目的 研究血塞通分散片和普通片在比格犬体内的药动学。方法 采用双周期交叉试验,6只比格犬分别单剂量口服100 mg血塞通分散片和普通片,测定比格犬血浆中人参皂苷Rb1和Rg1的浓度来比较血塞通分散片和普通片的药动学参数。结果 血塞通分散片在比格犬血浆中人参皂苷Rb1和Rg1的达峰浓度显著高于血塞通普通片,血塞通分散片在比格犬血浆中人参皂苷Rg1的达峰时间显著早于血塞通普通片,Rb1的达峰时间也有提前的趋势,这符合分散片剂型在体内崩解迅速和吸收快的制剂特点。结论 2种制剂中人参皂苷Rb1和Rg1在比格犬血浆中的暴露基本相当,无显著性差异。但血塞通分散片中主要成分人参皂苷Rb1和Rg1的ρmax显著高于薄膜衣片,而达峰时间显著缩短,有利于药物更快的起效。
Abstract
OBJECTIVE To compare the pharmacokinetic parameters of Xuesaitong dispersible tablets and common tablets in Beagle dogs. METHODS Using double cycle crossover trial, six Beagle dogs were treated with single oral dose of 100 mg of Xuesaitong dispersible tablets and conventional tablets and determining the pharmacokinetic parameters of ginsenoside Rb1 and Rg1 in Xuesaitong dispersible tablets and conventional tablets in Beagle dog plasma. RESULTS The ginsenoside Rb1 and Rg1 peak concentration of Xuesetong dispersible tablets in Beagle dog plasma was significantly higher than that of Xuesaitong tablets, the ginsenoside Rg1 peak time of Xuesaitong dispersible tablets in Beagle dog plasma was significantly earlier than that of Xuesaitong tablets. Additionally, the ginsenoside Rb1 peak time exhibited ahead of the trend, which is in line with the characteristics of rapid disintegration and absorption of preparation in vivo. CONCLUSION The plasma exposure in two preparation of ginsenoside Rb1 and Rg1 in Beagle dog holds fairly basic and no significant difference. But the ρmax of the main ingredients of Panax ginseng saponins Rb1 and Rg1 in Xuesaitong dispersed tablets, is significantly higher than that of the film coated tablets, and peak time is significantly shortened, which could promote the drug absorption.
关键词
三七总皂苷 /
高效液相色谱-串联质谱法 /
药动学
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Key words
Panax notoginseng saponin /
LC-MS /
pharmacokinetics
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中图分类号：
R969.1
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参考文献
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脚注
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基金
云南省科技计划生物医药重大科技专项资助项目(2016RA036)
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