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盐酸小檗碱在黄连水煎液中的生物药剂学分类系统属性研究 被引量:21
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作者 隗丽 朱美玲 +4 位作者 董月柳 董玲 刘洋 陈江鹏 尹秀文 《中国中药杂志》 CAS CSCD 北大核心 2016年第7期1192-1197,共6页
中药生物药剂学分类系统的基础研究之一是在多成分环境下对单一成分进行研究,即除成分自身溶解性和渗透性外,需结合多成分环境下造成的溶解性和渗透性各自提升度进行分类研究。该研究以小檗碱为主要研究对象,探究其在黄连水煎液中的水... 中药生物药剂学分类系统的基础研究之一是在多成分环境下对单一成分进行研究,即除成分自身溶解性和渗透性外,需结合多成分环境下造成的溶解性和渗透性各自提升度进行分类研究。该研究以小檗碱为主要研究对象,探究其在黄连水煎液中的水溶解性及肠渗透性变化规律。其中采用经典摇瓶法和高效液相色谱法测定小檗碱在不同p H缓冲液及不同浓度的黄连水煎液中的溶解度,并分别采用在体单向灌流模型及肠道灌流并行采血模型进行小檗碱的肠吸收和入血吸收的研究。 展开更多
关键词 黄连 小檗碱 溶解 渗透性 中药生物药剂学分类系统
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Intestinal permeability in patients after surgical trauma and effect of enteral nutrition versus parenteral nutrition 被引量:19
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作者 Xiao-Hua Jiang Ning Li Jie-Shou Li, Research Institute of General Surgery, Medical School of Nanjing University, Nanjing 210002, Jiangsu Province, China 《World Journal of Gastroenterology》 SCIE CAS CSCD 2003年第8期1878-1880,共3页
AIM: To study the intestinal permeability (IP) following stress of abdominal operation and the different effects on IP of enteral nutrition (EN) and parenteral nutrition (PN).METHODS: Forty patients undergoing abdomin... AIM: To study the intestinal permeability (IP) following stress of abdominal operation and the different effects on IP of enteral nutrition (EN) and parenteral nutrition (PN).METHODS: Forty patients undergoing abdominal surgery were randomized into EN group and PN group. Each group received nutritional support of the same nitrogen and calorie from postoperative day (POD) 3 to POD 11. On the day before operation (POD-1), POD 7 and POD 12, 10 g of lactulose and 5 g of mannitol were given orally, and urine was collected for 6 hours. Urine excretion ratios of lactulose and mannitol (L/M) were measured.RESULTS: L/M ratios of EN group on POD-1, POD 7 and POD 12 were 0.026±0.017, 0.059±0.026, 0.027±0.017,respectively, and those of PN group were 0.025±0.013,0.080±0.032, 0.047±0.021, respectively. Patients of both groups had elevated L/M ratios on POD 7 vs. POD-1. However the ratio returned toward control level in EN group by POD 12.In contrast, PN group still had elevated L/M ratios on POD 12.CONCLUSION: L/M ratio increases for a period of time after surgical trauma and the loss of gut mucosal integrity can be reversed by substitution of enteral nutrition. 展开更多
关键词 手术后 内营养 内营养 渗透性
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铁皮石斛超微粉对LPS致肠黏膜损伤小鼠的保护作用研究 被引量:12
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作者 杨志远 苏洁 +6 位作者 俞静静 黄启迪 陈思敏 陈建真 陈素红 吕圭源 颜美秋 《中国中药杂志》 CAS CSCD 北大核心 2021年第7期1667-1673,共7页
