姜黄素自纳米乳分散后药物存在形式对肠吸收的影响  被引量:6

Effect of existing form of curcumin on intestinal absorption after Cur-SNEDDS dispersion

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作  者:陈绪龙 梁新丽 刘欢 周国平 赵国巍 温佳豪 廖正根 CHEN Xu-long;LIANG Xin-li;LIU Huan;ZHOU Guo-ping;ZHAO Guo-wei;WEN Jia-hao;LIAO Zheng-gen(Key Laboratory of Modern Preparation of TCM,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China;Jiangxi Institute for Drug Control,Nanchang 330029,China)

机构地区:[1]江西中医药大学,现代中药制剂教育部重点实验室,江西南昌330004 [2]江西省药品检验检测研究院,江西南昌330029

出  处:《中草药》2020年第18期4637-4645,共9页Chinese Traditional and Herbal Drugs

基  金:江西省一流学科项目(JXSYLXK-ZHYAO059);江西省卫生计生委科技计划项目(20181140)。

摘  要:目的研究姜黄素自纳米乳(Cur-SNEDDS)在人工胃肠液中分散后药物存在形式对肠吸收的影响。方法以姜黄素浓度-时间曲线的变化趋势,表示沉淀增长的变化,利用偏振光显微镜(PLMC)、HPLC、紫外全波长(UV)扫描、X-射线粉末衍射(XRD)、差示扫描量热仪(DSC)、红外光谱(FT-IR)、拉曼光谱及核磁共振氢谱(1H-NMR)对沉淀含量及存在形式进行研究,同时采用大鼠外翻肠囊模型,考察SNEDDS对姜黄素表观渗透系数(Papp)的影响。结果Cur-SNEDDS分散后产生的沉淀中姜黄素含量约为姜黄素原料药的95%,且未发生化学结构改变,但晶型发生了改变,产生了无定型沉淀,姜黄素在分散体系中发生了分子间相互作用,有氢键形成。与姜黄素原料药相比,Cur-SNEDDS显著提高了姜黄素体外释放的速度与程度,并增强了姜黄素在十二指肠、空肠、回肠及结肠吸收,Papp值分别增大了6.22、12.97、25.71、36.75倍。结论Cur-SNEDDS分散后改变了姜黄素原料药的晶体结构,以游离、无定型和晶体形式存在,显著提高了姜黄素的体外释放度和肠吸收。Objective To study the relationship between the drug form of curcumin self-nano-emulsion(Cur-SNEDDS) after being dispersed in artificial gastrointestinal fluid and intestinal absorption in rats. Methods The change trend of curcumin concentration-time curve was used to express the change of precipitation growth. The content and existing form of precipitation were studied by polarized light microscope(PLMC), HPLC, UV full-wavelength(UV) scanning, X-ray powder diffraction(XRD), differential scanning calorimeter(DSC), infrared spectrum(FT-IR), Raman spectrum and nuclear magnetic resonance hydrogen spectrum(1 H-NMR). At the same time, the rat valgus intestinal sac model was used to investigate the effect of SNEDDS on the apparent permeability coefficient(Papp) of curcumin. Results The content of curcumin in the precipitation produced by Cur-SNEDDS dispersion was about 95% of that of curcumin API, and the chemical structure did not change, but the crystal form changed, resulting in amorphous precipitation. Curcumin intermolecular interaction occurred in the dispersion system, and hydrogen bonds were formed. Compared with curcumin, Cur-SNEDDS significantly increased the release rate and degree of curcumin in vitro, and enhanced the absorption of curcumin in duodenum, jejunum, ileum and colon, and the Papp value increased by 6.22, 12.97, 25.71 and 36.75 times, respectively. Conclusion After Cur-SNEDDS dispersion, the crystal structure of curcumin is changed, which exists in free, amorphous and crystal form, so as to significantly improve the in vitro release and intestinal absorption of curcumin.

关 键 词:姜黄素 自纳米乳 人工胃肠液 存在形式 肠吸收 表观渗透系数 

分 类 号:R283.6[医药卫生—中药学]

 

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