Pharmacokinetics of intravenous and oral bolus doses of L-carnitine in healthy subjects

Summary

The pharmacokinetics of single intravenous and oral doses of L-carnitine 2 g and 6 g has been investigated in 6 healthy subjects on a low carnitine diet.

Carnitine was more rapidly eliminated from plasma after the higher dose. Comparing the 2-g and 6-g doses, the t_1/2β of the elimination phase (β) was 6.5 h vs 3.9 h, the elimination constant was 0.40 vs 0.50 h⁻¹ and the plasma carnitine clearance was 5.4 vs 6.11 × h⁻¹ (p<0.025), thus showing dose-related elimination.

Saturable kinetics was not found in the range of doses given. The apparent volumes of distribution after the two doses were not significantly different and they were of the same order as the total body water. Urinary recoveries after the 2-g and 6-g doses were 70% and 82% during the first 24 h, respectively.

Following the two oral dosing, there was no significant difference in AUCs of plasma carnitine. Urinary recoveries were 8% and 4% for the 2-g and 6-g doses during the first 24 h. The oral bioavailability of the 2-g dose was 16% and of the 6 h dose 5%. The results suggest that the mucosal absorption of carnitine is already saturated at the 2-g dose.