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目的:考察冰片对川芎嗪经皮给药在大鼠体内药物动力学的影响。方法:制备基于微乳(microemulsion,ME)的川芎嗪-冰片复方经皮给药系统(TMP-Borneol-ME-TDDS)和川芎嗪单方经皮给药系统(TMP-ME-TDDS);将10只SD大鼠随机分为川芎嗪-冰片复方组和川芎嗪单方组,于不同时间采集血样,HPLC法测定川芎嗪的血药浓度;采用SPSS 18.0统计软件和DAS 2.0药动学处理软件对药物动力学结果进行分析。结果:TMP-Borneol-ME-TDDS组川芎嗪的血浆药物浓度-时间曲线下面积(AUC)大于TMP-METDDS组,TMP-Borneol-ME-TDDS组中川芎嗪的表观分布容积(V)小于TMP-ME-TDDS组,差异均具有统计学意义(P<0.05);TMP-Borneol-ME-TDDS的相对生物利用度为131.94%。结论:冰片可提高川芎嗪经皮给药的相对生物利用度,并有可能对其组织分布行为产生影响。
Objective: To investigate the effects of borneol on pharmacokinetics of ligustrazine in rats. Methods: TMP-Borneol-ME-TDDS and TMP-ME-TDDS were prepared based on microemulsion (ME). Ten Only SD rats were randomly divided into ligustrazine-borneol group and ligustrazine-unilateral group, blood samples were collected at different time, and HPLC was used to determine the concentration of ligustrazine. SPSS 18.0 statistical software and DAS 2.0 pharmacokinetic software Kinetic results were analyzed. Results: The plasma concentration-time curve (AUC) of TMP in the TMP-Borneol-ME-TDDS group was greater than that in the TMP-METDDS group. The apparent volume of distribution (V) of TMP in the TMP-Borneol-ME-TDDS group was less than TMP-ME-TDDS group, the differences were statistically significant (P <0.05); The relative bioavailability of TMP-Borneol-ME-TDDS was 131.94%. CONCLUSION: Borneol can increase the relative bioavailability of Ligustrazine transdermal delivery and may affect its tissue distribution behavior.