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 t...

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Bibliographic Details
Published in:European journal of drug metabolism and pharmacokinetics 2004-07, Vol.29 (3), p.199-203
Main Authors: WANG, Chang-Hong, WANG, Zheng-Tao, BLIGH, S. W, WHITE, Kenneth N, BRANFORD WHITE, Christopher J
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Biological and medical sciences
Female
General pharmacology
Gentiana
Glucosides - administration & dosage
Glucosides - pharmacokinetics
Injections, Intravenous
Iridoid Glucosides
Iridoids - administration & dosage
Iridoids - pharmacokinetics
Male
Medical sciences
Mice
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Pyrans - administration & dosage
Pyrans - pharmacokinetics
Tissue Distribution - drug effects
Tissue Distribution - physiology
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Summary: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.
ISSN:0378-7966
2107-0180
DOI:10.1007/bf03190598