黄芩苷及其磷脂复合物与自微乳在大鼠体内的药动学比较性研究  

Comparative pharmacokinetic study of baicaline,baicalin-phospholipid complex,and self-microemulsifying drug delivery systems of baicalin-phospholipid and baicalin in rats

作　　者：刘昌顺[1] 龙晓英[1] 梁浩明[1] 袁飞[1] 

机构地区：[1]广东药学院中药学院,广州510006

出　　处：《中国新药杂志》2015年第2期195-198,211,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30973953C1909)

摘　　要：目的：比较黄芩苷（baicalin,BA）、黄芩苷磷脂复合物（baicalin-phospholipid complex,BA-PC）、黄芩苷磷脂复合物的自微乳给药系统（self-microemulsifying drug delivery systems of baicalin-phospholipid,BAPC-SMEDDS）和黄芩苷自微乳给药系统（self-microemulsifying drug delivery systems of baicalin,BA-SMEDDS）在大鼠体内的药动学,预测BA-PC-SMEDDS提高药物生物利用度的能力。方法：用相当于BA有效成分剂量为68 mg·kg^-1的BA,BA-PC,BA-PC-SMEDDS和BA-SMEDDS,对大鼠进行口服给药和眼眶取血,HPLC色谱法测定血浆中BA的含量。结果：BA体内的药时曲线具有明显双峰现象,较BA单一成分,BA-PC,BA-PCSMEDDS与BA-SMEDDS的血浆浓度均有增加,Cmax分别为BA本身的3.89,6.70和11.01倍。BA-PC的AUC0～24h为BA的2.46倍,BA-PC-SMEDDS的AUC0～24h为78.19μg·h·m L^-1,比BA-PC促进BA的吸收提高了2.38倍。但却发现BA-SMEDDS的AUC0～24h高达96.02μg·h·m L^-1,显示其促进BA吸收有更強的能力。结论：BA-PC,BA-PC-SMEDDS和BA-SMEDDS显著增加了BA的吸收。BA-PC-SMEDDS进一步改善了BAPC促进BA吸收的能力,BA-SMEDDS较其他BA制剂促进BA的吸收更強。Objective： To compare the pharmacokinetics of baicalin（ BA）,baicalin-phospholipid complex（ BA-PC）,self-microemulsifying drug delivery systems of baicalin-hospholipid complex（ BA-PC-SMEDDS） and baicalin（ BA-SMEDDS） in rats,and evaluate the ability of BA-PC-SMEDDS to improve bioavailability. Methods：BA,BA-PC,BA-PC-SMEDDS,and BA-SMEDDS were orally administered to rats at the equivalent dose of BA of 68mg·kg^-1,orbital blood smaples were taken,and the concentration of BA in plasma was determined by HPLC. Results： The pharmacokinetic curve of BA has obvious double peaks. The peak plasma concentrations（ Cmax） of BAPC,BA-PC-SMEDDS,and BA-SMEDDS groups were enhanced by 3. 89,6. 70,and 11. 01 folds,respectively,compared with the BA group. The area under the curve（ AUC0-24h） of BA-PC was 2. 46 times of that in BA group,and the AUC0-24 hvalue of BA-PC-SMEDDS was 78. 19 μg·h·m L^-1,which further increased about 2. 38 folds compared to that of BA-PC. Interestingly,it was found that the AUC0-24 hvalue of BA-SMEDDS was up to 96. 02 μg·h·m L^-1,indicating that it was the best formulation to improve the bioavailability of BA among the investigated preparations.Conclusion： BA-PC,BA-PC-SMEDDS,and BA-SMEDDS significantly increased the absorption of BA. BA-PCSMEDDS further improved the ability of BA-PC to promote the BA absorption,and BA-SMEDDS showed the besteffect on promoting BA uptake compare with other preparations.

关 键 词：黄芩苷 自微乳 磷脂复合物 药动学 

分 类 号：R969.1[医药卫生—药理学]