uu.seUppsala University Publications
Change search
ReferencesLink to record
Permanent link

Direct link
The effects of food on the dissolution of poorly soluble drugs in human and in model small intestinal fluids
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Show others and affiliations
2005 (English)In: Pharmaceutical research, ISSN 0724-8741, E-ISSN 1573-904X, Vol. 22, no 12, 2141-2151 p.Article in journal (Refereed) Published
Abstract [en]

Purpose  This study was conducted to determine the effect of food on drug solubility and dissolution rate in simulated and real human intestinal fluids (HIF). Methods  Dissolution rate obtained via the rotating disk method and saturation solubility studies were carried out in fed and fasted state HIF, fed dog (DIF), and simulated (FeSSIF) intestinal fluid for six aprotic low solubility drugs. The intestinal fluids were characterized with respect to physical–chemical characteristics and contents. Results  Fed HIF provided a 3.5- to 30-times higher solubility compared to fasted HIF and FeSSIF, whereas fed DIF corresponded well (difference of less than 30%) to fed HIF. The increased solubility of food could mainly be attributed to dietary lipids and bile acids. The dissolution rate was also 2 to 7 times higher in fed HIF than fasted HIF. This was well predicted by both DIF and FeSSIF (difference of less than 30%). Conclusions  Intestinal solubility is higher in fed state compared to fasted state. However, the dissolution rate does not increase to the same extent. Dog seems to be a good model for man with respect to dissolution in the small intestine after intake of a meal, whereas FeSSIF is a poorer means of determining intestinal saturation solubility in the fed state.

Place, publisher, year, edition, pages
2005. Vol. 22, no 12, 2141-2151 p.
Keyword [en]
bile acids, dissolution rate, food effects, poorly soluble drugs, solubility
National Category
Pharmaceutical Sciences
URN: urn:nbn:se:uu:diva-75382DOI: 10.1007/s11095-005-8192-xPubMedID: 16247711OAI: oai:DiVA.org:uu-75382DiVA: diva2:103292
Available from: 2008-01-31 Created: 2008-01-31 Last updated: 2010-05-26Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full textPubMedhttp://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=PubMed&cmd=Retrieve&list_uids=16247711&dopt=Citation

Search in DiVA

By author/editor
Knutson, LarsLennernäs, Hans
By organisation
Department of PharmacyDepartment of Surgical Sciences
In the same journal
Pharmaceutical research
Pharmaceutical Sciences

Search outside of DiVA

GoogleGoogle Scholar
The number of downloads is the sum of all downloads of full texts. It may include eg previous versions that are now no longer available

Altmetric score

Total: 206 hits
ReferencesLink to record
Permanent link

Direct link