Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs
文献类型：期刊论文
| 作者 | Lu, You-li1; Li, Shui-jun1; Liu, Gang-yi1; Li, Xiao-chuan2; Yang, Ding3; Jia, Jing-ying1; Zhang, Meng-qi1; Zheng, Hong-chao1; Yu, Chen1; Zhu, Fu1 |
| 刊名 | EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
 |
| 出版日期 | 2017-06 |
| 卷号 | 42期号:3页码:453-459 |
| ISSN号 | 0378-7966 |
| DOI | 10.1007/s13318-016-0360-3 |
| 文献子类 | Article |
| 英文摘要 | Background and Objectives Sulcardine sulfate is a newly developed candidate drug used to control arrhythmias. The aim of this research was to investigate the pharmacokinetics, bioavailability and excretion characteristics of sulcardine in animals. Methods Sprague-Dawley rats were orally and intravenously given sulcardine at 20 and 40 mg/kg. Beagle dogs were also orally and intravenously dosed at 10 mg/kg. Both [H-3]-labeled sulcardine and unlabeled sulcardine were given to rats. Feces, urine and bile were collected at 0-72 h for mass balance study. The contents of unlabeled sulcardine and radioactivity in samples were determined by a validated LC-MS/MS method and by liquid scintillation counting, separately. Results Sulcardine was rapidly eliminated in rats after dosing. The oral bioavailability was 34-35 % in rats, while a higher exposure was observed in dogs (bioavailability = 62.7 %). More than 90 % of dosed sulcardine was recovered, and approximately 20-40 % of the dose excreted into urine as the original form, and the remaining was found in feces and bile, most of which (about 40 %) was transformed into metabolites. No difference was observed between sexes. Metabolism may occur to a large extent after oral administration in rats but to a smaller extent in dogs. Conclusions Sulcardine was extensively absorbed in both rats and dogs after oral administration. The mass balance data indicated that sulcardine was widely metabolized in rats after oral administration. |
| WOS关键词 | CHANGROLIN ; CELLS |
| 资助项目 | Ministry of Science and Technology of China[2010ZX09502-003] ; Shanghai Committee of Science and Technology, China[15DZ2291800] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000400988000010 |
| 出版者 | SPRINGER FRANCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272651]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Wang, Yi-ping |
| 作者单位 | 1.Fudan Univ, Shanghai Xuhui Cent Hosp, Zhongshan Xuhui Hosp, Cent Lab,Shanghai Clin Ctr,Chinese Acad Sci, Shanghai 200031, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Pharmacol, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Wuhan Inst Phys & Math, Wuhan 430071, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lu, You-li,Li, Shui-jun,Liu, Gang-yi,et al. Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs[J]. EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,2017,42(3):453-459. |
| APA | Lu, You-li.,Li, Shui-jun.,Liu, Gang-yi.,Li, Xiao-chuan.,Yang, Ding.,...&Wang, Yi-ping.(2017).Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs.EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,42(3),453-459. |
| MLA | Lu, You-li,et al."Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague-Dawley Rats and Beagle Dogs".EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS 42.3(2017):453-459. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。