枳实总黄酮提取物中柚皮苷和新橙皮苷的大鼠药代动力学  

Pharmacokinetics of naringin and neohesperidin in the total flavanones of Zhishi extract in rats

作　　者：马雪琴[1] 李辰[1] 袁林华[1] 王世俊[1] 柳晓泉[1] 

机构地区：[1]中国药科大学药物代谢动力学研究中心,南京210009

出　　处：《中国药科大学学报》2013年第2期161-166,共6页Journal of China Pharmaceutical University

摘　　要：研究大鼠灌胃给予含相同剂量枳实总黄酮提取物、柚皮苷、新橙皮苷和柚皮苷-新橙皮苷后柚皮苷与新橙皮苷在大鼠体内的药代动力学。将SD大鼠随机分为4组,分别灌胃给予枳实总黄酮提取物(80 mg/kg)、柚皮苷(32 mg/kg)、新橙皮苷(27.2 mg/kg)、柚皮苷-新橙皮苷(柚皮苷32 mg/kg和新橙皮苷27.2 mg/kg),利用葡萄糖醛酸酶对血样进行预处理,采用LC-MS/MS法测定血浆中总苷元柚皮素及橙皮素,间接比较4组中柚皮苷和新橙皮苷的药代动力学。结果表明,枳实总黄酮提取物组中柚皮素和橙皮素的AUC0-t、cmax显著性高于柚皮苷单体组、新橙皮苷单体组,与柚皮苷-新橙皮苷组的主要药代动力学参数无显著性差异;柚皮苷-新橙皮苷组中柚皮素和橙皮素的AUC0-t、cmax较柚皮苷单体组、新橙皮苷单体组均有所增加,但增加程度低于枳实总黄酮提取物组。大鼠灌胃给药后,枳实总黄酮提取物中柚皮苷与新橙皮苷存在相互促进吸收的作用,而枳实总黄酮提取物中其他成分协同促进两者的吸收。The purpose of the study was to investigate the pharmacokinetic behaviour of naringin and neohesperidin in rats after oral administration of different groups of flavanones,including the total flavanones of Zhishi extract（ZS）,naringin（NA）,neohesperidin（NHE）,and naringin-neohesperidin（NA-NHE）.Twenty-four Sprague-Dawley rats divided into four groups were treated with ZS（80 mg/kg）,NA（32 mg/kg）,NHE（27.2 mg/kg）,and NA-NHE（NA 32 mg/kg and NHE 27.2 mg/kg）,respectively.By using β-glucuronidase,free naringenin and hesperetin were obtained from the naringenin-glucronaide and hesperetin-glucronaide in plasma,and the aglycons in plasma were determined by LC-MS/MS.The pharmacokinetic parameters of naringenin and hesperetin in these groups were evaluated to indicate the pharmacokinetics of naringin and neohesperidin in these groups.Comparing the pharmacokinetic parameters of naringenin and hesperetin in the ZS group with the monomeric group,the AUC0-t and cmax of naringenin and hesperetin increased significantly,while less difference with the NA-NHE group;the AUC0-t and cmax of naringenin and hesperetin in the NA-NHE group also increased more than the monomeric group with the enhancive extension less than those of ZS group.The result showed that naringin and neohesperidin accelerated their absorption degrees with each other in accord with other components in the total flavanones of Zhishi extraction.

关 键 词：总黄酮 枳实提取物 柚皮苷 新橙皮苷 柚皮素 橙皮素 药代动力学 

分 类 号：R285.5[医药卫生—中药学]