黃芩傳統水煎劑與濃縮散劑於人體內生體可用率之比較   全文下載

Relative Flavone Bioavailability of Scutellariae Radix between Traditional Decoction and Commercial Powder Preparation in Humans

黃芩為富含黃酮類成分之傳統中藥。本研究探討黃芩傳統水煎劑及濃縮散劑中之黃酮類成分黃芩?、黃芩?元、漢黃芩?和漢黃芩素在人體內吸收之比較。八位受試者以隨機交叉設計給藥，分別口服給予90毫升之傳統水煎劑（相當於9克之藥材）或4.3克之濃縮散劑（約相當於9克之藥材），以高效液相層析法測定傳統水煎劑及濃縮散劑中黃芩?、黃芩?元、漢黃芩?和漢黃芩素以及它們在尿中之結合態代謝物之含量。尿液中代謝物之檢測是經由s-葡萄糖醛酸?及硫酸?水解之後，定量其黃芩?元和漢黃芩素之濃度。兩種劑型相對生體可用率係比較服藥後之三十六小時內，其尿中結合態代謝物之總排出率。定量結果顯示，口服傳統水煎劑後，尿中黃芩?元及漢黃芩素代謝物之平均總排出量分別為66.0 ± 8.7 μmol（平均排出率為4.0 ± 0.5%）及30.8 ± 8.2μmol（平均排出率為7.1 ± 1.8%），而濃縮散劑則為40.2 ± 6.0 μmol（2.2 ± 0.3%）及14.7 ± 3.7 μmo（4.1 ± 1.0%）。因此口服濃縮散劑之黃芩?／黃芩?元和漢黃芩?／漢黃芩素平均生體可用率，比傳統水煎劑分別顯著減少了44.2 ± 0.1%及42.3 ± 0.1%。此結果顯示黃芩之傳統水煎劑與濃縮散劑無生物相等性。

Baicalin, baicalein, wogonoside and wogonin are bioactive flavone constituents of Scutellariae Radix with a wide range of beneficial activities. The purpose of this study attempted to compare the absorption of baicalin, baicalein, wogonoside and wogonin between traditional decoction and a commercial powder preparation of Scutellariae Radix. Eight healthy male volunteers received 90 mL traditional decoction (equivalent to 9 g crude drug) and 4.3 g commercial powder preparation (comparable to 9 g crude drug) of Scutellariae Radix in a randomized crossover design. The contents of baicalin, baicalein, wogonoside and wogonin in traditional decoction and commercial preparation as well as their metabolites in urine were determined by HPLC methods. The relative flavone bioavailability was obtained by comparing urinary recoveries of glucuronides/sulfates of wogonin and baicalein within 36 hr after dosing. The mean (± S.E.) cumulated renal excretion of glucuronides/sulfates of baicalein and wogonin after intake of traditional decoction were 66.0 ± 8.7 μmol (4.0 ± 0.5% of dose) and 30.8 ± 8.2 μmol (7.1 ± 1.8% of dose), whereas those for commercial preparation were 40.2 ± 6.0 μmol (2.2 ± 0.3% of dose) and 14.7 ± 3.7 μmol (4.1 ± 1.0% of dose), respectively. The results indicated that the bioavailability of wogonin/wogonoside was about two times when compared to that of baicalein/baicalin from either traditional decoction or the commercial preparation. The flavone bioavailability from commercial preparation was significantly lower by 44.2± 0.1% for baicalin/baicalein and by 42.3 ± 0.1% for wogonoside/wogonin than those from traditional decoction. 黃芩為富含黃酮類成分之傳統中藥。本研究探討黃芩傳統水煎劑及濃縮散劑中之黃酮類成分黃芩苷、黃芩苷元、漢黃芩苷和漢黃芩素在人體內吸收之比較。八位受試者以隨機交叉設計給藥，分別口服給予90毫升之傳統水煎劑（相當於9克之藥材）或4.3克之濃縮散劑（約相當於9克之藥材），以高效液相層析法測定傳統水煎劑及濃縮散劑中黃芩苷、黃芩苷元、漢黃芩苷和漢黃芩素以及它們在尿中之結合態代謝物之含量。尿液中代謝物之檢測是經由ß-葡萄糖醛酸酶及硫酸酶水解之後，定量其黃芩苷元和漢黃芩素之濃度。兩種劑型相對生體可用率係比較服藥後之三十六小時內，其尿中結合態代謝物之總排出率。定量結果顯示，口服傳統水煎劑後，尿中黃芩苷元及漢黃芩素代謝物之平均總排出量分別為66.0 ± 8.7 μmol（平均排出率為4.0 ± 0.5%）及30.8 ± 8.2μmol（平均排出率為7.1 ± 1.8%），而濃縮散劑則為40.2 ± 6.0 μmol（2.2 ± 0.3%）及14.7 ± 3.7 μmo（4.1 ± 1.0%）。因此口服濃縮散劑之黃芩苷／黃芩苷元和漢黃芩苷／漢黃芩素平均生體可用率，比傳統水煎劑分別顯著減少了44.2 ± 0.1%及42.3 ± 0.1%。此結果顯示黃芩之傳統水煎劑與濃縮散劑無生物相等性。