Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A.
作者： Chung-Ping Yu , Hui-Ju Lin , Shiuan-Pey Lin , Chi-Sheng Shia , Pei-Hua Chang
DOI: 10.3109/00498254.2015.1117159
关键词: Rheum palmatum 、 Monoclonal 、 Dose 、 P-glycoprotein 、 Chemistry 、 Bioavailability 、 In vivo 、 Ingestion 、 Pharmacology 、 Cmax
摘要: 1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine. 2. Cyclosporine (CSP) immunosuppressant with narrow therapeutic window. The oral bioavailability CSP was associated P-glycoprotein (P-gp) and CYP 3A4. used as a probe substrate to investigate the vivo modulation effects RP on P-gp 3A. 3. Rats were orally administered 2.5 mg/kg without 0.25 1.0 g/kg RP. blood concentration determined by specific monoclonal fluorescence polarization immunoassay. 4. Both dosages significantly decreased Cmax AUC0-t rats. Mechanism studies indicated that activated functions 5. RP ingestion reduced systemic exposure through activating
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