玳玳果黄酮降脂滴丸大鼠体内口服生物利用度及药动学研究  

Pharmacokinetics and Bioavailability in Vivo Rats of Daidai Flavonoids Lipid-Lowering Dropping Pills

作　　者：连赟芳[1] 陈丹[1] 廖淑彬 谢平[1] 黄娇[1] 朱仙慕 马国萍[1] 陈红[2] 

机构地区：[1]福建中医药大学药学院,福州350122 [2]福建省立医院干一科老年病研究所,福州350001

出　　处：《中国药学杂志》2017年第13期1171-1176,共6页Chinese Pharmaceutical Journal

基　　金：福建省战略性新兴产业发展专项产业技术开发项目资助(闽发改高技[2011]1598号);福建省科技计划项目资助(2010Y2004);福建省医学创新项目资助(2016-CX-45)

摘　　要：目的建立UPLC-MS同时测定大鼠血浆中玳玳果黄酮降脂滴丸药效组分新橙皮苷和柚皮苷的定量分析方法,比较玳玳果黄酮降脂滴丸与玳玳果总黄酮降脂提取物在大鼠体内的药动学特性。方法采用UPLC-MS联用分析技术,测定大鼠血药浓度及拟合药-时曲线;大鼠分别灌胃给药玳玳果总黄酮降脂提取物、玳玳果黄酮降脂滴丸,分析比较其体内药动学过程,考察玳玳果黄酮降脂滴丸口服生物利用度的改善情况。结果药动学试验结果表明,含药血浆中新橙皮苷的ρ_(max)分别为(1.68±0.02)_(提取物)和(5.54±0.09_(滴丸)mg·L^(-1),柚皮苷的ρ_(max)分别为(1.50±0.05)提取物和(4.83±0.10_(滴丸)mg·L^(-1),玳玳果黄酮降脂滴丸的ρmax、AUC_(0-∞)显著高于玳玳果总黄酮降脂提取物(P<0.05);滴丸的MRT、t_(1/2)相比于玳玳果总黄酮降脂提取物明显缩短;以玳玳果总黄酮降脂提取物为参比,滴丸中新橙皮苷和柚皮苷的相对生物利用度分别提高了278.52%和258.59%。结论玳玳果黄酮降脂滴丸明显改善了玳玳果总黄酮降脂提取物中药效成分新橙皮苷和柚皮苷的口服生物利用度。OBJECTIVE To establish an UPLC-MS method for simultaneously determining the contents medical components of neohespiridin and naringin in rat plasma, meanwhile to investigate the pharmacokinetics for Daidai flavonoids lipid-lowering dropping pills and Daidai flavones extraction were compared in rats. METHODS We are established an UPLC-MS method to simultaneously determine the content of effective components（ neohesperidin and naringin） of Daidai fruit flavones lipid-lowering dropping pills in rat plasma, measured blood drug concentration in rats, fitted medicine curve, analyzed and compared the pharmacokinetic process in vivo of Daidai fruit flavones lipid-lowering dropping pills and Daidai fruit flavonoids extracts, to evaluate the oral bioavailability improvement of Daidai fruit flavones lipid-lowering dropping pills. RESULTS The pharmacokinetics experimental results of rat gastric drug delivery with Daidai fruit flavonoids extract compared with that of rat with Daidai fruit flavones lipid-lowering dropping pills showed that the ρmax of neohesperidin in medicated serum is （1.68 ± 0. 02） extract and（5.54 ± 0. 09） dropping pills mg ·L^-1, respectively; the ρmax of naringin is（ 1.50 ±0.05） and（4. 83 ±0. 10） dropping pills mg ·L^-1 , respectively; the Pmax and AUC0-∞ of Daidai fruit flavones lipid-lowering dropping pills were significantly higher than that of Daidai fruit flavonoids extraction（ P 〈 0. 05 ）, and MRT and t,/2 of Daidai fruit flavones lipid-lowering dropping pills were significantly shorter than that of Daidai fruit flavonoids extracts. With Daidai fruit flavonoids extract as reference, the relative bioavailability of neohesperidin and naringin in dropping pills were 278.52% and 258.59% , respectively. CONCLUSION Daidai flavones dropping pill can significantly improve the medical components of neohespiridin and naringin oral bioavailability of Daidai flavones extraction.

关 键 词：玳玳果黄酮降脂滴丸 新橙皮苷 柚皮苷 药动学 液相质谱联用仪 

分 类 号：R969.1[医药卫生—药理学]