中文摘要：

目的：研究比阿培南对丙戊酸钠在大鼠红细胞内、外分布的影响。方法：取大鼠随机分为对照组（丙戊酸钠50mg·kg^-1）和实验组（比阿培南15mg·kg^-1＋丙戊酸钠50mg·kg^-1），每组6只，禁食12h，麻醉固定后分别在股静脉和动脉行套管插入术，经股静脉给予相应药物，给药前注射肝素，采用荧光偏振免疫分析法考察给药后180min内各组大鼠血浆和全血中丙戊酸钠的浓度，并用非房室模型法估算药动学参数。结果：与对照组比较，实验组大鼠全血中丙戊酸钠浓度无明显变化，血浆中浓度有所降低，由此推算试验组大鼠红细胞内的丙戊酸钠浓度有所增加。实验组与对照组血浆中丙戊酸钠的AUC0-3h分别为（134．89±18．88）、（189．35±34．76）μg·h·mL^-1，t1/2分别为（0．95±0．04）、（1．13±0．16）h，2组间AUC0-3h和t1/2均存在显著性差异（P〈0．05）。结论：比阿培南能够明显增加丙戊酸钠在大鼠红细胞内的分布．同时降低大鼠血浆中丙戊酸钠的浓度。

英文摘要：

OBJECTIVE： To investigate the effect of biapenem on the distribution of valproic acid （VPA） in inner and outer sides of erythrocytes of rats. METHODS： Rats were randomly assigned into control group （VPA 50 mg·kg^-1） and trial group （biapenem 15 mg·kg^-1＋VPA 50 mg·kg^-1） with 6 rats in each group. Rats were fasting 12 hours. After the rats were anesthetized, cannulation （closed catheter system） was made at femoral vein and artery. Heparin was injected before giving medicine via femoral vein. The blood and plasma VPA levels were determined by fluorescence polarization immunoassay （FPIA） 180 min after administration. Pharmacokinetic parameters were calculated using non-compartment model. RESULTS： Compared with control group, the VPA level in blood sample of trial group had no obvious change while VPA level in plasma sample decreased. Then we estimated that VPA level in erythrocytes increased. The pharmacokinetic parameters of VPA in trial group vs. control group were as follows： AUC0-3h： （134.89 ± 18.88） μg·h·mL^-1 vs.（189.35 ±34.76） μg·h·mL^-1; h/2：（0.95 ±0.04） h vs.（1.13 ±0.16） h. The results showed that the AUC0-3 h and tt/2 had significant difference between 2 groups （P〈0.05）. CONCLUSION： Biapenem increases the distribution of VPA in erythrocytes, while it markedly reduces VPA levels in plasma.