TABLE 1

Effect of organic solvents on the kinetics of CYP2B6-mediated bupropion hydroxylation in the presence of HLM

Kinetic parameters are expressed as % Control (mean ± S.D.).

	Solvent (%, v/v)
	Methanol	Ethanol	Acetonitrile	DMSO
K _m
0 (Control)	100.0 ± 4.2	100.0 ± 8.5	100.0 ± 3.9	100.0 ± 2.3
0.2	115.1 ± 0.5	118.1 ± 1.1	108.2 ± 2.5	114.7 ± 1.5
0.5	110.9 ± 2.0	139.5 ± 1.6^a	125.4 ± 1.2^a	162.3 ± 0.6^b
1	209.8 ± 45.9^a	N.E.	N.E.	N.E.
2	174.1 ± 3.0^c	444.7 ± 14.5^c	311.0 ± 6.7^b	332.3 ± 40.4^a
5	341.2 ± 22.5^c	1327.8 ± 293.0^a	901.4 ± 18.4^b	763.2 ± 126.6^a
V _max
0 (Control)	100.0 ± 3.2	100.0 ± 2.0	100.0 ± 3.6	100.0 ± 3.4
0.2	95.6 ± 3.0	96.1 ± 1.2	93.2 ± 1.4	93.3 ± 3.0
0.5	93.4 ± 1.9	91.7 ± 2.4	92.2 ± 2.2	92.2 ± 1.0
1	105.0 ± 5.6	N.E.	N.E.	N.E.
2	82.4 ± 0.9^c	73.3 ± 1.5^c	86.1 ± 0.7^a	93.9 ± 8.1
5	69.0 ± 0.4^c	54.1 ± 9.1^a	65.2 ± 1.9^c	72.3 ± 7.8^a
CL_int
0 (Control)	100.0 ± 4.6	100.0 ± 6.5	100.0 ± 7.5	100.0 ± 5.7
0.2	82.9 ± 3.0	81.1 ± 0.2	86.0 ± 3.3	81.4 ± 3.6
0.5	84.2 ± 3.2	65.5 ± 0.9^a	73.4 ± 1.1^a	56.8 ± 0.8^a
1	50.5 ± 8.4^a	N.E.	N.E.	N.E.
2	47.3 ± 1.4^c	16.4 ± 0.2^c	27.7 ± 0.4^c	28.3 ± 1.0^c
5	20.3 ± 1.2^c	4.1 ± 0.2^c	7.2 ± 0.1^c	9.5 ± 0.6^c

N.E., not evaluated.
↵ a Significantly different from control: P < 0.05, Student's t test.
↵ b Significantly different from control: P < 0.001, Student's t test.
↵ c Significantly different from control: P < 0.01, Student's t test.