探究铁皮石斛Dendrobium officinale对脂多糖(lipopolysaccharide, LPS)诱导肠黏膜损伤的预防作用。采用40只SPF级8周龄C57BL/6J雄性小鼠,随机分为正常组(NC组)、模型组(LPS组)、铁皮石斛超微粉不同剂量组(DOF-L组和DOF-H组,剂量分别为0... 探究铁皮石斛Dendrobium officinale对脂多糖(lipopolysaccharide, LPS)诱导肠黏膜损伤的预防作用。采用40只SPF级8周龄C57BL/6J雄性小鼠,随机分为正常组(NC组)、模型组(LPS组)、铁皮石斛超微粉不同剂量组(DOF-L组和DOF-H组,剂量分别为0.30,0.60 g·kg^(-1)),每组10只。给药组小鼠每天灌胃等体积铁皮石斛超微粉混悬液,NC组和LPS组小鼠灌胃等量纯净水,连续7 d后,除NC组外,其余各组均腹腔注射5 mg·kg^(-1) LPS建立肠黏膜损伤小鼠模型。LPS注射6 h后,收集血浆和肠组织样本。生化法检测小鼠血浆中二胺氧化酶(diamine oxidase, DAO)和D-乳酸的水平;ELISA法检测促炎因子白细胞介素6(interleukin-6, IL-6)和肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)的水平;苏木素-伊红染色法观察小鼠回肠组织结构的病理变化;透射电镜观察小鼠回肠超微结构的变化;免疫组化法检测肠组织紧密连接蛋白claudin-1,occludin和F4/80的表达;蛋白免疫印迹法检测空肠Toll样受体4(Toll-like receptor 4, TLR-4)、核转录因子κB(nuclear factor kappa B p65, NF-κB p65)蛋白的表达。结果显示,连续灌胃7 d铁皮石斛超微粉能明显减轻模型小鼠肠黏膜的病理损伤和超微结构改变;显著降低模型小鼠血浆中DAO和D-乳酸的水平(P<0.05);明显增加回肠组织中claudin-1和occludin蛋白的表达;下调空肠组织中TLR-4和NF-κB p65蛋白的表达(P<0.01),显著降低血浆中TNF-α和IL-6的水平(P<0.05),并减少F4/80+巨噬细胞的浸润。提示铁皮石斛能明显减轻LPS所致肠黏膜损伤,降低肠道渗透性,其机制可能与其下调TLR-4/NF-κB p65信号通路、增加紧密连接蛋白的表达有关。 展开更多
关键词 铁皮石斛 黏膜损伤 脂多糖 TLR-4 紧密连接 渗透性
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Effect of glutamine on change in early postoperative intestinal permeability and its relation to systemic inflammatory response 被引量:11
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作者 Zhu-FuQuan ChongYang NingLi Jie-ShouLi 《World Journal of Gastroenterology》 SCIE CAS CSCD 2004年第13期1992-1994,共3页
AIM: To study the effects of glutamine (Gin) on the change of intestinal permeability and its relationship to systemic inflammatory response in early abdominal postoperative patients.METHODS: A prospective, randomized... AIM: To study the effects of glutamine (Gin) on the change of intestinal permeability and its relationship to systemic inflammatory response in early abdominal postoperative patients.METHODS: A prospective, randomized, double-blind and controlled trial was taken. Twenty patients undergoing abdominal surgery were randomized into Gin group (oral administration of glutamine, 30 g/d, for 7 d, n=10) and placebo group (oral administration of placebo, 30 g/d, for 7 d, n=-10). Temperatures and heart rates of all patients were daily recorded. White blood cell counts(WBC) and biochemical variables were measured before operation and 4 and 7 d alter drug administration. Serum concentrations of glutamine, endotoxin, diamine oxidase and malondialdehyde and urine lactulose/mannito (L/M) ratio were measured before and 7 d alter drug administration.RESULTS: The patients in the 2 groups were comparable prior to drug administration. Serum