Scintigraphic evaluation of colon targeting pectin-HPMC tablets in healthy volunteers

L.A. Hodges, S.M. Connolly, J. Band, B. O'Mahony, T. Ugurlu, M. Turkoglu, C.G. Wilson, H.N.E. Stevens

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

The in vivo evaluation of colon-targeting tablets was conducted in six healthy male volunteers. A pectin-hydroxypropyl methylcellulose coating was compressed onto core tablets labelled with 4 MBq 99mTc-DTPA. The tablets released in the colon in all subjects; three in the ascending colon (AC) and three in the transverse colon (TC). Tablets that released in the TC had reached the AC before or just after food (Group A). The other three tablets released immediately upon AC entry at least 1.5 h post-meal (Group B). Release onset for Group B was earlier than Group A (343 min vs 448 min). Group B tablets exhibited a clear residence period at the ileocaecal junction (ICJ) which was not observed in Group A. Prolonged residence at the ICJ is assumed to have increased hydration of the hydrogel layer surrounding the core tablet. Forces applied as the tablets progressed through the ICJ may have disrupted the hydrogel layer sufficiently to initiate radiolabel release. Conversely, Group A tablets moved rapidly through the AC to the TC, possibly minimising contact times with water pockets. Inadequate prior hydration of the hydrogel layer preventing access of pectinolytic enzymes and reduced fluid availability in the TC may have retarded tablet disintegration and radiolabel diffusion.
LanguageEnglish
Pages144-150
Number of pages6
JournalInternational Journal of Pharmaceutics
Volume370
Issue number1-2
DOIs
Publication statusPublished - 31 Mar 2009

Fingerprint

Tablets
Healthy Volunteers
Colon
Ascending Colon
Transverse Colon
Hydrogel
pectin
Pentetic Acid
Meals
Food
Water
Enzymes

Keywords

  • compression-coated tablets
  • colon-specific drug delivery
  • gamma scintigraphy
  • HPMC
  • pectin

Cite this

Hodges, L.A. ; Connolly, S.M. ; Band, J. ; O'Mahony, B. ; Ugurlu, T. ; Turkoglu, M. ; Wilson, C.G. ; Stevens, H.N.E. / Scintigraphic evaluation of colon targeting pectin-HPMC tablets in healthy volunteers. In: International Journal of Pharmaceutics. 2009 ; Vol. 370, No. 1-2. pp. 144-150.
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Scintigraphic evaluation of colon targeting pectin-HPMC tablets in healthy volunteers. / Hodges, L.A.; Connolly, S.M.; Band, J.; O'Mahony, B.; Ugurlu, T.; Turkoglu, M.; Wilson, C.G.; Stevens, H.N.E.

In: International Journal of Pharmaceutics, Vol. 370, No. 1-2, 31.03.2009, p. 144-150.

Research output: Contribution to journalArticle

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