Tags

Type your tag names separated by a space and hit enter

The manufacture and characterisation of hot-melt extruded enteric tablets.
Eur J Pharm Biopharm. 2008 May; 69(1):264-73.EJ

Abstract

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.

Authors+Show Affiliations

School of Pharmacy, The Queen's University of Belfast, Belfast, Northern Ireland, UK. g.andrews@qub.ac.uk <g.andrews@qub.ac.uk>No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18164604

Citation

Andrews, Gavin P., et al. "The Manufacture and Characterisation of Hot-melt Extruded Enteric Tablets." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 69, no. 1, 2008, pp. 264-73.
Andrews GP, Jones DS, Diak OA, et al. The manufacture and characterisation of hot-melt extruded enteric tablets. Eur J Pharm Biopharm. 2008;69(1):264-73.
Andrews, G. P., Jones, D. S., Diak, O. A., McCoy, C. P., Watts, A. B., & McGinity, J. W. (2008). The manufacture and characterisation of hot-melt extruded enteric tablets. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 69(1), 264-73. https://doi.org/10.1016/j.ejpb.2007.11.001
Andrews GP, et al. The Manufacture and Characterisation of Hot-melt Extruded Enteric Tablets. Eur J Pharm Biopharm. 2008;69(1):264-73. PubMed PMID: 18164604.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The manufacture and characterisation of hot-melt extruded enteric tablets. AU - Andrews,Gavin P, AU - Jones,David S, AU - Diak,Osama Abu, AU - McCoy,Colin P, AU - Watts,Alan B, AU - McGinity,James W, Y1 - 2007/11/13/ PY - 2007/08/16/received PY - 2007/11/01/revised PY - 2007/11/06/accepted PY - 2008/1/1/pubmed PY - 2008/8/12/medline PY - 2008/1/1/entrez SP - 264 EP - 73 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 69 IS - 1 N2 - 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. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/18164604/The_manufacture_and_characterisation_of_hot_melt_extruded_enteric_tablets_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(07)00367-0 DB - PRIME DP - Unbound Medicine ER -