Xu Shun-Jun, Zhu Ya-Ling, Yu Jie-Jing, Sun Shuai, Xu Yi-Juan, Yang Liu
Guangzhou ImVin Pharmaceutical Co., Ltd., Guangzhou 510663, China.
Guangdong Second Traditional Chinese Medicine Hospital, Guangzhou 510095, China.
Zhongguo Zhong Yao Za Zhi. 2016 Jan;41(1):129-133. doi: 10.4268/cjcmm20160125.
To study pharmacokinetic characteristics of epimedin A, B, C and icariin after intermuscular administration of Chuankezhi injection to rat. The established RRLC-MS/MS method was applied for simultaneous determination of four analytes in rat plasma and calculating their pharmacokinetic parameters. As a result, each analyte showed a good linear relationship in the concentration range of 1-1 000 μg•L⁻¹.The intra-day precise was 96.9%-107.5% with RSD<5.99%, inter-day precise was 92.3%-105.0% with RSD<10.16%. The relative recovery of four analytes was 88.1%-101.1% with RSD<7.9% and their absolute recovery was 72.0%-86.6% with RSD<6.3%. After intermuscular administration of Chuankezhi injection, the plasma concentration of four flavonoid glycosides rapidly arose to peaks at about 10 min, and then quickly declined in rat. Tmax of epimedin A, B, C and icariin was 0.21, 0.19, 0.16 and 0.49 h, respectively, and their mean elimination half-life(t1/2z) was 0.60, 0.62, 0.47 and 0.49 h. The established method was validated to be sensitive, rapid and specific for determination of the four analytes. Serum concentration of 4 species of epimedium flavonoids in Chuankezhi injection was low, and their absorption and elimination seem quickly, displaying similar pharmacokinetic characteristics in this study.
研究穿琥宁注射液肌肉注射给药后大鼠体内淫羊藿苷A、B、C及淫羊藿苷的药代动力学特征。采用所建立的快速液相色谱-串联质谱（RRLC-MS/MS）法同时测定大鼠血浆中4种分析物，并计算其药代动力学参数。结果显示，各分析物在1～1000μg•L⁻¹浓度范围内呈良好的线性关系。日内精密度为96.9%～107.5%，相对标准偏差（RSD）<5.99%；日间精密度为92.3%～105.0%，RSD<10.16%。4种分析物的相对回收率为88.1%～101.1%，RSD<7.9%；绝对回收率为72.0%～86.6%，RSD<6.3%。穿琥宁注射液肌肉注射给药后，4种黄酮苷的血浆浓度在约10min迅速升至峰值，随后在大鼠体内迅速下降。淫羊藿苷A、B、C及淫羊藿苷的达峰时间（Tmax）分别为0.21、0.19、0.16和0.49h，其平均消除半衰期（t1/2z）分别为0.60、0.62、0.47和0.49h。所建立的方法经验证对4种分析物的测定具有灵敏、快速和特异的特点。穿琥宁注射液中4种淫羊藿黄酮的血清浓度较低，其吸收和消除较快，在本研究中显示出相似的药代动力学特征。
