The apparent solubilizing capacity of simulated intestinal fluids for poorly water-soluble drugs

被引：28
作者：
Schwebel, Herve J. [1 ]
van Hoogevest, Peter [1 ]
Leigh, Mathew L. S. [1 ]
Kuentz, Martin [2 ]
机构：
[1] Phares AG, Muttenz, Switzerland
[2] Univ Appl Sci NW Switzerland, Inst Pharma Technol, CH-4132 Muttenz, Switzerland
来源：
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY | 2011年 / 16卷 / 03期
关键词：
Poorly soluble drugs; biorelevant media; FeSSIF; FaSSIF; apparent solubilizing capacity; BIORELEVANT DISSOLUTION MEDIA; HUMAN GASTROINTESTINAL-TRACT; BILE-SALT; FENOFIBRATE; FORMULATION; ABSORPTION; BIOAVAILABILITY; PREDICTION; LECITHIN; MICELLE;
D O I：
10.3109/10837451003664099
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Drug solubility testing in biorelevant media has become an indispensable tool in pharmaceutical development. Despite this importance, there is still an incomplete understanding of how poorly soluble compounds interact with these media. The aim of this study was to apply the concept of the apparent solubilization capacity to fasted and fed state simulated intestinal fluid (FaSSIF and FeSSIF, respectively). A set of non-ionized poorly soluble compounds was studied in biorelevant media prepared from an instantly dissolving complex (SIF (TM) Powder) at 37 degrees C. The values of the solubilization capacity were different between FaSSIF and FeSSIF but correlated. Drug inclusion into the mixed micelles was highly specific for a given compound. The ratio of the FeSSIF to FaSSIF solubility was in particular considered and discussed in terms of the apparent solubilizing capacity. The apparent solubilization concept appears to be useful for the interpretation of biorelevant solubility tests. Further studies are needed to explore acidic and basic drugs.
引用
收藏
页码：278 / 286
页数：9
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