咖啡酸苯乙酯固体分散体的制备
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摘要
目的制备咖啡酸苯乙酯固体分散体。方法以PVP K30为载体,溶剂法制备固体分散体;以咖啡酸苯乙酯溶解度、溶出度为评价指标,筛选药物(咖啡酸苯乙酯)-载体(PVP K30)比例。然后,通过透射电镜(SEM)、差示扫描量热(DSC)、X射线衍射(XRD)对固体分散体进行鉴定分析。结果药物-载体比例为1∶10时,咖啡酸苯乙酯溶解度、溶出度最高,并以无定形状态分散在载体中。结论固体分散体技术可明显提高咖啡酸苯乙酯溶解度、溶出度。
AIM To prepare caffeic acid phenethyl ester solid dispersions. METHODS For the solid dispersions prepared by solvent method with PVP K30 as a carrier,drug( caffeic acid phenethyl ester)-carrier( PVP K30) ratio was screened with the solubility and dissolution rates of caffeic acid phenethyl ester as evaluation indices. Subsequently,scanning electron microscope( SEM),differential scanning calorimetry( DSC) and X-ray diffraction( XRD) were adopted in the identification and analysis of solid dispersions. RESULTS Dispersed in an amorphous state,caffeic acid phenethyl ester demonstrated the highest solubility and dissolution rates at the drugcarrier ratio of 1 ∶ 10. CONCLUSION Solid dispersion technology can obviously improve the solubility and dissolution rates of caffeic acid phenethyl ester.
AIM To prepare caffeic acid phenethyl ester solid dispersions. METHODS For the solid dispersions prepared by solvent method with PVP K30 as a carrier,drug( caffeic acid phenethyl ester)-carrier( PVP K30) ratio was screened with the solubility and dissolution rates of caffeic acid phenethyl ester as evaluation indices. Subsequently,scanning electron microscope( SEM),differential scanning calorimetry( DSC) and X-ray diffraction( XRD) were adopted in the identification and analysis of solid dispersions. RESULTS Dispersed in an amorphous state,caffeic acid phenethyl ester demonstrated the highest solubility and dissolution rates at the drugcarrier ratio of 1 ∶ 10. CONCLUSION Solid dispersion technology can obviously improve the solubility and dissolution rates of caffeic acid phenethyl ester.
引文
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[9]邓莉.咖啡酸苯乙酯衍生物的设计合成及生物活性测定[D].重庆:西南大学,2011.
[10]王洁,金刚,薛健飞,等.水难溶性药物硝苯地平固体分散体的制备及体外溶出度研究[J].吉林化工学院学报,2014,31(9):31-33.
[11]冯春来,丁洋洋,李文静,等.漆黄素固体分散体的制备[J].中成药,2017,39(12):2503-2507.
[12]国家药典委员会.中华人民共和国药典:2015年版四部[S].北京:中国医药科技出版社,2015:通则0921.
[2]马伟.蜂胶中咖啡酸苯乙酯的提取及抗Ⅱ型糖尿病作用研究[D].西安:陕西科技大学,2016.
[3]杨九凌,祝晓玲,李成文,等.咖啡酸及其衍生物咖啡酸苯乙酯药理作用研究进展[J].中国药学杂志,2013,48(8):577-582.
[4]龚频,文和,王兰,等.咖啡酸苯乙酯对糖尿病大鼠肾的保护作用[J].中国临床药理学杂志,2016,32(11):1021-1023,1030.
[5]王秀芳,翟嵩,党双锁.咖啡酸苯乙酯的药理作用及机制研究进展[J].国外医学(医学地理分册),2010,31(3):187-190.
[6] Kumar M,Kaur D,Bansal N. Caffeic acid phenethyl ester(CAPE)prevents development of STZ-ICV induced dementia in rats[J]. Pharmacogn Mag,2017,13(Suppl 1):S10-S15.
[7] Bansal N,Kaur D,Kumar M. Caffeic acid phenethylester abrogates intracerebroventricular streptozocin-induced memory deficits in rats[J]. Alzheimers Dement,2016,12(7):P653.
[8] Du Q,Hao C Z,Gou J,et al. Protective effects of p-nitro caffeic acid phenethyl ester on acute myocardial ischemiareperfusion injury in rats[J]. Exp Ther Med,2016,11(4):1433-1440.
[9]邓莉.咖啡酸苯乙酯衍生物的设计合成及生物活性测定[D].重庆:西南大学,2011.
[10]王洁,金刚,薛健飞,等.水难溶性药物硝苯地平固体分散体的制备及体外溶出度研究[J].吉林化工学院学报,2014,31(9):31-33.
[11]冯春来,丁洋洋,李文静,等.漆黄素固体分散体的制备[J].中成药,2017,39(12):2503-2507.
[12]国家药典委员会.中华人民共和国药典:2015年版四部[S].北京:中国医药科技出版社,2015:通则0921.