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[摘要]
目的 对舌下含服和口服给予家兔治咳川贝枇杷滴丸(CBPP)后的入血成分进行定性和定量研究,旨在明确CBPP的药效物质基础,比较两种给药方式的差异。方法 UPLC-Q/TOF-MS法采用Waters ACQUITY UPLC BEH C18(100mm×2.1 mm,1.7 μm)色谱柱;流动相为乙腈(A)-0.05%甲酸水(B),梯度洗脱,体积流量为0.4 mL/min;质谱采用正、负离子扫描,扫描范围m/z 50~1500。舌下含服和口服两种给药方式分别给予家兔CBPP(200 mg/kg),给药后于不同时间点耳缘静脉取血0.5 mL,分离血浆,UPLC-Q/TOF-MS结合多元统计分析方法用于区分不同血浆样本,旨在寻找对分组贡献率较大的生物标志物(Marker)即为潜在的入血成分,并通过对其峰面积进行积分比较了两种给药方式下的相对含量。结果 在舌下含服和口服给药下的血浆中共解析出6种入血成分,定量结果表明该6种成分在体内达到最高值的时间均在1 h以内,且在各个时间点下舌下含服的血药浓度均大于口服给药。结论 从药效物质基础层面证明了舌下含服优于口服给药,为CBPP的进一步临床应用与发展提供依据。
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[Abstract]
Objective To carry out the qualitative and quantitative analysis of the components in plasma after oral and sublingual administration of Zhikechuanbeipipa dropping pills (CBPP).Methods An Waters ACQUITY UPLC BEH C18 (100 mm×2.1 mm, 1.7 μm) was used with 0.05% formic acid aqueous solution-acetonitrile as mobile phases by gradient elution. The metabolites were detected by electrospray ion (ESI) source in both positive and negative mode mode. Rabbits were dosed with CBPP (200 mg/kg) by oral and sublingual administration Blood samples of 0.4 mL were taken from auricular vein at different time points and plasma components and contents were determined by UPLC-Q/TOF-MS.Results A total of 6 components were identified in rabbit plasma, and the peak areas of all the 6 components in sublingual administration were higher than oral administration.Conclusion Sublingual administration is better than oral administration based on the material basis of CBPP, which will provide a basis for further clinical application and development of CBPP.
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