Universität zu Köln

Liu, Ruijuan, Li, Xia, Wei, Jingyao, Liu, Shuaibing, Chang, Yuanyuan, Zhang, Jiali, Zhang, Ji, Zhang, Xiaojian, Fuhr, Uwe, Taubert, Max ORCID: 0000-0001-8925-7782 and Tian, Xin (2019). A Single Dose of Baicalin Has No Clinically Significant Effect on the Pharmacokinetics of Cyclosporine A in Healthy Chinese Volunteers. Front. Pharmacol., 10. LAUSANNE: FRONTIERS MEDIA SA. ISSN 1663-9812

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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.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Liu, Ruijuan UNSPECIFIED UNSPECIFIED UNSPECIFIED Li, Xia UNSPECIFIED UNSPECIFIED UNSPECIFIED Wei, Jingyao UNSPECIFIED UNSPECIFIED UNSPECIFIED Liu, Shuaibing UNSPECIFIED UNSPECIFIED UNSPECIFIED Chang, Yuanyuan UNSPECIFIED UNSPECIFIED UNSPECIFIED Zhang, Jiali UNSPECIFIED UNSPECIFIED UNSPECIFIED Zhang, Ji UNSPECIFIED UNSPECIFIED UNSPECIFIED Zhang, Xiaojian UNSPECIFIED UNSPECIFIED UNSPECIFIED Fuhr, Uwe UNSPECIFIED UNSPECIFIED UNSPECIFIED Taubert, Max UNSPECIFIED orcid.org/0000-0001-8925-7782 UNSPECIFIED Tian, Xin UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-148235
DOI:	10.3389/fphar.2019.00518
Journal or Publication Title:	Front. Pharmacol.
Volume:	10
Date:	2019
Publisher:	FRONTIERS MEDIA SA
Place of Publication:	LAUSANNE
ISSN:	1663-9812
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language IN-VITRO; CHEWABLE TABLETS; P-GLYCOPROTEIN; PERFORMANCE; METABOLISM; ABSORPTION; TRANSPLANTATION; KETOCONAZOLE; DISSOLUTION; AGLYCONE Multiple languages Pharmacology & Pharmacy Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/14823