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环泊酚在孕鼠与胎鼠体内的药动学特征研究
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| 篇名： | 环泊酚在孕鼠与胎鼠体内的药动学特征研究 |
| TITLE： | Study on pharmacokinetic characteristics of ciprofol in pregnant and fetal rats |
| 摘要： | 目的 研究环泊酚在孕鼠与胎鼠体内的药动学特征，为环泊酚在剖宫产中的应用提供参考。方法取孕鼠8只，尾静脉单次给予2.4mg/kg环泊酚，分别于环泊酚给药后2、4、8、12、16、25、35、45、60、90min取出1只胎鼠，然后同时采集孕鼠与胎鼠全血；采用高效液相色谱-串联质谱（HPLC-MS/MS）法测定孕鼠和胎鼠体内各时间点环泊酚血药浓度，计算各时间点胎鼠血药浓度与孕鼠血药浓度的比值（F/M值），并绘制F/M时间曲线，再采用DAS2.0软件计算非房室模型药动学参数。结果与孕鼠相比，胎鼠体内环泊酚的cmax、AUC0-90min、AUC0-∞均显著降低，平均滞留时间（MRT）显著升高（P＜0.05）。环泊酚的F/M时间曲线呈先上升后下降的趋势，F/M值在0.16～0.84之间，且在45min时达到最大值（0.84）。结论环泊酚在孕鼠与胎鼠体内的药动学参数存在较大差异，其虽能透过胎盘屏障，但是在胎鼠体内的暴露量远低于孕鼠，有望成为剖宫产理想的麻醉用药。 |
| ABSTRACT： | OBJECTIVE To study the pharmacokinetic characteristics of ciprofol in pregnant and fetal rats， and provide reference for the application of ciprofol in cesarean section. METHODS Eight pregnant rats were selected. A single dose of 2.4 mg/kg of ciprofol was administered via the tail vein. One fetal rat was selected at 2， 4， 8， 12， 16， 25， 35， 45， 60， and 90 minutes respectively after ciprofol administration. Subsequently， whole blood samples were collected simultaneously from both the pregnant rats and fetal rats. HPLC-MS/MS method was used to determine the concentration of ciprofol in the bodies of pregnant and fetal rats. The ratios of fetal-to-maternal blood concentrations （F/M ratios） at each time point were calculated， and the F/M-time curves were plotted. Subsequently， non-compartmental pharmacokinetic parameters were computed using DAS 2.0 software. RESULTS Compared with pregnant rats， cmax， AUC0-90 min and AUC0-∞ of ciprofol in fetal rats were decreased significantly， while MRT was increased significantly （P＜0.05）. The F/M curve of ciprofol initially increased and then decreased， and between 0.16- 0.84， reaching a maximum value of 0.84 at 45 minutes. CONCLUSIONS Ciprofol can penetrate the placental barrier， and there are significant differences in pharmacokinetic parameters between pregnant and fetal rats. Moreover， the exposure level of ciprofol in fetal rats is much lower than that in pregnant rats. Therefore， ciprofol shows promise as an ideal anesthetic agent for cesarean section delivery. |
| 期刊： | 2025年第36卷第11期 |
| 作者： | 褚文昊；秦源蔓；张甜甜；许佳琪；李颖；张志清 |
| AUTHORS： | CHU Wenhao，QIN Yuanman，ZHANG Tiantian，XU Jiaqi，LI Ying，ZHANG Zhiqing |
| 关键字： | 环泊酚；孕鼠；胎鼠；胎盘屏障；药动学；血药浓度 |
| KEYWORDS： | ciprofol； pregnant rats； fetal rats； placental barrier； pharmacokinetics； blood concentration |
| 阅读数： | 6 次 |
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