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Pharmacokinetic and pharmacodynamic properties of β‐hydroxyphospho‐carnitine (1064.1)
Author(s) -
MendozaRivera Brissa,
ReyesEsparza Jorge,
De La Cruz Cordero Ricardo,
RodriguezFragoso Lourdes
Publication year - 2014
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.28.1_supplement.1064.1
Subject(s) - pharmacokinetics , cmax , pharmacodynamics , steatosis , medicine , pharmacology , cholesterol , endocrinology , oral administration , chemistry
The aim of this investigation was to study the pharmacokinetics properties in two species and the pharmacodynamics effects of β‐HPC in obese Zucker fa/fa rats administered during a period of time. Lean and obese Zucker fa/fa rats were treated for 14 weeks with β‐HPC (100 mg/kg) to assess its impact on glucose, triglycerides and cholesterol in liver and blood samples, and on hepatic steatosis. Besides of that, we described the first study about the pharmacokinetic properties of β‐HPC after single oral administration in rats and rabbits. β‐HPC reduced the levels of glucose, triglycerides and cholesterol in the liver, the levels of triglycerides and cholesterol in serum, and improved the architecture and reduced steatosis in the liver in obese rats. After a single oral dose of β‐HPC (100 mg/kg) the elimination half‐life (t1/2), clearance and the area under the concentration vs time (AUC) in rats and rabbits were 23.7 vs 8.87 h, 13.9 vs 151.1 mL/h, and 2174.4 vs 3128 µg.h/mL, respectively. The values of Tmax, Cmax, and Ka in rats and rabbits were 0.58 vs 1.5 h, 62.4 vs 221.4 µg/mL, and 0.02 vs 2.40 h‐1, respectively. This study demonstrated that, although there exist differences between species, the β‐HPC administered orally is rapidly absorbed, highly distributed and efficiently cleared. According with the pharmacodynamics properties β‐HPC could be useful for treating some metabolic alterations present in metabolic syndrome. Grant Funding Source : CONACYT