利用生物相关溶解介质预测药物的体内性能。
The use of biorelevant dissolution media to forecast the in vivo performance of a drug.
机构信息
Institute of Pharmacy, Biopharmacy and Pharmaceutical Technology, Ernst Moritz Arndt University, 17 Friedrich Ludwig Jahn Street, Greifswald 17489, Germany.
出版信息
AAPS J. 2010 Sep;12(3):397-406. doi: 10.1208/s12248-010-9203-3. Epub 2010 May 11.
Abstract
Simulation of gastrointestinal conditions is essential to adequately predict the in vivo behavior of drug formulations. To reduce the size and number of human studies required to identify a drug product with appropriate performance in both the fed and fasted states, it is advantageous to be able to pre-screen formulations in vitro. The choice of appropriate media for such in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies. The present paper gives an overview of the development and composition of biorelevant dissolution media that can be used for the in vitro simulation of different dosing conditions (fasted and fed states). In addition, the application of these media to predicting food effects is described in several case examples.
摘要
模拟胃肠道条件对于充分预测药物制剂的体内行为至关重要。为了减少在确定具有良好进食和禁食状态下性能的药物产品所需的人体研究的数量和规模，能够在体外预先筛选制剂是有利的。选择适当的介质进行此类体外测试对于其正确预测药代动力学研究中的食物效应至关重要。本文概述了可用于模拟不同给药条件（禁食和进食状态）的生物相关溶解介质的开发和组成。此外，还描述了这些介质在预测食物效应中的应用的几个实例。
相似文献
1
The use of biorelevant dissolution media to forecast the in vivo performance of a drug.利用生物相关溶解介质预测药物的体内性能。
AAPS J. 2010 Sep;12(3):397-406. doi: 10.1208/s12248-010-9203-3. Epub 2010 May 11.
2
Forecasting in vivo oral absorption and food effect of micronized and nanosized aprepitant formulations in humans.预测人体口服米氮平和纳米阿瑞匹坦制剂的体内吸收和食物效应。
Eur J Pharm Biopharm. 2010 Sep;76(1):95-104. doi: 10.1016/j.ejpb.2010.05.009. Epub 2010 Jun 1.
3
Predicting pharmacokinetic food effects using biorelevant solubility media and physiologically based modelling.使用生物相关溶解介质和基于生理的模型预测药代动力学食物效应。
Clin Pharmacokinet. 2006;45(12):1213-26. doi: 10.2165/00003088-200645120-00006.
4
Prediction of food effect on in vitro drug dissolution into biorelevant media: Contributions of solubility enhancement and relatively low colloid diffusivity.预测食物效应对体外药物在生物相关介质中溶解的影响：溶解度增强和相对较低胶体扩散系数的贡献。
Eur J Pharm Sci. 2022 Oct 1;177:106274. doi: 10.1016/j.ejps.2022.106274. Epub 2022 Aug 6.
5
In vitro biorelevant models for evaluating modified release mesalamine products to forecast the effect of formulation and meal intake on drug release.用于评估美沙拉嗪缓释产品以预测制剂和进餐对药物释放影响的体外生物相关模型。
Eur J Pharm Biopharm. 2015 Nov;97(Pt A):39-50. doi: 10.1016/j.ejpb.2015.09.002. Epub 2015 Sep 21.
6
Precipitation in the small intestine may play a more important role in the in vivo performance of poorly soluble weak bases in the fasted state: case example nelfinavir.在禁食状态下，小肠中的沉淀可能在难溶性弱碱性药物的体内性能中发挥更重要的作用：以奈非那韦为例。
Eur J Pharm Biopharm. 2011 Oct;79(2):349-56. doi: 10.1016/j.ejpb.2011.04.005. Epub 2011 Apr 18.
7
Prediction of food effects on the absorption of celecoxib based on biorelevant dissolution testing coupled with physiologically based pharmacokinetic modeling.基于生物相关溶解试验结合生理基于药代动力学模型预测塞来昔布的食物对吸收的影响。
Eur J Pharm Biopharm. 2009 Sep;73(1):107-14. doi: 10.1016/j.ejpb.2009.05.009. Epub 2009 May 22.
8
Dissolution media simulating the proximal canine gastrointestinal tract in the fasted state.模拟空腹状态下近犬胃肠道的溶解介质。
Eur J Pharm Biopharm. 2013 Aug;84(3):633-41. doi: 10.1016/j.ejpb.2013.01.010. Epub 2013 Feb 19.
9
Current methods for predicting human food effect.预测人体食物效应的当前方法。
AAPS J. 2008 Jun;10(2):282-8. doi: 10.1208/s12248-008-9025-8. Epub 2008 May 24.
10
Forecasting the in vivo performance of four low solubility drugs from their in vitro dissolution data.根据四种低溶解度药物的体外溶出数据预测其体内性能。
Pharm Res. 1999 Dec;16(12):1876-82. doi: 10.1023/a:1018959511323.
引用本文的文献
1
Dissolution Profile of Tosufloxacin Tosylate in Biorelevant Bicarbonate Buffer Containing Sodium Chloride: Precipitation of Hemi-hydrochloride Salt at the Particle Surface.托氟沙星甲苯磺酸盐在含氯化钠的生物相关碳酸氢盐缓冲液中的溶出曲线：颗粒表面半盐酸盐的沉淀
Pharm Res. 2025 Aug;42(8):1363-1372. doi: 10.1007/s11095-025-03905-4. Epub 2025 Aug 11.
2
Development of a pH Gradient Dissolution Condition to Predict the Behavior of Delayed Release Formulations under Fed In Vivo Condition.开发一种pH梯度溶解条件以预测迟释制剂在进食体内条件下的行为。
AAPS PharmSciTech. 2025 Aug 11;26(7):211. doi: 10.1208/s12249-025-03186-5.
