二苯乙烯苷及其β-环糊精包合物在大鼠体内药代动力学研究*

Pharmacokinetics of stilbene glycoside and its β-cyclodextrin inclusion in rats

关键词:  二苯乙烯苷  β-环糊精  高效液相  药代动力学

Key words:  stilbene glycoside (THSG)  β-cyclodextrin  HPLC  pharmacokinetics

摘要:

[目的]研究二苯乙烯苷(THSG)单体及其β-环糊精包合物大鼠灌胃后药代动力学行为。[方法]SD大鼠分别灌胃THSG单体及其β-环糊精包合物,HPLC-UV测定血浆样品中THSG含量,采用DAS1.0软件计算主要药代动力学参数。[结果]测定方法准确可靠,符合生物样品测定要求。THSG单体及其β-环糊精包合物的Cmax分别为(0.24±0.09)、(1.16±0.80)mg/L;AUC分别为(11.50±3.97)、(32.24±7.77)μg/(L·min),经t检验两者差异有统计学意义(P<0.05)。[结论]β-环糊精的包合作用可通过促进THSG的吸收及减缓其消除,有效的提高THSG的体内生物利用度。

Abstract:

[Objective] The pharmacokinetics characteristics of stilbene glycoside (THSG) and itsβ-cyclodextrin inclusion after oral administration in rats were studied.[Methods] After the administration,blood samples were collected at regular times from orbital venous plexus.The plasma concentration of THSG was determined quantitatively by HPLC-UV.[Results] The HPLC-UV method was available for analysing THSG in plasma and met the requirements of biological sample analysis.The pharmacokinetic parameters were calculated by using DAS(Drug and Statistics)VER 1.0 software.The fast absorption of THSG contributed to a higher Cmax of complex and that of free THSG[(1.16±0.80)mg/L vs.(0.24±0.09)mg/L for complex and free THSG,respectively,P<0.05].It was also found that AUC was dramatically higher for complex than that of free THSG [(32.24±7.77)mg(L·min) vs.(11.50±3.97)mg/(L·min) for complex and free THSG,respectively,P<0.05].[Conclusion] Pharmacokinetic studies of THSG/β-cyclodextrin complex in rats have indicated that the complex has higher bioavailability compared to free THSG,suggesting that the complex may exhibit better therapeutic efficacy.