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稳态时难治性癫痫大鼠体内脑心清对卡马西平药动学及脑组织分布的影响

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目的 研究难治性癫痫大鼠体内稳态时脑心清对卡马西平药动学及脑组织分布的影响。方法 采用脑立体定位技术向SD大鼠侧脑室内注入红藻氨酸(KA)建立难治性癫痫模型,造模成功后,将难治性癫痫模型大鼠随机分为卡马西平组和脑心清+卡马西平组,卡马西平组给予卡马西平 80 mg/kg及生理盐水 5 ml灌胃,脑心清+卡马西平组给予脑心清 550 mg/kg+卡马西平 80 mg/kg灌胃,连续给药60 d。在不同时间点采集血样及脑组织样品,测定血浆与脑组织中卡马西平的浓度,计算药动学参数并进行统计学分析。结果 与单用卡马西平组相比,脑心清联合卡马西平组的药动学参数差异无统计学意义;而脑心清联合卡马西平组的脑药浓度明显高于单用卡马西平组。结论 长期给药脑心清不影响卡马西平在难治性癫痫大鼠体内的稳态血药浓度,且对卡马西平通过血脑屏障具有一定的促进作用,提高了卡马西平的稳态脑药浓度。
Effects of Naoxinqing on the pharmacokinetics and brain tissue distribution of carbamazepine at steady state in refractory epilepsy rats
Objective Exploring the effects of Naoxinqing on the pharmacokinetics and brian tissue distribution of carbamazepine at steady state in refractory epilepsy rats.Methods The refractory epilepsy rat model was established by injection of Kainic acid into the lateral ventricles of SD rats using stereolocalization technique,after the model was successfully established,the refractory epilepsy model rats were randomly divided into carbamazepine group and Naoxinqing+carbamazepine group,the carbamazepine group was given carbamazepine(80 mg/kg)and 5 ml of normal saline by intragastric administration,and the Naoxinqing+carbamazepine group was given Naoxinqing(550 mg/kg)+carbamazepine(80 mg/kg)by intragastric administration,continuous administration for 60 days.Blood samples and brain tissue samples were collected at different time points,the concentrations of carbamazepine in plasma and brain tissue were determined,and the pharmacokinetic parameters were calculated and statistically analyzed.Results Compared with carbamazepine alone group,there was no significant difference in pharmacokinetic parameters of Naoxinqing combined with carbamazepine group;However,the concentration of brain drug in Naoxinqing combined with carbamazepine group was significantly higher than that in carbamazepine alone group.Conclusion After long-term administration,Naoxinqing don't affect the steady blood concentration of carbamazepine in rats with refractory epilepsy,and it has a certain role in promoting carbamazepine to pass through the blood brain barrier,and increase the steady state brain drug concentration of carbamazepine.

Refractory epilepsyNaoxinqingCarbamazepinePharmacokineticBrain tissue distribution

牛倩倩、党翔吉、牛国强、宋霞、焦海胜

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兰州大学第二医院(第二临床医学院)药剂科,兰州 730030

联勤保障部队第940医院普通外科,兰州 730050

难治性癫痫 脑心清 卡马西平 药动学 脑组织分布

甘肃省青年科技基金项目甘肃省自然科技基金项目兰州大学第二医院"萃英科技创新"计划项目

22JR5RA101722JR5RA982CY2022-QN-B02

2024

中国处方药
南方医药经济研究所

中国处方药

影响因子:0.649
ISSN:1671-945X
年,卷(期):2024.22(2)
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