西那普肽脂质体气溶胶体外评价

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制备并评价了西那普肽脂质体。冻干前后脂质体的平均粒径、ζ电位和包封率分别为556.5和651.2 nm、-56.8和-41.6mV、83.8%和70.4%。冻干脂质体中残余水分含量为1.48%,氯仿和甲醇的残留量低于中国药典2015年版的限度要求。利用Pari雾化器将用生理盐水复溶后的西那普肽脂质体雾化,形成气溶胶,再分别采用双级撞击器、新一代撞击器(next generation impactor,NGI)、飞行时间(time-of-flight,TOF)空气动力学粒径谱仪对气溶胶的体外沉积性质进行考察。结果表明,双级撞击器、NGI和TOF测得的体外沉积性质相似;双级撞击器和NGI测得空气动力学粒径小于6.4 um的脂质体气溶胶中的西那普肽含量占总药量的比例为50.86%和43.87%,NGI和TOF测得的空气动力学质量中位径(mass median aerodynamic diameter,MMAD)值为3.09和2.81 um。这些结果提示西那普肽脂质体气溶胶能够在肺部沉积,具有较好的开发应用前景。 Cinamon peptide liposomes were prepared and evaluated. The average particle size, zeta potential and entrapment efficiency of the liposomes before and after lyophilization were 556.5 and 651.2 nm, -56.8 and -41.6 mV, 83.8% and 70.4%, respectively. Residual moisture content in the freeze-dried liposomes was 1.48%, and the residues of chloroform and methanol were lower than the limits of the Chinese Pharmacopoeia 2015 edition. The paclitaxel liposomes reconstituted with saline were atomized by Pari atomizer to form aerosols, which were then treated with two stage impactor, next generation impactor (NGI), time of flight ( time-of-flight, TOF) aerodynamic particle size spectroscopy was used to investigate the in vitro deposition of aerosols. The results showed that the in vitro deposition properties measured by two-stage impactor, NGI and TOF were similar. The content of cinacalcin in the liposomal aerosols with aerodynamic size less than 6.4 μm measured by two-stage impactor and NGI accounted for The ratios of doses were 50.86% and 43.87%, respectively, and the mass median aerodynamic diameters (MMAD) measured by NGI and TOF were 3.09 and 2.81 um. These results suggest that cinnarizine liposomal aerosol can be deposited in the lungs and has a good prospect of development and application.
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