OUYANG Danwei, XIAO Feng, QIN Yan, SHAO Yan, KONG Deyun*
2014, 45(5): 460-465.
An LC-MS method was established for the determination of the triterpenoid saponins in Centella total glucosides (CTG) in rat plasma and the pharmacokinetic properties of CTG in rats were studied after oral and intravenous administrations. A Kromasil C18 column was used with the mobile phase of 0.1% formic acid solution (containing 10 mmol/L ammonium formate)∶methanol by gradient elution. A mass spectrometry was applied with ESI ion source in the positive ion multiple reaction monitoring (MRM) mode. All pharmacokinetic parameters were processed by noncompartmental analysis with DAS 2.0 software. After CTG was intravenously administered at 5 mg/kg dose, the main pharmacokinetic parameters of asiaticoside, madecassoside+asiaticoside B, asiatic acid and madecassic acid were as follows: t1/2 (1.65±0.80), (3.02±0.55), (3.75±1.93) and (0.31±0.08)h; cmax (2 622±555), (23 800±2 138), (483±128) and (605±124)ng/ml; AUC0→t(572±125), (7 703±639), (185±32) and (100±22)ng·h·ml-1; AUC0→∞(581±127), (7 722±639), (206±37) and (101±22)ng·h·ml-1. While after CTG was orally administered at 150 mg/kg dose, the main pharmacokinetic parameters of madecassoside+asiaticoside B and asiatic acid were as follows: t1/2 (3.41±1.27) and (5.25±2.50)h, cmax (97.6±38.2) and (42.3±14.0)ng/ml, AUC0→t(435±38) and (377±52)ng·h·ml-1, AUC0→∞(446±38) and (427±72)ng·h·ml-1. The concentration-time profiles of madecassoside+asiaticoside B and asiatic acid showed double-peak phenomenon after oral administration, inferring that there might be a hepato-enteral circulation. The absolute bioavailability of CTG was (0.081±0.011)%.