Effect of Orange Juice on Bioavailability of Levofloxacin
Rebeca Sultana, Ashik Ullah Maruf Mohammad Akbor, Mohammad Abul Kalam Azad, , A. H. M. Mahbub Latif and Abul Hasnat
Objective: This work was designed to observe the effect of orange juice on the bioavailability of levofloxacin in healthy Bangladeshi volunteers.
Methods: A randomized 2-way crossover design was used with a washout period of 2 weeks. The volunteers ingested either 200 mL of orange juice or water 3 times a day for the first 3 days and 2 times a day on the fourth day. On the morning of Day 3, each subject was given a 250-mg levofloxacin tablet under fasting condition with 200 mL of orange juice or water. Thirteen blood samples were collected from each volunteer over a 24-hour period. Serum levofloxacin concentrations were determined by high performance liquid chromatography using UV detection, and pharmacokinetic parameters were determined by the non-compartmental method.
Results: The mean value of the peak plasma concentration (Cmax) of levofloxacin decreased significantly (26.36%,P value < 0.001; 90% CI, 125.18%-145%) in the volunteers who had taken the drug with orange juice (Cmax, 2.57 ± 0.46 μg/mL) than those who had taken the drug with water (Cmax, 3.49 ± 0.75 μg/mL).The area under the serum concentration-time curve extrapolated from t = 0 to infinity (AUC0-) value was also reduced by 17.33%; this change was not within the acceptable range of bioequivalence (90% CI, 111.38%-127.90%). Similarly, the value of area under the serum concentration-time curve extrapolated from t = 0 to t = 24 hours (AUC0-24) was decreased by 14.98%; this change was marginally within the bioequivalence acceptable range (90% CI, 113.31%-122.10%). The values of AUMC0-, serum elimination half-life, time to reach peak serum concentration, elimination rate constant, and mean resident time did not change significantly.
Conclusion: As the values of Cmax and AUC0-were not within the bioequivalence acceptable range, the serum therapeutic concentration of levofloxacin will be severely affected in the presence of orange juice, ultimately affecting its bioavailability and therapeutic efficacy. So, levofloxacin should not be taken with orange juice under any circumstances.
Source: Journal of Applied Research , 8(1), 34-42.