摘要
目的 :建立人血浆中克林霉素浓度的高效液相色谱 -质谱法 ,测定志愿者口服盐酸克林霉素胶囊后的血药浓度 ,并对供试制剂和参比制剂的生物等效性进行评价。方法 :血浆中加入内标西沙必利后碱化 ,以乙酸乙酯提取 ,进行高效液相色谱 -质谱法检测。色谱柱为 Kromasil ODS1 5 0× 4 .6 mm,5 μm,流动相为甲醇 -1 %冰醋酸 ( 5 7∶ 4 3) ,流速 0 .8ml/min,质谱检测采用选择性离子检测方法。 2 0名健康志愿者随机分成两组 ,分别服用供试胶囊和参比胶囊 ,临床实验方案采用双交叉实验设计法。结果 :克林霉素的线性范围为 0 .0 0 5～ 1 5 μg/ml,最低检测浓度为 1 ng/ml,本测定方法的提取回收率在 1 0 0 .5 %～ 1 0 5 .2 % ,用本法测定了 2 0名志愿者随机交叉口服单剂量 6 0 0 mg后血浆中药物的浓度经时变化过程 ,并对其药动学参数进行估算。测得的 2种胶囊的主要药代动力学参数无显著性差异。结论 :该法简便 ,准确 。
AIM A LC-MS method was established for the study of pharmacokinetics and bioavailability of clindamycin in human body. METHODS Cisapride was used as an internal standard. After adding cisapride and 0.1 mol/L NaOH 100 μl, the plasma samples were extracted with ethyl acetate and determined by LC-MS. The mobile phase is CH 3OH-1% HOAc(57∶43, v/v). Analyses were run at a flow rate of 0.8 ml/min. The plasma concentration of clindamycin was determined by this LC-MS method following a single oral dose of 600 mg of two formulations given to each 20 volunteers in an open randomized two-way crossover design. RESULTS The extraction recovery of this method ranged from 100.5%~105.2%. The assay exhibited a linear range of 0.005-15 μg/ml and gave a correlation(r) of 0.9997. The bioavailability results of two formulations were similar. CONCLUSION The method is simple, sensitive and rapid.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2002年第1期28-31,共4页
Journal of China Pharmaceutical University
