Interactor compound Clinical Study AUC ratio Cmax ratio CL ratio Talinolol Quantification Ref. R-Verapamil Healthy volunteers were orally co-administered with talinolol (50 mg) and R-verapamil (120 mg) AUC0-24: 0.76   0.66 CLR ≈ 1.0 HPLC [195] Erythromycin Healthy male volunteer co-administered orally with talinolol (50 mg) and erythromycin (2 g) AUC0-∞  increased 52% Cmax increased 26% CL/F ≈1.0 HPLC [196] Carbamazepine Healthy volunteers pre-treated with oral CBZ (600 mg id): for 18 days and repeated oral administration of talinolol 0.86 - CL/F: 1.15 - [197] for 18 days after infusion of talinolol (30 mg /30 min) 1.03 - CL/F: 0.99 TPGS Intra-duodenal perfusion on healthy male volunteers AUC0-∞ : 1.39 AUC0-6: 2.11 2.00 - LC-MS/MS [192] Poloxamer 188 AUC0-∞ : 0.91 AUC0-6: 0.99 1.13 - GFJ Healthy volunteers pre-treated with GFJ (900 mL; id) for 6 days and orally administered with talinolol (50 mg) AUC decreased 56% Cmax decreased 57% - HPLC [195] Curcumin Healthy volunteers pre-treated with curcumin (300 mg) orally administered for 6 days. AUC0-∞ : 0.67 0.72 CL/F: 1.54 HPLC-ESI-MS/MS [198] SJW Healthy volunteers co-administered with single oral dose of SJW (900 mg) and oral talinolol (50 mg) AUC0-24 : 0.68 AUC0-∞: 0.69 0.79 CL/F: 1.93 CLR: 0.83 HPLC [189] and IV talinolol (30 mg / 30 min infusion) AUC0-24 : 0.98 AUC0-∞: 0.93 - CLR: 0.87 CLNR: 1.35 GBE Healthy male volunteers co-administered with single oral dose of GBE (120 mg) and talinolol (100 mg) AUC0-24 : 0.90 AUC0-∞: 0.91 0.88 - HPLC-UV [199] Healthy male volunteers pre-treated with GBE (120 mg; tid) orally administered for 14 days AUC0-24 : 1.26 AUC0-∞: 1.22 1.36 - Silymarin Healthy volunteers pre-treated with silymarin (140 mg; tid) for 14 days AUC0-36 increased 36.2% - Decreased 23.1% HPLC-MS [200] Duloxetine Healthy volunteers orally administered with duloxetine (30 mg) and talinolol (50 mg) AUC0-60 : 0.87 0.87 - HPLC-ESI-MS/MS [102]

Table 10: In vivo clinical assays using talinolol as P-gp probe. AUC, area under the curve; CBZ, carbamazepine; CL/F, total clearance; CLR, renal clearance; Cmax, maximum plasma concentration; ESI, electrospray ionization; GBE, Ginkgo biloba extract; GFJ, grapefruit juice; HPLC, high performance liquid chromatography; id, once daily; LC-MS/MS, liquid chromatography with tandem mass detection; MS, mass spectrometry detection; SJW, St John’s wort; tid, three times a day; TPGS, D-α- tocopherylpolyethylene glycol 1000 succinate; UV, ultraviolet.

Goto home»