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Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends.
Eur J Pharm Biopharm. 2010 Nov; 76(3):486-92.EJ

Abstract

The objective of this study was to develop pH-erosion-controlled compression-coated tablets for potential colonic drug delivery with improved gastric resistance and pulsatile release based on compression-coatings of powder blends of the enteric polymer Eudragit® L100-55 and the extended release polymer ethylcellulose. Tablet cores containing model drugs of varying solubilities (acetaminophen, carbamazepine and chlorpheniramine maleate) were compression-coated with different ratios of Eudragit® L100-55:ethylcellulose 10cP FP at different compression forces and tablet core:compression-coat ratios. The compression-coated tablets were characterized by drug release, media uptake, erosion behaviour and wettability. All drugs were released in a pulsatile fashion in higher pH-media after a lag time, which was controlled by the erosion properties of the Eudragit L:ethylcellulose compression-coating. The addition of ethylcellulose avoided premature drug release in lower pH-media and significantly increased the lag time in higher pH-media because of a reduction in wettability, media uptake and erosion of the compression-coatings. Importantly, ethylcellulose also reduced the pH-dependency of the erosion process between pH 5.5 and 7.4. The lag time could also be increased by increasing the compression force and decreasing the core:compression-coat ratio. In conclusion, tablets compression-coated with blends of Eudragit L and ethylcellulose resulted in excellent release properties for potential targeting to the lower intestinal tract with no release in lower pH-media and rapid release after a controllable lag time in higher pH-media.

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Authors+Show Affiliations

Rujivipat S
College of Pharmacy, Freie Universität Berlin, Berlin, Germany.
Bodmeier R
No affiliation info available

MeSH

CelluloseColonDrug Delivery SystemsExcipientsHydrogen-Ion ConcentrationIntestine, SmallPharmaceutical PreparationsPharmacokineticsPolymersPolymethacrylic AcidsPowdersSolubilityTablets

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20868750

Citation

Rujivipat, Soravoot, and Roland Bodmeier. "Improved Drug Delivery to the Lower Intestinal Tract With Tablets Compression-coated With Enteric/nonenteric Polymer Powder Blends." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 76, no. 3, 2010, pp. 486-92.
Rujivipat S, Bodmeier R. Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends. Eur J Pharm Biopharm. 2010;76(3):486-92.
Rujivipat, S., & Bodmeier, R. (2010). Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 76(3), 486-92. https://doi.org/10.1016/j.ejpb.2010.09.004
Rujivipat S, Bodmeier R. Improved Drug Delivery to the Lower Intestinal Tract With Tablets Compression-coated With Enteric/nonenteric Polymer Powder Blends. Eur J Pharm Biopharm. 2010;76(3):486-92. PubMed PMID: 20868750.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends. AU - Rujivipat,Soravoot, AU - Bodmeier,Roland, Y1 - 2010/09/22/ PY - 2010/06/22/received PY - 2010/08/17/revised PY - 2010/09/13/accepted PY - 2010/9/28/entrez PY - 2010/9/28/pubmed PY - 2011/5/27/medline SP - 486 EP - 92 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 76 IS - 3 N2 - The objective of this study was to develop pH-erosion-controlled compression-coated tablets for potential colonic drug delivery with improved gastric resistance and pulsatile release based on compression-coatings of powder blends of the enteric polymer Eudragit® L100-55 and the extended release polymer ethylcellulose. Tablet cores containing model drugs of varying solubilities (acetaminophen, carbamazepine and chlorpheniramine maleate) were compression-coated with different ratios of Eudragit® L100-55:ethylcellulose 10cP FP at different compression forces and tablet core:compression-coat ratios. The compression-coated tablets were characterized by drug release, media uptake, erosion behaviour and wettability. All drugs were released in a pulsatile fashion in higher pH-media after a lag time, which was controlled by the erosion properties of the Eudragit L:ethylcellulose compression-coating. The addition of ethylcellulose avoided premature drug release in lower pH-media and significantly increased the lag time in higher pH-media because of a reduction in wettability, media uptake and erosion of the compression-coatings. Importantly, ethylcellulose also reduced the pH-dependency of the erosion process between pH 5.5 and 7.4. The lag time could also be increased by increasing the compression force and decreasing the core:compression-coat ratio. In conclusion, tablets compression-coated with blends of Eudragit L and ethylcellulose resulted in excellent release properties for potential targeting to the lower intestinal tract with no release in lower pH-media and rapid release after a controllable lag time in higher pH-media. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/20868750/Improved_drug_delivery_to_the_lower_intestinal_tract_with_tablets_compression_coated_with_enteric/nonenteric_polymer_powder_blends_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(10)00226-2 DB - PRIME DP - Unbound Medicine ER -