Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations  

作　　者：Sivacharan Kollipara Rajesh Kumar Gandhi 

机构地区：[1]Formulations Department,Pharmaceutical&Analytical Development,Technical R&D,Novartis Healthcare Pvt.Ltd.,Hyderabad 500078,Andhra Pradesh,India

出　　处：《Acta Pharmaceutica Sinica B》2014年第5期333-349,共17页药学学报（英文版）

摘　　要：Lipid-based formulations have been an attractive choice among novel drug delivery systems for enhancing the solubility and bioavailability of poorly soluble drugs due to their ability to keep the drug in solubilized state in the gastrointestinal tract.These formulations offer multiple advantages such as reduction in food effect and inter-individual variability,ease of preparation,and the possibility of manufacturing using common excipients available in the market.Despite these advantages,very few products are available in the present market,perhaps due to limited knowledge in the in vitro tests(for prediction of in vivo fate)and lack of understanding of the mechanisms behind pharmacokinetic and biopharmaceutical aspects of lipid formulations after oral administration.The current review aims to provide a detailed understanding of the in vivo processing steps involved after oral administration of lipid formulations,their pharmacokinetic aspects and in vitro in vivo correlation(IVIVC)perspectives.Various pharmacokinetic and biopharmaceutical aspects such as formulation dispersion and lipid digestion,bioavailability enhancement mechanisms,impact of excipients on efflux transporters,and lymphatic transport are discussed with examples.In addition,various IVIVC approaches towards predicting in vivo data from in vitro dispersion/precipitation,in vitro lipolysis and ex vivo permeation studies are also discussed in detail with help of case studies.

关 键 词：PHARMACOKINETICS LIPOLYSIS IVIVC Efflux transporters Lymphatic delivery Food effect 

分 类 号：TN9[电子电信—信息与通信工程]