葛根素自微乳在大鼠体内药代动力学分析  

Pharmacokinetics of Puerarin Self-microemulsions in Rats

作　　者：陈顺尧[1] 雷凯君[1] 吴颖欣[1] 王汝上 

机构地区：[1]广东省佛山市中医院,广东佛山528000 [2]广州康臣药物研究有限公司,广州510530

出　　处：《中国实验方剂学杂志》2014年第10期106-108,共3页Chinese Journal of Experimental Traditional Medical Formulae

摘　　要：目的：考察葛根素自微乳在大鼠体内的血药浓度经时过程，评价葛根素自微乳的药代动力学及相对生物利用度。方法：单剂量给予大鼠葛根素自微乳和葛根素混悬液，采用HPLC测定血浆中葛根素质量浓度，检测波长250 nm，流动相甲醇（A）-0.1%磷酸水溶液（B）梯度洗脱（0-30 min，20%-25%A；30-40 min，25%-40%A；40-50 min，40%A），运用DAS 2.1.1程序拟合药物浓度-时间曲线，计算药代动力学参数及生物利用度。结果：葛根素自微乳和混悬液的t_max分别为0.71，1.1 h，C_max分别为2.052，1.120 mg·L^-1，AUC_0-24 h依次为2.901，2.013 mg·hL^-1，葛根素自微乳相对于混悬液的生物利用度144.11%。结论：与葛根素混悬液相比，葛根素自微乳能显著提高葛根素在大鼠体内的生物利用度。Objective： To estabolish a quantitative analysis method for pharmacokinetics and bioavailability of puerarin self-microemulsions in rats. Method： Puerarin self-microemulsions and suspensions were given by a single dose,HPLC was adopted to determine the concentration of puerarin in plasma with detection wavelength at 250 nm and mobile phase of methanol（A）-0.1% phosphoric acid solution（B） for gradient elution（0-30 min,20%-25%A;30-40 min,25%-40%A;40-50 min,40%A）,pharmacokinetics parameters and bioavailability was calculated by DAS 2.1.1 programs. Result： t_max of puerarin self-microemulsions and suspensions were 0.71,1.1 h,C_max were 2.052,1.120 mgL-1,AUC_0-24 h were 2.901,2.013 mg·hL^-1, respectively.Relative bioavailability of puerarin self-microemulsions to suspensions was 144.11%. Conclusion： Compared with puerarin suspensions,puerarin self-microemulsion could significantly improve bioavailability in rats.

关 键 词：葛根素 自微乳 药代动力学 生物利用度 

分 类 号：R283.6[医药卫生—中药学] R945[医药卫生—中医学]