摘要
目的研究磷酸川芎嗪(tetramethylpyrazine phosphate,TMPP)凝胶膏剂、片剂及注射剂在大鼠体内药动学差异。方法将18只SD大鼠随机分为凝胶膏剂组、口服给药组及静脉注射组,每组各6只。采用高效液相色谱法(HPLC)内标法测定不同时间点3组大鼠体内血药浓度,采用DAS 3.0软件计算各组药动学参数,并采用t检验和Wilcoxon秩和检验进行统计分析。结果 TMPP凝胶膏剂的AUC_(0-t)分别是片剂及注射剂的1.4倍和2.6倍,t_(1/2)分别是片剂及注射剂的8.6倍和4.1倍,平均滞留时间、达峰时间与片剂和注射剂相比,差异有统计学意义(P<0.05),血药浓度释放平稳。结论 TMPP凝胶膏剂能够降低血药浓度波动,具有一定缓释作用,值得进一步研究开发。
Objective To study the pharmacokinetic differences of tetramethylpyrazine phosphate(TMPP gel ointment,tablets and injections in rats.Methods A total of 18 SD rats were randomly divided into the gel ointment group,oral administration group and intravenous injection group,and each group consisted of 6 rats.The rats' plasma concentrations of the three groups at different time points were determined by the internal standard method of high performance liquid chromatography(HPLC).The pharmacokinetic parameters of each group were calculated by the software DAS 3.0 and the statistical analysis was performed by t test and Wilcoxon rank sum test.Results The AUC_(0-t) of TMPP gel ointment was 1.4 times and 2.6 times as much as that of tablets and injections respectively,and its t_(1/2) was 8.6 times and 4.1 times as much as that of tablets and injections respectively.The mean residence time and peak time of TMPP gel ointment were significantly different with the steady release of the plasma concentration when compared with those of tablets and injections(P<0.05).Conclusion TMPP gel ointment could reduce the fluctuation of plasma concentrations with a certain sustained-release effect,so it is worthy of further research and development.
引文
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