CAJ | 학술논문

[目的]制备利福平PLGA纳米粒,考察其体外释放特性并评价该纳米粒在大鼠体内的药动学特征.[方法]以乳酸-羟基乙酸共聚物(PLGA)为载体,采用改良的自乳化溶剂蒸发法制备利福平PLGA纳米粒,考察其形态、粒径、包封率、载药量,采用透析袋法研究其体外释放特性,考察纳米粒经雾化吸入给药后在大鼠体内的药动学特征.[结果]制备的纳米粒外观呈球形或类球形,平均粒径为(128.73±4.07)nm,包封率和载药量分别为(65.84±1.08)%和(3.78±0.14)%.药动学结果显示,纳米粒组的tmax是溶液组6倍,Cmax比溶液组降低30%.[结论]采用改良的自乳化溶剂蒸发法可成功制备利福平PLGA纳米粒;经雾化吸入给药后,能显著减缓利福平进入体循环的速度并使药物全身暴露减少,具备进一步开发价值.
[목적]제비리복평PLGA납미립,고찰기체외석방특성병평개해납미립재대서체내적약동학특정.[방법]이유산-간기을산공취물(PLGA)위재체,채용개량적자유화용제증발법제비리복평PLGA납미립,고찰기형태、립경、포봉솔、재약량,채용투석대법연구기체외석방특성,고찰납미립경무화흡입급약후재대서체내적약동학특정.[결과]제비적납미립외관정구형혹류구형,평균립경위(128.73±4.07)nm,포봉솔화재약량분별위(65.84±1.08)%화(3.78±0.14)%.약동학결과현시,납미립조적tmax시용액조6배,Cmax비용액조강저30%.[결론]채용개량적자유화용제증발법가성공제비리복평PLGA납미립;경무화흡입급약후,능현저감완리복평진입체순배적속도병사약물전신폭로감소,구비진일보개발개치.
Objective]To prepare Rifampicin-loaded PLGA nanoparticles and evaluate the in vitro release behavior and the pharmacokinetics of the nano-particles in rats. [Method] The rifampicin nanoparticles with PLGA as carrier material were prepared by a modified spontaneous emulsification solvent dif-fusion method and characterized in terms of shape, particle size, encapsulation efficiency and drug loading. The in vitro release behavior was determined by dialysis method and the pharmacokinetics of the nanoparticles after nebulized inhalation in rats was evaluated. [Result] The optimal nanoparticles were spherical with the mean diameter of(128.73±4.07)nm. The encapsulation efficiency was(65.84±1.08)%and drug loading was(3.78±0.14)%. The phar-macokinetics results showed that tmax of nanoparticles group was increased by 6 times while the Cmax was nearly 30% lower than the solution group. [Con-clusion] Rifampicin-loaded PLGA nanoparticles were successful y prepared by a modified spontaneous emulsification solvent diffusion method. The nanoparticles with slower absorption after nebulized inhalation as wel as the less general exposure dose would be worthy of further study.