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氯吡格雷对大鼠体内环泊酚药动学和药效学的影响
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| 篇名： | 氯吡格雷对大鼠体内环泊酚药动学和药效学的影响 |
| TITLE： | Effects of clopidogrel on the pharmacokinetics and pharmacodynamics of ciprofol in rats |
| 摘要： | 目的 考察氯吡格雷对大鼠体内环泊酚药动学和药效学的影响。方法18只雄性SD大鼠随机分为对照组、氯吡格雷正常剂量组和氯吡格雷高剂量组，每组6只。氯吡格雷正常剂量组和氯吡格雷高剂量组大鼠分别灌胃7.5、15mg/kg的氯吡格雷，对照组大鼠灌胃同体积的0.5%羧甲基纤维素钠溶液，每天1次，连续给药14d后于大鼠尾静脉注射环泊酚2.4mg/kg。在结束注射后2、4、8、12、16、20、30、45、60min时于眼内眦取血，统计各组大鼠的翻正反射消失（LORR）持续时间。大鼠血浆经乙腈沉淀蛋白后，以氘代环泊酚为内标，以SymmetryC18为色谱柱，以乙腈-含5mmol/L乙酸铵的0.01%氨水溶液（梯度洗脱）为流动相，采用液相色谱-串联质谱法检测血浆中环泊酚的质量浓度，采用DAS2.0软件计算各组大鼠的药动学参数。结果与对照组比较，氯吡格雷正常剂量组和氯吡格雷高剂量组大鼠体内环泊酚的药时曲线下面积和平均驻留时间均显著增加或延长，血浆清除率均显著降低，LORR持续时间分别延长了19.5%和23.9%，差异均有统计学意义（P＜0.05）。氯吡格雷两个剂量组大鼠体内环泊酚药动学参数和LORR持续时间比较差异均无统计学意义（P＞0.05）。结论氯吡格雷可抑制环泊酚的体内代谢，并延长大鼠的LORR持续时间。 |
| ABSTRACT： | OBJECTIVE To investigate the effects of clopidogrel on the pharmacokinetics and pharmacodynamics of ciprofol in rats. METHODS Eighteen male SD rats were randomly divided into control group， clopidogrel normal-dose group and clopidogrel high-dose group， with 6 rats in each group. Among them， rats in the normal-dose group and high-dose group were given 7.5 mg/kg and 15 mg/kg clopidogrel by gavage， respectively， and rats in the control group were given the same volume of 0.5% sodium carboxymethyl cellulose solution， once a day， for 14 consecutive days. Afterward， 2.4 mg/kg ciprofol was injected by tailvein and blood samples were collected from the inner canthus of the eye at 2， 4， 8， 12， 16， 20， 30， 45 and 60 min after the end of the administration. During this period， the duration of the loss of righting reflex （LORR） in rats was counted. After the proteins were precipitated by acetonitrile， the rat plasma sample was analyzed by LC-MS/MS using deuterated ciprofol as the internal standard， Symmetry C18 as the chromatographic column， and acetonitrile-0.01% ammonia solution containing 5 mmol/L ammonium acetate （gradient elution） as the mobile phase to detect the concentration of ciprofol in the plasma. The pharmacokinetic parameters in rats were calculated by using DAS 2.0 software. RESULTS Compared with control group， area under the drug concentration-time curve and mean residence time of ciprofol increased or prolonged significantly， while plasma clearance decreased significantly in clopidogrel normal-dose and high-dose groups； the duration of LORR in rats was prolonged by 19.5% and 23.9%， with statistical difference （P＜0.05）. However， there was no statistically significant difference in the pharmacokinetic parameters or LORR duration of ciprofol between the different dose groups of clopidogrel （P＞0.05）. CONCLUSIONS Clopidogrel could inhibit the metabolism of ciprofol in rats and prolong the duration of LORR. |
| 期刊： | 2025年第36卷第02期 |
| 作者： | 路明；尹晓玉；李文利；李珊；李相晨；张志清 |
| AUTHORS： | LU Ming，YIN Xiaoyu，LI Wenli，LI Shan，LI Xiangchen，ZHANG Zhiqing |
| 关键字： | 氯吡格雷；环泊酚；药物-药物相互作用；药动学；药效学 |
| KEYWORDS： | clopidogrel； ciprofol； drug-drug interactions； pharmacokinetics； pharmacodynamics |
| 阅读数： | 4 次 |
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