Population pharmacokinetics of CPRC1 in patients with duodenal ulcer following intravenous administr

来源 :2015年第一届药代动力学朝阳论坛 | 被引量 : 0次 | 上传用户:linxiao13421
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
  CPRC1 is a novel investigated proton pump inhibitor, which shows dramaticsuccess in the management of acid-related disorders.Now this drug is being developed in Phase Ⅱ study in China.In this paper for the first time, a population pharmacokinetic (PopPK) model was developed to describe the PK characters of CPRC1 in patients with duodenal ulcer after receiving 20 mg CPRC1 intravenously.Plasma samples were collected and concentrations of CPRC1 were detected by a validated UPLC-MS/MS method.The PopPK model was developed using Phoenix NLME 1.2 with a non-linear mixed-effect model, and the following covariates were tested: weight, height, age, gender, alanine aminotransferase (ALT), aspartate aminotransferase (AST),total bilirubin (TBIL), direct bilirubin (DBIL), albumin (ALB), creatinine (CR) and genotype of CYP2C19.Covariate effects on parameters describing the pharmacokinetics relationship were screened using stepwise forward inclusion/backward elimination.
其他文献
Prediction of human PK at the preclinical stage can aid: ① human efficacious dose prediction, ②) human safety risk assessment based on detailed pharmacokinetic information such as the maximum concentr
会议
The diversity in xenobiotic metabolic pathways catalyzed by P450 or other drug-metabolizing enzymes is large.We often observe that xenobiotics are metabolized by unexpected and unusual pathways.In thi
会议
Drug metabolism has become an integral part of drug discovery and development from the earliest stage, and this change may have been driven by the evolution of better analytical technologies, in parti
会议
LC-MS analysis of in vivo xenobiotic and endogenous components plays a key in drug metabolism and metabolomic studies, which is much more challenging than in vitro analysis due to chemical complexity,
会议
Our study aimed at the investigation of in vivo anticancer effect of the combination use of dexamethasone (DEX) and gemcitabine (GM) as well as the development of pharmacokinetic/pharmacodynamic (PK/P
会议
Many furan-containing compounds have been reported to be toxic and/or carcinogenic.Furanoids occur in a wide range of fruits, herbs, foods, and beverages.The demand to identify harmful furans potentia
会议
Diosbulbin B (DIOB) is the most abundant component of Dioscorea bulbifera L.(DB), a traditional Chinese medicine herb.DIOB and DB extracts have been reported to cause liver injury in animals.The mecha
会议
Human carboxylesterase 1 (hCE-1) are a representative B-esterase, involved in the hydrolysis of many endogenous and exogenous compounds and are thus responsible for the activation of many prodrugs.Dys
会议
Tanshinol has desirable antianginal and pharmacokinetic properties and is a key compound of Salvia miltiorrhiza roots (Danshen).The reported effective concentrations of tanshinol in vitro are higher (
会议
Fast metabolism is one of key issues for many drug candidates, which could result in poor bioavailability, short half-life and significant drug-drug interactions.To identify the issue in early phase o
会议