TY - JOUR 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 DO - 10.1124/dmd.111.040097 SP - dmd.111.040097 AU - Masaya Munekage AU - Hiroyuki Kitagawa AU - Kengo Ichikawa AU - Junko Watanabe AU - Katsuyuki Aoki AU - Toru Kono AU - Kazuhiro Hanazaki Y1 - 2011/01/01 UR - http://dmd.aspetjournals.org/content/early/2011/07/01/dmd.111.040097.abstract N2 - The pharmacokinetics of Daikenchuto (TJ-100), a pharmaceutical grade traditional Japanese medicine, were investigated in healthy Japanese volunteers after single oral administration of 2.5, 5 and 10g 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 LC-MS/MS. The results indicated that HAS an ingredient derived from Zanthoxylum fruit, exhibited the highest plasma concentration among the 6 ingredients investigated. The plasma concentrations of HAS, HBS, 6S and 10S reached maximum concentration (approximately 400, 80, 0.14 and 0.6 ng/mL, respectively after 5 g administration of TJ-100) within 30 min after administration and the mean half-life was approximately 2 hr. Thus, these compounds were rapidly absorbed and eliminated. The plasma concentration of GRB1 reached maximum concentration (2 ng/mL after 5 g administration of TJ-100) at approximately 4 hr after administration and the half life of GRB1 was approximately 40hr. 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 g 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. ER -