山楂叶总黄酮磷脂复合物大鼠在体肠吸收动力学研究

Study on the Adsorption Kinetics of Hawthorn Leaves Flavonoids Phospholipids Complex in Rats Intestine

关键词:  山楂叶总黄酮  磷脂复合物  肠吸收  在体循环肠灌流模型

Key words:  hawthorn leaves flavonoids  phospholipid complex  intestinal absorption  intestinal recirculating perfusion

摘要:

目的 研究山楂叶总黄酮磷脂复合物的大鼠在体小肠吸收动力学特征。方法 采用大鼠在体肠单向灌流模型，以山楂叶总黄酮原料药为对照，采用分光光度法测定灌流液中总黄酮含量，计算肠吸收速率常数(Ka值)与单位时间吸收转化率(A值)，考察药物浓度与pH值对山楂叶总黄酮磷脂复合物肠吸收的影响。结果 浓度为0.1 mg·mL^?1的山楂叶总黄酮和山楂叶总黄酮磷脂复合物，Ka值与A值分别为0.010 9 h^?1，1.20%和0.039 1 h^?1，3.73%；药物浓度为0.1 mg·mL^?1，pH为6.0，7.4，8.0的肠循环液，山楂叶总黄酮和山楂叶总黄酮磷脂复合物的Ka值分别为0.007 6，0.010 9，0.005 6 h^?1和0.037 6，0.039 1，0.030 5 h^?1，A值分别为0.69%，1.20%，0.42%和3.19%，3.73%，2.81%；表明在总黄酮浓度和溶液pH相同条件下，山楂叶总黄酮磷脂复合物的大鼠在体肠吸收明显优于山楂叶总黄酮。结论 磷脂固体分散技术可改善山楂叶总黄酮的小肠吸收。

Abstract:

OBJECTIVE To study the adsorption kinetics of hawthorn leaves flavonoids phospholipids complex (HLF-PPC) in rats intestine. METHODS The in situ rat single-pass intestinal perfusion model was used. The concentration of the index component of HLF-PPC, flavonoids in the perfusate were determined by spectrophotometry, the absorption constant (Ka) and absorption conversion rate in time unit (A) were calculated, and the effects of drug content and pH value were investigated. RESULTS Drug concentration of HLF and HLF-PPC were 0.1 mg·mL^?1, the Ka and A values were 0.010 9 h^?1, 1.20% and 0.039 1 h^?1, 3.73%; and when the drug concentration of HLF and HLF-PPC were 0.1 mg·mL^?1, in pH 6.0, 7.4 or 8.0 of the intestinal loop solution, the Ka values were 0.007 6, 0.010 9, 0.005 6 h^?1 and 0.037 6, 0.039 1, 0.030 5 h^?1, A values were 0.69%, 1.20%, 0.42% and 3.19%, 3.73%, 2.81%, respectivly. That showed the intestinal absorption in rats of HLF-PPC was obviously better than HLF in the same drug concentration and pH value. CONCLUSION The solid dispersion technology of phospholipid can improve the intestinal absorption of HLF.