| 引用本文: | 庄星星,李萌,倪受东,苗仁华.丙戊酸钠和丙戊酸镁在大鼠体内的药动学研究[J].中国现代应用药学,2019,36(14):1787-1791. |
| ZHUANG Xingxing,LI Meng,NI Shoudong,Miao Renhua.Pharmacokinetic Comparison of Sodium Valproate and Magnesium Valproate in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(14):1787-1791. |
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| 摘要: |
| 目的 研究丙戊酸钠和丙戊酸镁在大鼠体内的药动学特征，评价其优势丙戊酸盐，为临床合理用药提供参考。方法 SD大鼠随机分为2组，分别灌胃给予丙戊酸钠片和丙戊酸镁片。于不同时间点眼眶取血。采用HPLC测定血清中丙戊酸的血药浓度，计算2种丙戊酸盐在大鼠体内的药动学参数，并比较2种丙戊酸盐之间的差异。结果 HPLC测定丙戊酸血药浓度方法专属性好，血清丙戊酸浓度在10.00~110.00 μg·mL-1内线性关系良好。精密度、稳定性和回收率均符合要求。丙戊酸钠和丙戊酸镁在大鼠体内的主要药动学参数：T1/2分别为（14.02±3.86） h和（12.11±1.95） h；Tmax分别为（3.67±0.58） h和（2.67±0.26） h；Cmax分别为（67.10±10.87）μg·mL-1和（75.67±12.94）μg·mL-1；AUC（0-t）分别为（969.86±72.08）μg·mL-1·h和（1 093.56±48.69）μg·mL-1·h；AUC（0-∞）分别为（1 178.10±185.29）μg·mL-1·h和（1 279.35±109.18）μg·mL-1·h；MRT0-t分别为（10.73±2.05） h和（13.06±3.24） h。Vd分别为（16.31±2.18） L和（23.47±2.19） L；CL分别为（0.056 3±0.009） L·h-1和（0.051 1±0.004） L·h-1。结论 与丙戊酸钠相比，丙戊酸镁在大鼠体内的药动学参数具有一定的优势，可能是一种更具有治疗优势的丙戊酸盐。 |
| 关键词: 丙戊酸钠 丙戊酸镁 药动学 高效液相色谱法 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.14.012 |
| 分类号:R917.101 |
| 基金项目:2016-2017年度安徽医科大学校科研基金项目（2017xkj063）；北京医学奖励基金会资助项目（YJHYXKYJJ-414） |
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| Pharmacokinetic Comparison of Sodium Valproate and Magnesium Valproate in Rats |
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ZHUANG Xingxing, LI Meng, NI Shoudong, Miao Renhua
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Department of Pharmacy, Chaohu Hospital of Anhui Medical University, Chaohu 238000, China
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| Abstract: |
| OBJECTIVE To investigate the differences of pharmacokinetic characteristics between sodium valproate and magnesium valproate in rats, and provide reference for clinical rational use of drugs. METHODS SD rats were randomly divided into 2 groups and gavaged with sodium valproate and magnesium valproate respectively. Blood was taken from the orbit at different time points. An HPLC method was established to determinate the blood concentration of valproic acid in serum. The pharmacokinetic parameters of sodium valproate and magnesium valproate in rats were calculated and compared. RESULTS The HPLC method showed a good specificity, and a good linearity was obtained over the range of 10.00-110.00 μg·mL-1. The mean recovery and precision values were favorable. The pharmacokinetic parameters of sodium valproate and magnesium valproate were as follows:T1/2 was (14.02±3.86)h and (12.11±1.95)h; Tmax was (3.67±0.58)h and (2.67±0.26)h; Cmax was (67.10±10.87)μg·mL-1 and (75.67±12.94)μg·mL-1; AUC(0-t) was (969.86±72.08) μg·mL-1·h and (1 093.56±48.69)μg·mL-1·h; AUC(0-∞) was (1 178.10±185.29) μg·mL-1·h and (1 279.35±109.18)μg·mL-1·h; MRT0-t was (10.73±2.05)h and (13.06±3.24)h; Vd was (16.31±2.18)L and (23.47±2.19)L; CL was (0.056 3±0.009)L·h-1 and (0.051 1±0.004)L·h-1. CONCLUSION Compared with sodium valproate, magnesium valproate showed some advantages in pharmacokinetics in rats, may be a more therapeutic advantage of valproic acid salt. |
| Key words: sodium valproate magnesium valproate pharmacokinetic HPLC |
