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目的 为改善阿米卡星肺部靶向性和渗透性差以及混悬液剂型在使用便利性和储运稳定性方面的不足,研制阿米卡星脂质体吸入粉雾剂,并初步评价其理化特性。方法 采用逆相蒸发法制备阿米卡星脂质体,并通过喷雾干燥技术将其转化为干粉。对制得粉体的外观形态、密度、休止角、粒径分布、水分含量、吸湿性、装置排空率、空气动力学性质、溶解性以及复溶后的包封率保留率、粒径和Zeta电位进行表征。结果 制备的阿米卡星脂质体吸入粉雾剂收率为(78.21±3.92)%;呈规则球形或类球形颗粒;压缩度为(24.18±0.004)%,休止角为41°;空气动力学直径(Da)为(2.67±0.11)μm;水分含量为(4.13±0.05)%;在相对湿度为25%时几乎无吸湿性;装置排空率为(98.48±0.67)%;中位空气动力学直径为(5.09±0.09)μm,几何标准偏差为(1.69±0.03),细小颗粒组分分数为(41.34±0.82)%;产品溶解性良好,复溶后脂质体包封率保留率为(87.04±0.44)%,脂质体平均粒径有所增大,Zeta电位略有下降,但总体稳定。结论 采用逆相蒸发法结合喷雾干燥技术可制备出符合吸入粉雾剂质量要求的阿米卡星脂质体吸入粉雾剂,为后续体内药效学研究及产业化开发奠定坚实的基础。
Abstract：Objective To improve the poor pulmonary targeting and permeability of amikacin,as well as the limitations in convenient use,storage and transportation stability of its suspension dosage form,to develop an amikacin liposome dry powder inhalation and evaluate its physicochemical properties.Methods Amikacin liposomes were prepared by the reverse-phase evaporation method and were converted to dry powder by spray drying technology.The powders were characterized from morphology,density,angle of repose,particle size distribution,moisture content,hygroscopicity,device emptying rate,aerodynamic properties,solubility and the retention of encapsulation efficiency,particle size and Zeta potential after the reconstitution.Results The prepared dry powder inhalation showed a yield of(78.21±3.92)%.The powder presented regular spherical or near-spherical particles,with a compressibility index at(24.18±0.004)%,and an angle of repose of 41°.The aerodynamic diameter was(2.67±0.11) μm.The moisture content was(4.13±0.05)%,and the powder exhibited almost negligible hygroscopicity at 25% relative humidity.The device emptying rate was(98.48±0.67)%,mass median aerodynamic was(5.09±0.09) μm,geometric standard deviation was(1.69±0.03),and the fine particle fraction was(41.34±0.82)%.The dry powder inhalation displayed good solubility.After the reconstitution,the liposomes retained an encapsulation efficiency of(87.04±0.44)%,the average particle size of liposomes slightly increased,and the Zeta potential slightly decreased,maintaining overall stability.Conclusion The combination of reverse-phase evaporation method and spray drying technology helps prepare amikacin liposome dry powder inhalation that meets the quality criteria and lays a solid foundation for subsequent in vivo pharmacodynamic studies and industrialization development.
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基本信息:
中图分类号:R943
引用信息:
[1]陈中会,陈斌.阿米卡星脂质体吸入粉雾剂的制备及初步理化性质评价[J].中南药学,2026,24(06):22-28.
基金信息:
“重大新药创制”国家科技重大专项基金资助项目(No.2017ZX09201004); 广东省“珠江人才计划”引进第六批创新创业团队资助项目(No.2016ZT06Y229)
2026-04-14
2026-04-14
2026-04-14