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Novel mesalamine-loaded beads in tablets for delayed release of drug to the colon.
Pharm Dev Technol. 2012 Jan-Feb; 17(1):73-83.PD

Abstract

Novel 'beads-in-a-tablet' formulations (total weight ∼740-780 mg) have been prepared that meet USP 31 requirements for Delayed Release of mesalamine. Several methods are presented that overcome breakage of beads during tablet compaction were explored. Bead formulations comprise a combination of extrusion and spheronization to produce a relatively high drug load (80%), followed by coating (25%) with a colonic-targeted drug release polymer (polymethacrylates, Eudragit(®) S100), overcoated (3%) with hydroxypropyl methylcellulose (Opadry(®)) to improve bead binding and compactability, and using 20% coat of lactose/sodium starch glycolate (Explotab(®)) as binder/disintegrant/cushioning agent, thus allowing a sufficiently thick coating to be uniform and without being broken during tablet compaction. Then, the aforementioned beads were compressed into tablets at 1500 pounds of pressure containing 400 mg of mesalamine, and finally coating the compressed tablets with Surelease(®) (ethylcellulose):Opadry(®) = 1:0.5 ranging from 1.5-2.5% weight gain; the resulting tablets met USP 31 dissolution requirements for delayed release tablets.

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Publisher Full Text

Authors+Show Affiliations

Nguyen C
Industrial Department of Pharmacy, Hanoi University of Pharmacy, Hanoi, Vietnam.
Christensen JM
No affiliation info available
Ayres JW
No affiliation info available

MeSH

Anti-Inflammatory Agents, Non-SteroidalCelluloseChemistry, PharmaceuticalColonDelayed-Action PreparationsDrug CompoundingDrug Delivery SystemsExcipientsMesalaminePolymethacrylic AcidsPolyvinylsSolubilityTablets

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20923254

Citation

Nguyen, Chien, et al. "Novel Mesalamine-loaded Beads in Tablets for Delayed Release of Drug to the Colon." Pharmaceutical Development and Technology, vol. 17, no. 1, 2012, pp. 73-83.
Nguyen C, Christensen JM, Ayres JW. Novel mesalamine-loaded beads in tablets for delayed release of drug to the colon. Pharm Dev Technol. 2012;17(1):73-83.
Nguyen, C., Christensen, J. M., & Ayres, J. W. (2012). Novel mesalamine-loaded beads in tablets for delayed release of drug to the colon. Pharmaceutical Development and Technology, 17(1), 73-83. https://doi.org/10.3109/10837450.2010.516436
Nguyen C, Christensen JM, Ayres JW. Novel Mesalamine-loaded Beads in Tablets for Delayed Release of Drug to the Colon. Pharm Dev Technol. 2012 Jan-Feb;17(1):73-83. PubMed PMID: 20923254.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Novel mesalamine-loaded beads in tablets for delayed release of drug to the colon. AU - Nguyen,Chien, AU - Christensen,J Mark, AU - Ayres,James W, Y1 - 2010/10/05/ PY - 2010/10/7/entrez PY - 2010/10/7/pubmed PY - 2012/4/11/medline SP - 73 EP - 83 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 17 IS - 1 N2 - Novel 'beads-in-a-tablet' formulations (total weight ∼740-780 mg) have been prepared that meet USP 31 requirements for Delayed Release of mesalamine. Several methods are presented that overcome breakage of beads during tablet compaction were explored. Bead formulations comprise a combination of extrusion and spheronization to produce a relatively high drug load (80%), followed by coating (25%) with a colonic-targeted drug release polymer (polymethacrylates, Eudragit(®) S100), overcoated (3%) with hydroxypropyl methylcellulose (Opadry(®)) to improve bead binding and compactability, and using 20% coat of lactose/sodium starch glycolate (Explotab(®)) as binder/disintegrant/cushioning agent, thus allowing a sufficiently thick coating to be uniform and without being broken during tablet compaction. Then, the aforementioned beads were compressed into tablets at 1500 pounds of pressure containing 400 mg of mesalamine, and finally coating the compressed tablets with Surelease(®) (ethylcellulose):Opadry(®) = 1:0.5 ranging from 1.5-2.5% weight gain; the resulting tablets met USP 31 dissolution requirements for delayed release tablets. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/20923254/Novel_mesalamine_loaded_beads_in_tablets_for_delayed_release_of_drug_to_the_colon_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837450.2010.516436 DB - PRIME DP - Unbound Medicine ER -