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The Absorption Mechanism of TCM Constitutes and Their Combination Dosage Form

机译:中药成分的吸收机理及其组合剂型

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@@To understand the GI transport mechanism and the interaction in vivo among TCM constitutes, some constitutes of TCM and their formulations were fully investigated based on the GI absorption and metabolism. Panax notoginseng Rg1, hydroxysafflor yellow A (HyA), ferulic acid (FA) and Chuangxiong essential oil (CEO) were studied in their physicochemiacl and biopharmaceutical properties. A new traditional Chinese combination preparation(TCCP) was developed according to constituents combination principle. In order to provide the reasonable basis, the difference of pharmacodynamics and pharmacokinetics between effective constituents group (SECG) of new TCCP and original TCCP (SXT), the later was composed of crude extracts Chuangxion root and red flower and the powder of panax notoginseng. Moreover, the pharmacodynamics of SECG was compared with SXT. The results demonstrated both preparations showed similar effect on anticogulated blood, antithrombus and myocardial preservation experiments. Their dose-response relationship and result of action are similar. However, some pharmacokinetics parameters of active ingredients had significant change after oral administration of different combinations of SXT constituents. The oral bioavailability of HyA, FA and Rg1 was improved by 6.056, 2.854 and 2.055 folds when CEO was co-administered (25 mg/kg), respectively. CEO can significantly decreased the transepithelial electrical resistance (TEER) and influenced the distribution and expression of Claudin-1 to open the tight junctions.
机译:为了了解胃肠道的转运机制和中药成分在体内的相互作用,根据胃肠道的吸收和代谢,对中药的一些成分及其配方进行了充分的研究。研究了三七Rg1,羟基红花黄A(HyA),阿魏酸(FA)和创熊精油(CEO)的理化特性和生物药学特性。根据成分组合原则,研制了一种新的中药复方制剂(TCCP)。为了提供合理的依据,新TCCP的有效成分组(SECG)与原始TCCP(SXT)的药效学和药代动力学之间的差异,后者由粗提取物创雄根和红色花以及三七粉组成。此外,比较了SECG和SXT的药效学。结果表明两种制剂对抗凝血液,抗血栓和心肌保存实验均显示相似的作用。它们的剂量反应关系和作用结果相似。但是,口服不同剂量的SXT成分组合后,活性成分的某些药代动力学参数发生了显着变化。联合使用CEO(25 mg / kg)时,HyA,FA和Rg1的口服生物利用度分别提高了6.056、2.854和2.055倍。 CEO可以显着降低跨上皮电阻(TEER),并影响Claudin-1的分布和表达以打开紧密连接。

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