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Biopharmaceutical Characterization and Bioavailability Study of a Tetrazole Analog of Clofibric Acid in Rat

Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, 62209 Cuernavaca, Morelos, Mexico
Departamento de Farmacia, Universidad de Guanajuato, 36050 Guanajuato, Guanajuato, Mexico
Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Molecules 2017, 22(2), 282;
Received: 19 December 2016 / Revised: 6 February 2017 / Accepted: 7 February 2017 / Published: 14 February 2017
(This article belongs to the Section Medicinal Chemistry)
PDF [2302 KB, uploaded 14 February 2017]


In 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
Keywords: diabetes; bioavailability; clofibric acid; 11β-HSD1; tetrazole; dyslipidemia diabetes; bioavailability; clofibric acid; 11β-HSD1; tetrazole; dyslipidemia

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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.

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