| 摘要: | 黃連解毒湯由黃連、黃芩、黃柏及梔子等四藥組成，臨床常用於細菌性痢疾、黃疸等症狀。本研究首先開發出家兔體內之血漿中黃連解毒湯三種指標成份小蘗鹼、黃芩?及梔子?之高效液相層析法。層析管柱為VERCOPAK Intertsil ODS-2 （4.6*150mm），使用濃度梯度移動相：A相（乙?）和B相（0.02%磷酸緩衝溶液pH=2.6），0-19分鐘，A相（84%）：B相（16%）；20-30分鐘，A相（78%）：B相（22%）；31-42分鐘，A相（70%）：B相（30%），內標準品為間羥基苯甲酸。紫外光檢測波長：0-18分鐘，240nm；18-42分鐘，277nm。分別定量血漿檢品中並驗證具有選擇性、精確性及安定性。 六隻家兔在試驗設計下，進行指標成份注射液、黃連解毒湯注射液及口服液之試驗給藥。家兔在黃連解毒湯注射液給藥後，血漿中小蘗鹼、黃芩?及梔子?呈現二室體模式。家兔在給予黃連解毒湯注射液後與指標成分注射液之結果比，發現黃芩?的排除半衰期延長 (由80.79±17.16增為118.05±29.90min.)，小蘗鹼(64.85±5.58 vs. 60.64±1.29 min.) 、梔子?(54.97±11.98 vs. 51.22±18.83 min.)的排除半衰期沒有明顯改變黃芩?的排除半衰期延長 (由約80 min.增為約118 min.)，小蘗鹼、梔子?的排除半衰期沒有明顯改變。家兔口服黃連解毒湯後之指標成份小蘗鹼、黃芩?及梔子?之生體可用率分別約為6.88﹪、7.27﹪、10.33﹪。以上研究結果可供黃連解毒湯在劑型設計、製劑品管、生物藥劑學及臨床藥動學之研究參考。; Huang-Lian-Jiee-Dwu-Tang (HLJDT), a traditional Chinese medicine formulation containing Coptidis Rhizoma, Scutellariae Radix, Phellodendric Cortex and Gardeniae Fluctus, are widely used in the treatment of bacillary dysentery and jaundice. In this study, a high-performace liquid chromatographic method for determination of berberine, baicalin and geniposide in rabbit blood. An VERCOPAK Intertsil ODS-2 (4.6*150mm) column with the mobile phase consisted of solvent A (100% CH3CN), and solvent B (H2O-H3PO4 pH=2.6) was used. The 1 ml/min gradient was follow: 0-19 min, solvent A (84%)-solvent B (16%); 20-30 min, solvent A (78%)-solvent B (22%); 31-42 min, solvent A (70%)-solvent B (30%). The internal standard was m-hydroxybenzoic acid. The monitoring wavelength was: 0-18 min, 240 nm; 19-42 min, 277 nm. After IV administration of the HLJDT to the rabbits, the plasma level-time profiles of berberine, baicalin and geniposide were adequately described by an open two-compartment model. The elimination half-lives of baicalin was prolonged (118.05±29.90 vs 80.79±17.16 minutes), berberine (60.64±1.29 vs 64.85±5.58 minutes) and (51.22±18.83 vs 54.97±11.98minutes) geniposide were not different clearly by compared with that of pure berberine, baicalin and geniposide injection after IV administration. The absolute bioavailability of berberine, baicalin and geniposide after oral administration of the HLJDT were 6.88, 7.27 and 10.33 % respectively. This result suggests that repeated dose is necessary for HLJDT when in clinical use. |
