Table 1

Effect of solubility of HIV protease inhibitors on drug absorption in dogs after a 5-mg/kg p.o. dose

Compound	R	C_max(μM)^1-a	Solubility (mg/ml) at pH 7.4 (or 3.5)	logP
L-732,747	benzyloxycarbonyl	<0.10	<0.001	4.67
L-735,482	8-quinolinylsulfonyl	<0.10	<0.001	3.70
L-738,891	2,4-difluorophenylmethyl	0.73 ± 0.15	0.0012	3.69
L-735,524	3-pyridylmethyl	11.4 ± 2.3	0.07 (60)	2.92

↵1-a C_max, maximum drug concentration in plasma. See figure 1. Data excerpted from Dorsey et al. (1994).