阿魏酸钠胃漂浮缓释片Beagle犬体内药动学研究

Pharmacokinetic Study of Sodium Ferulate Gastric Floating Sustained-release Tablets in Beagle Dogs

关键词:  阿魏酸钠  胃漂浮缓释片  高效液相色谱法  药动学  血药浓度

Key words:  sodium ferulate  gastric floating sustained-release tablets  HPLC  pharmacokinetics  plasma concentration

摘要:

目的 建立高效液相法测定Beagle犬血浆中阿魏酸钠浓度，考察单次给药后阿魏酸钠胃漂浮缓释片和阿魏酸钠普通片的药动学行为，以及考察阿魏酸钠胃漂浮缓释片的缓释效果。方法 采用双周期交叉实验设计，分别服用阿魏酸钠胃漂浮缓释片和阿魏酸钠普通片(分别相当于阿魏酸钠100 mg)，以甲醇-10%三氯乙酸(1∶1)作为蛋白沉淀剂，按血浆-蛋白沉淀剂(3∶2)沉淀血浆，离心后取上清液进样分析。采用3P97药动学软件进行药动学参数的考察。结果 胃漂浮缓释片达峰时间(t_max)明显延长，达峰浓度(C_max)也明显降低，实验中未发现突释现象，达到了很好的缓释效果。结论 本实验血浆处理方法简单，方法的回收率高，测得阿魏酸钠胃漂浮缓释片具有明显的缓释特征。

Abstract:

OBJECTIVE To establish an HPLC method to determinate sodium ferulate in Beagle dogs and compare the pharmacokinetic pararmeters between sodium ferulate gastric floating sustained-release tablets and sodium ferulate tablets by single dose in Beagle dogs. And to demonstrate the controlled release effect of sodium ferulate gastric floating sustained-release tablets. METHODS Use a standard two period cross-over design, the plasma concentration of sodium ferulate was determined by HPLC after a single oral dosage(equal to 100 mg sodium ferulate). Methanol-10% TCA (1∶1) was used as a protein precipitant agent with a ratio of plasma-protein precipitant agent(3∶2). After centrifugation, the supernatant was analyzed and the pharmacokinetic parameters were obtained by 3P97 statistical analysis software. RESULTS Sodium ferulate gastric floating sustained-release tablets indicated a good controlled release profiles with prolonged t_max, lower C_max and no burst effect. CONCLUSION The HPLC method meets the requirement of sensitivity, specific and recovery and is capable to determine sodium ferulate in Beagle dogs. Sodium ferulate gastric floating sustained-release tablets indicates a marked sustained release profiles.