三七总皂苷微乳在家兔眼部的药动学研究

Pharmacokinetics of total Panax notoginseng saponins microemulsions in rabbit eyes

目的研究三七总皂苷微乳在家兔眼部的药动学。方法微透析探针植入家兔眼前房室内,灌流平衡1 h,耳缘静脉注射微乳和注射用血栓通(冻干)。然后,LC-MS/MS法测定不同时间点(0.5、1、1.5、2、2.5、3、3.5、4、4.5、5、5.5、6、7、8 h)人参皂苷Rg1、三七皂苷R1含有量。结果微乳组人参皂苷Rg1、三七皂苷R1的Cmax、AUC0~8 h、AUC0~∞高于注射用血栓通(冻干)组(P<0.01),Vz/F、CL/F降低(P<0.05,P<0.01),这2种成分生物利用度分别为(290.62±63.64)%、(587.78±148.07)%。结论三七总皂苷微乳可提高药物在家兔眼部的生物利用度,为其进一步研发奠定了基础。

AIM To study the pharmacokinetics of total Panax notoginseng saponins microemulsions in rabbit eyes.METHODS After the implantation of microdialysis probe into the anterior chamber of rabbits and 1-hour perfusion balance, the ear edge was intravenously injected either with microemulsions or Xueshuantong Freeze-dried Powder. Subsequently, LC-MS/MS was adopted in the content determination of ginsenoside Rg1 and notoginsenoside R1at different time points(0.5,1,1.5,2,2.5,3,3.5,4,4.5,5,5.5,6,7,8 h).RESULTS The microemulsions group demonstrated higher Cmax, AUC0-8 h and AUC0-∞ of ginsenoside Rg1 and notoginsenoside R1 than the Xueshuantong Freeze-dried Powder group(P<0.01), along with decreased Vz/F and CL/F(P<0.05, P<0.01). The bioavailabilities of ginsenoside Rg1 and notoginsenoside R1 reached(290.62±63.64)% and(587.78±148.07)%, respectively.CONCLUSION Total Panax notoginseng saponins microemulsions can enhance drug bioavailability in rabbit eyes, which can lay a foundation for the further research and development.