4,689
Views
315
CrossRef citations to date
0
Altmetric
Technology Evaluation

Eudragit®: a technology evaluation

, &
Pages 131-149 | Published online: 26 Oct 2012

Bibliography

  • Elias HG. Makromolecukule. Volume 1 Chemische struktur und syntheses. 6th edition. P 303ff Wiley-VCH; Weinheim: 1999
  • Evonik: Eudragit Application Guidelines 11th editoin, 09/2009. Available from: http://www.pharma-polymers.com/pharmapolymers/en/downloads
  • Rowe RC, Sheskey PJ, Weller PJ. Handbook of pharmaceutical excipients. 4th edition. The Pharmaceutical Press; London: 2003
  • Dittgen M, Durrani M, Lehmann K. Acrylic polymers: a review of pharmaceutical applications. STP Pharm Sci 1997;7(6):403-37
  • Sauer D. An investigation of formulation factors and processing parameters for the powder-coating of tablets. The University of Texas; Austin: 2008
  • Sharma M, Sharma V, Panda AK, Majumdar DK. Development of enteric submicron particle formulation for oral delivery of papain. Int J Nanomedicine 2011;6:2097-111
  • Lin SH, Yu HL. Microscopic fourier transform infrared/differential scanning calorimetry system used to study the different thermal behaviours of polymethacrylate copolymers of Eudragit RS, RL, E 30D or E. J Appl Polym Sci 2000;78:829-35
  • Tu J, Shen Y, Mahalingam R, Polymers in oral modified release systems. Chapter 5. In: Wen H, Park K, editiors Oral controlled release formulation design and drug delivery: theory to practice. John Wiley and Sons; New Jersey: 2010. p. 71-87
  • O'Donnel PB, McGinity JW. Mechanical properties of polymeric films prepared from aqueous polymeric dispersions. In: McGinity JW, editior Aqueous polymeric coatings for pharmaceutical dosage forms. 2nd ednition. Marcel Dekker Inc; New York: 1993. p. 517-48
  • Lin SY, Chen KS, Run-Chu L. Organic esters of plasticizers affecting the water absorption, adhesive property, glass transition temperature and plasticizer permanence of Eudragit acrylic films. J Control Release 2000;68:343-50
  • Chang RK, Hsiao C. Eudragit RL and RS pseudolatices: properties and peformance in pharmaceutical coating as a controlled release mechanism for theophylline pellets. Drug Dev Ind Pharm 1989;15:187-96
  • Cole G, Hogan J, Aulton M. Pharmaceutical coating technology. Taylor and Francis; London: 1995. p. 1-5
  • Bose S, Bogner RH. Solvent less pharmaceutical coating processes: a review. Pharm Dev Technol 2007;12:115-31
  • Fahie BJ, Nangia A, Chopra SK, Use of NMR imaging in the optimization of a compression-coated regulated release system. J Control Release 1998;51:179-84
  • Pearnchob N, Bodmeier R. Dry powder coating of pellets with micronized Eudragit RS for extended drug release. Pharm Res 2003;20:1970-6
  • Cerea M, Zheng W, Young CR, McGinity JW. A novel powder coating process for attaining taste masking and moisture protective films applied to tablets. Int J Pharm 2004;279:127-39
  • Zheng W, Cerea M, Sauer D, McGinity JW. Properties of theophylline tablets powder-coated with methacrylate ester copolymers. J Drug Deliv Sci Technol 2004;14:319-25
  • Sauer D, Zheng W, Coots LB, McGinity JW. Influence of processing parameters and formulation factors on the drug release from tablets powder-coated with Eudragit L 100-55. Eur J Pharm Biopharm 2007;67:464-75
  • Whiteman M, Hallett MD, Feather DH, Electrostatic application of powder material to solid dosage forms. WO061841; 2003
  • Hallett MD. Method and apparatus for applying powder in a pattern to a substrate. US20060099350; 2006
  • Qiao M, Luo Y, Zhang L, Sustained release coating of tablets with Eudragit RS/RL using a novel electrostatic dry powder coating process. Int J Pharm 2010;399:37-43
