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斑蝥酸钠对卡培他滨在大鼠体内药动学行为的影响
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| 篇名： | 斑蝥酸钠对卡培他滨在大鼠体内药动学行为的影响 |
| TITLE： | Effects of disodium cantharidinate on the pharmacokinetic behavior of capecitabine in rats |
| 摘要： | 目的 考察斑蝥酸钠对卡培他滨在大鼠体内药动学行为的影响。方法将大鼠随机分为2个对照组和2个实验组，每组6只。2个对照组大鼠腹腔注射生理盐水，2个实验组腹腔注射斑蝥酸钠注射液0.5mL/kg，连续给药7d；第8天给药后，对照1组和实验1组大鼠灌胃卡培他滨5mg/kg，对照2组和实验2组大鼠静脉注射卡培他滨5mg/kg。于给药后不同时间点采集血样。血样经乙酸乙酯萃取后，以甲苯磺丁脲为内标，采用超高效液相色谱-串联质谱法测定大鼠血浆中卡培他滨的浓度，采用DAS2.0软件计算主要药动学参数。结果与对照1组比较，实验1组无穷大时间内的平均滞留时间（MRT0－∞）、峰浓度（cmax）、30h内的药-时曲线下面积（AUC0－30h）、AUC0－∞和生物利用度（F）均显著升高，表观清除率（CLz/F）显著降低（P＜0.01）；与对照2组比较，实验2组的半衰期（t1/2）、MRT0－30h、MRT0－∞、AUC0－30h、AUC0－∞均显著升高（P＜0.01）。结论斑蝥酸钠能增加卡培他滨在大鼠体内的血浆暴露量，提高口服生物利用度，延长平均滞留时间，降低清除率。 |
| ABSTRACT： | OBJECTIVE To study the effects of disodium cantharidinate on the pharmacokinetic behavior of capecitabine in rats. METHODS Rats were randomly divided into two control groups and two experimental groups with 6 rats in each group. Two control groups were intraperitoneally injected with normal saline， and two experimental groups were intraperitoneally injected with Disodium cantharidinate injection of 0.5 mL/kg， for 7 consecutive days. Eight days after medication， control group 1 and experimental group 1 were given capecitabine 5 mg/kg intragastrically， while control group 2 and experimental group 2 were given capecitabine 5 mg/kg intravenously. Blood samples were collected at different time points after administration. After extraction with ethyl acetate， the concentration of capecitabine in rat plasma was determined by UPLC-MS/MS method using tolbutamide as the internal standard. The pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS Compared with control group 1， MRT0－∞， cmax， AUC0－30 h， AUC0－∞ and F of experimental group 1 were increased significantly， while CLz/F was decreased significantly （P＜0.01）. Compared with control group 2， t1/2， MRT0－30 h， MRT0-∞， AUC0－30 h and AUC0－∞ of experimental group 2 were increased significantly （P＜0.01）. CONCLUSIONS Disodium cantharidinate can increase the plasma exposure of capecitabine in rats， improve its oral bioavailability， prolong the average residence time， and reduce its clearance rate. |
| 期刊： | 2023年第34卷第18期 |
| 作者： | 胡克荣；陈瑞；班玉娟；黄静 |
| AUTHORS： | HU Kerong，CHEN Rui，BAN Yujuan，HUANG Jing |
| 关键字： | 斑蝥酸钠；卡培他滨；药物相互作用；超高效液相色谱-串联质谱法 |
| KEYWORDS： | disodium cantharidinate； capecitabine； drug interaction； UPLC-MS/MS |
| 阅读数： | 72 次 |
| 本月下载数： | 4 次 |
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