Characteristics of Delayed Excretion of Flavonoids in Human Urine after Administration of Shosaiko-to, a Herbal Medicine

• Published in: Biological & pharmaceutical bulletin Vol. 21; no. 12; pp. 1251 - 1257
• Main Authors: LI, Chuan, HOMMA, Masato, OKA, Kitaro
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01.12.1998; Maruzen; Japan Science and Technology Agency
• Subjects: Adult; Biological and medical sciences; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - metabolism; Drugs, Chinese Herbal - pharmacokinetics; flavonoids; Flavonoids - urine; General pharmacology; Glucose - metabolism; Humans; Male; Medical sciences; Metabolic Clearance Rate; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; renal excretion; Shosaiko-to; Stereoisomerism; Time Factors; Asia; Japan; Human; Excretion; Healthy subject; Pharmacognosy; Single dose; Oral administration; Metabolism; Flavonoid; Medicinal plant; Absorption; Folk medicine; Plant origin; Pharmacokinetics
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.21.1251

There has been little explanation of herbal medicines by modern medical sciences, including pharmacokinetics, whereas physicians follow empirical indications written in classical literature. Recent reports of herb-induced adverse reactions compelled us to proceed the investigation of a herbal medicine Shosaiko-to (TJ-9) from a pharmacokinetic point of view.To five healthy volunteers, a single 5g dose of TJ-9, consisting of 7 herbs, was administered. We conducted HPLC analysis of the timed-urine specimens to disclose the type and amount of compounds excreted. Excretion rate-time curves were analyzed individually.Four flavonoids, liquiritigenin, baicalein, wogonin and oroxylin A, were found both in the urine and TJ-9. The glycosides in TJ-9 were absorbed after microflora hydrolysis. Davidigenin, which was not found in TJ-9, was an intestinal metabolite of liquiritigenin. Also, two flavanones, S-dihydrowogonin and S-dihydrooroxylin A, were identified as the metabolites of wogonin and oroxylin A, respectively. Excretion rate-time curves of the flavonoids were divided into three types of structure-dependent absorption, i.e. (1) the fast absorption of herbal-origin aglycons, (2) the moderately-delayed absorption of aglycons derived from herbal glycosides, and (3) markedly-delayed absorption after the molecular transformation of herbal compounds.Individual excretion profiles seemed to depend on microflora activities. Two types of flavonones, S-dihydrowogonin and S-dihydrooroxylin A, were found in a half of the volunteers, suggesting there might be two kinds of volunteers, namely, rapid and poor metabolizers of flavonoids.