Jejunal absorption of aprepitant from nanosuspensions: Role of particle size, prandial state and mucus layer.

↓ Direkt till sidans innehåll
↓ Direkt till sidans sekundära innehåll (sidomenyn)

Search: onr:"swepub:oai:DiVA.org:uu-363157" > Jejunal absorption ...

1 of 1
Previous record
Next record
To hitlist

Details
MARC

Roos, CarlUppsala universitet,Institutionen för farmaci (author)

Jejunal absorption of aprepitant from nanosuspensions : Role of particle size, prandial state and mucus layer.

Article/chapterEnglish2018

Publisher, publication year, extent ...

Elsevier BV,2018
printrdacarrier

Numbers

LIBRIS-ID:oai:DiVA.org:uu-363157
https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-363157URI
https://doi.org/10.1016/j.ejpb.2018.09.022DOI

Supplementary language notes

Language:English
Summary in:English

Part of subdatabase

SwePubSwePub

Classification

Subject category:ref swepub-contenttype
Subject category:art swepub-publicationtype

Notes

The number of highly lipophilic active pharmaceutical ingredients (APIs) in pharmaceutical development has been constantly increasing over recent decades. These APIs often have inherent issues with solubility and dissolution, limiting their oral bioavailability. Traditionally, a reduction in particle size to the micrometer range has been used to improve dissolution. More recently, size reduction to the nanometer range has been introduced, which further increases the dissolution rate, but may also involve other mechanisms for increasing bioavailability. The effect of particle size on the absorption of aprepitant was investigated using the single-pass intestinal perfusion (SPIP) model in the rat jejunum. Phosphate buffer, fasted-state simulated intestinal fluid (FaSSIF), and fed-state simulated intestinal fluid (FeSSIF) were used as perfusion media to increase understanding of the processes involved and the effects of colloidal structures. The role of mucus on intestinal absorption was investigated by adding the mucolytic agent N-acetyl-cysteine (NAC). The absorption of aprepitant from the nanosuspensions was similar with all perfusion media (buffer = FaSSIF = FeSSIF), whereas food had a pronounced effect on absorption from the microsuspensions (FeSSIF > FaSSIF > buffer). The colloidal structures hence contributed to absorption from the microsuspensions. Partitioning of aprepitant from the nanosuspension into the colloidal structures decreased the amount of nanoparticles available, which offset the effect of food. The appearance flux of aprepitant in blood was non-significantly decreased for nanosuspensions of aprepitant with NAC versus without NAC in buffer (ratio of 2:1), indicating that particle deposition in the mucus may have been decreased as the layer thinned, with subsequently reduced intestinal absorption. The study also showed that the SPIP model is suitable for investigating detailed absorption mechanisms using complex perfusion media, which increase the biorelevance of the model.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

Dahlgren, DavidUppsala universitet,Institutionen för farmaci(Swepub:uu)davda219 (author)
Sjögren, Erik,1977-Uppsala universitet,Institutionen för farmaci(Swepub:uu)ersjo473 (author)
Sjöblom, Markus,1973-Uppsala universitet,Fysiologi(Swepub:uu)msj20812 (author)
Hedeland, MikaelUppsala universitet,Analytisk vetenskap(Swepub:uu)mikahede (author)
Lennernäs, HansUppsala universitet,Institutionen för farmaci(Swepub:uu)hanslenn (author)
Uppsala universitetInstitutionen för farmaci (creator_code:org_t)

Related titles

In:European journal of pharmaceutics and biopharmaceutics: Elsevier BV132, s. 222-2300939-64111873-3441

Internet link

Find in a library

European journal of pharmaceutics and biopharmaceutics (Search for host publication in LIBRIS)

To the university's database

1 of 1
Previous record
Next record
To hitlist

Find more in SwePub

By the author/editor: Roos, Carl; Dahlgren, David; Sjögren, Erik, 1 ...; Sjöblom, Markus, ...; Hedeland, Mikael; Lennernäs, Hans

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Pharmaceutical S ...

Articles in the publication: European journal ...

By the university: Uppsala University

Search outside SwePub

Extend your search to:: Google; Google Book Search; Google Scholar

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

LIBRIS.kb.se