HUMAN PHARMACOKINETICS OF CHLOROQUINE AND PROGUANIL DELIVERED IN A SINGLE CAPSULE FOR MALARIA CHEMOPROPHYLAXIS

Two antimalarial prophylactic regimens were compared in 17 healthy vol unteers. Regimen A consisted of daily ingestion of a single capsule co ntaining 100 mg base chloroquine (CQ) and 200 mg proguanil (PG). Regim en B consisted of daily ingestion of separate tablets of CQ (100 mg ba se) and PG (two 100 mg tablets). Both treatments lasted for 12 days. E ffective chloroquine levels were reached after 72 hours with both regi mens (49.9 ng/ml for treatment A and 36.7 ng/ml for treatment B). Prog uanil and cycloguanil plasma levels were significantly lower on sampli ng obtained at H3 (three hours later) and H6 (six hours later) on day 1 in the regimen A (p < 0.002). Thereafter there were no significant d ifference between the two regimens. Both regimens were well tolerated, but regimen A using the capsule appeared better accepted and facilita tes compliance.