葛根水煎劑與濃縮散劑於健康人體尿藥動力學之比較   全文下載

Comparison of Urinary Kinetics between Traditional Decoction and Concentrated Powders of Puerariae Radix in Healthy Men

葛根為常用中藥，富含異黃酮成分，如puerarin 、daidzin 、daidzein等。本研究比較葛根水煎劑與濃縮散劑於健康人體的尿藥動力學。十位男性志願受試者口服葛根水煎劑與濃縮散劑，以交叉設計給藥，收集尿液36 h。尿液樣品於水解之前與之後利用HPLC分析。研究結果顯示，尿中異黃酮主要以daidzein之sulfates 、glucuronides等結合態代謝物的形式存在。Daidzein sulfates/glucuronides 的半生期約5-7 h。綜言之，口服葛根水煎劑與濃縮散劑後，異黃酮幾全代謝成daidzein sulfates/glucuronides，主要為sulfates。藉由葛根兩種劑型間尿藥動力學之比較，結果顯示daidzin 、 daidzein是可為生物體利用的異黃酮，因此對葛根之療效而言，其含量比puerarin重要。

Puerariae Radix (PR), the roots of Pueraria lobata (Leguminosae), is widely used in clinical Chinese medicine and also as a food in oriental countries. PR is a rich source of isoflavones including puerarin, daidzin and daidzein. This study was aimed to compare the urinary kinetics of isoflavones between traditional decoction (TD) and concentrated powders (CP) of PR in healthy man. Ten male volun-teers were given two dosage forms of PR in a crossover design and their urine was collected at specific intervals until 36 h. Urine samples were assayed by an HPLC method before and after hydrolysis with β-glucuronidase and sulfatase. The results indicated that the parent forms of puerarin, daidzin and daidzein were not detected in urine, whereas daidzein sulfates/glucuronides were predominant, mainly sulfates. The half-lives of daidzein sulfates/glucuronides were 5 - 7 h. In conclusion, the isoflavones were exclusively metabolized to sulfates/glucuronides of daidzein following administration of TD and CP of PR. Through the comparison of urine kinetics between two dosage forms, we suggest that the standardization of the contents of daidzin and daidzein, which are bioavailable, is more important than puerarin content for the efficacy of PR.