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右莰醇对缺血性脑卒中大鼠体内依达拉奉药代动力学的影响
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| 篇名： | 右莰醇对缺血性脑卒中大鼠体内依达拉奉药代动力学的影响 |
| TITLE： | Effects of dexborneol on pharmacokinetics of edaravone in cerebral ischemic stroke rats |
| 摘要： | 目的 探究在缺血性脑卒中（CIS）病理状态下，右莰醇对大鼠体内依达拉奉药代动力学参数的影响。方法将20只雄性SD大鼠随机分为依达拉奉组和依达拉奉右莰醇注射用浓溶液（EDB注射液）组，每组10只。采用改良Longa线栓法构建大鼠大脑中动脉阻塞（MCAO）模型，缺血再灌注5min内尾静脉注射相应药液，给药剂量均为2.5mg/kg（以依达拉奉计）。分别于注射后0.08、0.5、1、3、6、18、24h从大鼠眼眶静脉丛采集血液，以卡马西平为内标，采用超高效液相色谱-串联质谱（UPLC-MS/MS）法测定大鼠体内依达拉奉的血药浓度，以DAS软件计算药代动力学参数并进行比较。结果与依达拉奉组比较，EDB注射液组大鼠体内依达拉奉的峰浓度（cmax）显著升高（P＜0.05），半衰期、达峰时间、清除率及曲线下面积差异均无统计学意义（P＞0.05）。结论在CIS病理状态下，右莰醇可升高依达拉奉在模型大鼠血浆中的cmax，但对依达拉奉的全身暴露量与清除能力无明显影响。 |
| ABSTRACT： | OBJECTIVE To investigate the effects of dexborneol on the pharmacokinetic parameters of edaravone in rats under the pathological condition of cerebral ischemic stroke （CIS）.METHODS Twenty male SD rats were randomly divided into the edaravone group and the Edaravone and dexborneol concentrated solution for injection （EDB injection） group， with 10 rats in each group. A middle cerebral artery occlusion （MCAO） rat model was established using the modified Longa suture method. Within 5 min of ischemia-reperfusion， the corresponding drug solutions were injected via the tail vein at a dose of 2.5 mg/kg （calculated by edaravone）. Blood samples were collected from the orbital venous plexus at 0.08， 0.5， 1， 3， 6， 18， and 24 h after injection. With carbamazepine as the internal standard， the plasma concentration of edaravone was determined by ultra-performance liquid chromatography-tandem mass spectrometry （UPLC-MS/MS） method. Pharmacokinetic parameters were calculated using DAS software and compared between the two groups.RESULTS Compared with the edaravone group， the peak concentration （ c max ） of edaravone in the EDB injection group was significantly increased （ P ＜0.05）， while no statistically significant differences were observed in the half life， time to peak， clearance， or area under curve （ P ＞0.05）.CONCLUSIONS Under the pathological condition of CIS， dexborneol can increase the c max of edaravone in the plasma of model rats， but has no significant effect on the systemic exposure or clearance of edaravone. |
| 期刊： | 2026年第37卷第20期 |
| 作者： | 郝娟；孟志强；田晓晓；段学礼；侯苗；王芳；侯锐钢 |
| AUTHORS： | HAO Juan，MENG Zhiqiang，TIAN Xiaoxiao，DUAN Xueli，HOU Miao，WANG Fang，HOU Ruigang |
| 关键字： | 缺血性脑卒中;依达拉奉;右莰醇;药代动力学;超高效液相色谱-串联质谱法 |
| KEYWORDS： | cerebral ischemic stroke;Edaravone;dexborneol;pharmacokinetics;UPLC-MS/MS method |
| 阅读数： | 2 次 |
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