【摘要】 合成并表征了聚酰胺-胺(PAMAM)G5.0树枝状聚合物,平衡透析法制备氟尿嘧啶-聚酰胺-胺复合物(5-Fu-PAMAM),研究PAMAM对5-Fu的结合能力;高效液相色谱法研究大鼠经口给予5-Fu混悬液和5-Fu-PAMAM复合物的药代动力学。结果显示,当5-Fu与PAMAM G5.0的物质的量比在250附近达到最大结合,制备的复合物粒径为(30.2±4.9)nm。大鼠经口给予复合物组的Ka,cmax均较混悬液组有显著增加(P<0.01),AUC0-∞是混悬液组的1.37倍。研究表明PAMAM能显著增加5-Fu的口服吸收,提高5-Fu制剂的生物利用度。更多还原

【Abstract】 Polyamidoamine(PAMAM) G5.0 dendrimers were synthesized and characterized.The complex of PAMAM with fluorouracil(5-Fu) was prepared by equilibrium dialysis,and the binding capacity of PAMAM to 5-Fu was studied.The pharmacokinetics in rats receiving oral dosing of 5-Fu suspension and complex were investigated by HPLC.The maximum combination of complex occurred when molar ratio of 5-Fu and PAMAM G5.0 was about 250.The average size of complex was(30.2±4.9) nm.Oral pharmacokinetics in rats showed that the Ka,cmax of the complex had a significant increase(P<0.01),and AUC0-∞ was 1.37 times to that of the suspension group.These results indicated that PAMAM can increase the absorption of 5-Fu significantly and improve its oral bioavailability.更多还原