RT Journal Article
SR Electronic
T1 Pharmacokinetics of Daikenchuto, a Traditional Japanese Medicine (Kampo) after Single Oral Administration to Healthy Japanese Volunteers
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 1784
OP 1788
DO 10.1124/dmd.111.040097
VO 39
IS 10
A1 Masaya Munekage
A1 Hiroyuki Kitagawa
A1 Kengo Ichikawa
A1 Junko Watanabe
A1 Katsuyuki Aoki
A1 Toru Kono
A1 Kazuhiro Hanazaki
YR 2011
UL http://dmd.aspetjournals.org/content/39/10/1784.abstract
AB The pharmacokinetics of daikenchuto (TJ-100), a pharmaceutical-grade traditional Japanese medicine, were investigated in healthy Japanese volunteers after a single oral administration of 2.5-, 5-, and 10-g doses. Six ingredients [hydroxy-α-sanshool (HAS), hydroxy-β-sanshool (HBS), [6]-shogaol (6S), [10]-shogaol (10S), ginsenoside Rb1(GRB1), and ginsenoside Rg1(GRG1)] of TJ-100 were determined by using liquid chromatography-tandem mass spectrometry. The results indicated that HAS, an ingredient derived from Zanthoxylum piperitum fruit, exhibited the highest plasma concentration among the six ingredients investigated. The plasma concentrations of HAS, HBS, 6S, and 10S reached the maximum concentration (approximately 400, 80, 0.14, and 0.6 ng/ml, respectively, after a 5-g administration of TJ-100) within 30 min after administration, and the mean half-life was approximately 2 h. Thus, these compounds were rapidly absorbed and eliminated. The plasma concentration of GRB1 reached the maximum concentration (2 ng/ml after a 5-g administration of TJ-100) at approximately 4 h after administration and the half-life of GRB1 was approximately 40 h. The plasma concentration of GRG1 was extremely low (<0.023 ng/ml). The pharmacokinetics of HAS, HBS, 6S, and 10S, were linear within the range of 2.5 to 10 g/day of TJ-100. On the other hand, the kinetics of GRB1 and GRG1 were not proportional to dosage, and plateauing was observed.