盐巴戟天有效成分在体肠灌流研究  

Study on Effective Components of Salt-processing Morinda officinalis by in situ Intestinal Perfusion Model

作　　者：华悦 魏晓峰 李喆 张超 史辑[1,2,3] HUA Yue;WEI Xiaofeng;LI Zhe;ZHANG Chao;SHI Ji(School of Pharmacy,Liaoning University of Traditional Chinese Medicine,Dalian 116600,China;State Administration of Traditional Chinese Medicine Key Laboratory of Analysis of Processing Principle,Dalian 116600,China;Liaoning Research Center of Traditional Chinese Medicine Processing Engineering,Dalian 116600,China)

机构地区：[1]辽宁中医药大学药学院,辽宁大连116600 [2]国家中医药管理局炮制原理解析重点实验室,辽宁大连116600 [3]辽宁省中药炮制工程技术研究中心,辽宁大连116600

出　　处：《中国中医药信息杂志》2021年第9期105-110,共6页Chinese Journal of Information on Traditional Chinese Medicine

基　　金：国家自然科学基金(81473350);辽宁省自然科学基金(201602490)。

摘　　要：目的研究盐巴戟天中环烯醚萜苷类和寡糖类成分在大鼠体内的肠吸收动力学特征。方法采用HPLC和超高效液相色谱三重四极杆串联质谱(UPLC-QqQ-MS/MS)技术分别建立巴戟天中环烯醚萜苷类成分水晶兰苷、去乙酰车叶草苷酸和寡糖类成分耐斯糖在小肠液的定量分析方法。基于大鼠在体单向肠灌流模型,以吸收速率常数(K_(a))和表观渗透系数(P_(app))为评价指标,探究不同pH值、不同药物浓度、不同肠段(十二指肠、空肠、回肠)及盐制对巴戟天中水晶兰苷、去乙酰车叶草苷酸和耐斯糖肠吸收的影响。结果建立了盐巴戟天中3种有效成分在大鼠小肠液中的定量分析方法,符合方法学要求。3种成分在pH 7.4灌流液中的P_(app)和K_(a)均大于pH 6.8和pH 5.4灌流液,在中剂量(270 g/L)灌流液中的吸收参数均明显大于高剂量(540 g/L)和低剂量(135 g/L)。3种成分在小肠各肠段均有吸收且不同肠段间无明显差异,水晶兰苷K_(a)为空肠>十二指肠>回肠,去乙酰车叶草苷酸K_(a)为回肠>空肠>十二指肠,耐斯糖K_(a)为回肠>十二指肠>空肠;同一肠段耐斯糖与水晶兰苷、去乙酰车叶草苷酸K_(a)有明显差异(P<0.05),耐斯糖>去乙酰车叶草苷酸>水晶兰苷。盐巴戟天中3种成分在小肠不同肠段的P_(app)均大于巴戟肉,其中耐斯糖最为显著(P<0.01)。结论盐巴戟天中3种成分在小肠不同肠段中均有较好的吸收,水晶兰苷的主要吸收部位在空肠,去乙酰车叶草苷酸和耐斯糖的主要吸收部位在回肠,耐斯糖的吸收速率明显大于水晶兰苷和去乙酰车叶草苷酸。3种成分在中剂量(270 g/L)、pH 7.4灌流液中吸收较好,均存在自身浓度抑制现象。盐巴戟天中3种成分的肠吸收特性优于巴戟肉。Objective To investigate the rat intestinal absorption characteristics of iridoids glycoside and oligosaccharides from salt-processing Morinda officinalis.Methods The quantitative analysis method of iridoid glycoside components such as monotropein,deacetylasperulosidic acid and oligosaccharide nystose in salt-processing Morinda officinalis was established by high performance liquid chromatography tandem mass spectrometry(UPLC-QqQ-MS/MS)method.Based on the rat in vivo unidirectional intestinal perfusion model,the absorption rate constant(K_(a))and apparent permeability coefficient(P_(app))were used as evaluation indicators to explore different pH values,different drug concentrations,and different intestinal segments(duodenum,jejunum,Ileum)and the influence of Morinda officinalis on the intestinal absorption of monotropein,deacetylasperulosidic acid and nytose before and after steaming.Results The UPLC-QqQ-MS/MS quantitative analysis method of three kinds of effective components in salt-processing Morinda officinalis was established,which met the methodological requirements.The P_(app) and K_(a) of pH 7.4 were higher than those of pH 6.8 and pH 5.4.The absorption parameters of the middle dosage(270 g/L)were significantly higher than those of the high dosage(540 g/L)and low dosage(135 g/L),and there was self concentration inhibition.There was no significant difference in the absorption rate of the three kinds of effective components in the three intestinal segment.The K_(a) value of monotropein was jejunum>duodenum>ileum,and K_(a) value of deacetylasperulosidic acid and nystose was ileum>duodenum>jejunum;in the same intestinal segment,the absorption rate of nystose,monotropein and deacetylasperulosidic acid was significantly different(P<0.05),and nystose>deacetylasperulosidic acid>monotropein.The P_(app) of three active components in salt-processing Morinda officinalis was higher than those in Morinda officinalis in different intestinal segments,and the difference of P_(app) of nystosel was the most significant(P<0.

关 键 词：盐巴戟天 肠吸收 在体单向肠灌流 水晶兰苷 去乙酰车叶草苷酸 耐斯糖 大鼠 

分 类 号：R285.5[医药卫生—中药学]