TranscutolP对痛宁凝胶中延胡索乙素在大鼠体内的药代动力学影响

Effects of Transcutol P on pharmacokinetics of Tetrahydropulmatine in Tongning gel in rats

关键词:  延胡索乙素|痛宁凝胶|UPLC-MS/MS|药代动力学

Key words:  Tetrahydropulmatine|Tongning gel|UPLC-MS/MS|pharmacokinetics

摘要:

[目的] 建立一种快速灵敏的超高效液相色谱-串联质谱（UPLC-MS/MS）方法测定大鼠血浆中延胡索乙素含量，研究含7%单乙基二甘醇油醚（TransP）的痛宁凝胶在大鼠体内的药代动力学过程，考察其透皮吸收促进效果。[方法] 采用血药浓度法，UPLC-MS/MS测定大鼠体内痛宁凝胶中延胡索乙素含量，同时与空白痛宁凝胶体内药代动力学参数进行比较。[结果] 7% Trans P组的T_max、C_max与空白对照组相比差异具有显著性（p<0.05），药时曲线下面积AUC_{（0→24h）}和AUC_{（0→∞）}与空白对照组相比差异具有显著性（p<0.05）。[结论] 应用UPLC-MS/MS技术测定痛宁凝胶中延胡索乙素的血药浓度，药代动力学参数表明7%TransP组促渗效果明显优于空白对照组，可进一步应用于痛宁凝胶制剂中。

Abstract:

[Objective] To establish a highly sensitive UPLC-MS/MS method for the quantification of plasma Tetrahydropalmatine in rats, investigate the effects of 7%Transcutol P on the pharmacokinetics of Tetrahydropulmatine in Tongning gel in rats and study its promoting effect for transdermal absorption. [Methods] Using a method of UPLC-MS/MS to measure plasma concentration of Tetrahydropulmatine at different time after transdermal administration a pharmacokinetics comparison with the results of control group was performed. [Results] The pharmacokinetic parametersT_max and C_max between these two groups of 7%Transcutol Pand control were statistically significant (p<0.05). The AUC(0→24 h) and UC(0→∞) values were higher than those of the control solution, respectively with statistically significant difference (P<0.05). [Conclusion] This UPLC-MS/MS method is successfully applied in the determining of plasma Tetrahydropalmatine concentration in rats. The pharmacokinetic parameters have indicated that the enhancing effect of 7% Transcutol P is significant and can be further used in the preparation of Tongning gel.