Simultaneous milk and saliva samples were collected over a seven-day period from five lactating subjects after they had ingested two tablets of chloroquine sulfate (300 mg base). The samples were analyzed for chloroquine content by use of a combination of thin-layer chromatography and spectrophotometry. Regression analysis of two variables subject to error was used to determine the milk:saliva levels relationship. The Student's t test for paired data at .05 level of significance was used to evaluate the relationship between chloroquine levels in milk and saliva. The milk:saliva chloroquine concentrations ratio obtained by regression analysis was 0.89 +/- 0.08 (r = .93; P less than .05), and this compared favorably with the value of 0.99 +/- 0.07 obtained from the ratio of the AUC. There were no significant differences in the Tmax, Cmax, AUC, clearance, and elimination half-life values of chloroquine in milk and saliva (P greater than .05). Milk and saliva appear to be part of the central compartment. The amount of chloroquine estimated to be consumed by a nursling over a 24-hour period is about 0.55% of a 300-mg dose consumed by the mother. The data suggest that milk chloroquine levels can be estimated from saliva levels.

Five healthy male volunteers participated in this study, after informed consent, to determine the effect of chloroquine administration on plasma albumin, bilirubin, amylase, alkaline phosphatase and blood urea. Each subject took 600 mg of chloroquine base (i.e. four tablets containing a 150-mg base per tablet) and blood samples were obtained over a 7-day period. The plasma samples were assayed for albumin, bilirubin, amylase, alkaline phosphatase and blood urea. Results indicate that at the dose used chloroquine administration does not produce any significant change in the plasma levels of albumin and bilirubin. However, serum amylase and urea were decreased while alkaline phosphatase was increased by the chloroquine treatment. These changes are of no clinical significance as the new values are within the normal ranges.