  • Eisele J, Haynes G, Rosamilia T. Characterisation and toxicological behaviour of Basic Methacrylate Copolymer for GRAS evaluation. Regul Toxicol Pharmacol 2011;61:32-43
  • Nunziata A. Praparat 12991/1 (F) aus Plex 4110: Acute oral toxicity study in the rat (Study number 5090, Research Toxicology Centre SpA, Via Tito Speri 12, 00040 Pomezia (RM), Italy) (1995)
  • Eileraas M. Eudragit FS 30 D: 4 week oral toxicity study in dogs (Study 8101, Research Toxicity Centre SpA, 00040 Pomezia (RM) (2004)
  • Venturella S. Eudragit FS 30D Freeze Dried: 26 week oral toxicity study in the rat followed by 4 week recovery period (Report 7250/T/346/2000, Research Toxicology Centre SpA, 00040, Pomezia (RM), Italy (2000)
  • Wollny HE. Cell mutation assay at the thymidine kinase locus (TK+/-) in mouse lymphoma L5178Y cells with Eudragit FS 30 D freeze dried (Study 689302, RCC Cytotest Cell Research GmbH, 64389 Roβdorf, Germany) (2001)
  • FDA, Centre for Drug Evaluation and Research, Inactive Ingredients for Approved Drug Products. Available from: http://www.accessdata.fda.gov/scripts/cder/iig/index.cfm [Accessed 15 September 2012]
  • Davenport HW. Physiology of the digestive tract. 3rd edition. Year Book Medical Publishers; New York: 1971
  • Evans DF, Pye G, Bramley R, Measurement of gastrointestinal pH profiles in normal ambulant human subject. Gut 1988;29:1035-41
  • Basit AW. Advances in colonic drug delivery. Drugs 2005;65:1991-2007
  • Dew MJ, Hughes PJ, Lee MG, An oral preparation to release drugs in human colon. Br J Clin Pharmacol 1982;14:163-9
  • Dew MJ, Ryder REJ, Evans N, Rhodes J. Colonic release of 5-aminosalicylic acid from oral preparation in active ulcerative colitis. Br J Clin Pharmacol 1983;16:185-7
  • Jain D, Panda AK, Majumdar DK, Eudragit S. 100 entrapped Insulin microspheres for oral delivery. AAPS Pharm Sci Tech 2005;06:E100-7
  • Jain D, Panda AK, Majumdar DK. Insulin loaded Eudragit L100 microspheres for oral delivery: preliminary in vitro studies. J Biomater Appl 2006;21(2):195-211
  • Thomas P, Richards D, Richards A. Absorption of delayed release prednisolone in ulcerative colitis and Crohn's disease. J Pharm Pharmacol 1985;37:757-8
  • Thakral NK, Ray AR, Bar-Shalom D, Soluplus-solubilized citrated camptothecin-a potential drug delivery strategy in colon cancer. AAPS PharmSciTech 2012;13(1):59-66
  • Hardy JG, Evans DF, Zaki I, Evaluation of an enteric coated naproxen tablet using gamma scintigraphy and pH monitoring. Int J Pharm 1987;37:245-50
  • Kim CK, Shin HJ, Yang SG, Once a day oral dosing regimen of cyclosporine A: combined therapy of cyclosporine a premicroemulsion concentrate and enteric coated solid-state premicroemulsion concentrates. Pharm Res 2001;18:454-9
  • Watts PJ, Illum L. Colonic drug delivery. Drug Dev Ind Pharm 1997;23:893-913
  • Khan MZ, Prebeg Z, Kurjakovic N. A pH dependent colon targeted oral drug delivery system using methacrylic acid copolymers. I manipulation of drug release using Eudragit L 100-55 and Eudragit S100 combinations. J Control Release 1999;58:215-22
  • Ji C, Xu H, Wu W. In vitro evaluation and pharmacokinetics in dogs of guar gum and Eudragit FS 30-D coated-colon-targeted pellets of indomethacin. J Drug Target 2007;15:123-31
  • Gao C, Huang J, Jiao Y, In vitro release and in vivo absorption in beagle dogs of meloxicam from Eudragit FS 30 D-coated pellets. Int J Pharm 2006;322:104-12
  • Li Y, Li HJ, Yang GR, Colon-specific delivery tablets of sodium 4-amino salicylic acid. Yao Xue Xue Bao 2006;41:927-32
  • Chu JS. Advances in colon specific drug delivery system employing CODESTH, The Drug Delivery Companies Report, Autumn/Winter Pharmaventure Ltd (2003)
