Pharmacokinetic and pharmacological effects of β-hydroxyphosphocarnitine in animal models.

The purpose of this research was to describe the pharmacokinetic parameters of β-hydroxyphosphocarnitine (β-HPC; CAS No. 1220955-20-3) after a single oral dose in rats and rabbits as well as to assess the impact of 14 weeks of β-HPC (100 mg/kg) treatment on the serum metabolites and liver enzymes, body weight, and hepatic steatosis of lean and obese Zucker fa/fa rats. In the case of the rat and rabbit study, the β-HPC area under the curve, biological half-life, and clearance were 2,174.4 versus 3,128 μg ∙ h/ml, 23.7 versus 8.87 h, and 13.9 versus 151.1 ml/h in the rats versus the rabbits, respectively. The values for the time of maximal concentration were 0.58 versus 1.53 h, for the maximal concentration, they were 62.4 versus 221.4 μg/ml, and for the absorption rate constant 0.02 versus 2.40 h(-1), respectively. In the case of the Zucker fa/fa rat study, β-HPC administered orally once a day reduced insulin, triglyceride, and cholesterol levels in the liver and serum; it also reduced weight gain and decreased liver steatosis in obese rats after 14 weeks. β-HPC could therefore potentially be used in the treatment of metabolic syndrome.