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Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid.
Eur J Pharm Biopharm. 2005 Jan; 59(1):85-97.EJ

Abstract

Hot-melt extruded tablets were prepared using Eudragit S 100 as the polymeric carrier to target delivery of 5-aminosalicylic acid (5-ASA) to the colon. Scanning electron microscopy, modulated differential scanning calorimetry and X-ray diffraction analysis of the hot-melt tablet extrudates demonstrated that 5-ASA remained crystalline and was homogeneously dispersed throughout the polymer matrix. A pre-plasticization step was necessary when incorporating triethyl citrate (TEC) into the formulation in order to achieve uniform mixing of the polymer and plasticizer, effectively reduce the polymer glass transition temperature (T(g)), and to lower the processing temperatures. The concentration of TEC in the extrudates not only influenced the processing temperature, but also influenced the drug release rates from the extruded tablets due to leaching of the TEC during dissolution testing. Citric acid monohydrate was found to plasticize Eudragit S 100, and when combined with TEC in the powder blend, the temperatures required for processing were reduced. Tablets containing citric acid released drug at a slower rate as a result of the suppression of polymer ionization due to a decrease in the micro-environmental pH of the tablet. The drug release profiles of the extruded tablets were found to fit both diffusion and surface erosion models.

Authors+Show Affiliations

Quintiles, Inc., Kansas City, MO 64137, USA. diane.bruce@quintiles.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

15567305

Citation

Bruce, L Diane, et al. "Properties of Hot-melt Extruded Tablet Formulations for the Colonic Delivery of 5-aminosalicylic Acid." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 59, no. 1, 2005, pp. 85-97.
Bruce LD, Shah NH, Malick AW, et al. Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid. Eur J Pharm Biopharm. 2005;59(1):85-97.
Bruce, L. D., Shah, N. H., Malick, A. W., Infeld, M. H., & McGinity, J. W. (2005). Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 59(1), 85-97.
Bruce LD, et al. Properties of Hot-melt Extruded Tablet Formulations for the Colonic Delivery of 5-aminosalicylic Acid. Eur J Pharm Biopharm. 2005;59(1):85-97. PubMed PMID: 15567305.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid. AU - Bruce,L Diane, AU - Shah,Navnit H, AU - Malick,A Waseem, AU - Infeld,Martin H, AU - McGinity,James W, PY - 2004/03/24/received PY - 2004/06/25/accepted PY - 2004/11/30/pubmed PY - 2005/4/20/medline PY - 2004/11/30/entrez SP - 85 EP - 97 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 59 IS - 1 N2 - Hot-melt extruded tablets were prepared using Eudragit S 100 as the polymeric carrier to target delivery of 5-aminosalicylic acid (5-ASA) to the colon. Scanning electron microscopy, modulated differential scanning calorimetry and X-ray diffraction analysis of the hot-melt tablet extrudates demonstrated that 5-ASA remained crystalline and was homogeneously dispersed throughout the polymer matrix. A pre-plasticization step was necessary when incorporating triethyl citrate (TEC) into the formulation in order to achieve uniform mixing of the polymer and plasticizer, effectively reduce the polymer glass transition temperature (T(g)), and to lower the processing temperatures. The concentration of TEC in the extrudates not only influenced the processing temperature, but also influenced the drug release rates from the extruded tablets due to leaching of the TEC during dissolution testing. Citric acid monohydrate was found to plasticize Eudragit S 100, and when combined with TEC in the powder blend, the temperatures required for processing were reduced. Tablets containing citric acid released drug at a slower rate as a result of the suppression of polymer ionization due to a decrease in the micro-environmental pH of the tablet. The drug release profiles of the extruded tablets were found to fit both diffusion and surface erosion models. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/15567305/Properties_of_hot_melt_extruded_tablet_formulations_for_the_colonic_delivery_of_5_aminosalicylic_acid_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(04)00193-6 DB - PRIME DP - Unbound Medicine ER -