Pharmacokinetics of the immunomodulatory 1,2-O-isopropylidene-3-O-3'-(N',N'-dimethyl-amino-n-propyl)-D-glucofuranose hydrochloride in normal human volunteers.

1,2-O-Isopropylidene-3-O-3'(N',N'-dimethyl-amino-n-propyl)-D-glucofuranose hydrochloride, I, is a substituted sugar with claimed immunomodulatory action. Pharmacokinetic studies in 10 volunteers (bolus i.v., 100 mg) showed respective half-lives for each exponential in the sum of two exponentials that characterized plasma level decay with time of 4.6 +/- 0.4 (SEM) min, t1/2(lambda 1), and 244 +/- 20 min, t1/2(lambda 2)), The total and renal clearances were 277 +/- 20 and 254 +/- 18 (SEM) ml/min, indicative of tubular secretion. Urinary recovery was 93 +/- 2%. The estimated volumes of distribution of the central compartment and overall equilibrated tissues were 14.7 +/- 1.9 and 96 +/- 8 liters, respectively. Sequential daily oral administration of large amounts in capsules (1.2, 2.1, 2.9, 4.1, and 5.0 g) permitted an estimate of 63 +/- 4 (SEM)% bioavailability from urinary recovery of drug, with estimated terminal half-lives of 454 +/- 25 min from minimal data. Orally administered 2.03 g showed a rapid absorption (t1/2 = 10 min) after a lag time of 23 min, and a terminal plasma half-life of 344 min. Plasma protein binding of I was negligible. The erythrocyte/plasma water partition coefficient was close to unity.