Alteration of oral salivary pharmacokinetics of paracetamol by an investigational anti-malarial phytomedicine, in healthy human volunteers.
Effect of an investigational anti-malarial phytomedicine (AM1) on the salivary pharmacokinetics of paracetamol (PCM), in healthy human volunteers was examined. The drug salivary level of paracetamol was determined using spectrophotometric method. Lower concentrations of PCM was observed in concomitant administration of 1000mg PCM tablets with 250mg AM1 capsule compared with administration of 1000mg paracetamol tablets alone (control). The area under the curve (AUC), time for maximum concentration (t(max)), maximum concentration (Cmax) were generated using the GRAPHPAD PRISM software version 2.0. The pharmacokinetic parameters were calculated from the semi-logarithmic plots of concentration-time data for PCM. The absorption kinetics parameters kab, lag-time, t1/2ab for both test (0.03min(-1), 9min, 18min.) and control (0.03min(-1), 9min, 22.8min.) were identical. There were statistically significant reductions in the bioavailability parameters AUC, Cmax, between control (1856microg/ml/min, 8.08microg/ml) and test (847.87microg/ml/min, 4.59microg/ml/) experiments. There were also insignificant but definite alterations in the elimination phase kinetic parameters kel, t1/2el, between control (0.1172min(-1), 69min.) and test (0.01027min(-1), 75min). The study shows that the botanical anti-malarial remedy (AM1) reduced the systemic availability of PCM when used concomitantly.
Obodozie
O
O
Department of Medicinal Chemistry and Quality Control, National Institute for Pharmaceutical Research and development, Abuja, Nigeria.
Mustapha
K
K
Inyang
U
U
D000082:Acetaminophen / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000284:Administration, Oral; D000328:Adult; D000962:Antimalarials / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D018592:Cross-Over Studies; D015507:Drugs, Investigational / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D016018:Least-Squares Analysis; D008297:Male; D008517:Phytotherapy / Q000379:methods; D012463:Saliva / Q000737:chemistry / Q000378:metabolism*
D000962:Antimalarials; D015507:Drugs, Investigational; D000082:Acetaminophen