三七皂苷R1和人参皂苷Rg1的大鼠在体肠吸收动力学研究

 目的研究三七皂苷R₁和人参皂苷Rg₁在大鼠胃肠道的吸收动力学,并考察不同的药物浓度和常用的吸收促进剂对其吸收速率的影响。方法进行大鼠在体肠循环实验,研究三七皂苷R₁和人参皂苷Rg₁在胃肠道的吸收情况,并分别考察十二烷基硫酸钠、卡波姆和冰片对吸收的促进作用。结果三七皂苷R₁在胃、十二指肠、空肠、回肠的吸收速率分别为0.056,0.114,0.076,0.085 h^-1,人参皂苷Rg1则为0.052,0.121,0.065,0.055 h^-1;三七皂苷R₁在低、中、高3个浓度下的吸收速率分别为0.122,0.095,0.090 h^-1,人参皂苷Rg1则为0.117,0.113,0.109 h^-1;对不同种类和不同浓度的十二烷基硫酸钠、卡波姆和冰片的促吸收结果进行统计学检验,结果卡波姆和冰片能显著提高肠吸收速率,而十二烷基硫酸钠则没有作用。结论三七皂苷R₁和人参皂苷Rg₁在小肠上段吸收速率较大,而在胃中吸收速率较小;其吸收速率随着浓度的增加而逐渐减小,药物在小肠中的吸收不呈现一级动力学过程,吸收机制除了被动扩散以外,可能还有易化扩散和主动转运;卡波姆和冰片对它们在小肠的吸收有显著促进作用。

Studies on Absorption Kinetics of Sanchinoside R1 and Ginsenoside Rg1 in Rat Intestine

OBJECTIVE To investigate the absorption kinetics of sanchinoside R₁ and ginsenoside Rg₁ at different intestinal segments of rats and the influence of concentration and co-administration with absorptive promoter on the absorptive kinetics.METHODS An in situ intestinal perfusion model was employed to investigate systemically the absorptive kinetics of sanchinoside R₁ and sanchinoside Rg₁.RESULTS The absorptive rate constants(K_a) of sanchinoside R₁ were 0.056, 0.114,0.076,0.085 h^-1,and the ka of qinsenoside were 0.052,0.121,0.065,0.055 h^-1 at gastric,jejunum,duodenum,ileum,respectively.The K_a of sanchinoside R₁ at the concentrations of 0.02,0.2,2 g·L^-1 were 0.122,0.095,0.090 h^-1,and the K_a ginsenoside Rg₁ were 0.117,0.113,0.109 h^-1,respectively.The K_a,while being co-administered with carbomer and borneol,were significantly higher than that of references group.CONCLUSION Sanchinoside R₁ and ginsenoside Rg₁ are well absorbed at the superior segment of intestine in rats.With the decrease of sanchinoside R₁ and ginsenoside Rg₁ concentration,the absorption rate is increased,their absorption was is first-order process,besides the passive diffusion mechanism,facilitated diffusion and active transport may also take part in the transport process.Carbomer and borneol significantly increase the absorptive rate in intestine.