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采用乳化-溶剂蒸发法制得了平均粒径(108.5±31)nm、电位(-16.97±0.27)mV、包封率(37.25±1.38)%和载药量(2.07±0.12)%的载长春西汀(1)聚乙二醇-聚乳酸纳米粒。体外释药试验表明,1纳米粒在pH 7.4磷酸盐缓冲液(含0.5%Tween-80)和大鼠空白血浆中初始4 h的释药速度均较迅速,4 h后则缓慢释药;并且在血浆中的释药速度略慢。采用LC-MS/MS法测定大鼠单剂量尾静脉注射1纳米粒及市售1注射液后血浆中的1。结果表明,1纳米粒组和1注射液组相比,t1/2和MRT0→t延长,AUC0→t和AUC0→∞增加,总清除率减少。1纳米粒的绝对生物利用度是1注射液的30倍。
The average particle size (108.5 ± 31) nm, potential (-16.97 ± 0.27) mV, entrapment efficiency (37.25 ± 1.38)% and drug loading (2.07 ± 0.12)% were obtained by emulsion- (1) Polyethylene glycol-polylactic acid nanoparticles. In vitro drug release tests showed that 1 NP released rapidly in initial pH 7.4 phosphate buffer (containing 0.5% Tween-80) and in blank plasma for 4 h and released slowly after 4 h; and In the plasma release rate slightly slower. LC-MS / MS method was used to determine the concentration of 1 in the tail vein of a rat injected with 1 nanoparticle and 1 commercially available injection. The results showed that the t1 / 2 and MRT0 → t prolongs, the AUC0 → t and AUC0 → ∞ increase in 1 nanoparticle group and 1 injection group, and the total clearance rate decreases. 1 The absolute bioavailability of nanoparticle is 30 times that of 1 injection.