中链脂肪酸对木通皂苷D大鼠经口吸收的影响

Influence of medium chain fatty acid on oral absorption of Akebia saponin D in rats

目的考察不同碳链长度的中链脂肪酸对木通皂苷D大鼠经口吸收的影响。方法将SD大鼠随机分为5组,灌胃给予木通皂苷D水溶液,溶液中含不同种类和浓度的脂肪酸钠,每组木通皂苷D的给药剂量为100 mg/kg,各组中脂肪酸钠的给药剂量如下:不含脂肪酸、辛酸钠200 mg/kg、癸酸钠200 mg/kg、月桂酸钠200 mg/kg和癸酸钠1000 mg/kg,于不同时间点眼眶取血,用液相色谱-串联质谱(LC-MS/MS)法检测血浆中药物浓度。结果在给药后1 h内脂肪酸钠对木通皂苷D大鼠经口吸收有明显的促进作用,各组的血药浓度在给药后20 min最高,随着时间的延长迅速下降;剂量为200 mg/kg时,辛酸钠对木通皂苷D大鼠经口吸收促进作用最强。1000 mg/kg癸酸钠对木通皂苷D大鼠经口吸收促进作用较200 mg/kg强,且木通皂苷D血药浓度随着时间延长下降得更为缓慢。结论碳链为8(辛酸钠)、10(癸酸钠)和12(月桂酸钠)的脂肪酸盐对木通皂苷D大鼠经口吸收有明显的促进作用,癸酸钠给药剂量的提高有利于其经口吸收促进作用的维持。

Objective To investigate the influence of the medium chain fatty acid（MCFA） on the oral absorption of the Akebia saponin D. Methods The SD rats were randomized into 5 groups. Dose of 100 mg/kg Akebia saponin D was administered by gastrointestinal tract. The dosages of MCFA in each group were as follows ： no MCFA, 200 mg/kg sodium caprylate, 200 mg/kg sodium caprate, 200 mg/kg sodium laurate, and 1000 mg/kg sodium caprylate. Blood samples were collected at different intervals after administration through orbit vein. Plasma drug concentration was detected by LC-MS/MS. Results After Akebia saponin D was administered within one hour, MCFA had obvious promoting effect on the oral absorption of Akebia saponin D. The drug plasma concentration in each group was the highest at 20 min, and decreased fast with the time. Sodium caprylate was the best absorption promoter when the dosage was 200 mg/kg. The absorption promoting effect of 1000 mg/kg sodium caprate was better than that of 200 mg/kg, and the plasma drug concentration decreased more slowly. Conclusion MCFA with the chain length of 8（ sodium caprylate） , 10（ sodium caprate）, and 12（ sodium laurate） has obvious promoting effect on the oral absorption of Akebia saponin D in rats. The improvement of adminitration dosage is profitable for maintaining the drug oral absorption effect.