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Molecules 2017, 22(2), 282; doi:10.3390/molecules22020282

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

1
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, 62209 Cuernavaca, Morelos, Mexico
2
Departamento de Farmacia, Universidad de Guanajuato, 36050 Guanajuato, Guanajuato, Mexico
*
Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 19 December 2016 / Revised: 6 February 2017 / Accepted: 7 February 2017 / Published: 14 February 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2302 KB, uploaded 14 February 2017]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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