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目的:研究冠心Ⅱ号方不同制备方法对主要有效成分丹参素、阿魏酸在犬体内药代动力学过程的影响。方法:比格犬分别灌服冠心Ⅱ号全方汤剂(全方混煎制备)和全方有效组分重组复方(全方中各药材有效组分提取物的混合),应用液相色谱-质谱/质谱联用的方法(LC-MS/MS),检测药前及药后不同时间点时血浆中丹参素和阿魏酸的含量。利用药代动力学软件计算药代动力学参数,并进行组间比较。结果:对于丹参素,全方汤剂组达峰浓度(Cmax)和药时曲线下面积(AUC)均显著高于全方有效组分重组复方组(均P<0.05),达峰时间(Tmax)和清除半衰期(t1/2)与全方有效组分重组复方组无显著性差异;而对于阿魏酸,则全方汤剂组的Cmax显著低于全方有效组分重组复方组(P<0.05),Tmax较全方有效组分重组复方组显著延长(均P<0.05),AUC和t1/2与全方有效组分重组复方组比无统计学差异。结论:冠心Ⅱ号全方汤剂的丹参素入血浓度高、生物利用度高,但阿魏酸入血浓度低、达峰时间长,生物利用度低。即冠心Ⅱ号不同制备方法对方中不同有效成分药代动力学过程的影响不同,应结合药效学指标确定最佳制备方法。
Objective: To study the effects of different preparation methods of Guanxin Ⅱ on the pharmacokinetics of danshensu and ferulic acid in dogs. Methods: Beagle dogs were fed with Guanxin Ⅱ Decoction (all-round decoction preparation) and the all-round effective components recombinant compound (all medicinal ingredients in the mixture), the application of liquid chromatography Mass spectrometry / mass spectrometry (LC-MS / MS) was used to detect the contents of Danshensu and Ferulic acid in plasma at different time points before and after treatment. Pharmacokinetic parameters were calculated using pharmacokinetic software and compared between groups. Results: For Danshensu, the peak concentration (Cmax) and the area under the curve (AUC) of the Decoction group were significantly higher than that of the recombinant compound group (P <0.05). The peak time (Tmax ) And clearance half-life (t1 / 2) were not significantly different from those of the active compound in the whole recipe. For ferulic acid, the Cmax of the recipe was significantly lower than that of the compound recipe (P (P <0.05). Tmax was significantly longer than that of all the effective components (P <0.05). There was no significant difference between AUC and t1 / 2 and all the effective components in the compound treatment group. Conclusion: Danshensu decoction of Guanxin Ⅱ Decoction decoction has high blood penetration and bioavailability, but the concentration of ferulic acid into the blood is low, the peak time is long, and the bioavailability is low. The different preparation methods of Guanxin Ⅱ different pharmacokinetic effects of different active ingredients process different should be combined with pharmacodynamic indicators to determine the best preparation.