二甲基姜黄素固体分散体的制备及表征
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摘要
分别以聚乙二醇(PEG)4000、PEG6000、聚乙烯吡咯烷酮(PVPK30)、泊洛沙姆188为载体材料,采用熔融法或溶剂蒸发法制备难溶性药物二甲基姜黄素(1)固体分散体。通过考察其体外溶出行为,筛选出最佳载体以及最佳药载比。利用傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、扫描电镜(SEM)对制品进行表征。结果表明,上述4种载体材料制备的1固体分散体均可显著提高1的溶出速度和程度;其中,以PVPK30为载体材料、药载比为1∶10的制品改善溶出的效果最好,5min溶出率达到83%以上。FTIR、XRD及SEM分析显示,药物以无定形形式存在于载体中。
The solid dispersions(SDs) of dimethylcurcumin with polyethylene glycol(PEG) 4000, PEG6000, and poloxamer 188 as carriers by fusion method and with polyvinylpyrrolidone(PVP K30) as carriers by solvent evaporation method were respectively prepared. The in vitro dissolution behaviors of four SDs were investigated to screen the optimal carrier and drug to carrier ratio. Then the optimal SDs were characterized by Fourier transform infrared spectroscopy(FTIR), X-ray diffraction(XRD), and scanning electron microscopy(SEM). The results showed that the dissolution rates of all prepared dimethylcurcumin solid dispersions were significantly improved compared with the bulk drug and physical mixture. Among them, the solid dispersion prepared with PVP K30, in which the ratio of dimethylcurcumin to PVP K30 was 1∶10, displayed the optimal dissolution behavior, with cumulative dissolution more than 83% in 5 minutes. The results of FTIR, XRD and SEM analyses showed that dimethylcurcumin was dispersed in the PVP K30 in an amorphous form.
The solid dispersions(SDs) of dimethylcurcumin with polyethylene glycol(PEG) 4000, PEG6000, and poloxamer 188 as carriers by fusion method and with polyvinylpyrrolidone(PVP K30) as carriers by solvent evaporation method were respectively prepared. The in vitro dissolution behaviors of four SDs were investigated to screen the optimal carrier and drug to carrier ratio. Then the optimal SDs were characterized by Fourier transform infrared spectroscopy(FTIR), X-ray diffraction(XRD), and scanning electron microscopy(SEM). The results showed that the dissolution rates of all prepared dimethylcurcumin solid dispersions were significantly improved compared with the bulk drug and physical mixture. Among them, the solid dispersion prepared with PVP K30, in which the ratio of dimethylcurcumin to PVP K30 was 1∶10, displayed the optimal dissolution behavior, with cumulative dissolution more than 83% in 5 minutes. The results of FTIR, XRD and SEM analyses showed that dimethylcurcumin was dispersed in the PVP K30 in an amorphous form.
引文
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[10]沈松,吴琳,戚雪勇,等.不同载体固体分散体对尼群地平和硝苯地平的增溶效果考察[J].中国医药工业杂志,2013,44(12):1249-1252.
[11]何丹,杨林,范琦.丹参酮ⅡA固体分散体的制备及溶出度考察[J].中国医院药学杂志,2009,29(8):649-651.
[12]靖博宇,王志远,李燕,等.非洛地平固体分散体的制备和体外溶出度考察[J].沈阳药科大学学报,2010,27(3):185-190.
[13]巫剑峰,邱佩斯,陈彦雯,等.丹参提取物固体分散体的制备与溶出特性[J].中国医院药学杂志,2010,30(11):900-905.
[2]PULIDO-MORAN M,MORENO-FERNANDEZ J,RAMIREZ-TORTOSA C,et al.Curcumin and health[J].Molecules,2016,21(3):264.
[3]ARSHAD L,HAQUE M A,ABBAS BUKHARI S N,et al.An overview of structure-activity relationship studies of curcumin analogs as antioxidant and anti-inflammatory agents[J].Future Med Chem,2017,9(6):605-626.
[4]戴汉松,单堂云,高艳,等.姜黄素的提取及其甲基化研究[J].天然产物研究与开发,2008,20(2):254-256.
[5]周舒文,徐德锋,杨幸群,等.脂质体的粒径大小对二甲基姜黄素抗癌能力的影响研究[J].常州大学学报:自然科学版,2016,28(6):14-17.
[6]LI R,XU D F,YANG X Q,et al.Preparation and stability studies of dimethyl curcumin niosomes[J].J Chin Pharm Sci,2017,26(4):265-270.
[7]王凤飞,章晓茜,曹聪,等.高效液相色谱-质谱联用测定大鼠全血中二甲基姜黄素的浓度[J].中国药学杂志,2015,50(22):1996-1999.
[8]徐德锋.一种二烷基姜黄素的制备方法:中国,103254051A[P].2013-08-21.
[9]徐文杰,朱颖,孙冬梅.布渣叶总黄酮固体分散体的制备及体外溶出度测定[J].中国医院药学杂志,2015,35(2):119-125.
[10]沈松,吴琳,戚雪勇,等.不同载体固体分散体对尼群地平和硝苯地平的增溶效果考察[J].中国医药工业杂志,2013,44(12):1249-1252.
[11]何丹,杨林,范琦.丹参酮ⅡA固体分散体的制备及溶出度考察[J].中国医院药学杂志,2009,29(8):649-651.
[12]靖博宇,王志远,李燕,等.非洛地平固体分散体的制备和体外溶出度考察[J].沈阳药科大学学报,2010,27(3):185-190.
[13]巫剑峰,邱佩斯,陈彦雯,等.丹参提取物固体分散体的制备与溶出特性[J].中国医院药学杂志,2010,30(11):900-905.