中国中药杂志

2019, v.44(23) 5143-5150

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炮制辅料羊脂油对宝藿苷Ⅰ-胆酸盐自组装胶束形成与吸收的影响
Effect of processing excipient suet oil on formation and absorption of baohuoside Ⅰ-bile salt self-assembled micelles

顾慧敏;孙娥;李杰;侯健;贾晓斌;
GU Hui-min;SUN E;LI Jie;HOU Jian;JIA Xiao-bin;Third Clinical Medicine School,Nanjing University of Chinese Medicine;Key Laboratory of New Drug Delivery System of Chinese Materia Medica,Jiangsu Provincial Academy of Chinese Medicine;School of Chinese Materia Medica,China Pharmaceutical University;

摘要(Abstract):

淫羊藿传统炮制方法为羊脂油炙,具有增强淫羊藿温肾助阳的功效。该文创新性从药剂学角度,基于淫羊藿黄酮自组装胶束体内形成机制,探讨炙淫羊藿炮制辅料羊脂油的增效机制。选取炙淫羊藿代表性黄酮成分宝藿苷Ⅰ,通过测定胶束粒径、电位及透射电镜观察胶束形态,并采用Caco-2细胞模型、大鼠在体肠灌流模型以及体内血药浓度法,研究羊脂油对宝藿苷Ⅰ-胆酸盐自组装胶束形成与吸收的影响。淫羊藿活性黄酮宝藿苷Ⅰ能够在脱氧胆酸钠的作用下自组装形成胶束,加入炮制辅料羊脂油后,胶束粒径降低、电位绝对值升高、多分散系数PDI降低、包封率及载药量均有显著提高,显示羊脂油能明显改善胶束在体内的形成。加入羊脂油后,宝藿苷Ⅰ在Caco-2单层细胞模型中的转运及大鼠在体肠灌流模型中4段肠道(十二指肠、空肠、回肠、结肠)的渗透系数较宝藿苷Ⅰ-胆酸盐胶束组提高,而体内药动学研究表明加入羊脂油形成胶束后宝藿苷Ⅰ在大鼠体内的生物利用度明显改善,进一步证明炮制辅料羊脂油能够促进宝藿苷Ⅰ自组装胶束的形成与吸收,从而发挥其增效作用。
The fried method with suet oil,which can strengthen the effect of Epimedium in warming kidney and enhancing Yang,has been widely used in the processing of Epimedium in traditional Chinese medicine. Based on the formation mechanism of Epimedium flavonoids self-assembled micelles in vivo,the synergistic mechanism of processing excipient suet oil was investigated in this paper from the perspective of pharmaceutics. Baohuoside Ⅰ,as representative component of processed Epimedium,was selected as model drug.Average size and zeta potential were measured and the morphology of micelles was observed under transmission electron microscopy. Caco-2 monolayer cell model,rat intestinal perfusion model and in vivo serum drug concentration method were established to investigate the effect of suet oil on the formation and absorption of the baohuosideⅠ bile salt self-assembled micelles. Baohuoside Ⅰ can form selfassembled micelles under the action of sodium deoxycholate. While,adding suet oil into the baohuoside Ⅰ-bile salt micelles( BSDOC) can make it form a more stable system with a smaller average size,higher Zeta potential,lower polydispersity index( PDI) value,significantly improved encapsulation efficiency and drug loading,indicating that suet oil could significantly improve the micelle formation in vivo. In addition,the permeability coefficient of baohuoside Ⅰ in Caco-2 monolayer cells and the four intestinal organs( duodenum,jejunum,ileum and colon) was increased and the oral bioavailability was also improved after adding the suet oil to BS-DOC.All the results demonstrated that the suet oil can promote the formation and absorption of baohuoside Ⅰ self-assembled micelles,so as to enhance its synergistic effects.

关键词(KeyWords): 羊脂油;自组装胶束;宝藿苷Ⅰ;Caco-2细胞;大鼠在体肠灌流;生物利用度
suet oil;self-assembled micelles;baohuoside Ⅰ;Caco-2 monolayer cell model;rat intestinal perfusion model;oral bioavailability

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81274088,81503253);; 江苏省青年医学重点人才项目(QNRC2016635)

作者(Author): 顾慧敏;孙娥;李杰;侯健;贾晓斌;
GU Hui-min;SUN E;LI Jie;HOU Jian;JIA Xiao-bin;Third Clinical Medicine School,Nanjing University of Chinese Medicine;Key Laboratory of New Drug Delivery System of Chinese Materia Medica,Jiangsu Provincial Academy of Chinese Medicine;School of Chinese Materia Medica,China Pharmaceutical University;

Email:

DOI: 10.19540/j.cnki.cjcmm.20190916.311

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