摘要
目的：研究黄芩苷灌胃给药经兔眼血-房水屏障的通透性。方法：建立测定黄芩苷兔眼房水和血浆药物浓度的HPLC方法，色谱条件：Diamonsil C18色谱柱（200mm×4．6mm，5μm）；流动相为甲醇-0．2％磷酸溶液（47：53）；流速为1．0mL·min^-1；检测波长为279nm；柱温为35℃；以对二甲氨基苯甲醛为内标物。健康纯种日本长耳白兔单剂量灌胃黄芩苷80mg·kg^-1后，比较不同时间兔眼房水和血浆药物浓度，绘制药物浓度-时间曲线，用3p87药动学软件计算黄芩苷在房水和血浆中的药动学参数。结果：在本色谱条件下，黄芩苷在房水和血浆中的线性范围分别为0．02～0．25和0．0125～24．0mg·L^-1，相关系数（r）分别为0．9968和0．9982。黄芩苷在房水中的AUC0-12h显著低于血浆[（0．639±0．067）vs（80．1±2．1）h·mg·L^-1，P〈0．01]，各个时间点比较，黄芩苷在房水中的质量浓度均显著低于其血浆中的质量浓度（P〈0．01）。结论：黄芩苷经灌胃给药较难通过血-房水屏障进入眼内。
Objective：To study the ability of baicalin penetrating blood-aqueous barrier after intragastric administration in rabbits. Methods： An HPLC method for determining baicalin level in aqueous humor and plasma was established. The HPLC condition was as follows： a Diamonsil C18 column （200 mm × 4.6 mm,5 μm） , the mobile phase composed of methanol and 0.2% phosphate （47： 53） , a 279 nm UV detector, a column temperature of 35 ℃ , and a flow rate of 1.0 mL·min^-1 , and an internal standard of p-dimethylaminobenzaldehyde. Mean baicalin concentration-time curve was piloted after single dose of baicalin 80 mg·kg^-1 , and the pharmacokinetic parameters were evaluated using 3p87 statistic software. Results： The linear ranges of baicalin in aqueous humor and plasma were 0.02-0.25 mg·L^-1（r=0.9968） and0.0125 -24.0mg·L^-1（r=0.9968）, respectively. The AUC of baiealin was markedly lower in aqueous humor than in plasma [ （0.639±0.067） vs （80.1±2.1） h·mg·L^-1 ,P 〈 0.01 ] ; the concentration of baicalin was also significantly lower in aqueous humor than in plasma at all the designed time points （P 〈 0.01 ）. Conclusion： The ability of baiealin penetrating blood-aqueous barriers into the eye is very poor after intragastric administration.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2008年第13期1134-1137,共4页
Chinese Journal of New Drugs
基金
黑龙江省中医药管理局科研项目(060018)