Gin concentration was significantly decreased in the placebo group and increased in the Gin group 7 d alter drug administration. Urine L/M ratio was significantly increased in the placebo group and decreased in the Gin group. The serum concentration of endotoxin, diamine oxidase and malondialdehyde was significantly decreased in the Gin group compared with those in the placebo group. Temperatures, heart rates and WBC counts were significantly lower in the Gin group than those in the placebo group.CONCLUSION: Gut is one of the sources of systemic inflammatory response in abdominal postoperative patients and glutamine can decrease intestinal permeability, maintain intestinal barrier and attenuate systemic inflammatory response in early postoperative patients. 展开更多
关键词 谷氨酰胺 早期 手术治疗 渗透性 系统 反应 腹部外科
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中药生物药剂学分类系统中多成分环境对葛根素渗透性的影响 被引量:10
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作者 刘洋 王刚 +4 位作者 董玲 唐明敏 朱美玲 董红环 侯成波 《中国中药杂志》 CAS CSCD 北大核心 2014年第23期4505-4508,共4页
中药生物药剂学分类系统(biopharmaceutics classification system of Chinese materia medica,CMMBCS)中的渗透性评价,需多成分作为整体来开展研究,即使在研究具体某一成分时,也应将其放在多成分环境中审视。该实验以此为原则,将葛根... 中药生物药剂学分类系统(biopharmaceutics classification system of Chinese materia medica,CMMBCS)中的渗透性评价,需多成分作为整体来开展研究,即使在研究具体某一成分时,也应将其放在多成分环境中审视。该实验以此为原则,将葛根芩连汤中的高含量成分作为多成分环境影响因素,考察葛根素的肠渗透性,运用在体肠单向灌流模型,对葛根素肠渗透性的相关参数进行测定,评价其他高含量成分对其肠渗透性的影响。实验结果表明不同比例的黄芩苷、甘草酸和小檗碱对葛根素的肠渗透性均有一定的影响,甘草酸能显著抑制葛根素的肠吸收,高浓度小檗碱会促进葛根素的吸收。该研究结果表明中药生物药剂学分类系统的渗透性评价充分考虑多成分环境中其他成分的影响是重要的研究思想。 展开更多
关键词 葛根素 多成分环境 在体单向灌流 渗透性
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黄连提取物的中药生物药剂学分类系统研究 被引量:10
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作者 刘洋 尹秀文 +4 位作者 王子禹 李雪莲 潘孟 李彦萍 董玲 《中国中药杂志》 CAS CSCD 北大核心 2017年第21期4127-4134,共8页
中药生物药剂学分类系统(CMMBCS)的优势之一,是将分类归属的研究层面从单成分扩展到中药多成分,进而从多成分扩展到中药整体研究层面。该研究以黄连提取物中的生物碱为主要研究对象,探究生物碱单一成分及黄连提取物中各生物碱成分的水... 中药生物药剂学分类系统(CMMBCS)的优势之一,是将分类归属的研究层面从单成分扩展到中药多成分,进而从多成分扩展到中药整体研究层面。该研究以黄连提取物中的生物碱为主要研究对象,探究生物碱单一成分及黄连提取物中各生物碱成分的水溶解性及肠渗透性变化规律,并对黄连提取物整体做中药生物药剂学分类系统归属研究。其中采用经典摇瓶法和高效液相色谱法测定生物碱单一成分及提取物中各生物碱成分的溶解度变化及分类,采用在体单向肠灌流法进行生物碱吸收定量研究,同时采用自定义权重系数法对黄连提取物整体进行渗透系数计算。 展开更多
关键词 黄连提取物 生物碱 溶解 渗透性 中药生物药剂学分类系统
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葛根芩连汤中小檗碱的中药生物药剂学分类系统属性研究 被引量:9
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作者 刘洋 朱美玲 +4 位作者 孙慧娟 王子禹 陈江鹏 董月柳 董玲 《中国中药杂志》 CAS CSCD 北大核心 2017年第8期1545-1550,共6页
中药生物药剂学分类系统(CMMBCS)的顶层研究之一是中药复方对单一成分的影响研究,除单成分自身溶解性和渗透性外,需结合复方中多成分环境下其溶解性和渗透性各自提升度来进行分类。该文主要是研究葛根芩连复方中小檗碱的CMMBCS分类属性... 中药生物药剂学分类系统(CMMBCS)的顶层研究之一是中药复方对单一成分的影响研究,除单成分自身溶解性和渗透性外,需结合复方中多成分环境下其溶解性和渗透性各自提升度来进行分类。该文主要是研究葛根芩连复方中小檗碱的CMMBCS分类属性的变化,即小檗碱在葛根芩连汤中的溶解性和渗透性,考察其在整个复方环境中的变化及分类。采用经典摇瓶法和高效液相色谱法测定其在复方中的溶解度变化,并采用大鼠离体外翻肠囊实验进行小檗碱肠吸收定性,采用在体单向灌流法进行小檗碱肠吸收定量研究,同时和肠道血管并行采血实验进行吸收入血的定性和定量研究。 展开更多
