灯盏乙素溶液剂混悬剂在大鼠体内动力学比较与研究.pdfVIP

灯盏乙素溶液剂与混悬剂在大鼠体内动力学的比较研究 1* 2 2 1 郝秀华 ,邹梅娟 ,程刚 杨锦竹 （1. 吉林大学药学院药剂教研室，长春 130021 ；2 沈阳药科 大学药学院药剂教研室，沈阳 110016 ） 摘要：目的 研究灯盏乙素溶液剂与混悬剂在大鼠体内的药动学，探讨其在大鼠体内的 动力学特征。方法 建立高效液相色谱法测定血浆中灯盏乙素及水解后苷元浓度的变化， 应用3P87药动学程序对血药浓度数据进行拟合。结果 灯盏乙素及其苷元在0.11～8.66 nmol·mL-1浓度范围内呈良好线性关系，其相关系数r分别为0.9998和0.9968，提取平均 回收率为91.0 ％和96%，日内、日间RSD15％。灯盏乙素药时曲线符合一室开放模型。 灯盏乙素混悬剂和溶液剂的绝对生物利用度分别为4.9%和5.6% 。结论 灯盏乙素溶液剂 与混悬剂在大鼠体内动力学参数tmax ，t1/2、AUC没有明显区别。 关键词：灯盏乙素；溶液剂；混悬剂；药动学 中图分类号：R969 文献标识码：A 文章编号： Pharmacokinetics in Rats after Intragastric Administration of Scutellarin Solution and Suspension 1* 2 2 1 HAO Xiu-hua , ZOU Mei-juan , CHENG Gang YANG Jin-zhu (1 Jilin University, Changchun 130021, China; 2. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China) ABSTRACT: OBJECTIVE To consult the Pharmacokinetic characteristics of scutellarin in rats by comparing the pharmacokinetics of scutellarin Solution and suspension. METHODS Reverse phase chromatography was developed to determine the concentration of scutellarin and scutellarein in plasma. The data of plasma concentration was fitted by 3P87. RESULTS The standard curves for scutellarin and scutellarein showed linearity (r=0.9998, r=0.9968) over the selected concentration range from 0.11 to 8.66 nmol·mL-1 . The average recoveriy of scutellarin and scutellarein were about 91%, 96% respectively. The within-day and between-day precisions were less than 15%. The plasma concentration–time curve of scutellarin was best conformed to one-compartment open model. The absolute bioavailability of scutellarin solution and suspension were 4.9% and 5.6%, respectively. CONCLUSION There is no difference of the pharmacokinetic parameters tmax, t1/2 and AUC bet