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目的制备大黄酸聚乳酸纳米粒,并考察其在大鼠体内的药动学特征,以期提高大黄酸口服生物利用度。方法以聚乳酸为载体材料,采用改良的自乳化溶剂扩散法制备大黄酸聚乳酸纳米粒;透射电镜观察纳米粒的形态;激光粒度仪考察粒径和Zeta电位;超速离心法测定其包封率及载药量;透析袋法研究其体外释药特性;以大黄酸混悬液为对照组,进行大鼠口服大黄酸聚乳酸纳米粒的药动学研究。结果纳米粒外观呈圆形或类圆形,平均粒径为(134.37±3.61)nm,Zeta电位为(-18.41±0.07)mV,包封率和载药量分别为(60.37±1.52)%和(1.32±0.09)%;体外释药符合Higuchi方程;大鼠口服大黄酸混悬液和纳米粒后,ρmax分别为(5.788±0.15)和(11.607±0.56)mg.L-1,tmax分别为(0.193±0.01)和(1.102±0.13)h,AUC0→t分别为(8.077±2.98)和(34.583±3.93)mg.h.L-1,t1/2β分别为(3.319±0.23)和(21.721±6.13)h。结论聚乳酸纳米粒可显著改善大黄酸的药动学行为,有效提高其口服生物利用度。
Objective To prepare rhein polylactic acid nanoparticles and study its pharmacokinetics in rats in order to improve the oral bioavailability of rhein. Methods Polylactic acid was used as carrier material to prepare rhein polylactic acid nanoparticles by modified self-emulsifying solvent diffusion method. The morphology of nanoparticles was observed by transmission electron microscopy. The particle size and zeta potential were measured by laser particle size analyzer. The entrapment efficiency And drug loading; dialysis bag method in vitro release characteristics; rhein suspension as a control group, rat oral rhein polylactic acid nanoparticles pharmacokinetic study. Results The nanoparticles showed a round or round shape with an average diameter of (134.37 ± 3.61) nm and a zeta potential of (-18.41 ± 0.07) mV. The entrapment efficiency and drug loading were (60.37 ± 1.52)% and (1.32 ± 0.09)%, respectively. The in vitro drug release was in accordance with the Higuchi equation. After oral administration of rhein and nanoparticles, the ρmax were (5.788 ± 0.15) and (11.607 ± 0.56) mg.L-1, respectively (0.193 ± 0.01) and (1.102 ± 0.13) h, AUC0 → t were (8.077 ± 2.98) and (34.583 ± 3.93) mg.hL-1 respectively, and t1 / 2β were (3.319 ± 0.23) and (21.721 ± 6.13 h. Conclusion Polylactic acid nanoparticles can significantly improve the pharmacokinetics of rhein and effectively improve its oral bioavailability.