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以α-细辛脑为模型药物,单甲氧基聚乙二醇-聚乳酸共聚物(m PEG-PLA)为载体,采用快速膜乳化法制备经鼻给药载药微粒。所得微粒表面光滑、外观圆整,平均粒径为360 nm,多分散系数(PDI)为0.030,载药量及包封率分别为(11.5±0.045)%(n=3),(86.34±0.11)%(n=3)。X射线衍射和差示扫描量热结果均表明α-细辛脑是以无定形或分子态存在于m PEG-PLA载体中,而不同于简单的物理混合物。模拟人鼻腔内环境体外释放试验研究结果显示α-细辛脑原料药在102 h即释放接近94%,释放较快,符合一级动力学模型(R~2=0.981 9),而m PEG-PLA载药微粒释放只达54%,具有缓释作用,符合Riger-Peppas模型(R~2=0.967 9,n=0.630 2),为非Fick扩散,释放由药物的扩散和骨架溶蚀双重控制,为后续经鼻给药的体内药代动力学研究提供依据。
Taking a-Asarone as a model drug and monomethoxy polyethylene glycol-polylactic acid copolymer (m PEG-PLA) as carrier, nasal drug-loaded particles were prepared by rapid membrane emulsification. The average particle size was 360 nm, the polydispersity (PDI) was 0.030, the drug loading and entrapment efficiency were (11.5 ± 0.045)% (n = 3), (86.34 ± 0.11 )% (n = 3). Both X-ray diffraction and differential scanning calorimetry results show that α-asarone is present in the m PEG-PLA carrier in an amorphous or molecular state unlike the simple physical mixture. Simulated human nasal environment in vitro release test results showed that α-Asarone brain drug release at 102 h was nearly 94% release faster, in line with the first-order kinetic model (R ~ 2 = 0.981 9), and m PEG- The release of PLA was only 54% with sustained release, which was in accord with Riger-Peppas model (R ~ 2 = 0.967 9, n = 0.630 2), which was non-Fick diffusion controlled by drug diffusion and skeleton erosion. It provided the basis for the pharmacokinetics of nasal administration in vivo.