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期 刊 ：中国中药杂志 2006年 31卷 05期 页码：376.

关键词：芎归散；超临界CO2萃取物；固体脂质纳米粒；熔融超声分散法；体外释药；

Keywords:Xionggui powder, supercritical carbon dioxide fluid extraction, solid lipid nanoparticles, hot dispersion-ultrasonic technique, drug release in vitro,

摘 要 ：目的:研究芎归散超临界CO₂萃取物固体脂质纳米粒的制备和体外释药特性。方法:采用熔融超声分散法制备芎归散超临界CO₂萃取物固体脂质纳米粒混悬液,以包封率为考察指标,采用正交试验筛选最佳处方,并考察其物理化学性质;采用动态透析法考察其在不同介质中的释药特性。结果:最佳处方为大豆卵磷脂∶泊洛沙姆F-68:单甘酯=5∶2∶1,包封率为96.3%,所得纳米粒为类球形实体粒子,平均粒径为245.8 nm,平均zeta电位为-33.5 mV,在生理盐水中的释药特性符合Weibull模型,在pH7.4磷酸盐缓冲液(40%乙醇)中的释药特性符合单指数模型。结论:芎归散超临界CO₂萃取物固体脂质纳米粒的制备工艺基本可行,药物释放较完全。

Abstract:Objective: To study the preparation of solid lipid nanoparticles loaded with Xionggui powder-supercritical carbon dioxide fluid extraction and their evaluation in vitro release.Method: To prepare solid lipid nanoparticles(SLN) loaded with Xionggui powder-supercritical carbon dioxide fluid extraction(XG-CO₂-SFE) using a hot dispersion-ultrasonic technique,establishing the best prescription of XG-CO₂-SFE-SLN through orthogonal design methods using entrapment efficiency of nanoparticles as index,and investigating their physicochemical characterizations.The invro release action of SLN was studied in different dissolution mediums using dynamic dialyse method.Result: The best prescription was: phospholipid∶F-68∶stearie acid glyceride=5∶2∶1,the entrapment efficiency of nanoparticles was 96.3%,and the results revealed the nanoparticles were sphere like with the mean size of 245.8 nm,the mean Zeta potential was-33.5 mV.The in vitro release meet to Weibull distribution in physiological brine and to single-index model in pH 7.4 phosphate liquid(40% EtOH).Conclusion: The preparation method of the XG-CO₂-SFE-SLN was appropriate,and the XG-CO₂-SFE-SLN was released completely.

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