• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

哪些体外筛选方法可指导口服吸收和分布容积的预测?

Which in vitro screens guide the prediction of oral absorption and volume of distribution?

作者信息

van de Waterbeemd Han

机构信息

Pfizer Global Research and Development, PDM, Sandwich Laboratories, IPC 664, Ramsgate Road, Sandwich, Kent CT13 9NJ, U.K.

出版信息

Basic Clin Pharmacol Toxicol. 2005 Mar;96(3):162-6. doi: 10.1111/j.1742-7843.2005.pto960304.x.

DOI:10.1111/j.1742-7843.2005.pto960304.x
PMID:15733210
Abstract

The development of medium to high-throughput in vitro screening of ADME (Absorption, Distribution, Metabolism, Excretion) properties has been the reply to higher demands on drug metabolism scientists to cope with progress in chemistry and biology. Two areas will be discussed here, namely screens for oral absorption and for volume of distribution. The prediction of these human pharmacokinetic parameters can be based on proper combination of simple physicochemical measurements. In the future in vitro screens most likely will be combined with in silico assessments of various ADME properties leading to the concept of in combo screening in drug discovery.

摘要

中高通量体外药物吸收、分布、代谢、排泄(ADME)特性筛选的发展,是为了满足药物代谢科学家应对化学和生物学进展提出的更高要求。这里将讨论两个领域,即口服吸收筛选和分布容积筛选。这些人体药代动力学参数的预测可以基于简单物理化学测量的适当组合。未来的体外筛选很可能会与各种ADME特性的计算机模拟评估相结合,从而形成药物发现中的联合筛选概念。

相似文献

1
Which in vitro screens guide the prediction of oral absorption and volume of distribution?哪些体外筛选方法可指导口服吸收和分布容积的预测?
Basic Clin Pharmacol Toxicol. 2005 Mar;96(3):162-6. doi: 10.1111/j.1742-7843.2005.pto960304.x.
2
In silico predictions of drug solubility and permeability: two rate-limiting barriers to oral drug absorption.药物溶解度和渗透性的计算机模拟预测:口服药物吸收的两个限速屏障。
Basic Clin Pharmacol Toxicol. 2005 Mar;96(3):156-61. doi: 10.1111/j.1742-7843.2005.pto960303.x.
3
Animal data: the contributions of the Ussing Chamber and perfusion systems to predicting human oral drug delivery in vivo.动物数据:尤斯灌流室和灌注系统对预测人体口服药物体内递送的贡献。
Adv Drug Deliv Rev. 2007 Sep 30;59(11):1103-20. doi: 10.1016/j.addr.2007.06.016. Epub 2007 Aug 22.
4
High-throughput screening for lead optimization: a rational approach.用于先导化合物优化的高通量筛选:一种合理的方法。
Curr Opin Drug Discov Devel. 2000 Jan;3(1):63-71.
5
Drug selection in early drug development: screening for acceptable pharmacokinetic properties using combined in vitro and computational approaches.早期药物研发中的药物选择:采用体外实验与计算方法相结合的方式筛选可接受的药代动力学特性
Curr Opin Drug Discov Devel. 1999 Jan;2(1):42-8.
6
When poor solubility becomes an issue: from early stage to proof of concept.当溶解度差成为一个问题时:从早期阶段到概念验证。
Eur J Pharm Sci. 2007 Aug;31(5):249-61. doi: 10.1016/j.ejps.2007.05.110. Epub 2007 May 21.
7
Compound optimization in early- and late-phase drug discovery: acceptable pharmacokinetic properties utilizing combined physicochemical, in vitro and in vivo screens.早期和晚期药物研发中的化合物优化:利用物理化学、体外和体内筛选相结合的方法获得可接受的药代动力学性质
Curr Opin Drug Discov Devel. 2000 Jan;3(1):30-41.
8
PK/DB: database for pharmacokinetic properties and predictive in silico ADME models.PK/DB:药物动力学特性及计算机辅助药物代谢和药物动力学预测模型数据库
Bioinformatics. 2008 Oct 1;24(19):2270-1. doi: 10.1093/bioinformatics/btn415. Epub 2008 Aug 6.
9
A strategy for preclinical formulation development using GastroPlus as pharmacokinetic simulation tool and a statistical screening design applied to a dog study.一种使用GastroPlus作为药代动力学模拟工具的临床前制剂开发策略以及应用于犬类研究的统计筛选设计。
Eur J Pharm Sci. 2006 Jan;27(1):91-9. doi: 10.1016/j.ejps.2005.08.011. Epub 2005 Oct 10.
10
Prediction of human pharmacokinetics--gastrointestinal absorption.人体药代动力学预测——胃肠道吸收
J Pharm Pharmacol. 2007 Jul;59(7):905-16. doi: 10.1211/jpp.59.7.0001.

引用本文的文献

1
Randomized, Double-Blind, Crossover Study Comparing the Bioavailability of 4 Ashwagandha ( (L.) Dunal) Extracts in Healthy Adults Under Fasting Condition.随机、双盲、交叉研究:比较4种南非醉茄(Withania somnifera (L.) Dunal)提取物在健康成年人空腹条件下的生物利用度。
Curr Ther Res Clin Exp. 2025 Jul 10;103:100805. doi: 10.1016/j.curtheres.2025.100805. eCollection 2025.
2
Rapid screening of drug-protein binding using high-performance affinity chromatography with columns containing immobilized human serum albumin.利用含固定化人血清白蛋白的高效亲和色谱柱快速筛选药物-蛋白结合。
J Anal Methods Chem. 2013;2013:439039. doi: 10.1155/2013/439039. Epub 2013 Mar 28.
3
Virtual screening for the discovery of bioactive natural products.
用于发现生物活性天然产物的虚拟筛选
Prog Drug Res. 2008;65:211, 213-49. doi: 10.1007/978-3-7643-8117-2_6.
4
Chemical substituent effect on pyridine permeability and mechanistic insight from computational molecular descriptors.化学取代基对吡啶渗透性的影响及基于计算分子描述符的机理洞察
Mol Pharm. 2006 Nov-Dec;3(6):745-55. doi: 10.1021/mp050096+.
5
Drug metabolism and pharmacokinetics, the blood-brain barrier, and central nervous system drug discovery.药物代谢与药代动力学、血脑屏障及中枢神经系统药物发现
NeuroRx. 2005 Oct;2(4):554-71. doi: 10.1602/neurorx.2.4.554.