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目的考察葛根素羧甲基壳聚糖微球的在体肠吸收特性。方法采用大鼠在体单向灌流法,以HPLC法测定葛根素的量,分别考察不同灌流体积流量、药物质量浓度、肠段对药物吸收的影响,并对比了葛根素原料药及载药微球的吸收特性。结果灌流体积流量对葛根素的吸收速率常数(Ka)和表观渗透系数(Papp)有显著性影响(P<0.05);葛根素的质量浓度对Ka和Papp无显著性影响(P>0.05);葛根素在空肠和回肠的Ka和Papp无显著性差异,但均显著大于在十二指肠处的值(P<0.05);载药微球在空肠的Ka和Papp值显著高于葛根素原料药(P<0.05)。结论葛根素羧甲基微球中葛根素的吸收机制为被动扩散,其在空肠和回肠段吸收较好,羧甲基壳聚糖作为载体能显著提高葛根素的吸收。
Objective To investigate the in vivo intestinal absorption of puerarin carboxymethyl chitosan microspheres. Methods The rats were subjected to one-way perfusion in vivo and the content of puerarin was determined by HPLC. The effects of different perfusion volume flow rate, drug concentration and intestinal segment on drug absorption were investigated. The effects of puerarin and drug loading Absorption characteristics of the ball. Results The perfusion volume flow had a significant effect on the absorption rate constant (Ka) and the apparent permeability coefficient (Papp) of puerarin (P <0.05). The concentration of Puerarin had no significant effect on Ka and Papp (P> 0.05) (P <0.05); Ka and Papp values of puerarin in jejunum and ileum were significantly higher than those in puerarin APIs (P <0.05). Conclusion The absorption mechanism of puerarin in puerarin carboxymethyl microspheres is passive diffusion, which is well absorbed in the jejunum and ileum. Carboxymethyl chitosan as a carrier can significantly increase the absorption of puerarin.