丁香苦苷单体与丁香苦苷PLGA纳米粒药动学比较

Comparative study on pharmacokinetics of syringopicroside monomer and syringopicroside PLGA-nanoparticles

测定大鼠血浆中含丁香苦苷的量,并对具有抗乙肝病毒的丁香苦苷单体和丁香苦苷PLGA纳米粒进行大鼠体内药动学比较研究.采用色谱柱:Diamonsil C18(5μm,250×4.6 mm)流动相为甲醇-水(50∶50,V/V);流速为1.0 mL/min;检测波长为221 nm;进样量为20μL.测定Wistar大鼠尾静脉注射丁香苦苷后不同时间血浆中的药物质量浓度.给药剂量相同(10 mg/mL)时,丁香苦苷PLGA溶液的T1/2α和T1/2β值是丁香苦苷溶液的1.23倍和2.25倍.AUC值是丁香苦苷溶液的3.09倍,血浆清除率约为丁香苦苷溶液的1/3.经过数据拟合发现丁香苦苷单体与丁香苦苷PLGA纳米粒在大鼠体内过程均符合二室模型,载药纳米粒给药后,使丁香苦苷能在体内较长时间维持较高的血药质量浓度,起到一定的缓释作用.

This paper determined the content of syringopicroside in the plasma of rats and to make a comparative study on pharmacokinetics of syringopicroside monomer with anti -HBV function and syringopicroside PLGA -nanoparticles in the vivo of rats .Chromatographic col-umn：Diamonsil C18（5 μm,250 ×4.6 mm）mobile phase： methanol-water（50∶50,V/V）;flow rate：1.0 mL/min;detected wavelength：221 nm;sample amount：20 μL.The concen-tration of syringopicroside in the plasma of Wistar rats was measured at different time points after intravenous injection .The T1/2αand T1/2βvalues of syringopicroside polylactic -co-gly-colic acid-nanoparticles were 2.25 times and 1.23 times of that of the syringopicroside so-lution respectively with the same dose （ 10 mg/mL ） .The AUC value of syringopicroside polylactic-co-glycolic acid-nanoparticles was 3.09 times of that of syringopicroside solu-tion and the plasma clearance rate of syringopicroside polylactic -co-glycolic acid-nanop-articles was one third of that of syringopicroside .Through the data fitting method , it was found that both syringopicroside monomer and syringopicroside polylactic -co-glycolic acid-nanoparticles in rats conformed to the two -compartment model .The SYR-PLGA-NP changed the feature of pharmacokinetics in the body of rats by making the syringopicroside＆amp;nbsp;remain relatively high concentration in plasma for a longer period ,having a slow -releasing effect.