树枝状聚合物PAMAM葛根素复合物的制备及肠吸收研究

Preparation and Intestinal Absorption of Poly(Amidoamine)(PAMAM) Dendrimer-Puerarin Complex

制备树枝状聚合物G3,G4,G5 PAMAM葛根素复合物,研究其在大鼠不同肠段的吸收情况.采用大鼠离体外翻肠囊法、高效液相色谱法测定葛根素大鼠小肠吸收参数,以未加PAMAM组作为空白对照组,计算累积透过量及表观通透系数(Papp).葛根素在空肠及回肠段吸收明显,表观通透系数分别为(2.98±0.22)×10-6(、3.94±0.30)×10-6 cm.s-1,PAMAM与葛根素形成复合物能增加葛根素大鼠小肠累积透过量及表观通透系数.其中G5 PAMAM对葛根素促进作用最为显著,葛根素空肠、回肠段表观通透系数分别增加了2.78、2.22倍(P<0.05).PAMAM能有效促进葛根素大鼠小肠吸收.

G3,G4 and G5 poly（amidoamine）（PAMAM） dendrimers-puerarin complexes are prepared and on intestinal absorption of puerarin in rats is studied.The reverted gut sac experiments are performed and the concentrations of puerarin permeated are determined by HPLC,puerarin solution without PAMAM dendrimers used as control.The cumulative amount of puerarin permeated and the permeability coefficient（Papp） of puerarin are calculated.The results show that puerarin is mainly absorbed in jejunum and ileum with the permeability coefficient of（2.98±0.22）×10-6 and（3.94±0.30）×10-6 cm·s-1,respectively.Puerarin is complexed with PAMAM dendrimer which can increase the cumulative amount of puerarin permeated and the permeability coefficient of puerarin.G5 PAMAM dendrimer shows the best absorption enhancement among the three dendrimers,the permeability enhancement ratio（ER） in jejunum and ileum is 2.78 and 2.22 times,compared to control,respectively.It is concluded that PAMAM dendrimer is an effective intestinal penetration enhancer and promising to improve the oral bioavailability of puerarin.