Pharmacokinetics and tissue distribution of Gentiopicroside following oral and intravenous administration in mice

• 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
• ISSN: 0378-7966; 2107-0180
• DOI: 10.1007/bf03190598

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.