title: Pharmacokinetic and pharmacological effects of β-hydroxyphosphocarnitine in animal models.
abstract: 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.
authors.affiliation: Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Mexico.
authors.forename: Jorge
authors.initials: J
authors.lastname: Reyes-Esparza
authors.forename: Brissa
authors.initials: B
authors.lastname: Mendoza-Rivera
authors.forename: Ricardo
authors.initials: R
authors.lastname: De la Cruz-Cordero
authors.forename: Miguel Ángel
authors.initials: MÁ
authors.lastname: Duarte-Vázquez
authors.forename: Jorge Luis
authors.initials: JL
authors.lastname: Rosado
authors.forename: Lourdes
authors.initials: L
authors.lastname: Rodríguez-Fragoso
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D002331:Carnitine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D002784:Cholesterol / Q000378:metabolism; D005234:Fatty Liver / Q000209:etiology / Q000473:pathology / Q000517:prevention & control*; D006207:Half-Life; D007328:Insulin / Q000378:metabolism; D008297:Male; D024821:Metabolic Syndrome / Q000188:drug therapy*; D009765:Obesity / Q000150:complications / Q000188:drug therapy*; D010755:Organophosphates / Q000493:pharmacokinetics / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D011924:Rats, Zucker; D013045:Species Specificity; D014280:Triglycerides / Q000378:metabolism; D015430:Weight Gain / Q000187:drug effects
chemical_list: D007328:Insulin; D010755:Organophosphates; D014280:Triglycerides; C000598410:beta-hydroxyphosphocarnitine; D002784:Cholesterol; D002331:Carnitine