The single oral dose pharmacokinetics of chloroquine was studied alone and after coadministration with phytomedicines NIPRID/92/001/1-1 (AM-1), Niprisan®, and Nifadin® in rats. Plasma chloroquine 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 co-administration of the herbal medicines with chloroquine produced decrease in the serum concentration of chloroquine at each sampling time. The highest decrease of 85% occurring at the time of peak concentration (lh) was recorded with NifadinR, followed by 75% with NiprisanR, the least was 50% with AM-1. Significant reduction was also observed in some other parameters, such as area under the serum concentration- time curve ((AUC 0–24) and maximum serum concentration (C max ) while the apparent volume of distribution (V d ) and elimination half-life (t 1/2β) increased significantly (P< 0.05). It was concluded that the gastric presence of the herbal medicines significantly impaired the absorption of chloroquine in rats.
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Kean B.H. (1979): Chloroquine-resistant falciparum malaria from Africa. JAMA, 241, 95.
Nicholas W. (1999): Antimalarial Drug resistance and combination chemotherapy. Trans. R. Soc. Lond., Pp. 739-749.
Trape J.F. (2001): The public health impact of chloroquine resistance in Africa. Am. J. Hygen. Trop. Med., 64: 12–17.
Hall A.P. (1973): Quinine and chloroquine antagonism in falciparium malarial. Tran. R. Soc. Trop. Med. Hyg., 67: 425–428.
Lown K.S., Bailey D.G., Fontana R.J., Janardan S.K., Adair C.H., Fortlage L.A. (1997): Grapefruit juice felodipine oral availability in human by decreasing intestinal CYP3A4 protein expression. J. Clin. Invest., 99: 2545–2553.
Bailey D.G., Malcolm J., Arnold O. and Spence J.D. (1998): Grapefruit juice-drug interaction [review]. Br. J. Clin. Pharmacol., 46: 101–110.
McNeece J (2002): Grapefruit juice interactions. Aust. Prescr., 25: 37–38.
Piscitelli S.C, Brstein A.H, Weldon N., Gallicano K.D. and Falloon J. (2002): The effect of garlic supplements on the pharmacokinetics of saquinavir. Clin. Infect. Dis., 34: 234–338.
Koury R.T.G.A. (2003): Issues warning on Hericum. J. Aust. Trad. Med. Soc., 6: 47- 49.
Lhote O., Decoodt A., Moulin A and Dufour A. (1991): In vivo approach To determine the route of optimal drug absorption in pharmacokinetics. Eur. J. Drug Metetabol. Pharmacokinet., Proceedings of the 4lh European Congress of Bio-harmaceutics and Pharmacokinetics, pp 43-46.
Ademowo O.G., Sodeinde O., Walker M.D. (2000): The disposition of chloroquine and its main metabolite desethyl-chloroquine in volunteers with and without chloroquine- induced pruritus: Evidence for decreased chloroquine metabolism in volunteers with pruritus. Clin. Pharmac. Therap., 67: 237–243.
Nwafor S.V., Peter A.A., Charles O.O., Adaoma C.O. and Chukwuemeka S.N. (2003): Interaction between chloroquine sulphate and aqueous extract of Azadirachta indica A. Juss (Meliaceae) in rabbits. Acta Pharm., 53: 305–311.
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Mustapha, K.B., Bakare-Odunola, M.T., Garba, M. et al. Effect of phytomedicines, AM-1, niprisan® and nifadin on the pharmacokinetics of chloroquine in rats. Eur. J. Drug Metabol. Pharmacokinet. 34, 151–155 (2009). https://doi.org/10.1007/BF03191166