Development and potential application of an oral ColoPulse infliximab tablet with colon specific release: A feasibility study

Jacoba M Maurer; Susan Hofman; Reinout C A Schellekens; Wouter F Tonnis; Annelien O T Dubois; Herman J Woerdenbag; Wouter L J Hinrichs; Jos G W Kosterink; Henderik W Frijlink

doi:10.1016/j.ijpharm.2016.03.027

Development and potential application of an oral ColoPulse infliximab tablet with colon specific release: A feasibility study

Int J Pharm. 2016 May 30;505(1-2):175-86. doi: 10.1016/j.ijpharm.2016.03.027. Epub 2016 Mar 17.

Authors

Jacoba M Maurer¹, Susan Hofman², Reinout C A Schellekens³, Wouter F Tonnis⁴, Annelien O T Dubois⁵, Herman J Woerdenbag⁶, Wouter L J Hinrichs⁷, Jos G W Kosterink⁸, Henderik W Frijlink⁹

Affiliations

¹ Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands. Electronic address: m.maurer@umcg.nl.
² Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands. Electronic address: s.hofman@umcg.nl.
³ Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands. Electronic address: reinout.schellekens@kpnplanet.nl.
⁴ Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: w.tonnis@gmail.com.
⁵ Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: a.o.t.dubois@gmail.com.
⁶ Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: h.j.woerdenbag@rug.nl.
⁷ Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: w.l.j.hinrichs@rug.nl.
⁸ Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands; Department of Pharmacotherapy and Pharmaceutical Care, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: j.g.w.kosterink@umcg.nl.
⁹ Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: h.w.frijlink@rug.nl.

PMID: 26997425
DOI: 10.1016/j.ijpharm.2016.03.027

Abstract

The monoclonal antibody infliximab is one of the cornerstones in the treatment of Crohn's disease. Local delivery of infliximab would be an alternative to overcome the inherent disadvantages of intravenous therapy. For this purpose 5mg infliximab tablets were developed. To stabilize the antibody during production and storage it was incorporated in a sugar glass containing the oligosaccharide inulin. To obtain colon-specific release a ColoPulse coating was applied. The tablets were stored for 16 months under different conditions based on ICH climatic zone I.

Keywords: ColoPulse; Colon specific delivery; Crohn’s disease; Formulation; Infliximab; Oral delivery; Protein stability.

MeSH terms

Chemistry, Pharmaceutical / methods
Colon / metabolism
Crohn Disease / drug therapy
Delayed-Action Preparations
Drug Delivery Systems*
Drug Stability
Drug Storage
Excipients / chemistry*
Feasibility Studies
Gastrointestinal Agents / administration & dosage*
Gastrointestinal Agents / chemistry
Infliximab / administration & dosage*
Infliximab / chemistry
Inulin / chemistry
Tablets
Time Factors

Substances

Delayed-Action Preparations
Excipients
Gastrointestinal Agents
Tablets
Inulin
Infliximab