Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat
AbstractIn the current investigation, the physicochemical, biopharmaceutical and pharmacokinetic characterization of a new clofibric acid analog (Compound 1) was evaluated. Compound 1 showed affinity by lipophilic phase in 1 to 5 pH interval, indicating that this compound would be absorbed favorably in duodenum or jejunum. Also, Compound 1 possess two ionic species, first above of pH 4.43 and, the second one is present over pH 6.08. The apparent permeability in everted sac rat intestine model was 8.73 × 10−6 cm/s in duodenum and 1.62 × 10−5 cm/s in jejunum, suggesting that Compound 1 has low permeability. Elimination constant after an oral administration of 50 μg/kg in Wistar rat was 1.81 h−1, absorption constant was 3.05 h−1, Cmax was 3.57 μg/mL at 0.33 h, AUC0–α was 956.54 μ/mL·h and distribution volume was 419.4 mL. To IV administration at the same dose, ke was 1.21 h−1, Vd was 399.6 mL and AUC0–α was 747.81 μ/mL·h. No significant differences were observed between pharmacokinetic parameters at every administration route. Bioavailability evaluated was 10.4%. Compound 1 is metabolized to Compound 2 probably by enzymatic hydrolysis, and it showed a half-life of 9.24 h. With these properties, Compound 1 would be considered as a prodrug of Compound 2 with potential as an antidiabetic and anti dyslipidemic agent. View Full-Text
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Vara-Gama, N.; Valladares-Méndez, A.; Navarrete-Vazquez, G.; Estrada-Soto, S.; Orozco-Castellanos, L.M.; Rivera-Leyva, J.C. Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat. Molecules 2017, 22, 282.
Vara-Gama N, Valladares-Méndez A, Navarrete-Vazquez G, Estrada-Soto S, Orozco-Castellanos LM, Rivera-Leyva JC. Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat. Molecules. 2017; 22(2):282.Chicago/Turabian Style
Vara-Gama, Nancy; Valladares-Méndez, Adriana; Navarrete-Vazquez, Gabriel; Estrada-Soto, Samuel; Orozco-Castellanos, Luis M.; Rivera-Leyva, Julio C. 2017. "Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat." Molecules 22, no. 2: 282.