摘要
为了提高槲皮素(1)的溶出度和口服生物利用度,文章采用微流控技术制备1纳米晶(QNCs)。考察了1溶液流速、反溶剂相流速、1浓度等因素对QNCs粒径的影响,并采用TEM、DSC法、PXRD法进行表征。结果表明,微流控技术可通过调节溶液流速和1浓度有效控制QNCs粒径。所制备的QNCs为无定型态,粒径为(79.23±0.45)nm,PDI为(0.144±0.008)。随后进行了在pH 7.4 PBS中的体外溶出试验;并以大鼠为模型,灌胃给予QNCs或1原料药,以探究QNCs的体内药动学行为。研究表明,QNCs的体外溶出速率和口服生物利用度均显著优于1原料药,提示微流控技术在提高难溶性药物生物利用度方面具有良好的应用前景。
In an effort to enhance the solubility and oral absorption of quercetin(1),this study employed microfluidic technology to formulate quercetin nanocrystals(QNCs).The research investigated the influences of 1 solution flow rate,anti-solvent phase flow rate,and 1 concentration on the particle size of QNCs.The QNCs were then characterized by a variety of techniques including TEM,DSC,and PXRD.The findings revealed that the particle size of the QNCs could be effectively managed by adjusting the solution flow rate and 1 concentration through microfluidic technology.The formulated QNCs exhibited an amorphous form with a particle size of(79.23±0.45)nm and a polydispersity index(PDI)of(0.144±0.008).Then,an in vitro dissolution test in pH 7.4 PBS was carried out.In addition,a comparative pharmacokinetic study was conducted in rats,in which either QNCs or bulk quercetin were administered orally.Moreover,the QNCs demonstrated an improved dissolution rate in vitro and superior oral bioavailability compared to the bulk drug.These results suggest that microfluidic technology offers significant potential for improving the bioavailability of drugs with poor solubility.
作者
郑光艳
吴文丽
刘泽梅
车鑫
王立红
ZHENG Guangyan;WU Wenli;LIU Zemei;CHE Xin;WANG Lihong(Guizhou University of Traditional Chinese Medicine,Guiyang 550025)
出处
《中国医药工业杂志》
EI
CAS
CSCD
2024年第4期519-526,共8页
Chinese Journal of Pharmaceuticals
基金
贵州省自然科学基金项目(贵州省科技基金-ZK[2021]-524)
贵州省卫健委科技基金项目(GZWKJ2022-233)。
关键词
纳米晶
微流控技术
槲皮素
溶出度
药动学
nanocrystal
microfluidic technology
quercetin
dissolution
pharmacokinetics