关键词 葛根芩连汤 小檗碱 溶解 渗透性 中药生物药剂学分类系统
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基于抗炎活性的葛根芩连片整体的中药生物药剂学分类系统研究 被引量:9
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作者 王子禹 刘洋 +3 位作者 张鑫 李彦萍 程亚茹 董玲 《中国中药杂志》 CAS CSCD 北大核心 2019年第17期3662-3671,共10页
中药生物药剂学分类系统(CMMBCS)研究最终应落实到中药复方整体研究层面,而中药复方整体的溶解度和渗透性等重要参数不止是各成分溶解度和渗透性的简单加和。该研究以葛根芩连片为研究对象,采用HPLC同时测定葛根芩连片中12个代表性成分... 中药生物药剂学分类系统(CMMBCS)研究最终应落实到中药复方整体研究层面,而中药复方整体的溶解度和渗透性等重要参数不止是各成分溶解度和渗透性的简单加和。该研究以葛根芩连片为研究对象,采用HPLC同时测定葛根芩连片中12个代表性成分葛根素、大豆苷、黄芩苷、大豆苷元、汉黄芩苷、黄芩素、汉黄芩素、甘草酸、盐酸黄连碱、表小檗碱、盐酸小檗碱、盐酸巴马汀的含量,得到各成分的质量权重;利用脂多糖(LPS)诱导RAW264. 7细胞构建体外炎症模型,考察葛根芩连片中12个代表性成分的抗炎作用,得到各成分的药效权重。通过经典摇瓶法和在体单向肠灌流法分别测定葛根芩连片中各有效成分的溶解度和有效渗透系数,并采用质量权重和药效权重相结合的方式进行整合,得到能够代表葛根芩连片整体性质的剂量数和有效渗透系数,结果表明葛根芩连片属于低溶解度、低渗透性药物,应归为CMMBCSⅣ类。 展开更多
关键词 葛根芩连片 溶解度 渗透性 中药生物药剂学分类系统
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游离蒽醌在人肠Caco-2细胞模型的转运(英文) 被引量:4
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作者 王莹 杨秀伟 《中国天然药物》 SCIE CAS CSCD 2008年第2期141-145,共5页
目的:研究1,8-二羟基蒽醌(1,8-dihydroxyanthraquinone,DQ)、大黄酚(chrysophanol,CP)、大黄素(emodin,EN)、大黄酸(rhein,RN)、芦荟大黄素(aloe-emodin,AE)和ω-羟基大黄素(citreorosein,CN)在人肠Caco-2细胞单层模型的转运。方法:以人... 目的:研究1,8-二羟基蒽醌(1,8-dihydroxyanthraquinone,DQ)、大黄酚(chrysophanol,CP)、大黄素(emodin,EN)、大黄酸(rhein,RN)、芦荟大黄素(aloe-emodin,AE)和ω-羟基大黄素(citreorosein,CN)在人肠Caco-2细胞单层模型的转运。方法:以人源Caco-2细胞单层为药物的肠吸收转运模型,将DQ、CP、EN、RN、AE和CN与其共温孵进行吸收转运,高效液相色谱法测定吸收转运量。结果:DQ、CP、EN、RN、AE和CN从顶侧(肠腔侧)向底侧(体循环侧)吸收转运的表观渗透系数(Papp)值分别为(2.16±0.38)×10-6、(3.00±0.09)×10-7、(1.99±0.94)×10-6、(4.58±0.20)×10-6、(6.24±0.19)×10-6和(7.34±0.61)×10-6cm.s-1;从底侧向顶侧吸收转运的Papp分别为(3.20±0.10)×10-6,(4.50±0.02)×10-7,(2.22±0.62)×10-6,(4.94±0.39)×10-6,(2.87±0.18)×10-6和(6.80±0.37)×10-6cm·s-1。DQ、EN、RN、AE和CN的Papp值比在Caco-2细胞单层模型上呈被动扩散机制、吸收良好的阳性对照化合物普萘洛尔的Papp值[(6.30±0.26)×10-5cm·s-1]小10倍,但比呈被动扩散机制、吸收不良的阳性对照化合物阿替洛尔的Papp值(<1×10-7cm.s-1)大10倍。CP的Papp值与阿替洛尔的Papp值基本上在同一数量级。ATP耗竭剂碘乙酰胺不影响AE在两个方向上的转运。结论:DQ、CP、EN、RN、AE和CN在人源Caco-2细胞单层模型的吸收转运机制为被动扩散;DQ、EN、RN、AE和CN属于中等吸收的化合物,CP属于吸收不良的化合物。 展开更多
关键词 1 8-二羟基蒽醌 大黄酚 大黄素 大黄酸 芦荟大黄素 ω-羟基大黄素 渗透性 CACO-2细胞单层
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对乙酰氨基酚通过共晶形成提高阿德福韦酯的溶出及肠吸收 被引量:3
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作者 邱培燊 高静 +2 位作者 钱帅 魏元锋 张建军 《药学学报》 CAS CSCD 北大核心 2018年第6期993-1001,共9页
本研究采用溶剂挥发法制备阿德福韦酯-对乙酰氨基酚共晶(摩尔比为1∶1),通过差示扫描量热法、粉末X-射线衍射法和红外光谱法等分析手段对其进行表征。结果表明,阿德福韦酯分子中的磷酯基与对乙酰氨基酚分子中的酰胺基通过氢键连接形成... 本研究采用溶剂挥发法制备阿德福韦酯-对乙酰氨基酚共晶(摩尔比为1∶1),通过差示扫描量热法、粉末X-射线衍射法和红外光谱法等分析手段对其进行表征。结果表明,阿德福韦酯分子中的磷酯基与对乙酰氨基酚分子中的酰胺基通过氢键连接形成阿德福韦酯-对乙酰氨基酚共晶。与对乙酰氨基酚形成共晶后,阿德福韦酯的溶解度与溶出速率均得到显著改善。此外,对乙酰氨基酚还可通过抑制阿德福韦酯外排而提高其肠渗透性、促进其肠吸收,这将有助于提高低渗透性药物阿德福韦酯的体内吸收。 展开更多
