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QiShenYiQi pills, a Chinese patent medicine, increase bioavailability of atorvastatin by inhibiting Mrp2 expression in rats.
- Source :
-
Pharmaceutical biology [Pharm Biol] 2022 Dec; Vol. 60 (1), pp. 185-194. - Publication Year :
- 2022
-
Abstract
- Context: Atorvastatin (ATV) and QiShenYiQi pills (QSYQ), a Chinese patent medicine, are often co-prescribed to Chinese cardiovascular patients. The effects of QSYQ on the pharmacokinetics of ATV have not been studied.<br />Objective: We investigated the influence of QSYQ on the pharmacokinetics of ATV and its metabolites upon oral or intravenous administration of ATV to rats.<br />Materials and Methods: Sprague-Dawley rats ( n = 5/group) were pre-treated with oral QSYQ (675 mg/kg) or vehicle control for 7 days and then orally administrated ATV (10 mg/kg) or intravenously administrated ATV (2 mg/kg). Serum concentrations of ATV and metabolites were determined by ultra-high performance liquid chromatography tandem mass spectrometry. Expression of metabolic enzymes and transporters in jejunum and ileum were measured by quantitative real-time PCR and Western blot.<br />Results: QSYQ resulted in an increase of AUC <subscript>0-12 h</subscript> of ATV from 226.67 ± 42.11 to 408.70 ± 161.75 ng/mL/h and of C <subscript>max</subscript> of ATV from 101.46 ± 26.18 to 198.00 ± 51.69 ng/mL and in an increased of para- hydroxy atorvastatin from 9.07 ± 6.20 to 23.10 ± 8.70 ng/mL in rats administered ATV orally. No change was observed in rats treated intravenously. The expression of multidrug resistance-associated protein 2 mRNA and protein decreased in ileum, and the mRNA of P-glycoprotein decreased in jejunum, though no change in protein expression was found.<br />Discussion and Conclusions: QSYQ increased bioavailability of ATV administered orally through inhibiting the expression of Mrp2 in ileum. Clinicians should pay close attention to potential drug-drug interactions between ATV and QSYQ.
- Subjects :
- Animals
Area Under Curve
Biological Availability
Chromatography, High Pressure Liquid
Hydroxymethylglutaryl-CoA Reductase Inhibitors pharmacokinetics
Ileum metabolism
Male
Rats
Rats, Sprague-Dawley
Tandem Mass Spectrometry
ATP-Binding Cassette Transporters genetics
Atorvastatin pharmacokinetics
Drugs, Chinese Herbal pharmacology
Herb-Drug Interactions
Subjects
Details
- Language :
- English
- ISSN :
- 1744-5116
- Volume :
- 60
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Pharmaceutical biology
- Publication Type :
- Academic Journal
- Accession number :
- 35001796
- Full Text :
- https://doi.org/10.1080/13880209.2021.2021949