Document Detail

The manufacture and characterisation of hot-melt extruded enteric tablets.
MedLine Citation:
PMID:  18164604     Owner:  NLM     Status:  MEDLINE    
The aim of this highly novel study was to use hot-melt extrusion technology as an alternative process to enteric coating. In so doing, oral dosage forms displaying enteric properties may be produced in a continuous, rapid process, providing significant advantages over traditional pharmaceutical coating technology. Eudragit L100-55, an enteric polymer, was pre-plasticized with triethyl citrate (TEC) and citric acid and subsequently dry-mixed with 5-aminosalicylic acid, a model active pharmaceutical ingredient (API), and an optional gelling agent (PVP K30 or Carbopol 971P). Powder blends were hot-melt extruded as cylinders, cut into tablets and characterised using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and dissolution testing conducted in both pH 1.2 and pH 6.8 buffers. Increasing the concentration of TEC significantly lowered the glass transition temperature (Tg) of Eudragit L100-55 and reduced temperatures necessary for extrusion as well as the die pressure. Moreover, citric acid (17% w/w) was shown to act as a solid-state plasticizer. HME tablets showed excellent gastro-resistance, whereas milled extrudates compressed into tablets released more than 10% w/w of the API in acidic media. Drug release from HME tablets was dependent upon the concentration of TEC, the presence of citric acid, PVP K30, and Carbopol 971P in the matrix, and pH of the dissolution media. The inclusion of an optional gelling agent significantly reduced the erosion of the matrix and drug release rate at pH 6.8; however, the enteric properties of the matrix were lost due to the formation of channels within the tablet. Consequently this work is both timely and highly innovative and identifies for the first time a method of producing an enteric matrix tablet using a continuous hot-melt extrusion process.
Gavin P Andrews; David S Jones; Osama Abu Diak; Colin P McCoy; Alan B Watts; James W McGinity
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Publication Detail:
Type:  Journal Article     Date:  2007-11-13
Journal Detail:
Title:  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V     Volume:  69     ISSN:  0939-6411     ISO Abbreviation:  Eur J Pharm Biopharm     Publication Date:  2008 May 
Date Detail:
Created Date:  2008-04-09     Completed Date:  2008-08-11     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9109778     Medline TA:  Eur J Pharm Biopharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  264-73     Citation Subset:  IM    
School of Pharmacy, The Queen's University of Belfast, Belfast, Northern Ireland, UK. <>
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MeSH Terms
Acrylates / chemistry
Acrylic Resins / chemistry
Calorimetry, Differential Scanning
Chemistry, Pharmaceutical / methods*
Citrates / chemistry
Citric Acid / chemistry
Hydrogen-Ion Concentration
Mesalamine / chemistry
Polymers / chemistry
Povidone / chemistry*
Tablets, Enteric-Coated / chemistry*
Technology, Pharmaceutical / methods*
X-Ray Diffraction
Reg. No./Substance:
0/Acrylates; 0/Acrylic Resins; 0/Citrates; 0/Eudragit L100-55; 0/Polymers; 0/Tablets, Enteric-Coated; 0/carbopol 971P; 77-92-9/Citric Acid; 77-93-0/ethyl citrate; 89-57-6/Mesalamine; 9003-39-8/Povidone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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