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Self-microemulsifying drug delivery system for improving the bioavailability of huperzine A by lymphatic uptake
  • ISSN号:2095-7246
  • 期刊名称:《安徽中医药大学学报》
  • 时间:0
  • 分类:R943[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:Anhui University of Chinese Medicine, National Chinese Medicinal Materials Products Quality Supervision and Inspection Center (Anhui), Key Laboratory of Xin’an Medicine Ministry of Education, Anhui '115' Xin’an Traditional Chinese Medical Research & Development Innovation Team, Anhui Province Key Laboratory of R&D of Chinese Medicine, School of Pharmacy, Anhui Medical University
  • 相关基金:supported by the National Natural Science Foundation of China(Grant Nos.81274100;81573615);Natural Science Foundation of Anhui Province of China(Grant No.1408085QH189);Key Project for the Excellent Higher Education of Anhui Province of China(Grant No.2013SQRL019ZD);Research Project for the Science and Technology of Bozhou city of China(Grant No.BK2015005)
中文摘要:

Huperzine A(Hup-A) is a poorly water-soluble drug with low oral bioavailability. A selfmicroemulsifying drug delivery system(SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion(SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time curve(AUC) of Hup-A SMEDDS was significantly higher than that of a Hup-A suspension(P <0.01).The absorption rate constant(Ka) and the apparent permeability coefficient(Papp) for Hup-A in different parts of the intestine suggested a passive transport mechanism, and the values of Ka and Papp of Hup-A SMEDDS in the ileum were much higher than those in other intestinal segments. The determination of Hup-A concentration in mesenteric lymph nodes can be used to explain the intestinal lymphatic absorption of Hup-A SMEDDS. For Hup-A SMEDDS, the values of AUC and maximum plasma concentration(Cmax) of the blocking model were significantly lower than those of the control model(P<0.05). The proportion of lymphatic transport of Hup-A SMEDDS and Hup-A suspension were about 40% and 5%,respectively, suggesting that SMEDDS can significantly improve the intestinal lymphatic uptake and transport of Hup-A.

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期刊信息
  • 《安徽中医药大学学报》
  • 主管单位:安徽省教育厅
  • 主办单位:安徽中医药大学
  • 主编:周美启
  • 地址:合肥市梅山路103号安徽中医药大学
  • 邮编:230038
  • 邮箱:ahxbbjb@163.com
  • 电话:0551-65169048
  • 国际标准刊号:ISSN:2095-7246
  • 国内统一刊号:ISSN:34-1324/R
  • 邮发代号:26-23
  • 获奖情况:
  • 2012年荣获第四届中国高校优秀科技期刊,2012年荣获华东地区优秀期刊.
  • 国内外数据库收录:
  • 被引量:754