国产与进口银杏叶片萜类内酯Beagle犬生物利用度的比较  

Relative bioavailability of terpene lactones in Beagle dogs after ig administration of domestic and imported Ginkgo Leaf Tablets

作　　者：柴战欣 宋英 高彩芳 王建新 CHAI Zhan-xin;SONG Ying;GAO Cai-fang;WANG Jian-xin(Luoyang Xinchundu Biopharmaceutical Co., Ltd., Luoyang 471001, China;Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China;Central Institute of Shanghai Pharmaceutical Group, Shanghai 201203, China;Shanghai Institute of Pharmaceutical Industry, Shanghai 201203, China)

机构地区：[1]洛阳新春都生物制药有限公司,河南洛阳471001 [2]复旦大学药学院智能化递药教育部重点实验室,上海201203 [3]上海医药集团中央研究院,上海201203 [4]上海医药工业研究院,上海201203

出　　处：《中草药》2018年第12期2840-2844,共5页Chinese Traditional and Herbal Drugs

摘　　要：目的比较国产与进口银杏叶片在Beagle犬体内的药动学参数和生物利用度。方法 Beagle犬分别ig国产与进口银杏叶片后,取血测定。采用LC-MS检测Beagle犬血浆中银杏叶片萜类内酯(银杏内酯A、银杏内酯B和白果内酯)的含量,绘制血药浓度-时间曲线,采用DAS软件计算药动学参数。结果 Beagle犬ig国产银杏叶片(80 mg/kg)后银杏内酯A、银杏内酯B和白果内酯的药-时曲线下面积(AUC0~t)分别为51.64、19.86和72.90 ng·h/m L,而ig进口银杏叶片(80 mg/kg)后三者的药-时曲线下面积(AUC0~t)分别为69.98、24.35和169.60 ng·h/m L。根据2种制剂中3种成分的含量,国产银杏叶片中银杏内酯A、银杏内酯B、白果内酯的相对生物利用度分别为37.77%、33.70%和95.98%。结论 Beagle犬ig国产银杏叶片后的萜类内酯生物利用度显著低于进口银杏叶片。Objective To compare the pharmacokinetic parameters and bioavailability of terpene lactones in Beagle dogs between domestic and imported Ginkgo Leaf Tablets. Methods Beagle dogs were ig administrated demestic and imported Ginkgo Leaf Tablets, and then the plasma of Beagle dogs were detected. LC-MS was used to determine the contents of terpene lactones（including ginkgolide A, ginkgolide B, and ginkgo lactone） in plasma of Beagle dogs. Plasma concentration-time curves were drawn and analyzed by DAS software to obtain pharmacokinetics parameter. Results The area under curve（AUC0-t） of GA, GB, and BB in Beagle dogs after ig administration domestic Ginkgo Leaf Tablets was 51.64, 19.86, and 72.90 ng·h/m L, while it was 69.98, 24.35, and 169.60 ng·h/m L after ig administration imported G. biloba leaf extract tablets, respectively. According to the contents of three components in two preparations, the relative bioavailability of GA, GB, and BB of domestic Ginkgo Leaf Tablets respectively was 37.77%, 33.70%, and 95.98%. ConclusionThe oral bioavailability of the terpene lactones in imported Ginkgo Leaf Tablets was significantly higher than that of domestic tablets.

关 键 词：银杏叶片 生物利用度 一致性评价 银杏内酯A 银杏内酯B 白果内酯 

分 类 号：R285[医药卫生—中药学]