Pharmacokinetics, tissue distribution, and excretion of nomegestrol acetate in female rats
文献类型：期刊论文
| 作者 | Huang, Qingbiao2; Chen, Xiaoke3; Zhu, Yan1; Cao, Lin1; Riviere, Jim E.4 |
| 刊名 | EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
 |
| 出版日期 | 2015-12 |
| 卷号 | 40期号:4页码:435-442 |
| 关键词 | Nomegestrol acetate NOMAC Pharmacokinetics Tissue distribution Excretion HPLC |
| ISSN号 | 0378-7966 |
| DOI | 10.1007/s13318-014-0224-7 |
| 文献子类 | Article |
| 英文摘要 | Nomegestrol acetate (NOMAC), a synthetic progestogen derived from 19-norprogesterone, is an orally active drug with a strong affinity for the progesterone receptor. NOMAC inhibits ovulation and is devoid of undesirable androgenic and estrogenic activities. The aim of this study was to evaluate the pharmacokinetics, tissue distribution, and excretion of NOMAC in female rats. Sprague-Dawley female rats were orally administered a single dose of NOMAC (10, 20 or 40 mg/kg) and drug plasma concentrations at different times were determined by RP-HPLC. Tissue distribution at 1, 2, and 4 h and excretion of NOMAC into bile, urine, and feces after dosing were investigated. The results showed that NOMAC was rapidly absorbed after oral administration, with of 1-2 h. The plasma concentration-time curves were fitted in a two-compartment model. The exposure to NOMAC ( and ) increased dose proportionally from 10 to 40 mg/kg. The average CL and were 5.58 L/(h center dot kg) and 10.8 h, respectively. The highest concentrations of NOMAC in ovary, liver, kidney, lung, heart, brain, spleen, muscle, and uterus were observed at 2 h, whereas the highest concentrations in stomach, pituitary, and hypothalamus appeared at 1 h. The total cumulative excretion of NOMAC in feces (0-72 h), urine (0-72 h), and bile (0-48 h) was 1.06, 0.03, and 0.08 % of the oral administered dose, respectively. This study indicated that NOMAC had a widespread distribution in tissues, including ovary, pituitary, and hypothalamus, which are main target tissues where NOMAC inhibits ovulation. NOMAC was excreted via both feces and urine with few unchanged NOMAC excreted. Enterohepatic circulation was found in the drug elimination; however, it did not significantly affect . |
| WOS关键词 | WOMEN ; PHARMACOLOGY ; PROFILE |
| 资助项目 | Shanghai Modern Biology and Drug Industry Development Foundation[955419004] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000365514000008 |
| 出版者 | SPRINGER FRANCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276310]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Huang, Qingbiao |
| 作者单位 | 1.Shanghai Inst Planned Parenthood Res, Dept Reprod Pharmacol, Shanghai 200032, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Pharmaceut Int Inc, Dept Res & Dev, Hunt Valley, MD 21031 USA; 4.Kansas State Univ, Inst Computat Comparat Med, Manhattan, KS 66506 USA |
| 推荐引用方式 GB/T 7714 | Huang, Qingbiao,Chen, Xiaoke,Zhu, Yan,et al. Pharmacokinetics, tissue distribution, and excretion of nomegestrol acetate in female rats[J]. EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,2015,40(4):435-442. |
| APA | Huang, Qingbiao,Chen, Xiaoke,Zhu, Yan,Cao, Lin,&Riviere, Jim E..(2015).Pharmacokinetics, tissue distribution, and excretion of nomegestrol acetate in female rats.EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS,40(4),435-442. |
| MLA | Huang, Qingbiao,et al."Pharmacokinetics, tissue distribution, and excretion of nomegestrol acetate in female rats".EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS 40.4(2015):435-442. |
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。