Disposition of Paeoniflorin and Paeonimetabolin I in Rats after Oral Administration of Toki-Shakuyaku-San (TS) and Shakuyaku-Kanzo-To (SK)

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After oral administration of a traditional Chinese prescription, Toki-Shakuyaku-San (TS) at doses of 100 and 500 mg to rats, the C_<max> values of paeoniflorin (PF) in the plasma were 146.3 and 165.1 ng/ml at 60 and ca. 45 min (with AUC values of 14305 and 19385 ng・min/ml), whereas the C_<max> values of paeonimetabolin I (PM-I, a major metabolite of PF) were 184 and 400.3 ng/ml at 120 and 180 min (with AUC values of 98497 and 182188 ng・min/ml). When another prescription, Shakuyaku-Kanzo-To (SK) was orally given at the same doses, the C_<max> values of PF and PM-I were 128.5 and 153.5 ng/ml, and 141.7 and 726.5 ng/ml, respectively at 5 min, and at 360 and 480 min, with AUC values of PF and PM-I (48857 and 32518 ng・min/ml, and 102136 and 469305 ng-min/ml), respectively. Considerable amounts of PM-I were still detected in the rat plasma 24 hr after p.o. administration of SK. It is concluded that following p.o. administration of TS or SK, PF, one of the main constituents of these prescriptions, was scarcely absorbed but PM-I, the intestinal bacterial metabolite, largely absorbed from the intestinal tract. Moreover, it seems likely that SK, which potentially reduces the gastric emptying rate or peristaltic movement of the intestine, takes longer time to reach the large bowel where most of PF is transformed to PM-I by intestinal bacteria.
日本生薬学会の論文
1998-06-20