3
3-O-trans-p-coumaroyl esterification enhances the anti-inflammatory effects of tormentic acid by targeting NF-κB signaling.3 - O - 反式对香豆酰酯化通过靶向NF - κB信号通路增强了 tormentic 酸的抗炎作用。
Redox Biol. 2025 Jun 14;85:103731. doi: 10.1016/j.redox.2025.103731.
4
The mechanism of action of nisin in promoting poultry through tight junction integrity and dendritic cell anti-inflammatory properties.乳链菌肽通过紧密连接完整性和树突状细胞抗炎特性促进家禽生长的作用机制。
Arch Microbiol. 2025 Jun 4;207(7):165. doi: 10.1007/s00203-025-04364-6.
5
Correlation Between Dissolution Profiles of Salt-Form Drugs in Biorelevant Bicarbonate Buffer and Oral Drug Absorption: Importance of Dose/ Fluid Volume Ratio.生物相关碳酸氢盐缓冲液中盐型药物溶出曲线与口服药物吸收之间的相关性：剂量/液体体积比的重要性。
Pharm Res. 2025 Apr;42(4):623-637. doi: 10.1007/s11095-025-03854-y. Epub 2025 Apr 4.
6
Mechanistic Investigation into the Phase Separation Behavior of Soluplus in the Presence of Biorelevant Media.在生物相关介质存在下对固体分散体载体（Soluplus）相分离行为的机理研究。
Mol Pharm. 2025 Apr 7;22(4):1958-1972. doi: 10.1021/acs.molpharmaceut.4c01140. Epub 2025 Mar 11.
7
RSM and AI based machine learning for quality by design development of rivaroxaban push-pull osmotic tablets and its PBPK modeling.基于响应面法（RSM）和人工智能的机器学习用于利伐沙班推拉渗透泵片的质量源于设计开发及其生理药代动力学（PBPK）建模
Sci Rep. 2025 Mar 7;15(1):7922. doi: 10.1038/s41598-025-91601-z.
8
Differential Enhancement of Fat-Soluble Vitamin Absorption and Bioefficacy via Micellization in Combination with Selected Plant Extracts In Vitro.通过胶束化结合特定植物提取物在体外对脂溶性维生素吸收和生物功效的差异增强作用
Nutrients. 2025 Jan 20;17(2):359. doi: 10.3390/nu17020359.
9
Evaluation of bioaccessibility, metabolic clearance and interaction with xenobiotic receptors (PXR and AhR) of cinnamaldehyde.肉桂醛的生物可及性、代谢清除率及其与外源性物质受体（孕烷X受体和芳烃受体）相互作用的评估。
Food Chem (Oxf). 2024 Dec 20;10:100237. doi: 10.1016/j.fochms.2024.100237. eCollection 2025 Jun.
10
Gastrointestinal Bile Salt Concentrations in Healthy Adults Under Fasted and Fed Conditions: A Systematic Review and Meta-Analysis for Mechanistic Physiologically-Based Pharmacokinetic (PBPK) Modelling.健康成年人禁食和进食状态下胃肠道胆汁盐浓度：基于生理药代动力学（PBPK）模型机制的系统评价和荟萃分析
AAPS J. 2025 Jan 22;27(1):31. doi: 10.1208/s12248-025-01016-x.
本文引用的文献
1
A standardized mini paddle apparatus as an alternative to the standard paddle.一种标准化的小型极板装置，可作为标准极板的替代品。
AAPS PharmSciTech. 2008;9(4):1179-84. doi: 10.1208/s12249-008-9161-6. Epub 2008 Nov 25.
2
Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update.模拟人体近端胃肠道环境的溶出介质：最新进展
Pharm Res. 2008 Jul;25(7):1663-76. doi: 10.1007/s11095-008-9569-4. Epub 2008 Apr 11.
3
Pharmacokinetics of itraconazole after intravenous and oral dosing of itraconazole-cyclodextrin formulations.伊曲康唑-环糊精制剂静脉注射和口服给药后伊曲康唑的药代动力学。
J Pharm Sci. 2007 Nov;96(11):3100-16. doi: 10.1002/jps.20878.
4
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.
5
Estimation of intragastric solubility of drugs: in what medium?药物胃内溶解度的评估：在何种介质中？
Pharm Res. 2007 May;24(5):909-17. doi: 10.1007/s11095-006-9209-9. Epub 2007 Mar 20.
6
Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs.脂质及基于脂质的制剂：优化亲脂性药物的口服给药
Nat Rev Drug Discov. 2007 Mar;6(3):231-48. doi: 10.1038/nrd2197.
7
Characterization of the human upper gastrointestinal contents under conditions simulating bioavailability/bioequivalence studies.模拟生物利用度/生物等效性研究条件下人体上消化道内容物的特性分析。
Pharm Res. 2006 Jan;23(1):165-76. doi: 10.1007/s11095-005-8476-1. Epub 2006 Dec 1.
8
Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds.模拟空腹胃部环境及其对亲脂性化合物体内溶解的重要性。
Eur J Pharm Biopharm. 2005 Aug;60(3):413-7. doi: 10.1016/j.ejpb.2005.03.002.
9
Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug.液体量和食物摄入量对难溶性药物达那唑绝对生物利用度的影响。
Eur J Pharm Sci. 2005 Mar;24(4):297-303. doi: 10.1016/j.ejps.2004.11.005. Epub 2005 Jan 5.
10
Influence of high fat diet (butter) on pharmacokinetics of phenytoin and carbamazepine.
Methods Find Exp Clin Pharmacol. 2004 Oct;26(8):634-8. doi: 10.1358/mf.2004.26.8.863730.
Zotero 插件