目的 測定青蒿素在不同pH緩沖液和7種非極性溶劑中的平衡溶解度以及在正辛醇-水中的表觀油水分配系數(shù)，為青蒿素新劑型的研究與開發(fā)提供實(shí)驗(yàn)基礎(chǔ)。方法 采用高效液相–柱后衍生化–紫外檢測法測定青蒿素在不同pH緩沖溶液及7種非極性溶劑中的平衡溶解度；采用搖瓶法測定青蒿素的表觀油水分配系數(shù)。結(jié)果 37 ℃時(shí)青蒿素在純水中的平衡溶解度為82.4 μg/mL，隨著pH的增大平衡溶解度呈先增大（pH 5.0～6.8）后減小（pH 6.8～8.0）的趨勢；37 ℃時(shí)青蒿素在肉豆蔻酸異丙酯（IPM）、油酸乙酯（EO）和中鏈甘油酸三酯（MCT）中平衡溶解度較大，分別為10.34、9.28、8.46 mg/mL，青蒿素的正辛醇-水表觀油水分配系數(shù)P為12.2（lg P＝1.09）。結(jié)論 青蒿素水溶性差，在非極性溶劑IPM、EO、MCT中平衡溶解度較大。

Objective To determine the equilibrium solubility of artemisinin in buffer with different pH values and seven kinds of nonpolar solvents as well as its apparent octanol/water partition coefficient in octanol-water/buffer solution, thus to provide the experimental basis for the research and development of new preparation of artemisinin. Methods The equilibrium solubility of artemisinin in buffer with different pH values and seven kinds of nonpolar solvents was measured by HPLC with post-column derivatization and UV detection. Shaking flask method was adopted to determine the apparent octanol/water partition coefficient of artemisinin. Results The equilibrium solubility of artemisinin in water was 82.4 μg/mL at 37 ℃, and as the pH value increased, it increased first (pH values from 5.0 to 6.8) and decreased afterwards (pH values from 6.8 to 8.0). At 37 ℃, the equilibrium solubility values of artemisinin in isopropyl myristate (IPM), ethyl oleate (EO), and medium-chain triglycerides (MCT) were 10.34, 9.28, and 8.46 mg/mL, respectively. The apparent octanol-water partition coefficient of artemisinin was 12.2 (lg P = 1.09). Conclusion Artemisinin has poor water solubility, while its equilibrium solubility is higher in IPM, EO, and MCT.

國家自然基金資助項(xiàng)目（30973589）；山西省回國留學(xué)人員科研項(xiàng)目（2009-47）