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

Abstract

1. This study was to investigate the effect of concomitantly administered curcumin on the pharmacokinetics of talinolol and association with ABCB1 C3435T genetic polymorphism.

2. 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.

3. The AUC_{0–48 h} and AUC_0–∞ 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 C_max 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 t_max and t_1/2 of talinolol were observed between the placebo- and curcumin-treated phases. AUC_0–48, AUC_0–∞, C_max of talinolol were extensively increased and CL_oral/F decreased in TT subjects.

4. 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).

Keywords::

• Curcumin
• talinolol
• pharmacokinetics
• P-glycoprotein
• multidrug resistance 1 (MDR1/ABCB1)
• polymorphism

Acknowledgement

This study was supported by National Sci-Tech Support Plan of China (Grant No. SQ2010BAJY1411-08), National Mega Project of Science Research of China (Grant No. 2012ZX09501), grant of Hunan Provincial Natural Science Foundation of China (Key Project, 10JJ2008) and 863 Project(No. 2012AA02A518).

Declaration of interest

The authors declared no conflict of interest.