DETERMINATION OF SOME PHARMACOKINETIC PROPERTIES OF ARTEMETHER-LUMEFANTRINE GRANULES IN ALBINO RATS

Edwin A. Ubieko; Emmanuel A. Ubieko

doi:10.22270/ujpr.v9i4.1163

Edwin A. Ubieko Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences University of Port Harcourt, Choba, Port Harcourt, Rivers State, Nigeria.
Emmanuel A. Ubieko Department of Physics, Faculty of Science, University of Port Harcourt, Choba, Port Harcourt. Rivers State, Nigeria.

10.22270/ujpr.v9i4.1163

Keywords:

Area under the curve (AUC), maximum concentration (Cmax), mean residence time (MRT), pharmacokinetic, time to reach the maximum concentration (Tmax)

Abstract

Aim and Objectives: Malaria is an infectious disease that is caused by plasmodium parasites which is rampant in Sahara Africa and children under 5 years of age are highly vulnerable to this infection by malaria. So the need for the formulation of dosage form for this population using naturally occurring excipients to replace imported ones being currently used by our local manufacturing industries in-order to formulate novel, readily available, affordable and effective antimalarial medicine for children.

Methods: Using the local excipients and its hybrid, the formulated artemether-lumefantrine granules for oral suspension were administered to albino rats, blood samples were collected at predetermined time 0, 1.5, 3, 6, 9, 12, 15, 18, 21, and 24 h respectively and drug contents; artemether-lumefantrine were determined within the stipulated period.

Results: Some pharmacokinetic parameters determined were; maximum concentration, C_max, time to reach the maximum concentration, T_max, half-life, t_1/2,area under the curve, AUC, and mean residence time, MRT, which were for artemether-lumefantrine were 3.9, 3.4, μg/L; 3.2, 6.0 h; 12.5, 14 h; 75.8, 168.5 μg/L.h; 24, 24 h respectively, for the marketed artemether-lumefanthrine granules for oral suspension.4.1, 3.2 μg/L; 1.4, 3.0 h; 3.0, undefined h, 67.0, 65.7 μg/L. h; 18, 18 respectively for hybrid formulated artemether-lumefantrine granules for oral suspension and 3.1, 3.8 μg/L; 2.5, 12.5 h; 4.8, 15 h; 20.2, 281.6 μg/L .h; 18, 18 respectively for the extracted pectin formulated granules.

Conclusion: Optimized formulated artemether-lumefantrine granules were superior to the marketed product in terms of pharmacokinetic values being closer to those of earlier workers.