更新于：2024-11-01

Imidol Hydrochloride

盐酸艾咪朵尔

更新于：2024-11-01

概要

概要

基本信息

药物类型

小分子化药

别名-

靶点-

作用机制

免疫调节剂、病毒复制抑制剂

治疗领域

感染消化系统疾病

在研适应症

慢性乙型肝炎乙型肝炎

非在研适应症-

原研机构

沈阳药科大学

在研机构

天津金泰源生物医药科技开发有限公司

沈阳药科大学

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评-

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结构

分子式C23H23BrClN3O4S

InChIKeyBEDJFMNFVSHROQ-UHFFFAOYSA-N

CAS号959745-01-8

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关联

项与盐酸艾咪朵尔相关的临床试验

CTR20132555 / Recruiting临床2期IIT

盐酸艾咪朵尔片治疗HBeAg阳性的慢性乙型肝炎多中心随机盲法多剂量安慰剂对照Ⅱa期临床试验

探索盐酸艾咪朵尔片对HBeAg阳性的慢性乙肝患者的临床疗效、安全性及临床有效剂量。

开始日期2011-10-09

申办/合作机构

沈阳药科大学

100 项与盐酸艾咪朵尔相关的临床结果

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100 项与盐酸艾咪朵尔相关的转化医学

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100 项与盐酸艾咪朵尔相关的专利（医药）

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项与盐酸艾咪朵尔相关的文献（医药）

2014-01-01·International Journal of Pharmaceutics2区 · 医学

A pharmacokinetic study on a novel anti-HBV agent imidol hydrochloride in rats

2区 · 医学

Article

作者: Sun, Guoxiang ; Ma, Bingjie ; Liu, Zhongbo ; Ping, Gong ; Peng, Ying ; Bi, Kashun ; Liu, Yingchun ; Guo, Yong

Imidol hydrochloride is a novel agent for the treatment of hepatitis B virus (HBV) infection, which is currently being evaluated in a phase II trial. This study investigated the absorption, excretion and tissue distribution of imidol after an oral dose in rats. The pharmacokinetic parameters were determined for both intravenous and oral dosing. A simple and sensitive UPLC-MS-MS method was employed to determine the imidol levels in rat biological samples. It was applied for the analysis of imidol in plasma, urine, feces, bile and various tissue samples. Imidol was found to have a moderate half-life (∼4 h), a relatively large apparent distribution volume and rapid clearance after an IV dose and oral doses up to 70 mg kg(-1). Dose-dependent linear relationships of AUC0-t and Cmax for imidol was found in the range of 10-70 mg kg(-1) after oral administration to rats. However, the oral bioavailability was low (17.6%). Most of the drug was metabolized and only 20% of the parent drug was excreted. Imidol excreted mainly in feces. The tissue distribution results show that imidol was quickly dispersed to various tissues following an oral dose. Relatively high concentration was found in liver, which is beneficial to the intended indication. Very low levels of imidol were found in brain and testes, indicating that it was difficult for imidol to cross the blood-brain barrier.

2012-04-01·Biomedical Chromatography4区 · 医学

Determination of imidol hydrochloride in human plasma and urine by high‐performance liquid chromatography–tandem mass spectrometry and its application to clinical pharmacokinetic study

4区 · 医学

Article

作者: Shi, Zhengyuan ; Li, Kexin ; Hu, Xin ; Chen, Xiaohui ; Gong, Ping ; Bi, Kaishun ; Li, Yang

ABSTRACTImidol hydrochloride is a novel drug for the treatment of hepatitis B virus infection. A simple, special and sensitive solid‐phase extraction liquid chromatography–tandem mass spectrometry method for determination of imidol in human plasma and urine was developed for the first time and applied to a pharmacokinetic study. The chromatographic separation was achieved on a C18 column (50 × 2.1 mm, 3.5 µm) using gradient elution with acetonitrile and water both containing 0.1% acetic acid at a flow rate of 0.25 mL/min. The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring mode via a positive eletrospray ionization source. The mass transition pairs of m/z 517.8 → 325 and m/z 298 → 174 were used to detect imidol and the (−)‐clausenamide (internal standard), respectively. The retention times of imidol and (−)‐clausenamide were 2.5 and 2.7 min, respectively. Linearity, accuracy, precision, recovery, matrix effect, dilution test and stability were evaluated during method validation over the range of 0.2–500 ng/mL in human plasma and 0.5–500 ng/mL in urine. The method was successfully applied to a clinical pharmacokinetic study of imidol in healthy volunteers following oral administration. Copyright © 2011 John Wiley & Sons, Ltd.

100 项与盐酸艾咪朵尔相关的药物交易

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