辣椒素固体分散体的处方工艺优化及表征
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篇名: 辣椒素固体分散体的处方工艺优化及表征
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摘要: 目的:制备辣椒素固体分散体,优化其处方工艺,并进行表征。方法:采用熔融法,以泊洛沙姆188(P188)或聚乙二醇4000(PEG4000)为载体制备辣椒素固体分散体。以60 min的累积释放度为指标,采用正交试验设计优化载体种类、药载比及搅拌时间,并进行验证;考察所制辣椒素固体分散体在温度40 ℃、相对湿度75%条件下0、30、180 d内的稳定性及X射线衍射法(XRD)分析是否有新峰出现;利用差示扫描量热法(DSC)、XRD对其进行物相表征。结果:以P188-PEG4000为载体,辣椒素-P188- PEG4000的质量比为1 ∶ 5 ∶ 3,搅拌20 min,所制辣椒素固体分散体体外60 min的累积释放度为84.6%(n=3),180 d内稳定性良好[含量RSD为3%(n=3),XRD显示未出现新峰];物相表征证明,辣椒素以无定型状态或分子状态高度分散于载体中。结论:通过此工艺制备了辣椒素固体分散体并且在60 min可体外溶出80%以上,稳定性好,工艺简便可行。
ABSTRACT: OBJECTIVE: To prepare Capsaicin solid dispersion, to optimize its formulation and characterize the dispersion. METHODS: Capsaicin solid dispersion was prepared by melting method using P188 or PEG4000 as carrier. Using 60 min accumulative dissolution rate in vitro as index, orthogonal test was used to optimize type of carrier, drug ratio and stirring time. Validation test was conducted. The stability of Capsaicin solid dispersion within 0, 30, 180 d was investigated at 40 ℃ under the relative humidity of 75%, and X-ray diffraction (XRD) was used to analyze whether there were peaks. Capsaicin solid dispersion was characterized by differential scanning calorimetry (DSC) and XRD. RESULTS: The optimized formula included P188-PEG4000 as carrier, capsaicin-P188-PEG 4000 mass ratio of 1 ∶ 5 ∶ 3, stirring for 20 min. Accumulative dissolution rate in vitro of Capsaicin solid dispersion was 84.6% within 60 min (n=3), and the preparation kept stable within 180 d [RSD of content was 3% (n=3); XRD showed that there was no peak]. The phase characteristics showed that capsaicin was highly dispersed in the amorphous or molecular state in carrier. CONCLUSIONS: The optimized technology can be used to prepare Capsaicin solid dispersion, and improves more than 80% dissolution rate in vitro at 60 min. It is stable, simple and feasible.
期刊: 2019年第30卷第11期
作者: 游国叶,樊轻亚,杜晶,李会娜
AUTHORS: YOU Guoye,FAN Qingya,DU Jing,LI Huina
关键字: 辣椒素;固体分散体;处方优化;释放度;表征
KEYWORDS: Capsaicin; Solid dispersion; Formula optimization; Dissolution rate; Characterization
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