Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
In Vitro and In Vivo Modeling of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Erosion Under Fasting and Postprandial Status
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
AstraZeneca, Pharmaceut Technol & Dev, Gothenburg, Sweden.;Janssen Pharmaceut NV, Turnhoutseweg 30, B-2340 Beerse, Belgium..
AstraZeneca, Adv Drug Delivery Pharmaceut Sci Innovat Med & Ea, Gothenburg, Sweden..
AstraZeneca, Drug Metab & Pharmacokinet, Cardiovasc & Metab Dis, Innovat Med & Early Dev, Gothenburg, Sweden..
Show others and affiliations
2017 (English)In: Pharmaceutical research, ISSN 0724-8741, E-ISSN 1573-904X, Vol. 34, no 4, 847-859 p.Article in journal (Refereed) Published
Abstract [en]

To develop a model linking in vitro and in vivo erosion of extended release tablets under fasting and postprandial status. A nonlinear mixed-effects model was developed from the in vitro erosion profiles of four hydroxypropyl methylcellulose (HPMC) matrix tablets studied under a range of experimental conditions. The model was used to predict in vivo erosion of the HPMC matrix tablets in different locations of the gastrointestinal tract, determined by magnetic marker monitoring. In each gastrointestinal segment the pH was set to physiological values and mechanical stress was estimated in USP2 apparatus rotation speed equivalent. Erosion was best described by a Michaelis-Menten type model. The maximal HPMC release rate (V-MAX) was affected by pH, mechanical stress, HPMC and calcium hydrogen phosphate content. The amount of HPMC left at which the release rate is half of V-MAX depended on pH and calcium hydrogen phosphate. Mechanical stress was estimated for stomach (39.5 rpm), proximal (93.3 rpm) and distal (31.1 rpm) small intestine and colon (9.99 rpm). The in silico model accurately predicted the erosion profiles of HPMC matrix tablets under fasting and postprandial status and can be used to facilitate future development of extended release tablets.

Place, publisher, year, edition, pages
2017. Vol. 34, no 4, 847-859 p.
Keyword [en]
food effect, hydroxypropyl methylcellulose, in vitro in vivo correlation, magnetic marker monitoring, NONMEM
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-321446DOI: 10.1007/s11095-017-2113-7ISI: 000396065400016PubMedID: 28155077OAI: oai:DiVA.org:uu-321446DiVA: diva2:1093127
Available from: 2017-05-05 Created: 2017-05-05 Last updated: 2017-05-05

Open Access in DiVA

fulltext(2252 kB)45 downloads
File information
File name FULLTEXT01.pdfFile size 2252 kBChecksum SHA-512
818bedc7026d43852bfe7c53388b362c3f986311522615ed475b60c8558923b3e459a9f82e60143f66f39974c00a4963a7b678da8c7879eb9c704e1a5de6d8d4
Type fulltextMimetype application/pdf

Other links

Publisher's full textPubMed

Search in DiVA

By author/editor
Guiastrennec, BenjaminBergstrand, Martin
By organisation
Department of Pharmaceutical Biosciences
In the same journal
Pharmaceutical research
Pharmaceutical Sciences

Search outside of DiVA

GoogleGoogle Scholar
Total: 45 downloads
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: 305 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf