DETERMINATION OF THE EFFECT OF ASCORBIC ACID ON THE PHARMACOKINETIC PROFILE OF ARTEMETHER IN RABBITS

Godfrey Eghosa Aghayere*, Henry Akpobor Okeri and Fabian Chukwugozie Amaechina

ABSTRACT

Background: Malaria is one of the major public health challenges in Nigeria. Treatment failure as a result of drug interaction is a major problem. A study of the effect of ascorbic acid on the antiplasmodial activity of artemether has been reported. Objective: This study was carried out to determine the effect of ascorbic acid on the pharmacokinetic profile of artemether. Method: Fourteen male rabbits weighing between 2.0 – 2.5 kg were used in this study. Four of the rabbits were used for determination of the efficiency, recovery studies and calibration curve while ten rabbits were randomly selected into Group A and B consisting of five rabbits each were used for the pharmacokinetic studies. Group A was administered a single dose of 10 mg/kg artemether while Group B was co-administered a single dose of 10 mg/kg artemeter and 10 mg/kg ascorbic acid intramuscularly. The dihydroartemisinin in the plasma was analysed using High Performance Liquid Chromatography. Results: The results showed that ascorbic acid affect the pharmacokinetic parameters of artemether. The time to reach maximum concentration (Tmax) increase from 30.00 min to 42.00 min while the maximum concentration (Cmax) and Area-under the Concentration Curve (AUC) decrease from 1461.9 (ng/mL) and 6566.7 (ng hr/mL) to 1331.1 (ng/mL) and 6105.8 (ng hr/mL), respectively. Conclusion: Ascorbic acid altered the pharmacokinetic profile of artemether. In clinical practice patients should be adviced not to co-administer ascorbic acid with artemether.

Keywords: Dihydroartemisinin, artemether, ascorbic acid, pharmacokinetic parameters.