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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:

22卷

期数:

2016年05期

页码:

448-451

栏目:

技术与方法

出版日期:

2016-09-20

文章信息/Info

Title:

Study on pharmacokinetics and bioequivalence of amoxicillin pulsatile- release tablets by UPLC-MS/MS in beagle dogs

文章编号:

1006-8147（2016）05-0448-4

作者:

秦 璐; 皮佳鑫; 祁东利; 张 谦; 黄 瑞; 韩润萍; 刘志东

(天津市现代中药重点试验室制剂室-省部共建国家重点试验室培育基地，天津现代中药发现与制剂技术教育部工程研究中心，天津中医药大学，天津300193）

Author(s):

QIN Lu;  PI Jia-xin; QI Dong-li; ZHANG Qian;  HUANG Rui;  HAN Run-ping;  LIU Zhi-dong

(Tianjin Modern Chinese Medicine Key Laboratory-Province and Ministry Co-established State Key Laboratory Cultivation Base, Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China)

关键词:

阿莫西林' target="_blank" rel="external">">阿莫西林; 脉冲片; 生物等效; 比格犬

Keywords:

?amoxicillin' target="_blank" rel="external">">?amoxicillin;  pulsatile-release tablets;  bioequivalent;  beagle dog

分类号:

R9

DOI:

-

文献标志码:

A

摘要:

目的：建立UPLC-MS/MS测定犬血浆中阿莫西林的方法并测定阿莫西林脉冲片的生物等效性。方法：以卡马西平为内标，血浆样品用高氯酸沉淀，并用UPLC-MS/MS测定血浆中阿莫西林含量。动物实验采用随机双交叉自身对照实验法，6只比格犬口服单剂量阿莫西林脉冲片参比制剂、受试制剂后测定其血药浓度，计算药动学参数，评价两制剂的等效性。结果：自制阿莫西林脉冲片单剂量给药其Ke为（0.50±0.16）h^-1，t_1/2为（1.53±0.57）h，AUC_0-12h为（113.21±30.63）(μg/mL)·h，C_max为（31.53±7.37）μg/mL，T_max为（1.83±0.41）h；市售阿莫西林脉冲片单剂量给药其Ke为（0.44±0.16）h^-1，t_1/2为（1.78±0.76）h，AUC_0-12h为（122.11±28.65）μg/（mL·h），C_max为（31.01±7.63）μg/mL，T_max为（2.08±0.58）h，相对生物利用度为（92.09±9.95）%。结论：以AUC_0-12h，C_max和T_max为评价指标，自制的阿莫西林脉冲释放片与市售的参比制剂在比格犬体内生物等效。

Abstract:

Objective ：To establish a UPLC-MS/MS method for determination of amoxicillin pulsatile-release tablets in dog plasma，and evaluate the pharmacokinetics and bioequivalence of amoxicillin pulsatile-release tablets after single oral dose administration. Methods：Carbamazepine was used as an internal standard，and the protein of plasma samples were precipitated by perchloric acid． According to randomized two-period self crossover study，six dogs were given single oral doses of the test preparation and reference preparation，then the concentration of amoxicillin in plasma were determined，and the pharmacokinetic parameters were calculated and the bioequivalence of the two preparations were evaluated Results：The pharmacokinetics of developed amoxicillin pulsatile-release tablets were as follows：Ke(0.50±0.16) h^-1，t_1/2(1.53±0.57) h，AUC_0-12h(113.21±30.63) μg/(mL?h)，C_max(31.53±7.37) μg/mL，Tmax(1.83±0.41) h；the pharmacokinetics of commercial amoxicillin pulsatile-release tablets were as follows：Ke(0.44±0.16) h^-1，t_1/2(1.78±0.76)h，AUC_0-12h(122.11±28.65)μg/(mL?h)，C_max(1.01±7.63)μg/mL，Tmax(2.08±0.58)h; The relative bioavailability of the test tablet was(92.09±9.95)%。 Conclusion: The developed amoxicillin pulsatile-release tablets may be bioequivalent to the commercial amoxicillin pulsatile-release tablets.

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备注/Memo

备注/Memo:

作者简介? 秦璐(1990-)，男，硕士在读, 研究方向：药物制剂；通信作者：刘志东，E- mail: lonerliuzd@163.com。

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更新日期/Last Update: 2016-09-20