北五味子油中五味子甲素与五味子乙素在大鼠体内的药动学

Pharmacokinetics of deoxyschizandrin and γ-Schizandrin in Schisandra chinensis oil in rat plasma

目的:建立高效液相色谱法测定北五味子油水溶液灌胃后大鼠血浆中五味子甲素与五味子乙素的含量,并研究其在大鼠血浆中的药动学行为。方法:采用KromasilC18柱(4.6mm×250mm,5μm);流动相:乙腈-水(80:20)为流动相,流速:1.0mL.min-1;检测波长:254nm;柱温:30℃。以黄体酮为内标,乙腈沉淀蛋白后,测定大鼠血浆中五味子甲素与五味子乙素的含量并计算药动学参数。结果:大鼠血浆样品中,五味子甲素与五味子乙素的线性范围分别为30.5～960.5μg.L-1和42.6～1330.0μg.L-1,日内、日间精密度均<13%。Cmax为(567.6±129.8)μg.L-1和(714.4±335.9)μg.L-1,tmax为(5.33±0.18)h和(5.45±0.21)h,t1/2为(4.4±1.7)h和(5.3±1.8)h。结论:该法准确快速,灵敏度高,可作为大鼠血浆中五味子甲素与五味子乙素的同时检测及其体内药动学研究。

OBJECTIVE To develop an HPLC method for determination of deoxyschizandrin and γ-Schizandrin in rat plasma after oral administration of Schisandra chinensis oil and study the pharmacokinetic parameters of them in rat plasma. METHODS A Kromasil C18（4. 6 mm× 250 mm, 5 um） column was used, the mobile phase consisted of acetonitrile and water（80：20）, the flow rate was 1.0 mL.min^-1,the UV detection wavelength was set at 254 nm and the column temperature was 30℃. Proges terone was used as internal standard. RESULTS In rat plasma,good linearities and the concentration were found in the range of 30. 5 960. 5ug·L^-1 and 42. 6 -1330. 0ug·L^-1 for deoxyschizandrin and 7 Schizandrin respectively, Intra-day and Inter-day RSD were both less than 13~. Cmax were （567.6± 129. 8） ug·L^-1 and（714. 4 ± 335.9）ug·L^-1 ,tmax were （5.33 ± 0. 18） h and （5.45 ± 0. 21 ）h,t1/2 were （4. 43 ± 1.74）h and （5.3± 1.8）h. CONCLUSION The method was accurate with good reproducibility. It can be used for the determination and pharmacokinetic studies of deoxyschizandrin and γ-Schizandrin in rat plasma.