TABLE 2

Kinetic parameters of diclofenac, etodolac, and ibuprofen glucuronidation in liver microsomes

Compound	Liver Microsome	Kinetic Parameter
Compound	Liver Microsome	K_m	V_max	K_i	CL_int
		μM	nmol/min per mg	mM	µl/min per mg
Etodolac	Humanized UGT1 mice^{^a}	483 ± 40	0.379 ± 0.003	―	0.79 ± 0.06
	Humans^{^a}	483 ± 50	0.246 ± 0.012	―	0.51 ± 0.03
	Mice^{^a}	1170 ± 287	0.201 ± 0.029	―	0.17 ± 0.01
Diclofenac	Humanized UGT1 mice^{^a}	31.8 ± 1.91	7.05 ± 0.04	―	222 ± 12.2
	Humans^{^b}	33.1 ± 1.70	10.4 ± 0.28	22.5 ± 1.00	313 ± 8.88
	Mice^{^a}	55.6 ± 1.52	11.8 ± 0.10	―	211 ± 5.62
rac-Ibuprofen	Humanized UGT1 mice^{^a}	319 ± 26	4.27 ± 0.12	―	13.4 ± 0.71
	Humans^{^a}	651 ± 8.1	6.44 ± 0.05	―	9.9 ± 0.05
	Mice^{^a}	364 ± 12	11.2 ± 0.19	―	30.7 ± 0.54
S-Ibuprofen	Humanized UGT1 mice^{^a}	381 ± 26	7.54 ± 0.16	―	19.9 ± 1.00
	Humans^{^a}	699 ± 34	8.71 ± 0.17	―	12.5 ± 0.38
	Mice^{^a}	364 ± 5.0	16.5 ± 0.19	―	45.1 ± 0.50
R-Ibuprofen	Humanized UGT1 mice^{^a}	320 ± 38	2.18 ± 0.07	―	6.87 ± 0.56
	Humans^{^a}	428 ± 11	3.37 ± 0.03	―	7.86 ± 0.13
	Mice^{^a}	424 ± 19	8.00 ± 0.09	―	18.9 ± 0.70

↵^a Calculated using the Michaelis–Menten equation.
↵^b Calculated using substrate inhibition.