摘要
研究一种新型共聚物负载辅酶Q10形成纳米悬浮剂能够增加CoQ10的水溶性,并且提高其口服生物利用度。本研究以槲皮素—木聚糖(QT-Xylan)共聚物偶联为基础进行合成,采用高剪切均质法进一步包载辅酶Q10,形成了一种新型载药纳米悬浮剂。采用单因素实验设计,并以粒径大小作为单因素实验的考察条件,影响其粒径大小的因素包括高压均质压力、高压均质次数、共聚物浓度、共聚物与CoQ10的质量比4个因素,并进行一系列体外实验评价。当均质压力为60 MPa,均质次数为7次,共聚物浓度为1 mg·mL^-1,共聚物与CoQ10的质量比为1∶1,是纳米悬浮剂的最佳制备工艺,此时粒径大小为166.7 nm。在最佳工艺条件下,在体外溶出实验中,包载CoQ10纳米悬浮剂的体外溶出率在人工胃液(SGF)和人工肠液(SIF)中分别是CoQ10原药的1.89和1.48倍。在体内生物利用度实验中,分别对大鼠灌胃CoQ10原药与载药纳米悬浮剂后,检测不同时间点的血药浓度,考察药物在大鼠体内的吸收和代谢情况,负载CoQ10的纳米悬浮剂在大鼠体内的血药浓度明显高于CoQ10原药,生物利用度提高为CoQ10原药的2.64倍。
A novel copolymer-supported coenzyme Q10 formed a nanometer suspension agent and increased the water solubility of CoQ10 and improved its oral bioavailability.The quercetin-Xylan(qt-xylan)copolymer coupling was used as the basis for synthesis.The single factor experiment design was adopted,and the particle size was used as the inspection condition of the single factor experiment.The factors affecting the particle size included high pressure homogenization pressure,high pressure homogenization times,copolymer concentration,mass ratio between copolymer and CoQ10,and a series of in vitro experiments were carried out.When the homogenization pressure was 60 MPa,the number of homogenization was 7,the copolymer concentration was 1 mg·mL^-1,and the mass ratio of copolymer to CoQ10 was 1∶1,it was the best preparation process for the nanometer suspension agent,and the particle size was 166.7 nm.Under the optimum technological conditions in vitro dissolution experiment,the dissolution rate of CoQ10 nanometer suspended agent coated in artificial gastric juice(SGF)and artificial intestinal juice(SIF)was 1.89 and 1.48 times that of CoQ10 active drug,respectively.The bioavailability in vivo experiments,rat were loaded on gastric CoQ10 and nanoparticle suspension agent respectively.Then the blood drug concentration,different time points in drug absorption and metabolism of rats were detected respectively.The load of CoQ10 nanometer suspending agent in rats blood drug concentration was significantly higher than that of CoQ10 technical,and the bioavailability of CoQ10 reversed-phased was improved 2.64 times.
作者
张晓雪
赵修华
刘艳杰
王玲玲
张茜
ZHANG Xiao-Xue;ZHAO Xiu-Hua;LIU Yan-Jie;WANG Ling-Ling;ZHANG Qian(College of Chemical Engineering and Resource Utilization,Northeast Forestry University,Northeast Forestry University,Key Laboratory of Forest Plant Ecology of Ministry of Education,Northeast Forestry University,Harbin 150040)
出处
《植物研究》
CAS
CSCD
北大核心
2020年第6期943-950,共8页
Bulletin of Botanical Research
基金
黑龙江省杰出青年基金(JC2018005)。
