Abstract
Article history: The single oral dose pharmacokinetics of chloroquine (5mg/kg body weight) and metronidazole (7.5mg/kg body weight) were studied in rats' serum. Chloroquine and metronidazole concentrations were measured using high - performance liquid chromatography (HPLC) method developed earlier in our laboratory. The data were fitted into a WinNonlin standard non-compartmental programme. The Maximum serum concentration Cmax (µg/ml) of chloroquine was 5.70 ± 1.41 while that of metronidazole was 3.13 0.30, Time to peak concentration tmax was 1.00 0.00 (h) and that of metronidazole was 0.83 ± 0.27, Volume of distribution Vd (L) 1.33 ± 0.26 for metronidazole 2.39 0.28; Elimination half-life t1/2 (h) 10.05 ± 3.01 for metronidazole 4.05 0.46. The values were comparable with the works of other authors. Compounds that show very high activity in -vitro may not have in vivo activity, or may be highly toxic using in- vivo models due to undesirable pharmacokinetic properties, and toxicity may result from formation of reactive metabolites. This study assures the quality of the brands of the drugs and encouraged the use of animal model in determining pharmacokinetic properties especially in drug design.
Highlights
Pharmacokinetics denotes the movement of drugs through the body over time, and addresses the absorption from the site of administration, distribution throughout the body, metabolism of the drug, and its elimination from the body
This study assures the quality of the brands of the drugs and encouraged the use of animal model in determining pharmacokinetic properties especially in drug design
According to the World Health Organization (WHO), malaria is endemic in 91 countries, predominantly in Africa, Asia, and Latin America, with about 40% of the world’s population at risk (WHO, 1996)
Summary
Pharmacokinetics denotes the movement of drugs through the body over time, and addresses the absorption from the site of administration, distribution throughout the body, metabolism of the drug, and its elimination from the body. A dosage regimen is the key to a drug producing the desired therapeutic effects. A regimen can be described in terms of the dose of the drug to be used, the frequency with which it should be established, the rate of administration and the formulation to be used. Chloroquine (CQ) and other 4-aminoquinolines, like amodiaquine and its metabolite desethylamodiaquine, attack the malaria parasite in its intra erythrocytic stages when it digests hemoglobin in its lysosome, releasing haematin, potentially toxic to the parasite. Metronidazole (MET) is a 5nitronimidazole derivative with activity against anaerobic protozoa and anaerobic bacteria; it has a radio sensitizing effects on hypoxic tumor cells. Metronidazole administered orally will produce an effective concentration of the drug in the blood and urine. This work reports the pharmacokinetic profiles of chloroquine, its metabolite and metronidazole in rat. Mustapha et al / Journal of Applied Pharmaceutical Science 5 (08); 2015: 090-094
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