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目的:研究川芎嗪在大鼠小肠的吸收动力学,考察不同浓度药物和黄芪提取物对其吸收速率的影响以及相关参数的变化。方法:运用大鼠在体肠循环实验,HPLC法研究川芎嗪在大鼠小肠中的吸收情况,并考察黄芪提取物对其吸收的促进作用。结果:不同浓度川芎嗪(0.2,0.4,0.8 mg.mL-1)在大鼠小肠的吸收速率常数分别为(0.243 4±0.001 3),(0.185 6±0.003 1),(0.074 6±0.003 9)h-1,进行Newman-Keuls法检验,药物浓度不同时川芎嗪肠吸收速率常数有差异显著性;0.2mg.mL-1川芎嗪溶液加入不同量黄芪提取物(0.5,1,2,3 mL)后的吸收速率常数分别为(0.246 4±0.004 6),(0.271 7±0.002 3),(0.289 4±0.001 3),(0.244 2±0.011 4)h-1,与未加黄芪提取物组进行Newman-Keuls法检验,川芎嗪吸收速率常数差异有显著性。结论:川芎嗪在大鼠小肠的吸收速率随着浓度的逐渐增加而减小,其在小肠内的吸收机制除了被动扩散之外,可能有主动转运、易化扩散等因素;黄芪可促进川芎嗪的大鼠肠吸收,且黄芪浓度对大鼠肠吸收的存在一定的影响。
OBJECTIVE: To study the absorption kinetics of tetramethylpyrazine in the small intestine of rats and investigate the effects of different concentrations of drug and astragalus extract on its absorption rate and the related parameters. Methods: The rat intestine circulation experiment was used to study the absorption of tetramethylpyrazine in rat intestine by HPLC and the promotion effect of astragalus extract on its absorption. Results: The absorption rate constants of tetramethylpyrazine (0.2,0.4,0.8 mg.mL-1) in rat intestine were (0.243 4 ± 0.001 3), (0.185 6 ± 0.003 1), (0.074 6 ± 0.0039 ) h-1, Newman-Keuls test was carried out. The intestinal absorption rate constants of ligustrazine were significantly different at different drug concentrations. 0.2mg.mL-1 ligustrazine solution was added with different amounts of astragalus extract (0.5,1,2,3 mL) were 0.246 4 ± 0.004 6, 0.2791 ± 0.0023, 0.289 4 ± 0.001 3 and 0.244 2 ± 0.011 4 h-1, respectively, which were similar to those of the extracts without Astragalus membranaceus Group Newman-Keuls test, ligustrazine absorption rate constant difference was significant. Conclusion: The absorption rate of tetramethylpyrazine in the small intestine of rats decreased with the increase of concentration, and the absorption mechanism of ligustrazine in the small intestine may be active transport, diffusion and other factors in addition to passive diffusion; Astragalus can promote tetramethylpyrazine Of rat intestinal absorption, and the concentration of Astragalus on intestinal absorption of rats there is a certain impact.