The efficacy of urine data in comparative bioavailability of proguanil after oral and rectal administration in man

Abstract

The bioavailability of proguanil formulated as suppository, was compared to the tablet formulation in a bid to evaluate the utility of the suppository dosage form as means of administering proguanil in children and high-risk groups, such as sickle cell patients, who may not tolerate oral route of administration. The study was a completely randomized cross over involving administration of 200 mg of proguanil suppository and tablet to twelve healthy volunteers. Biological fluids such as urine and blood were collected before and at predetermined time intervals following administration of the drug. The biological samples were analyzed for the unchanged proguanil using an earlier reported method. The relative bioavailability of proguanil suppository as compared to the tablet dosage form was found to be about 61% from both urine and plasma data. The findings showed for the first time that proguanil suppository could be sufficiently bioavailable and may therefore be useful in chemoprophylaxis of malaria in sickle cell patients and children, particularly under such conditions that made oral route become impracticable.

Key words: Proguanil, tablets, suppositories, plasma and urine data, bioavailability.