关键词 阿德福韦酯 对乙酰氨基酚 共晶 溶出速率 渗透性
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Increased intestinal macromolecular permeability and urine nitrite excretion associated with liver cirrhosis with ascites 被引量:16
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作者 Soong Lee Seung-Cheol Son +6 位作者 Moon-Jong Han Woo-Jin Kim Soo-Hyun Kim Hye-Ran Kim Woo-Kyu Jeon Ki-Hong Park Myung-Geun Shin 《World Journal of Gastroenterology》 SCIE CAS CSCD 2008年第24期3884-3890,共7页
AIM: To determine intestinal permeability, the serum tumor necrosis factor (TNF)-α level and urine nitric oxide (NO) metabolites are altered in liver cirrhosis (LC) with or without ascites. METHODS: Fifty-thr... AIM: To determine intestinal permeability, the serum tumor necrosis factor (TNF)-α level and urine nitric oxide (NO) metabolites are altered in liver cirrhosis (LC) with or without ascites. METHODS: Fifty-three patients with LC and 26 healthy control subjects were enrolled in the study. The intestinal permeability value is expressed as the percentage of polyethylene glycol (PEG) 400 and 3350 retrieval in 8-h urine samples as determined by high performance liquid chromatography. Serum TNF-α concentrations and urine NO metabolites were determined using an enzyme-linked immunosorbent assay (ELISA) and Greiss reaction method, respectively. RESULTS: The intestinal permeability index wassignificantly higher in patients with LC with ascites than in healthy control subjects or patients with LC without ascites (0.88 ± 0.12 vs 0.52 ± 0.05 or 0.53 ± 0.03, P 〈 0.05) and correlated with urine nitrite excretion (r = 0.98). Interestingly, the serum TNF-α concentration was significantly higher in LC without ascites than in control subjects or in LC with ascites (198.9 ± 55.8 pg/mL vs 40.9 ± 12.3 pg/mL or 32.1 ± 13.3 pg/mL, P 〈 0.05). Urine nitrite excretion was significantly higher in LC with ascites than in the control subjects or in LC without ascites( 1170.9± 28.7 μmol/L vs 903.1 ± 55.1 μmol/L or 956.7 ± 47.7 μmol/L, P 〈 0.05). COMCLUSIOM: Increased intestinal macromolecular permeability and NO is probably of importance in the pathophysiology and progression of LC with ascites, but the serum TNF-α concentration was not related to LC with ascites. 展开更多
关键词 Intestinal permeability Tumor necrosisfactor-R Nitric oxide Liver cirrhosis ASCITES
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Intestinal permeability and its association with the patient and disease characteristics in Crohn's disease 被引量:4
