积雪草酸脂质纳米粒的大鼠口服吸收研究

Oral Absorption of Asiatic Acid Lipid Nanoparticles in Rats

目的考察大鼠口服积雪草酸纳米结构脂质载体(asiatic acid loaded nanostructured lipid carriers,AA-NLC)的口服吸收情况。方法建立清醒大鼠胆汁引流模型,按50 mg·kg?1的剂量灌胃给予AA-NLC和积雪草酸(asiatic acid,AA)原料(对照组),采用柱前衍生化HPLC检测胆汁药物浓度,考察AA纳米粒的吸收状况。结果大鼠口服AA-NLC后,药物排泄峰值Cmax是对照组的1.7倍,达峰时间Tmax显著慢于对照组(P<0.05),AA-NLC的消除慢于对照,其消除半衰期T1/2是对照组的2.7倍,与纳米粒吸收有关的药时曲线下面积AUC0-24 h与对照组相比提高了150%。结论新建立的口服吸收评价方法,初步评价AA-NLC大鼠灌胃后的吸收特性,AA制备成纳米结构脂质载体后可增加口服生物利用度。

OBJECTIVE To investigate oral absorption of asiatic acid loaded nanostructured lipid carriers（AA-NLC） in rats. METHODS Biliary drainage model was established in conscious rats and pre-column derivatization HPLC was used to determine the concentration of AA in bile after oral administration of AA-NLC and AA（the control group） to rats respectively at the dosage of 50 mg·kg^-1. The absorption of AA nanoparticles was evaluated by comparing the concentrations of drugs. RESULTS In vivo study showed that the Cmax of AA-NLC group was 1.7 times of the control group. The Tmax of AA-NLC group prolonged significantly（P0.05） in biliary excretion and the elimination half-life T1/2 was 2.7 times of the control group. And the AUC0→24 h increased to 150% compared to the control group. CONCLUSION The new assessment method can evaluate oral absorption of AA-NLC preliminarily. Nanostructured lipid carriers can increase the oral bioavailability of AA in rats.