Pharmacokinetics and bioavailability of gentiopicroside from decoctions of Gentianae and Longdan Xiegan Tang after oral administration in rats--comparison with gentiopicroside alone.
The pharmacokinetics and bioavailability of gentiopicroside (GPS), an active component of the Gentian plant species, from orally administered decoctions of Gentianae (DG), or in combination with other plants in the prescription of Longdan Xiegan Tang (LXT), was compared in rats with oral administration of GPS alone, using doses adjusted to deliver equivalent amounts of GPS (150 mg/kg). Changes in plasma levels of GPS following oral administration of GPS or DG could be fitted to a one compartment open model with elimination half times (T(1/2)Ke) of 3.35+/-0.76 h and 6.21+/-3.07 h, respectively. Kinetics of plasma GPS following oral administration of LXT could be fitted to a two compartments open model with an elimination half time (T((1/2)beta)) of 3.83+/-1.54 h. The bioavailability of GPS from DG was markedly better, and that from LXT markedly worse, compared with GPS alone, as judged by the area under concentration-time curve (AUC) values of 70.0+/-13.9 microgh/ml (DG), 32.7+/-12.9 microgh/ml (GPS) and 19.1+/-5.9 microgh/ml (LXT). The study demonstrates the marked variability in pharmacokinetics and bioavailability of an active component from different herbal preparations.
Wang
Chang-hong
CH
Key Laboratory of Standardization of Chinese Medicines, Ministry of Education, 1200 Cailun Road, Shanghai, China.
Cheng
Xue-mei
XM
Bligh
S W Annie
SW
White
Kenneth N
KN
Branford-White
Christopher J
CJ
Wang
Zheng-tao
ZT
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002138:Calibration; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D005260:Female; D030012:Gentiana; D005960:Glucosides / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D006207:Half-Life; D057888:Iridoid Glucosides; D039823:Iridoids / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry; D011714:Pyrans / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012015:Reference Standards; D015203:Reproducibility of Results
D005960:Glucosides; D057888:Iridoid Glucosides; D039823:Iridoids; D011714:Pyrans; C012997:gentiopicroside