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

关键词:  积雪草酸  纳米结构脂质载体  胆汁引流模型  口服吸收

Key words:  asiatic acid  nanostructured lipid carriers  biliary drainage model  oral absorption

摘要:

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C_max是对照组的1.7倍，达峰时间T_max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T_1/2是对照组的2.7倍，与纳米粒吸收有关的药时曲线下面积AUC_{0-24 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。

Abstract:

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 C_max of AA-NLC group was 1.7 times of the control group. The T_max of AA-NLC group prolonged significantly(P<0.05) in biliary excretion and the elimination half-life T_1/2 was 2.7 times of the control group. And the AUC_{0→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.