目的 比较丹参酮II^A（TSN）脂微球与丹参酮II^A磺酸钠（STS）注射液iv给药后在大鼠体内的药动学行为及在小鼠组织中分布的差异。方法 建立测定大鼠血浆和小鼠组织中TSN和STS的RP-HPLC方法。比较大鼠及小鼠分别单次iv TSN脂微球5.40 mg/kg和STS注射液7.27 mg/kg（均相当于18.35 μmol/kg）后，TSN和STS在大鼠血浆中的水平和小鼠多个组织中的量，并对结果进行药动学拟合和统计学分析。结果 TSN脂微球在大鼠体内的生物利用度（AUC^0～∞）、达峰浓度（C^max）是STS注射液的2.14、2.22倍，清除率（CL）、表观分布容积（V）和滞留时间（MRT）也显著低于STS注射液（P＜0.05、0.01），其他药动学参数均没有显著性差异；TSN和STS在小鼠组织中分布的检测结果表明，TSN在心、肝、脾、肺、肾组织中的AUC^0～∞是等物质的量STS的1.94、0.11、0.98、1.65、0.28倍，且TSN在脑组织中的量显著增加，STS在脑组织中未检测到。结论 等物质的量剂量下TSN与STS的药动学行为、组织分布具有显著差异，TSN脂微球比STS注射液生物利用度高、达峰浓度高，且显著靶向分布于心、脑、肺组织。

Objective To study the absorption and transport characteristic of paeoniflorin (PF), oxypaeoniflorin (OP), benzoylpaeoniflorin (BP), tetraacetylpaeoniflorin (TP), pentaacetylpaeoniflorin (PP), and pentacacetylalbiflorin (PA) in human colon adenocarcinoma cell line Caco-2 cell monolayer model. Methods The Caco-2 cell monolayers were used as an intestinal epithelial cell model. The permeability of the tested compounds from apical (AP) side to basolateral (BL) side or from BL side to AP side was evaluated. The concentration of the tested compounds was measured by HPLC coupled with UV detector. The transport parameters and apparent permeability coefficients (P_app) were calculated, and the P_app values were compared with the reported values for model compounds, Propranolol and Atenolol. Results The P_app values of PF in the bi-directional transport and atenolol were at the quantitative degree of 10^?7 cm/s. Whereas those of OP, BP, TP, PP, and PA were between atenolol and propranolol used as a control substance for low and high permeability, respectively. The absorption and transport of the tested compounds were concentration-dependent at the concentration range of 10－200 μmol/L for PF, OP, and BP, 10－150 μmol/L for TP and PA, and 10－100 μmol/L for PP. Conclusion The six tested compounds could be absorbed across the intestinal epithelial cells by passive diffusion mechanism. PF is poorly absorbed compound and OP, BP, TP, PP, and PA are moderately absorbed compounds. BP has a role to promote atenolol uptake transporters in Caco-2 cell monolayer model.

“十二五”国家科技支撑计划资助项目（2011BAI07B08）