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在体单向肠灌流法研究胡黄连总苷中4个成分的大鼠肠吸收特性
张琬靖1, 曹宁宁1, 李晓璇1, 裴帅2, 蔡楠3, 肖学凤1
1.天津中医药大学中药学院, 天津 301617;2.成都先导药物开发股份有限公司研发化学中心, 四川 610200;3.天士力控股集团有限公司研究院 现代中药开发中心, 天津 300410
摘要:
[目的] 考察胡黄连总苷中胡黄连苷Ⅰ、胡黄连苷Ⅱ、胡黄连苷Ⅳ、草夹竹桃苷共4个成分在大鼠体内不同肠段的吸收情况,阐明胡黄连总苷中4个成分的肠吸收特性。[方法] 采用在体单向肠灌流法,运用高效液相色谱(HPLC)技术测定胡黄连总苷肠灌流液中4个成分的浓度,以吸收速率常数(Ka)和有效渗透系数(Peff)为评价指标,考察胡黄连总苷中4个成分分别在十二指肠、空肠、回肠、结肠的吸收特性。[结果] 胡黄连总苷中4个成分在大鼠不同肠段均Ka>1.65×10-2/min,Peff>2.0×10-5cm/min,表明这4个成分在不同肠段的吸收速度及吸收能力均良好,但各成分在不同肠段的吸收速度及吸收能力存在一定差异。胡黄连苷Ⅰ在不同肠段的KaPeff值差异无统计学意义(P>0.05),胡黄连苷Ⅰ无主要吸收部位;胡黄连苷Ⅱ、胡黄连苷Ⅳ和草夹竹桃苷在不同肠段的KaPeff值差异均有统计学意义(P<0.05),且胡黄连苷Ⅱ、胡黄连苷Ⅳ和草夹竹桃苷主要吸收部位分别为十二指肠、空肠和结肠。此外,草夹竹桃苷与其他3个成分比较,KaPeff值差异均有统计学意义(P<0.05),且其在不同肠段中吸收均最佳。[结论] 本研究阐明了胡黄连总苷中4个成分在不同肠段中吸收特性,为胡黄连总苷的临床合理用药提供参考。
关键词:  在体单向肠灌流法  胡黄连总苷  肠吸收特性
DOI:10.11656/j.issn.1672-1519.2022.12.17
分类号:R285.5
基金项目:国家自然科学基金资助项目(81973557);天津市自然科学基金重点项目(20JCZDJC00010);天津中医药大学研究生科研创新项目(YJSKC-20201013)。
Study on intestinal absorption characteristics of 4 components of total glucosides in picrorhiza scrophulariiflora by in situ singl-pass intestinal perfusion method
ZHANG Wanjing1, CAO Ningning1, LI Xiaoxuan1, PEI Shuai2, CAI Nan3, XIAO Xuefeng1
1.School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China;2.Discovery Chemistry Unit, HitGen Inc., Chengdu 610200, China;3.Traditional Chinese medicine Research Center, Tasly Holding Group Co., Ltd., Tianjin 300410, China
Abstract:
[Objective] To investigate the absorption characteristics of picrosideⅠ,picrosideⅡ,picroside Ⅳ and androsin in different intestinal segments of rats,and explore the intestinal absorption characteristics of four components of total glucosides in Picrorhiza scrophulariiflora (TGPS). [Methods] The in situ single pass intestinal perfusion method was used,and an HPLC system was utilized to determine the contents of four components of TGPS. The absorption characteristics of four components of TGPS in duodenum,jejunum, ileum and colon were investigated with the absorption rate constant (Ka) and the effective permeability coefficient (Peff) as evaluation indexes. [Results] The Ka and Peff of four components from TGPS in different intestinal segments of rats were respectively all greater than 1.65×10-2/min,2.0×10-5cm/min,indicating that the absorption rate and absorption capacity of the four components in different intestinal segments were good,but there were some differences in the absorption rate and absorption capacity of each component in different intestinal segments. There was no notable difference in in Ka and Peff of picroside Ⅰ in the different intestinal segments (P>0.05), suggesting that there was no main absorption site of picroside Ⅰ;the best absorption sites for picroside Ⅱ,picroside Ⅳ and androsin were the duodenum,jejunum and colon,respectively,and the differences between different intestinal segments were statistically significant (P<0.05). In addition,compared with the other three components,there were significant differences in Ka and Peff of androsin in different intestinal segments (P<0.05),and the absorption of androsin in different intestinal segments was the best. [Conclusion] The study investigated the absorption characteristics of four components of TGPS in different intestinal segment,so as to provide reference for the clinical rational use of TGPS.
Key words:  in situ single-pass intestinal perfusion method  total glucosides in picrorhiza scrophulariiflora  intestinal absorption characteristics
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