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作者 Jaya Benjamin Govind K Makharia +2 位作者 Vineet Ahuja Mani Kalaivan Yogendra K Joshi 《World Journal of Gastroenterology》 SCIE CAS CSCD 2008年第9期1399-1405,共7页
AIM:To assess the intestinal permeability (IP) in patients with Crohn's disease (CD) and study the association of IP with the patient and disease characteristics. METHODS: One hundred and twenty five consecutive p... AIM:To assess the intestinal permeability (IP) in patients with Crohn's disease (CD) and study the association of IP with the patient and disease characteristics. METHODS: One hundred and twenty five consecutive patients of CD (Males: 66) were diagnosed on the basis of a combination of standard clinical, endoscopic, imaging and histological features. CD activity index (CDAI) was used to calculate the activity of the disease while the behavior of the disease was assessed by the modified Montreal classification. IP was measured by the ratio of the percentage excretion of ingested doses of lactulose and mannitol in urine (LMR). The upper limit of normality of LMR (0.037) was derived from 22 healthy controls. RESULTS: Thirty six percent of patients with CD had increased IP. There was no significant difference in mannitol excretion (patients vs controls = 12.5% vs 14.2%, P = 0.4652), but lactulose excretion was significantly higher in patients compared to healthy controls (patients vs controls = 0.326% vs 0.293%, P = 0.0391). The mean LMR was also significantly higher in the patients as compared to healthy controls [0.027 (0.0029-0.278) vs 0.0164 (0.0018-0.0548), P = 0.0044]. Male patients had a higher LMR compared to females [0.036 (95% CI 0.029, 0.046) vs 0.022 (95% CI 0.0178, 0.028) (P = 0.0024), though there was no difference in the number of patients with abnormal IP in boththe sexes. Patients with an ileo-colonic disease had a higher LMR than those with only colonic disease [0.045 (95% CI 0.033, 0.06) vs 0.021 (95% CI 0.017, 0.025) (P < 0.001)]. Of patients with ileo-colonic disease, 57.8% had an abnormal IP, compared to 26.7% with colonic and 15.6% with small intestinal disease. Patients with a stricturing disease had significantly higher LMR compared to non-fistulising non-stricturing disease [0.043 (95% CI 0.032, 0.058) vs 0.024 (95% CI 0.019, 0.029) (P = 0.0062)]. There was no correlation of IP with age, disease activity, duration of illness, D-xylose absorption, upper GI involvement, perianal disease, and e 展开更多
关键词 Lactulose mannitol ratio Crohn's disease Inflammatory bowel disease Intestinal barrier Crohn's disease activity index Intestinal permeability
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