盐肤木提取物酚酸类成分的大鼠在体单向灌流肠吸收研究
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摘要
通过大鼠在体单向肠灌流模型,采用重量法对灌流液体积进行校正,HPLC测定肠灌流液中4种有效成分的含量,考察了盐肤木提取物中没食子酸、苔黑酚葡萄糖苷、没食子酸乙酯、五没食子酰葡萄糖4种酚酸类成分的大鼠在体肠吸收情况。结果显示,不同浓度的盐肤木提取物中4种酚酸类成分的吸收速率常数(K_a)和药物有效渗透系数(P_(eff))大多具有显著性差异(P<0.05),并在各个肠段的吸收存在着高浓度饱和现象。在同一浓度下,4种成分在各肠段的K_a和P_(eff)均有显著的差异(P<0.05);4种成分在肠道中吸收速率及渗透能力顺序是:五没食子酰葡萄糖>没食子酸乙酯>没食子酸>苔黑酚葡萄糖苷,且两两之间均存在显著性差异(P<0.05)。结果说明,没食子酸、苔黑酚葡萄糖苷、没食子酸乙酯、五没食子酰葡萄糖在整个肠道均有吸收,其吸收速率及渗透能力与肠道部位以及浓度有关,并且4种有效成分在肠道的转运过程中可能存在主动转运或促进扩散。
The intestinal absorption properties of four main effective components(gallic acid, ocinolglucoside, ethyl gallate and penta-O-galloyl-β-D-glucose) in Rhus chinensis extracts were investigated by in situ single-pass intestinal perfusion model in rats. The liquid accumulation of perfusion was corrected by gravimetry. The HPLC method was established to determine the concentration of the four effective components in the intestinal perfusion. It showed significant differences(P<0.05) in absorption rate constant(K_a) and effective permeability(P_(eff)) among the three concentrations of components, and the absorption of the four effective components in different intestinal segments was saturated at high concentrations. At the same concentration, there were significant differences in K_a and P_(eff) of the four components in each intestinal segment(P<0.05). The order of K_a and P_(eff) of the four components in the intestine was penta-O-galloyl-β-D-glucose>ethyl gallate>gallic acid>ocinolglucoside, with significant differences between them(P<0.05). In conclusion, gallic acid, orpheolglucoside, ethyl gallate and pentacyl-glucose could be absorbed in the whole intestine. Their absorption rate and permeation ability were related to the intestinal section and the perfusate concentration. These results indicated potential active transport or facilitated diffusion in the intestinal transport process of the four effective components.
The intestinal absorption properties of four main effective components(gallic acid, ocinolglucoside, ethyl gallate and penta-O-galloyl-β-D-glucose) in Rhus chinensis extracts were investigated by in situ single-pass intestinal perfusion model in rats. The liquid accumulation of perfusion was corrected by gravimetry. The HPLC method was established to determine the concentration of the four effective components in the intestinal perfusion. It showed significant differences(P<0.05) in absorption rate constant(K_a) and effective permeability(P_(eff)) among the three concentrations of components, and the absorption of the four effective components in different intestinal segments was saturated at high concentrations. At the same concentration, there were significant differences in K_a and P_(eff) of the four components in each intestinal segment(P<0.05). The order of K_a and P_(eff) of the four components in the intestine was penta-O-galloyl-β-D-glucose>ethyl gallate>gallic acid>ocinolglucoside, with significant differences between them(P<0.05). In conclusion, gallic acid, orpheolglucoside, ethyl gallate and pentacyl-glucose could be absorbed in the whole intestine. Their absorption rate and permeation ability were related to the intestinal section and the perfusate concentration. These results indicated potential active transport or facilitated diffusion in the intestinal transport process of the four effective components.
引文
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[3] 沈亚英.治疗冠心病新药——舒冠通糖浆[J].中国药学杂志,1980,15(5):28.
[4] 叶永华.盐肤木抗冠心病活性部位筛选及化学成分研究[D].福州:福建中医药大学,2018.
[5] 叶永华,张双,游立群,等.福林酚法测定闽产盐肤木根茎中总酚酸的含量[J].福建中医药,2018,49(2):66.
[6] 冯霞,张雅雯,梁泽华,等.积雪草酸的大鼠在体肠吸收动力学研究[J].中国现代应用药学,2013,30 (6):628.
[7] Wang X Y,Chen Y H,Zohra D F,et al.Amphiphiliccarboxymethyl chitosan-quercetin conjugate with P-gp inhibitory properties for oral delivery of paclitaxel[J].Biomaterials,2014,35(26):7654.
[8] 李俊松,杨欣文,彭稳稳,等.莲子心生物碱类成分的大鼠在体单向灌流肠吸收[J].中国药学杂志,2014,49(6):490.
[9] 邓少东,张鹏,林励,等.单向灌流法研究巴戟天低聚糖的大鼠肠吸收特性[J].中国中药杂志,2015,40(1):134.
[10] Zhang J,Liu D,Huang Y,et al.Biopharmaceutics classification and intestinal absorption study of apigenin[J].Int J Pharm,2012,436 (1/2):311.
[11] 许永崧,韩晓凤,龚慕辛,等.单向在体肠灌流在中药研究中的应用[J].中国实验方剂学杂志,2016,22(1):211.
[12] 王帅,李清清,王帆,等.葛根素药物纳米晶自稳定pickering乳的大鼠肠吸收特性研究[J].中国中药杂志,2018,43(10):2162.
[13] 吴干斌,褚延乐.大鼠在体单向肠灌流模型研究冬凌草乙素的吸收动力学[J].中国中药杂志,2018,43(15):3192.
[14] 巩仔鹏,李梅,侯靖宇,等.外翻肠囊法研究羊耳菊提取物在大鼠肠内的吸收[J].中国中药杂志,2018,43(3):609.
[15] 柏希慧,刘诗雨,王晶,等.单向灌流法评价复方龙脉宁汤剂配伍对葛根素肠吸收的影响[J].中国中药杂志,2017,42(1):157.
[16] 许海舰,刘一鑫,刘喜纲,等.黄芩苷镁盐和黄芩苷的肠吸收动力学和药代动力学比较[J].中国实验方剂学杂志,2018,24(4):78.