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Evaluation of Quercetin's Bioenhancing Effect on Oral Pharmacokinetics of Rosuvastatin in Wistar Rats Using RP-HPLC
Rachana S Bhimanwar1, Lata P Kothapalli1, Akshay Khawshi1
1Department of Pharmaceutical Chemistry, Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, India.
Cardiovascular & Hematological Agents in Medicinal Chemistry
|October 21, 2024
Summary
Quercetin (QUE) significantly enhances the bioavailability of rosuvastatin (RST) in rats by increasing plasma levels. This study validates a method to measure RST and confirms QUE
Area of Science:
- Pharmacology
- Analytical Chemistry
- Drug Metabolism
Background:
- Rosuvastatin (RST) exhibits low oral bioavailability (20%) and is primarily transported into hepatocytes via OATP-1B1.
- Quercetin (QUE), a known bioenhancer, inhibits OATP1B1, suggesting potential to improve RST pharmacokinetics.
Purpose of the Study:
- Develop and validate a RP-HPLC method for quantifying RST.
- Investigate the impact of QUE co-administration on RST bioavailability and pharmacokinetics in rats.
Main Methods:
- A Kromasil 100, C18 column with an acetonitrile:acetic acid buffer mobile phase was used for RP-HPLC analysis.
- Rosuvastatin (RST) and Quercetin (QUE) pharmacokinetics were studied in rats using non-compartmental analysis.
- Blood concentrations of RST were determined at 242 nm using validated RP-HPLC method.
Main Results:
- Co-administration of QUE significantly increased RST's maximum blood concentration (Cmax) from 67.3 ng/ml to 122.2 ng/ml (p < 0.001).
- Area under the curve (AUC) values (AUC0-t and AUC0-inf) for RST were significantly elevated (p < 0.0001 and p = 0.0005, respectively) when co-administered with QUE.
- The time to reach maximum concentration (tmax) for RST was observed at 120 minutes post-co-administration with QUE.
Conclusions:
- Quercetin (QUE) effectively enhances rosuvastatin (RST) plasma levels in rats.
- The observed herb-drug interaction highlights QUE's potential as a bioavailability enhancer for RST.
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