Effects of curcumin on the pharmacokinetics of talinolol in human with ABCB1 polymorphism

• Published in: Xenobiotica Vol. 42; no. 12; pp. 1248 - 1254
• Main Authors: He, X., Mo, L., Li, Z.-Y., Tan, Z.-R., Chen, Y., Ouyang, D.-S.
• Format: Journal Article
• Language: English
• Published: England Informa Healthcare 01.12.2012; Taylor & Francis
• Subjects: Administration, Oral; Adult; ATP Binding Cassette Transporter, Sub-Family B; ATP-Binding Cassette, Sub-Family B, Member 1 - genetics; Curcumin; Curcumin - administration & dosage; Curcumin - pharmacology; Genotype; Humans; Male; multidrug resistance 1 (MDR1/ABCB1); P-glycoprotein; pharmacokinetics; polymorphism; Polymorphism, Single Nucleotide - genetics; Propanolamines - administration & dosage; Propanolamines - blood; Propanolamines - pharmacokinetics; talinolol; Time Factors; Young Adult
• ISSN: 0049-8254; 1366-5928
• DOI: 10.3109/00498254.2012.697590

This study was to investigate the effect of concomitantly administered curcumin on the pharmacokinetics of talinolol and association with ABCB1 C3435T genetic polymorphism. A two-phase, randomized, single-blind, crossover study was carried out in 18 healthy male volunteers with different genotypes of ABCB1, including C3435C (CC, n = 6), C3435T (CT, n = 6) and T3435T (TT, n = 6). The pharmacokinetics of talinolol were measured after co-administration of placebo or 1000 mg curcumin capsules once daily for 14 days. The AUC0-48 h and AUC0-∞ of talinolol were increased by 67.0% (95% CI: 1.09~2.25; p = 0.002) and 80.8% (95% CI: 0.92~2.69; p = 0.005) respectively with curcumin co-administration. The Cmax of talinolol was significantly higher after curcumin administration as compared with placebo (p = 0.029).The CL/F of talinolol was decreased by 25.9% (p = 0.005) during the curcumin-treated phase. No significant change in tmax and t1/2 of talinolol were observed between the placebo- and curcumin-treated phases. AUC0-48, AUC0-∞, Cmax of talinolol were extensively increased and CLoral/F decreased in TT subjects. Co-administration of curcumin significantly increased the plasma concentration of talinolol in healthy volunteers. The effect of curcumin on talinolol was associated with ABCB1 genotypes (C3435T).