Absolute bioavailability of quinine formulations in Nigeria.
This study compared the absolute bioavailability of quinine sulphate as capsule and as tablet against the intravenous (i.v.) infusion of the drug in twelve male volunteers. Six of the volunteers received intravenous infusion over 4 h as well as the capsule formulation of the drug in a cross-over manner, while the other six received the tablet formulation. Blood samples were taken at predetermined time intervals and plasma analysed for quinine (QN) using reversed-phase HPLC method. QN was rapidly absorbed after the two oral formulations with average t(max) of 2.67 h for both capsule and tablet. The mean elimination half-life of QN from the i.v. and oral dosage forms varied between 10 and 13.5 hr and were not statistically different (P > 0.05). On the contrary, the maximum plasma concentration (C(max)) and area under the curve (AUC) from capsule were comparable to those from i.v. (P > 0.05), while these values were markedly higher than values from tablet formulation (P < 0.05). The therapeutic QN plasma levels were not achieved with the tablet formulation. The absolute bioavailability (F) were 73% (C.l., 53.3 - 92.4%) and 39 % (C.I., 21.7 - 56.6%) for the capsule and tablet respectively and the difference was significant (P < 0.05). The subtherapeutic levels obtained from the tablet form used in this study may cause treatment failure during malaria and caution should be taken when predictions are made from results obtained from different formulations of QN.
Babalola
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CP
Department of Pharmaceutical Chemistry, University of Ibadan, Ibadan, Nigeria. peacebab2001@yahoo.com
Bolaji
O O
OO
Ogunbona
F A
FA
Ezeomah
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E
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000962:Antimalarials / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002214:Capsules; D018592:Cross-Over Studies; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D011803:Quinine / Q000097:blood / Q000493:pharmacokinetics*; D013607:Tablets
D000962:Antimalarials; D002214:Capsules; D013607:Tablets; D011803:Quinine