Box-Behnken响应面法优化吲哚美辛固体脂质纳米粒处方 点击下载
论文标题: Box-Behnken响应面法优化吲哚美辛固体脂质纳米粒处方
英文标题:
中文摘要: 目的:优化吲哚美辛固体脂质纳米粒处方。方法:以吲哚美辛为模型药物、山嵛酸甘油酯为油相、泊洛沙姆188和聚乙二醇-12-羟基硬脂酸酯为乳化剂,以浊度、包封率、载药量为指标,采用Box-Behnken响应面法优化处方中油相用量、乳化剂-油相比例、药物-油相比例。采用扫描电镜、差示扫描热分析(DSC)表征固体脂质纳米粒的理化性质。结果:最优处方的油相用量为0.91%,乳化剂-油相比例为1 ∶ 1,药物-油相比例为1 ∶ 5;所制吲哚美辛固体脂质纳米粒的浊度为1 025~1 030 NTU,包封率为98.94%~99.08%,载药量为2.43%~2.46%,粒径为181.5~182.3 nm,多分散性指数(PDI)为0.340~0.341(n=3);DSC结果显示吲哚美辛不是以结晶状态存在于固体脂质纳米粒中。结论:成功筛选出最优处方,制得吲哚美辛固体脂质纳米粒。
英文摘要: OBJECTIVE: To optimize the formulation of indomethacin-loading solid lipid nanoparticle (SLN). METHODS: Using indomethacin as model drug, glyceryl behenate as oil phase, poloxamer 188 and polyethylene glycol-12-hydroxystearic acid as emulsifier, with turbidity, entrapment efficiency and drug loading amount as index, Box-Behnken response surface methodology was used to optimize the amount of oil phase, emulsifier-oil phase ratio, drug-oil phase ratio. The physicochemical properties of SLNs were characterized by SEM and DSC. RESULTS: The optimal formulation was as follows as oil phase of 0.91%, emulsifier- oil ratio of 1 ∶ 1, drug-oil phase ratio of 1 ∶ 5. The turbidity, entrapment efficiency and drug loading amount of prepared nanoparticle were 1 025-1 030 NTU, 98.94%-99.08%, 2.43%-2.46%, respectively; particle size and polydispersity index (PDI) were 181.5- 182.3 nm and 0.340-0.341 (n=3). The results of DSC showed that indomethacin was not present in crystalline state dispersed into SLNs. CONCLUSIONS: The optimal formulation is screened successfully, and indomethacin-loaded SLNs have been prepared.
期刊: 2016年第27卷第22期
作者: 陈凯,李收,金凯,赵晶,郝吉福
英文作者: CHEN Kai,LI Shou,JIN Kai,ZHAO Jing,HAO Jifu
关键字: 吲哚美辛;固体脂质纳米粒;Box-Behnken响应面法;优化处方
KEYWORDS: Indomethacin; Solid lipid nanoparticle; Box-Behnken response surface methodology; Formulation optimization
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