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丹参酮类组分自乳化释药系统的肠吸收特征研究
  • ISSN号:0253-2670
  • 期刊名称:《中草药》
  • 时间:0
  • 分类:R944.9[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:[1]西南大学,重庆400065, [2]九江学院基础医学院,九江市转化医学重点实验室,江西九江332000, [3]重庆市中药研究院重庆市中药资源重点实验室,重庆400065
  • 相关基金:九江学院课题(2015LGYB13); 重庆市自然科学基金项目(cstc2012jj A1415); 江西省教育厅课题(20173020)
中文摘要:

目的探讨丹参酮脂溶性成分自乳化释药系统(TC-SEDDS)的肠吸收特征。方法采用大鼠在体单向肠灌流实验,以隐丹参酮、丹参酮I和丹参酮IIA 3个成分的吸收[吸收速率常数(Ka)和表观吸收系数(Papp)]为指标,研究其在十二指肠、空肠、回肠和结肠不同肠段的吸收情况;并考察不同药物质量浓度、P-糖蛋白(P-gp)抑制剂盐酸维拉帕米、多药耐药蛋白(MRP2)抑制剂丙磺舒和能量抑制剂2,4-二硝基苯酚对3个成分肠吸收的影响。结果隐丹参酮、丹参酮I和丹参酮IIA在小肠全肠段均有吸收,且小肠上段(十二指肠)的吸收最佳;隐丹参酮和丹参酮I的吸收在实验质量浓度范围内(1.05~4.19 mg/L和1.22~5.56 mg/L)具有浓度依赖性,丹参酮IIA的吸收不受质量浓度(2.43~11.126 mg/L)影响;盐酸维拉帕米对隐丹参酮和丹参酮I的吸收无明显影响,却显著提高了丹参酮IIA的吸收;丙磺舒显著增加了隐丹参酮和丹参酮I的吸收,对丹参酮IIA的影响不显著;2,4-二硝基苯酚均能显著降低3个成分的吸收。结论隐丹参酮和丹参酮I可能是MRP2的底物,不是P-gp底物。丹参酮IIA可能是P-gp底物,不是MRP2底物。3个成分的吸收均有能量的参与。隐丹参酮、丹参酮I和丹参酮IIA的吸收可能均有主动吸收过程。

英文摘要:

Objective To explore the intestinal absorption characteristics of tanshinone components self emulsifying drug delivery system(SEDDS). Methods In situ single-pass perfusion method was used to investigate the absorption characteristics of cryptonshinone, tanshinone I, and tanshinone II_A in rats. The absorption parameters(Ka, Papp) of cryptotanshinone, tanshinone I, and tanshinone II_A were used as indicators to study their optimum absorption site among duodenum, jejunum, ileum, and colon. The effects of verapamil hydrochloride(P-glycoprotein inhibitor, P-gp inhibitor), probenecid(multi-drug resistant protein MRP2), and 2, 4-dinitrophenol(energy inhibitor) on the absorption of cryptonshinone, tanshinone I, and tanshinone II_A were also studied, as well as the effects of their different concentration. Results Cryptonshinone, tanshinone I, and tanshinone II_A could be absorbed at all four intestinal segments, and the optimum absorption site was the upper segment of small intestine. The absorption of cryptotanshinone and tanshinone I were concentration-dependent at experimental concentration levels(1.05—4.19 mg/L and 1.22—5.56 mg/L), while tanshinone II_A was not affected obviously by its concentrations(2.43—11.12 mg/L). Verapamil hydrochloride had no significant influence on the absorption of cryptotanshinone or tanshinone I, while the absorption of tanshinone II_A was improved remarkably. Probenecid increased the absorption of cryptonshinone and tanshinone I apparently, while had no obvious effect on that of tanshinone II_A. 2,4-Dinitrophenol could decrease the absorption of cryptonshinone, tanshinone I, and tanshinone II_A apparently. ConclusionCryptonshinone and tanshinone I are supposed to be the substrate of MRP2 instead of P-gp. Tanshinone II_A is supposed to be the substrate of P-gp, instead of MRP2. The energy participated in the absorption of cryptonshinone, tanshinone I, and tanshinone II_A. Active absorption maybe also involved in the absorption of cryptonshinone, tanshino

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期刊信息
  • 《中草药》
  • 北大核心期刊(2011版)
  • 主管单位:天津市科委
  • 主办单位:中国药学会 天津药物研究院
  • 主编:汤立达
  • 地址:天津市南开区鞍山西道308号
  • 邮编:300193
  • 邮箱:zcy@tiprpress.com
  • 电话:022-27474913 23006821
  • 国际标准刊号:ISSN:0253-2670
  • 国内统一刊号:ISSN:12-1108/R
  • 邮发代号:6-77
  • 获奖情况:
  • 国家期刊奖,国家“双奖”期刊,1992年获国家科委、中共中央宣传部、国家新闻出版...
  • 国内外数据库收录:
  • 美国国际药学文摘,美国化学文摘(网络版),英国农业与生物科学研究中心文摘,波兰哥白尼索引,荷兰文摘与引文数据库,荷兰医学文摘,美国剑桥科学文摘,日本日本科学技术振兴机构数据库,中国中国科技核心期刊,中国北大核心期刊(2004版),中国北大核心期刊(2008版),中国北大核心期刊(2011版),中国北大核心期刊(2014版),英国英国皇家化学学会文摘,中国北大核心期刊(2000版)
  • 被引量:90909