苏合香不同剂型在SD大鼠体内的口服药代动力学

Pharmacokinetics of styrax in different formulations after oral administration in SD rats

目的研究苏合香中主要成分肉桂酸在苏合香不同配伍和剂型在SD大鼠体内的药代动力学。方法 Sprague-Dawley(SD)大鼠分别口服苏合香(styrax)、二香活心软胶囊(erxianghuoxin softcapsules,简称ER)和二香亚微乳剂(erxiang submicron emulsion,简称EM),采用UPLC-MS/MS色谱法测定大鼠血浆中肉桂酸的浓度。用DAS2.0药动学软件处理血药浓度数据。用SPSS统计软件对所得的药动学数据进行显著性差异分析。结果大鼠口服Styrax、ER、EM三种制剂后,Styrax和ER中肉桂酸的药-时曲线符合单室模型,EM中肉桂酸的药-时曲线符合双室模型。口服Styrax和ER后,肉桂酸的药动学参数AUC0-t、AUC0-∞、ρmax、tmax、V无显著性差异(P>0.05),而口服EM后,ρmax、tmax显著性增加,V显著性减小(P<0.05),其他药动学参数无明显差异。结果表明降香油和苏合香合用后,苏合香中肉桂酸的药代动力学参数无显著性变化;制备成亚微乳剂后,提高了肉桂酸的血药浓度,减小了表观分布容积。结论降香油对苏合香主要成分肉桂酸的口服吸收无明显的促进作用。与一般制剂相比,亚微乳剂可以提高肉桂酸的血药浓度。

Objective To study the pharmacokinetics of styrax in different combinations and formulations after oral administration in SD rats.Methods Styrax,erxianghuoxin（traditional Chinese medicines）soft capsules（ER）and erxiang submicron emulsion（EM）were administrated orally to SD rats separately.The UPLC-MS/MS method was used to determine the concentrations of cinnamic acid in rat plasma.Pharmacokinetic parameters were obtained by the drug and statistics（DAS）version 2.0 software.Differences in pharmacokinetics of cinnamic acid were analyzed by the Student′s t-test using SPSS statistics software.Results After oral administration of styrax and ER,the pharmacokinetics parameters AUC0-t,AUC0-∞,ρmax,tmax,V of cinnamic acid showed no significant differences（P0.05）;but after oral administration of EM,ρmax and tmax increased,V decreased significantly（P0.05）,other parameters had no significant difference.After co-administration of styrax and lignum dalbergiae odoriferae oil,the pharmacokinetics parameters of the cinnamic acid showed no significant differences compared with that in styrax;but the sub-emulsion improved the cinnamic acid plasma concentrations and decreased the apparent volume of distribution.Conclusions Lignum dalbergiae odoriferae oil has no significant affection in promoting the oral absorption of cinnamic acid.Submicron emulsion can improve the plasma concentration of cinnamic acid.