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目的:建立HPLC-荧光法测定人血浆中左羟丙哌嗪浓度,研究其在中国健康人体内的药物动力学。方法:用1-羟基哌嗪为内标,血样经液———液萃取后进样,用HiQsil C18(150×4.6 mm,5μm)色谱柱,柱温30℃,0.1 M磷酸二氢钾(磷酸调pH值至2.51)∶乙腈∶甲醇(82∶3∶15)为流动相,流速0.6 ml/min,检测波长为Ex=240 nm,Em=350 nm。结果:血浆中杂质不干扰样品测定,线性范围为(3.5~886.0)ng/ml,最低可定量浓度为3.5 ng/ml(S/N=10),萃取回收率大于80%,方法回收率为106.1%~109.1%,日内和日间RSD均小于10%。左羟丙哌嗪的主要药动学参数:T1/2(2.93±0.54)h,Tmax(0.42±0.18)h,Cmax(345.2±113.6)ng/ml,AUC0-t(974.8±386.7)ng/h/ml,AUC0-∞(1008.2±397.2)ng/h/ml。结论:HPLC-荧光法灵敏、准确、重现性好,适合于左羟丙哌嗪的药动学研究。左羟丙哌嗪在中国健康人体内吸收迅速,消除快,安全性好。
OBJECTIVE: To establish a HPLC-fluorescence method for the determination of levodropropizine in human plasma and study its pharmacokinetics in Chinese healthy volunteers. Methods: 1-Hydroxypiperazine was used as an internal standard. The blood samples were extracted by liquid-liquid extraction. The samples were separated on a HiQsil C18 (150 × 4.6 mm, 5 μm) column at 30 ℃. 0.1 M potassium dihydrogen phosphate Phosphoric acid to adjust the pH to 2.51): acetonitrile: methanol (82: 3: 15) as the mobile phase at a flow rate of 0.6 ml / min with detection wavelengths of Ex = 240 nm and Em = 350 nm. Results: The impurities in the plasma did not interfere with the determination of the sample. The linear range was 3.5 ~ 886.0 ng / ml, the lowest quantifiable concentration was 3.5 ng / ml (S / N = 10) and the extraction recovery was more than 80% 106.1% ~ 109.1%. The daily and intraday RSD were less than 10%. The main pharmacokinetic parameters of levodropropizine were T1 / 2 (2.93 ± 0.54) h, Tmax 0.42 ± 0.18 h, Cmax 345.2 ± 113.6 ng / ml, AUC0-t 974.8 ± 386.7 ng / h / ml, AUC0-∞ (1008.2 ± 397.2) ng / h / ml. Conclusion: HPLC-fluorescence method is sensitive, accurate and reproducible. It is suitable for the pharmacokinetics of levodropropizine. Levodropropyrazide rapidly absorbed in Chinese healthy people, eliminating fast, good safety.