川楝子炒制前后对大鼠在体肠吸收特性的影响

Effect of Toosendan Fructus on Intestinal Absorption in Rats Before and After Stir-Frying Process

目的:考察炒制前后川楝子提取物中的指标成分川楝素的大鼠肠吸收特性差异。方法:采用在体肠灌流模型,以川楝素为指标成分用HPLC法测定其浓度。结果:川楝素在大鼠十二指肠、空肠、回肠、结肠的吸收速率常数(Ka)依次为生川楝子提取物中(746.30±40.31)/s^(347.84±111.67)/s,炒川楝子提取物中(473.77±22.05)/s^(243.33±19.58)/s,川楝素在大鼠各肠段的药物表观渗透系数(Papp)依次为生川楝子提取物中(83.66±7.00)cm/s^(58.33±16.49)cm/s,炒川楝子提取物中(43.57±8.63)cm/s^(33.89±1.55)cm/s。结论:川楝子的指标成分川楝素在肠道中的吸收良好,生川楝子和炒川楝子中的川楝素在不同肠段的吸收存在差异,说明川楝子炒制会影响川楝素的肠道速率和药物表观渗透,从肠吸收角度初步揭示了川楝子炮制减毒的机理。

Objective： To investigate the difference of intestinal absorption for toosendanin extracted from Toosendan Fructus before and after stir-frying process. Methods： The intestinal perfusion in vivo model was used to determine the concentration of toosendanin by HPLC. Results： Absorption rate constant（ Ka） of toosendanin in duodenum,jejunum,ileum,and colon were in the range of（ 746. 30 ± 40. 31/s - 347. 84 ± 111. 67/s） in raw extract,（ 473. 77 ± 22. 05/s -243. 33 ± 19. 58/s） in extract of stir-frying Toosendan Fructus（ same amount of crude herb）,and（ 724. 93 ±57. 59/s - 290. 78 ± 41. 66/s） in extract of stir-frying Toosendan Fructus（ same amount of toosendanin）. In terms of permeability coefficient（ Papp） in each segment of the intestine,it was（ 83. 66 ± 7. 00 cm/s - 58. 33 ± 16. 49 cm/s） in raw extract,（ 43. 57 ± 8. 63 cm/s - 33. 89 ± 1. 55 cm/s） in extract of stir-frying Toosendan Fructus（ same amount to crude herb）,and（ 81. 67 ± 13. 00 cm/s - 51. 86 ± 5. 78 cm/s） in extract of stir-frying Toosendan Fructus（ same amount of toosendanin）. Conclusions： The index component of Toosendan Fructus,toosendanin,has good intestinal absorption. There was difference in intestinal absorption of toosendanin between raw Toosendan Fructus and stir-frying Toosendan Fructus with the same amount of raw herb; there was no significant difference in intestinal absorption with the same amout of toosendanin. The results showed after stir-frying process,the content of toosendanin had changed,thus to influence its intestinal absorption. This study initially revealed the attenuation mechanism of stir-frying process for Toosendan Fructus.