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Evaluation the Impact of Grapefruit Juice on Sitagliptin Pharmacokinetics in Healthy Rats
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| Author:
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MAHER FARES, ISRAA AL-ANI, MOHAMMAD HAILAT, ANAS KHALEEL, PHIL COLLIER, ASMAA AL-ANI, WAEL ABU DAYYIH
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| Abstract:
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Background and Aim: Grapefruit is known in health care to interact with several medications. Interactions on the kinetic level are attributed to any change in pharmacokinetic parameters of the basic kinetic processes, Absorption, and Disposition when taking the drug concurrently with grapefruit juice. This study aims to develop an analytical method to measure Sitagliptin (an antidiabetic agent) in rat plasma alone and, in the presence of grapefruit juice, and evaluate grapefruit juice's impact on the fundamental pharmacokinetic parameters of Sitagliptin.
Methods:A simpleHPLC method was developed using water-acetonitrile (pH 6.8) mobile phase and U.V. detector at 267 nm. According to the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH), linearity, accuracy, and precision were evaluated.Sitagliptin solution (5.75 mg/Kg) was assigned to two groups of rats, a control group and a fed grapefruit juice group. The plasma-level vs. time profile was constructed for both groups for up to 24 hours. The pharmacokineticparameters were calculated for Sitagliptin with and without grapefruit juice using compartmental and non-compartmental analysis and statistically compared using t-test.
Results: The analysis methodsuccessfully measuredSitagliptin in rat plasma showing high linearity and accepted accuracy and precision levelsaccording to the ICH guidelines.Results also showed an increase insitagliptinthat reached systemic circulation when given with grapefruit juice. There was no observed change in elimination parameters or the drug's total residence time in the body, suggesting an interaction on absorption level.
Conclusion: Drug-food interaction is observed between sitagliptin and grapefruit, and hence, grapefruit juice consumption should be avoided with the concurrent use of sitagliptin.
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| Keyword:
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Sitagliptin, HPLC, methodvalidation, grapefruit, pharmacokinetic interactions.
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.02.271
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