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 investigate the absorption kinetics of tetramethylpyrazine(TMP) at small intestine of rats and the influence of concentration and Astragalus extract on the absorption kinetics and the changes of the related parameters. METHODS Using rat's in vivo intestinal circulation experiment and HPLC to investigate the effects of TMP's absorption at small intestine of rats, and investigate the stimulative effect of Astragalus extract on the absorption of TMP. RESULTS The absorptive rate constants (N) of TMP at the concentration of 0. 2,0. 4,0. 8 mg.mL-1 were (0. 243 4 ± 0. 001 3), (0. 185 6 ± 0. 001 3), (0. 074 6 ± 0. 003 9)h ' ;while adding different quantity of Astragalus extract to the concentration of 0. 2 mg.mL-1 of TMP, the K of TMP was (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 '. CONCLUSION Along with the decrease of the concentration, the absorption rate of TMP was increased, the absorption of TMP was first - order process. Besides the passive diffusion mechanism, facilitated diffusion and active transport may also take part in the transport process; Astragalus extract could promote the absorption of TMP at small intestine of rats, the concentration of Astragalus extract had some effects on the absorption of TMP.