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采用超声乳化均质法制备包裹ZL-004(1)的PLGA纳米粒(1-NP),其体外释放明显高于原药。以单向灌流法考察1-NP的大鼠在体肠吸收性质。结果表明,1-NP在大鼠各肠段均有吸收,且吸收系数(K a)与渗透系数(P eff)均显著大于其原药(P<0.01)。1-NP在小肠段(十二指肠、空肠和回肠)的K a与P eff均显著大于结肠(P<0.01),且各肠段吸收量随1浓度(5~20?g/ml)的增加而增加。
PLGA nanoparticle (1-NP) encapsulating ZL-004 (1) was prepared by phacoemulsification and homogenization. The in vitro release of PLGA nanoparticles was significantly higher than that of the original drug. One-way perfusion method was used to investigate the intestinal absorption of 1-NP in rats. The results showed that 1-NP was absorbed in all intestine segments of rats, and the absorption coefficient (K a) and permeability coefficient (P eff) were significantly higher than those of the original drug (P <0.01). The K a and P eff of 1-NP in the small intestine segment (duodenum, jejunum and ileum) were significantly higher than those in the colon (P <0.01), and the absorption of each segment varied with the concentration of 5-20 μg / Increase and increase.