姜油树脂自微乳载药体系的设计、表征及体外释放研究
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摘要
目的对姜油树脂自微乳载药体系进行设计及形态学表征,并进行体外释放的研究。方法以包封率和透光率为评价指标,通过单因素实验考察混合方式、混合温度、混合速度、混合时间以及姜油树脂与EO比例对姜油树脂自微乳制备工艺的影响;采用正交试验法对制备工艺参数进行优化,以综合加权评分法分析测定结果。测定姜油树脂自微乳进行粒径、Zate电位、表观形态、包封率和载药量并研究其体外释放。结果通过对姜油树脂自微乳载药体系的设计,得粒径为79. 5±5. 30 nm,Zeta电位为-30. 85±0. 52 m V,包封率为90. 33%±0. 20%,载药量为2. 5446±0. 03 mg·m L~(-1)的优化姜油树脂自微乳,形态学表征结果显示:制备的姜油树脂自微乳的分散性、稳定性良好,且12 h释放度达90. 58%±1. 65%。结论制得的姜油树脂自微乳粒径小、包封率较高、理化性质稳定,具有良好的药物释放性能,该结果对更好地开发利用姜油树脂有重要的意义。
OBJECTIVE To design ginger oleoresin self-micromulsifying drug delivery system( SMEDDS) and to characterize it by morphological and in vitro release study. METHODS The effects of the mixing mode,mixing temperature,mixing speed,mixing time and ratio of ginger oleoresin and EO on the preparation of ginger oleoresin self-emulsified microemulsion were investigated using Single factor experiment. The preparation parameters were optimized by Orthogonal test method,and the results were analyzed by Comprehensive weighted scoring method. The particle size,Zeta potential,apparent morphology,encapsulation efficiency,drug loading and in vitro release of ginger oleoresin self-emulsified microemulsion were studied. RESULTS Through the design of the ginger oleoresin SMEDDS,the obtained particle size was 79. 50 ± 5. 30 nm; the Zeta potential was-30. 85 ± 0. 52 m V; the encapsulation efficiency was 90. 33% ± 0. 20%; and the drug loading was 2. 5446 ± 0. 03 mg·m L~(-1).The optimized self-emulsifying microemulsion of ginger oleoresin was showed that it had good dispersibility and stability,and the release rate was 90. 58% ± 1. 65%. CONCLUSION The prepared ginger oleoresin self-emulsified microemulsion has small particle size,high encapsulation efficiency,stable physical and chemical properties,and the good drug release performance. This result has important practical significance for the better development of ginger oleoresin.
OBJECTIVE To design ginger oleoresin self-micromulsifying drug delivery system( SMEDDS) and to characterize it by morphological and in vitro release study. METHODS The effects of the mixing mode,mixing temperature,mixing speed,mixing time and ratio of ginger oleoresin and EO on the preparation of ginger oleoresin self-emulsified microemulsion were investigated using Single factor experiment. The preparation parameters were optimized by Orthogonal test method,and the results were analyzed by Comprehensive weighted scoring method. The particle size,Zeta potential,apparent morphology,encapsulation efficiency,drug loading and in vitro release of ginger oleoresin self-emulsified microemulsion were studied. RESULTS Through the design of the ginger oleoresin SMEDDS,the obtained particle size was 79. 50 ± 5. 30 nm; the Zeta potential was-30. 85 ± 0. 52 m V; the encapsulation efficiency was 90. 33% ± 0. 20%; and the drug loading was 2. 5446 ± 0. 03 mg·m L~(-1).The optimized self-emulsifying microemulsion of ginger oleoresin was showed that it had good dispersibility and stability,and the release rate was 90. 58% ± 1. 65%. CONCLUSION The prepared ginger oleoresin self-emulsified microemulsion has small particle size,high encapsulation efficiency,stable physical and chemical properties,and the good drug release performance. This result has important practical significance for the better development of ginger oleoresin.
引文
[1]孙凤娇,李振麟,钱士辉,等.干姜化学成分和药理作用研究进展[J].中国野生植物资源,2015,34(3):34-37
[2]Wei QY,Ma JP,Cai YJ,et al.Cytotoxic and apoptotic activities of diarylheptanoids and gingerol-related compounds from the rhizome of Chinese ginger[J].Ethnopharmacol,2005,102(2):177-184.
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[4]王娇,李葆林,何晓明,等.新型自乳化给药系统研究进展[J].中国现代应用药学,2016,33(1):119-121.
[5]屈雅丽.难溶性西药制剂中自微乳化释药的应用研究[J].中国医药指南,2013,11(34):338-339.
[6]何琳,罗丽青,欧丽红,等.灯盏花素固体自微乳剂的制备及体外溶出度的评价[J].华西药学杂志,2012,27(5):540-543.
[7]张菁楠,胡艳秋,张军威,等.Box-Behnken响应面法优化交泰丸有效部位口服自微乳的制备方法[J].华西药学杂志,2018,33(4):358-363.
[8]张建立,李公春.超临界CO2萃取姜油树脂的工艺研究[J].安徽农业科学,2011,39(16):9827-9828,9830.
[2]Wei QY,Ma JP,Cai YJ,et al.Cytotoxic and apoptotic activities of diarylheptanoids and gingerol-related compounds from the rhizome of Chinese ginger[J].Ethnopharmacol,2005,102(2):177-184.
[3]周长征.自微乳化药物传递系统的研究进展[J].内蒙古中医药,2012,31(10):122.
[4]王娇,李葆林,何晓明,等.新型自乳化给药系统研究进展[J].中国现代应用药学,2016,33(1):119-121.
[5]屈雅丽.难溶性西药制剂中自微乳化释药的应用研究[J].中国医药指南,2013,11(34):338-339.
[6]何琳,罗丽青,欧丽红,等.灯盏花素固体自微乳剂的制备及体外溶出度的评价[J].华西药学杂志,2012,27(5):540-543.
[7]张菁楠,胡艳秋,张军威,等.Box-Behnken响应面法优化交泰丸有效部位口服自微乳的制备方法[J].华西药学杂志,2018,33(4):358-363.
[8]张建立,李公春.超临界CO2萃取姜油树脂的工艺研究[J].安徽农业科学,2011,39(16):9827-9828,9830.
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