Pharmacokinetics and tissue distribution of gentiopicroside following oral and intravenous administration in mice.
The pharmacokinetics and tissue distribution of Gentiopicroside (GPS), one of the major active components of the Gentiana species of medicinal plants, was studied following oral and intravenous administration in mice. The distribution of GPS in mice after oral and intravenous doses could be fitted to a two-compartments open model. The serum half-life of GPS was 6.1 h and 2.8 h for intravenous and oral administration, respectively. The Tmax of GPS after oral administration was 0.50 h, and the bioavailability was 39.6%. The AUC gradient in individual tissues following intravenous administration was kidney >serum >liver >spleen >lung >thymus >fat >heart >muscle >stomach >intestinal >brain. The MRT gradient was muscle >serum >lung >spleen >lung >intestinal>heart >stomach >brain >liver >thymus >kidney >fat. Overall the data show that GPS could be absorbed rapidly in mice, but with a low bioavailability, and could distribute to tissues extensively, but was generally cleared quickly with short MRTs. The study demonstrates the need for repeated dosage, or better, a slow release formulation as an ideal means of administering GPS.
Wang
Chang-Hong
CH
Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Wang
Zheng-Tao
ZT
Bligh
S W Annie
SW
White
Kenneth N
KN
White
Christopher J Branford
CJ
D000284:Administration, Oral; D000818:Animals; D005260:Female; D030012:Gentiana; D005960:Glucosides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D057888:Iridoid Glucosides; D039823:Iridoids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D051379:Mice; D011714:Pyrans / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology
D005960:Glucosides; D057888:Iridoid Glucosides; D039823:Iridoids; D011714:Pyrans; C012997:gentiopicroside