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.

Highlights

  • The results indicated a significant reduction in glucose levels in the plasma, up to 77%

  • Given the potential of Compound 1 for the treatment of DMT2 and dyslipidemia, this study proposes the evaluation of its bioavailability in a rat model, as well as its biopharmaceutical characterization

  • Given the potential of Compound 1 for the treatment of DMT2 and dyslipidemia, this study proposes the evaluation of its bioavailability in a ratofmodel, well as its biopharmaceutical

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Summary

Introduction

There were 6.4 million adults over the age of 20 diagnosed with diabetes in 2012 (National Health and Nutrition Survey) [2]. Due to this growing epidemiological trend, Diabetes Mellitus (DM) is considered a very significant public health problem in this country and around the world, and is one of the primary causes of death in the Mexican population. The complications associated with DMT2 include damage to the capillaries of the kidney,. (causing glomerulonephritis and renal failure in its advanced stages), damage to the capillaries of the retina (causing blindness), peripheral neuropathy, myocardial infarction, cerebrovascular complications, and arteriosclerosis [3,4,5,6].

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