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三七总皂苷对大鼠阿司匹林药代动力学的影响。

Effect of Panax notoginseng saponins on the pharmacokinetics of aspirin in rats.

作者信息

Tian Zhihao, Pang Huanhuan, Du Shouying, Lu Yang, Zhang Lin, Wu Huichao, Guo Shuang, Wang Min, Zhang Qiang

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Chaoyang District, Beijing, People's Republic of China.

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Chaoyang District, Beijing, People's Republic of China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Jan 1;1040:136-143. doi: 10.1016/j.jchromb.2016.12.007. Epub 2016 Dec 6.

Abstract

Aspirin (ASA) is widely used to treat fever, pain, inflammation and cerebral infarction in clinic. Panax Notoginseng Saponins (PNS) is the extracts of Panax Notoginseng (PN)-a traditional Chinese medicine extensively used in cardiovascular diseases. Panax notoginseng saponins and ASA are both widely used to treat cerebral infarction in China. Good results in clinical practice have been achieved when the two drugs were taken together. To investigate the effect of PNS on ASA in vivo, the concentrations of salicylic acid (SA) in blood were measured after oral administration of ASA or ASA combined with PNS by UPLC-MS/MS. Sample preparation was carried out by the protein precipitation technique with an internal Saikosaponin A standard. The separation of two components was achieved by using an ACQUITY UPLC BEH C18 Column (1.7μm 2.1×100mm) by gradient elution using water (containing 0.2% formic acid) and acetonitrile (containing 0.2% formic acid) as the mobile phase at a flow rate of 0.2mL/min. The pharmacokinetic parameters were determined by using non-compartmental analysis. The results suggested that drug-drug interaction in vivo existed between PNS and ASA. The concentration of the SA was increasing when the two drugs were administered together. The transport of ASA and SA in MDCK -MDR1 cell monolayer was used to verify this conclusion. The values of apparent permeability coefficients (Papp) were significantly increased when the two drugs were used together. This result suggested PNS could increase the gastrointestinal tract absorption of ASA and SA. These findings provide more insight for wise use of two drugs to treat or prevent cardiovascular diseases.

摘要

阿司匹林(ASA)在临床上广泛用于治疗发热、疼痛、炎症和脑梗死。三七总皂苷(PNS)是三七(PN)的提取物,三七是一种广泛用于心血管疾病的传统中药。三七总皂苷和ASA在中国都广泛用于治疗脑梗死。两种药物联合使用时在临床实践中取得了良好效果。为了研究PNS在体内对ASA的影响,通过超高效液相色谱-串联质谱法(UPLC-MS/MS)测定口服ASA或ASA与PNS联合用药后血液中水杨酸(SA)的浓度。样品制备采用蛋白沉淀技术,以内标柴胡皂苷A为标准。使用ACQUITY UPLC BEH C18柱(1.7μm 2.1×100mm),以水(含0.2%甲酸)和乙腈(含0.2%甲酸)为流动相,流速为0.2mL/min,通过梯度洗脱实现两种成分的分离。采用非房室分析方法测定药代动力学参数。结果表明PNS与ASA在体内存在药物相互作用。两种药物联合使用时SA的浓度升高。利用ASA和SA在MDCK-MDR1细胞单层中的转运来验证这一结论。两种药物联合使用时,表观渗透系数(Papp)值显著增加。该结果表明PNS可增加ASA和SA在胃肠道的吸收。这些发现为合理使用这两种药物治疗或预防心血管疾病提供了更多的见解。

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