5
Methadone	0.78	ND^{^a}	14.8 ± 1.7	6.3 ± 0.8
Zolpidem	0.79	7.0 ± 2.2	3.1 ± 2.1	ND^{^a}
Trazodone	0.83	3.0 ± 0.0	5.8 ± 2.4	NDa
Repaglinide	0.89	2.2 ± 1.8	1.2 ± 3.5	1.3 ± 0.6
Quinidine	0.91	ND^{^a}	ND^{^a}	ND^{^a}
Indinavir	0.93	3.7 ± 1.4	25.2 ± 3.7	1.9 ± 1.0
Alprazolam	0.94	2.2 ± 1.2	1.5 ± 0.7	1.4 ± 0.6
Enalapril	0.97	ND^{^a}	ND^{^a}	ND^{^a}
Benzydamine	0.98	ND^{^a}	28.7 ± 0.0	18.6 ± 0.0
Carbazeran	NA^{^b}	2.1 ± 0.8	ND^{^a}	ND^{^a}
S-Mephenytoin	NA^{^b}	3.4 ± 0.0	ND^{^a}	ND^{^a}
Terbutaline	NA^{^b}	ND^{^a}	ND^{^a}	ND^{^a}

NA, data not available; ND, not determined.
↵^a CL_int values detected were below the limit of quantification; 1 μl/min per 10⁶ cells or 1 µl/min per milligram protein, corresponding to 97% of substrate remaining after 60 min of incubation.
↵^b Insufficient information in the literature to estimate human f_g.