Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/ MS method: An application to rat pharmacokinetic and tissue distribution studies
文献类型：期刊论文
| 作者 | Wang, Zeyu2,3; Tang, Pingming1; Dou, Caixia1; Shen, Jiale3; Peng, Ni3; Li, Yao1; Wang, Ju1; Chen, Xiaoyan2,3
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| 刊名 | JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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| 出版日期 | 2025-01-15 |
| 卷号 | 1251页码:9 |
| 关键词 | Crisugabalin (HSK16149) LC-MS/MS Pharmacokinetics Tissue distribution |
| ISSN号 | 1570-0232 |
| DOI | 10.1016/j.jchromb.2024.124396 |
| 英文摘要 | Crisugabalin (HSK16149), a novel VGCC alpha 2S ligand, has been approved for the treatment of adult diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). In this study, an LC-MS/MS method was developed for the determination of crisugabalin in rat plasma and tissues homogenate. Samples were extracted by protein precipitation and separated on a Hypersil GOLD aQ column with methanol and 2 mM ammonium acetate in water containing 0.1 % formic acid as mobile phase. Crisugabalin and its internal standard HSK7891 were ionized by electrospray ionization source and detected by multiple reaction monitoring with transitions of m / z 210.9-* 134.4 and m / z 246.0-* 129.3. Over the range of 0.0100-10.0 mu g/mL, the selectivity, linearity, precision and accuracy, matrix effect, stability, recovery and dilution integrity of crisugabalin were validated in rat plasma. Validation was also performed in rat liver homogenate at concentrations ranging from 0.0200-20.0 mu g/g. The method was then successfully applied to determine the pharmacokinetics and tissue distribution of crisugabalin. In rats, orally administered crisugabalin was completely and rapidly absorbed with a peak time of about 0.57 h, and was mainly distributed to kidney, bladder and liver tissues. Crisugabalin exhibited linear pharmacokinetics over the oral dose range of 3-30 mg/kg. |
| WOS关键词 | NEUROPATHIC PAIN ; MANAGEMENT |
| 资助项目 | National Natural Science Foundation of China[82073924] ; State Key Laboratory of Drug Research |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001408439500001 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/315995]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Wang, Ju; Chen, Xiaoyan |
| 作者单位 | 1.Haisco Pharmaceut Grp Co Ltd, Baili Rd 136, Chengdu, Sichuan Provinc, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Zeyu,Tang, Pingming,Dou, Caixia,et al. Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/ MS method: An application to rat pharmacokinetic and tissue distribution studies[J]. JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,2025,1251:9. |
| APA | Wang, Zeyu.,Tang, Pingming.,Dou, Caixia.,Shen, Jiale.,Peng, Ni.,...&Chen, Xiaoyan.(2025).Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/ MS method: An application to rat pharmacokinetic and tissue distribution studies.JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,1251,9. |
| MLA | Wang, Zeyu,et al."Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/ MS method: An application to rat pharmacokinetic and tissue distribution studies".JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES 1251(2025):9. |
入库方式： OAI收割
来源：上海药物研究所
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