Evidence of reduced oral bioavailability of paracetamol in rats following multiple ingestion of grapefruit juice

The aim of the current investigation was to assess the ability GFJ to modulate the pharmacokinetic profile of paracetamol following single or repeated administrations of GFJ in Sprague–Dawley rats. Diclofenac and carbamazepine were both used as positive controls. Rats received single GFJ or single d...

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Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 2016-04, Vol.41 (2), p.187-195
Main Authors: Qinna, Nidal A., Ismail, Obbei A., Alhussainy, Tawfiq M., Idkaidek, Nasir M., Arafat, Tawfiq A.
Format: Article
Language:English
Subjects:
Acetaminophen - pharmacokinetics
Animals
Area Under Curve
Beverages - adverse effects
Biological Availability
Biomedical and Life Sciences
Biomedicine
Carbamazepine - pharmacokinetics
Citrus paradisi - adverse effects
Diclofenac - pharmacokinetics
Eating
Food-Drug Interactions
Human Physiology
Male
Medical Biochemistry
Original Paper
Pharmaceutical Sciences/Technology
Pharmacology/Toxicology
Pharmacy
Rats
Rats, Sprague-Dawley
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Summary:The aim of the current investigation was to assess the ability GFJ to modulate the pharmacokinetic profile of paracetamol following single or repeated administrations of GFJ in Sprague–Dawley rats. Diclofenac and carbamazepine were both used as positive controls. Rats received single GFJ or single distilled water doses or pretreated with three doses of GFJ prior to test drug administration. Blood samples were collected, processed and analyzed using validated HPLC methods, and pharmacokinetic data were constructed for each group. Increase in the bioavailability of both diclofenac and carbamazepine following multiple GFJ ingestion was revealed. Conversely, the bioavailability of paracetamol was significantly reduced following multiple GFJ administration. The percentage of reduction in the C max and AUC of paracetamol were calculated as 31 and 51 %, respectively, compared to none-GFJ-treated control ( P  
ISSN:0378-7966
2107-0180
DOI:10.1007/s13318-014-0251-4