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QIAO Hong-zhi, LI Juan, WANG Yang, LI Qiang. Preparation of fluorouracil-polyamidoamine complex and its pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2011, 42(6): 510-515.
Citation: QIAO Hong-zhi, LI Juan, WANG Yang, LI Qiang. Preparation of fluorouracil-polyamidoamine complex and its pharmacokinetics in rats[J]. Journal of China Pharmaceutical University, 2011, 42(6): 510-515.

Preparation of fluorouracil-polyamidoamine complex and its pharmacokinetics in rats

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  • 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.
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