摘要
目的 测定 ip葛根素后不同时间新西兰白兔视网膜组织中葛根素含量 ,计算其药动学参数 ,研究药动学特点。方法 4 4只家兔随机分为 11组 ,各组每只家兔 ip葛根素 80 m g/ kg加等量 5 %葡萄糖液 ,在用药前 (0 h)和用药后 0 .5、1、2、3、4、6、8、12、16、2 4 h取视网膜组织 ,采用反相高效液相色谱法 (RP- HPL C)进行测定 ,3P87软件拟合药动学参数。结果 ip葛根素后在兔视网膜组织中药动学符合开放式二房室模型 ,药动学参数理论值为 :Cmax=1.0 8μg/ mg,tmax=1.5 2 h,t1 / 2α=1.0 2 h,t1 / 2β=7.37h,CL =2 .6 7g/ h,AUC=6 .89μg/ (h· m g)。实测值为 :30 min时视网膜中葛根素的量为 (0 .0 6± 0 .0 2 ) μg/ mg,在 2 h达到高峰 Cmax为 (0 .2 1± 0 .0 5 ) μg/ mg,随后逐渐下降 ,8h降至较低为 (0 .0 2± 0 .0 0 )μg/ mg。结论 本方法特异、准确、灵敏 ,可用于视网膜组织中葛根素含量测定 ,葛根素通过 ip给药能透过血 -视网膜屏障 ,进入视网膜组织。
Object To determine the concentration and pharmacokinetic changes of puerarin in retinal tissue of rabbits by ip administration. Methods Forty-four rabbits were randomly divided into 11 groups. Puerarin (80 mg/kg) in addition of 5% glucose solution was given by ip administration to each rabbit in every groups. After administration, the retinal tissue was collected at different time points such as 0 h pre-administration and 0.5, 1, 2, 3, 4, 6, 8, 12, 16, and 24 h post-administration and the concentration of puerarin was detected by RP-HPLC. The pharmacokinetic parameter was fitted by 3P87 software. Results The pharmacokinetics of puerarin in the retinal tissue was subjected to the two-compartment open model. The pharmacokinetic parameters were separately as following: C max=1.08 μg/mg, t max=1.52 h,t 1/2 α=1.02 h, t 1/2 β=7.37 h, CL=2.67 g/h, AUC=6.89 μg/(h·mg). The practical data of the concentration of puerarin in retinal tissue was (0.06±0.02) μg/mg at 30 min and maximum concentration was (0.21±0.05) μg/mg at 2 h, respectively. Then the concentration of puerarin in retinal tissue was gradually decreased to the lower level (0.02±0.00 μg/mg) at 8 h. Conclusion The method of RP-HPLC is particular, accurate, and sensitive. The puerarin by ip administration can penetrate the blood-retina barriers and enter the retinal tissue.
出处
《中草药》
CAS
CSCD
北大核心
2004年第12期1382-1384,共3页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金资助项目 (3 0 3 0 0 467)
广东省自然科学基金资助项目 (0 10 765 )
关键词
葛根素
药动学
视网膜
puerarin
pharmacokinetics
retina
