Ref. In vitro model Talinolol Quantification Study Aim Results
[190] Caco-2 HPLC-FD Investigate the effect of apricot extract on talinolol permeability through caco-2 cell monolayers. Talinolol R(B-A/A-B) ≈ 15.5
After addition of apricot extract:
talinolol Papp (B-A) reduced and
talinolol Papp (A-B) increased
R(B-A/A-B) ≈ 2.5
[191] Caco-2 LSC Identification of P-gp inhibitors among 12 antipsychotic drugs All the psychoactive compounds showed affinity to P-gp.
IC50 values ranged from 0.8 µM (quetiapine) to 902 µM (olanzapine).
[192] Caco-2 UV Spectro-photometry Investigate the effect of two surfactants (TPGS and Poloxamer 188) on intestinal absorption of talinolol. TPGS:
reduced talinolol Papp (B-A) 2.5-fold; increased talinolol Papp (A-B) 6.7-fold;
Poloxamer 188:
reduced talinolol Papp (A-B) 2-fold.
[182] Caco-2 HPLC-FL Investigate the potential interaction between GFJ ingredients and talinolol. GFJ reduced talinolol Papp (B-A) from 22x10-7 to 4.5x10-7cm/s
GFJ did not influenced significantly the talinolol Papp (A-B)
IC50 (Narigin): 2409 µM;
IC50 (Naringenin): 236 µM
[185] Rat intestine in Ussing chamber HPLC-PDA Investigate the effect of morin on P-gp using talinolol as a P-gp probe Morin (100 µM):
increased talinolol Papp (A-B)
from 6.83x10-6 to 14.95x10-6 cm/s;
decreased talinolol Papp (B-A)
from 25.30x10-6 to 7.46x10-6 cm/s.
References In vivo animal model Talinolol Quantification Study Aim Effects on pharmacokinetics of talinolol
[193] Rats HPLC-UV Investigate the effect of two varieties of GFJ (white and ruby red) White GFJ: no effect on talinolol pharmacokinetics
Ruby red on talinolol pharmacokinetics:
reduced AUC0-∞ by 2.4-fold;
reduced Cmax by 1.8-fold
[185] Rats HPLC-UV Investigate the effect of rat treatment with morin 20 min before oral (10 mg/Kg) or IV administration (1 mg/Kg) of talinolol. Morin administration (5 mg/Kg):
increased oral AUC and oral Cmax at least 2-fold;
decreased oral CL/F by 45%;
increased bioavailability from 52% to 98%.
[194] Rats LC-MS/MS Investigate in rats the potential utility of nasal route to enhance drug delivery to CNS. Talinolol was detected in CSF and brain after nasal administration;
After infusion of cyclosporin A:
Talinolol concentrations in CSF and brain was not changed when administered intranasally and remained undetectable after IV administration.
Table 9: In vitro and in vivo assays using talinolol as a probe substrate and their characteristics. AUC, area under the curve; CL/F, total clearance; Cmax, maximum plasma concentration; CNS, central nervous system; FL, fluorescence; GBE, Ginkgo biloba extract; GFJ, grapefruit juice; IC50, concentration that inhibits 50%; IV, intravenous; LSC, Liquid scintillation counter; LC-MS/MS, liquid chromatography with tandem mass detection; Papp, apparent permeability; PDA, photodiode array; R(B-A/A-B), efflux ratio given by the ratio between apparent permeability in efflux (B-A) and absorption (A-B) directions; TPGS, D-α-tocopherylpolyethylene glycol 1000 succinate; UV, ultraviolet.
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