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- Title
A Single Dose of Baicalin Has No Clinically Significant Effect on the Pharmacokinetics of Cyclosporine A in Healthy Chinese Volunteers.
- Authors
Liu, Ruijuan; Li, Xia; Wei, Jingyao; Liu, Shuaibing; Chang, Yuanyuan; Zhang, Jiali; Zhang, Ji; Zhang, Xiaojian; Fuhr, Uwe; Taubert, Max; Tian, Xin
- Abstract
Despite its narrow therapeutic window and large interindividual variability, cyclosporine A (CsA) is the first-line therapy following organ transplantation. Metabolized mainly by CYP3A and being a substrate of P-glycoprotein (P-gp), CsA is susceptible to drug–drug interactions. Baicalin (BG) is a drug used for adjuvant therapy of hepatitis in traditional Chinese medicine. Since its aglycone baicalein (B) inhibits CYP3A and P-gP, co-administration might affect CsA pharmacokinetics. This study investigated the effect of BG on CsA pharmacokinetics. In a two-period study, 16 healthy volunteers received a single 200 mg oral CsA dose alone (reference period) or in combination with 500 mg BG (test period). Pharmacokinetic evaluation of CsA was carried out using non-compartmental analysis (NCA) and population pharmacokinetics (popPK). Treatments were compared using the standard bioequivalence method. Based on NCA, 90% CIs of AUC and C max test-to-reference ratios were within bioequivalence boundaries. In the popPK analysis, a two-compartment model (clearance/F 62.8 L/h, central and peripheral volume of distribution/F 254 L and 388 L) with transit compartments for absorption appropriately described CsA concentrations. No clinically relevant effect of 500 mg BG co-administration on CsA pharmacokinetics was identified and both treatments were well tolerated.
- Subjects
PHARMACOKINETICS; CYCLOSPORINE; CHINESE medicine; VOLUNTEERS; TRANSPLANTATION of organs, tissues, etc.
- Publication
Frontiers in Pharmacology, 2019, pN.PAG
- ISSN
1663-9812
- Publication type
Article
- DOI
10.3389/fphar.2019.00518