LC-MS/MS法研究瓜蒌薤白胃内漂浮微丸在大鼠体内的药代动力学特征  

Pharmacokinetic Characteristics of Gualou-Xiebai Intragastric Floating Pellets in Rats by LC-MS/MS

作　　者：鄢海燕 孙德考 邹纯才 Yan Haiyan;Sun Dekao;Zou Chuncai(School of Pharmacy,Wannan Medical College,Wuhu,Anhui 241002,China;Jiangsu Kaiyuan Pharmaceutical Co.,Ltd.,Nanjing 222000,China)

机构地区：[1]皖南医学院药学院,安徽芜湖241002 [2]江苏开元药业有限公司,南京222000

出　　处：《大理大学学报》2021年第10期1-5,共5页Journal of Dali University

基　　金：安徽高校省级自然科学研究重大项目(KJ2016SD60);国家大学生创新创业训练计划项目(201810368008)。

摘　　要：目的:采用液相色谱-质谱串联(LC-MS/MS)法考察瓜蒌薤白胃内漂浮微丸(以下简称“瓜蒌薤白微丸”)中3,29-二苯甲酰基栝楼仁三醇(3,29-DK)在大鼠体内不同时间点的血药浓度及药代动力学特征。方法:SPF级SD雄性大鼠12只,随机分为瓜蒌薤白微丸组(2.0 g/kg)和瓜蒌薤白提取物组(1.4 g/kg)。瓜蒌薤白微丸组于大鼠灌胃给药前0 h及给药后第0.5、1、2、3、4、6、8、10、12、24、36、48 h眼内眦取血,瓜蒌薤白提取物组于给药前0 h及给药后第5、10、30 min,1、1.5、2、3、4、6、8 h眼内眦取血,计算药代动力学参数。结果:与瓜蒌薤白提取物组相比,瓜蒌薤白微丸组中3,29-DK达峰时间、AUC和t_(1/2)显著延长(P<0.05),MRT显著增加(P<0.05),CLz/F、C_(max)明显降低(P<0.05)。结论:瓜蒌薤白微丸中3,29-DK在大鼠体内释放速率较为平稳,无突释、速释现象,代谢时间延长。瓜蒌薤白微丸具有缓释作用。Objective:To study the plasma concentration and pharmacokinetics of 3,29-dibenzoyl-karounitriol(3,29-DK)in Gualou-Xiebai intragastric floating pellets(hereinafter referred to as"Gualou-Xiebai pellets")at different time points in rats by liquid chromatography tandem mass spectrometry(LC-MS/MS).Methods:12 SPF SD male rats were randomly divided into Gualou-Xiebai pellets group(2.0 g/kg)and Gualou-Xiebai extracts group(1.4 g/kg),the blood samples were taken from the orbit 0 h before administration and 0.5,1,2,3,4,6,8,10,12,24,36,48 h after administration in Gualou-Xiebai pellets group,the blood samples were taken from the orbit 0 h before administration and 5,10,30 min,1,1.5,2,3,4,6 and 8 h after administration in the Gualou-Xiebai extracts group,and the pharmacokinetic parameters were calculated.Results:Compared with the Gualou-Xiebai extracts group,the 3,29-DK peak time,AUC and t_(1/2) in the Gualou-Xiebai pellet group were significantly prolonged(P<0.05),and MRT was significantly increased(P<0.05),CLz/F,C_(max) was significantly reduced(P<0.05).Conclusion:The release rate of 3,29-DK in Gualou-Xiebai pellets was stable in rats,without sudden release and rapid release,and the metabolic time was prolonged.Gualou-Xiebai pellets have sustained-release effect.

关 键 词：LC-MS/MS 瓜蒌薤白胃内漂浮微丸 3 29-二苯甲酰基栝楼仁三醇 药代动力学 

分 类 号：R965[医药卫生—药理学]