The Validation and Determination of Empagliflozin Concentration in the Presence of Grapefruit Juice Using HPLC for Pharmacokinetic Applications

Type 2 diabetes mellitus is a multifactorial disorder whose primary manifestation usually initiates with elevated blood sugar levels. Several antidiabetic agents are used to manage type 2 diabetes mellitus, of which empagliflozin is an oral sodium-glucose co-transporter (SGLT-2) inhibitor in the kid...

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Published in:	Molecules (Basel, Switzerland) Switzerland), 2024-03, Vol.29 (6), p.1236
Main Authors:	Abu Dayyih, Wael, Zakaraya, Zainab, Hailat, Mohammad, Al-Tawarah, Nafe M, Alkharabsheh, Sahem, Nadher, Haya Khalid, Hailat, Zeyad, Alarman, Samia M, Khaleel, Anas, Awad, Riad
Format:	Article
Language:	eng
Subjects:	(SGLT-2) inhibitor Accuracy Animals Antidiabetics Area Under Curve Benzhydryl Compounds Beverages Blood sugar Chromatography, High Pressure Liquid Citrus - chemistry Citrus paradisi Diabetes Diabetes Mellitus, Experimental Diabetes Mellitus, Type 2 empagliflozin Enzymes Ethylenediaminetetraacetic acid Fruit juices Glucose Glucosides High performance liquid chromatography Insulin Metabolism Mortality Pharmacodynamics Pharmacokinetics Plasma Quality control Rats Sitagliptin sodium-glucose co-transporter inhibitor Type 2 diabetes type 2 diabetes mellitus
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Summary:	Type 2 diabetes mellitus is a multifactorial disorder whose primary manifestation usually initiates with elevated blood sugar levels. Several antidiabetic agents are used to manage type 2 diabetes mellitus, of which empagliflozin is an oral sodium-glucose co-transporter (SGLT-2) inhibitor in the kidney. This research aims to develop and validate a simple analytical method for determining empagliflozin levels in biological fluid and to further evaluate grapefruit juice's impact on empagliflozin pharmacokinetics in rats. High-Performance Liquid Chromatography (HPLC) was used to establish a simple, rapid, and accurate method for determining empagliflozin levels in rat plasma, in the presence of grapefruit juice. Four groups of rats ( = 10 rats in each) were used in the preclinical study. Group A (healthy rats) received empagliflozin alone; Group B (healthy rats) received empagliflozin with grapefruit; Group C (diabetic rats) received empagliflozin with grapefruit; and Group D (healthy, negative control) received no medication. The rats ( = 10) were given grapefruit juice instead of water for seven days before receiving the empagliflozin dose (0.16 mg/kg). Some pharmacokinetic parameters for each group were determined. The maximum plasma concentration (C ) and area under the curve (AUC) of empagliflozin in Group A without grapefruit intake were 730 ng/mL and 9264.6 ng × h/mL, respectively, with T (2 h). In Group B, C was 1907 ng/mL and AUC was 10,290.75 ng × h/mL in the presence of grapefruit, with T (1 h); whereas, in Group C, the C was 2936 ng/mL and AUC was 18657 ng × h/mL, with T (2 h). In conclusion, our results showed that the co-administration of grapefruit with empagliflozin should be cautiously monitored and avoided, in which grapefruit elevates the plasma level of empagliflozin. This may be attributed to the inhibition of the uridine enzyme in the grapefruit by hesperidin, naringin, and flavonoid.
ISSN:	1420-3049 1420-3049