  • Nugent SG, Kumar D, Rampton DS, Intestinal luminal pH in inflammatory bowel disease: possible determinants and implications for therapy with aminosalicylates and other drugs. Gut 2001;48:571-7
  • Safdi AV. Determination of 5-ASA in whole or partial mesalamine delayed-release tablets recovered from fecal samples of healthy volunteers. Am J Gastroenterol 2005;100:S159
  • Ibekwe VC, Lui F, Fadda HM, An investigation into the in vivo performance variability of pH responsive polymers for ileo-colonic drug delivery using gamma scintigraphy in human. J Pharm Sci 2006;95:2760-6
  • Friend DR. Colon-specific drug delivery. Adv Drug Deliv Rev 1991;7:149-99
  • Akhgari A, Farahmand F, Afrasiabi GH, Permeability and swelling studies on free films containing inulin in combination with different polymethacrylates aimed for colonic drug delivery. Eur J Pharm Sci 2006;28:307-14
  • Ibekwe VC, Khela MK, Evans DF, Basit AW. A new concept in colonic drug targeting: a combination of pH responsive and bacterially triggered drug delivery technology. Aliment Pharmacol Ther 2008;28:911-16
  • Cole ET, Scott RA, Connor AL, Enteric coated HPMC capsules designed to achieve intestinal targeting. Int J Pharm 2002;231:83-95
  • Sinha VR, Kumria R. Coating polymers for colon specific drug delivery: a comprehensive 1 in vitro evaluation. Acta Pharm 2003;53:41-7
  • Akhgari A, Garekani HA, Sadeghi F, Azimaie M. Statistical optimization of indomethacin pellets coated with pH dependent methacrylic polymers for possible colonic drug delivery. Int J Pharm 2005;305:22-30
  • Ibekwe VC, Fadda HM, Parsons GE, Basit AW. A comparative in vitro assessment of the drug release performance of pH-responsive polymers for ileo-colonic delivery. Int J Pharm 2006;308:52-60
  • Cheng G, An F, Zou MJ, Time and pH-dependent colon specific drug delivery for orally administered diclofenac sodium and 5-aminosalicylic acid. World J Gastroenterol 2004;10:1769-74
  • Mura P, Marstrelli F, Cirri M, Development of enteric coated pectin based matrix tablets for colonic delivery of theophylline. J Drug Traget 2003;11:365-71
  • Chourasia MK, Jain SK. Design and development of mutiparticulate system for targeted drug delivery to colon. Drug Deliv 2004;11:201-7
  • Mundargi RC, Patil SA, Agnihotri SA, Aminabhavi TM. Development of polysaccharide based colon targeted drug delivery systems for the treatment of amoebiasis. Drug Dev Ind Pharm 2007;33:255-64
  • Paharia A, Yadav AK, Rai G, Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting. AAPS PharmSciTech 2007;8:E87-93
  • Rahman Z, Kohli K, Khar RK, Characterization of 5-fluorouracil microspheres for colonic delivery. AAPS PharmSciTech 2006;7:E1-9
  • Umadevi SK, Thiruganesh R, Suresh S, Reddy KB. Formulation and evaluation of chitosan microspheres of aceclofenac for colon-targeted drug delivery. Biopharm Drug Dispos 2010;31:407-27
  • Zhang L, Cao F, Ding B, Eudragit S 100 coated calcium pectinate microspheres of curcumin for colon targeting. J Microencapsul 2011;28:659-67
  • Thakral NK, Ray AR, Majumdar DK. Eudragit S-100 Entrapped chitosan microspheres of valdecoxib for colon cancer. J Mater Sci Mater Med 2010;21:2691-9
  • Zimova L, Vetchy D, Muselik J, Stembirek J. The development and in vivo evaluation of a colon drug delivery system using human volunteers. Drug Deliv 2012;19:81-9
  • Asghar LF, Chandran S. Design and evaluation of matrices of Eudragit with polycarbophil and carbopol for colon-specific delivery. J Drug Target 2008;16:741-57
  • Kshirsagar SJ, Bhalekar MR, Patel JN, Preparation and characterisation of nanocapsules for colon-targeted drug delivery system. Pharm Dev Technol 2012;17(5):607-13
  • El-Bary AA, Aboelwafa AA, Al Sharabi IM. Influence of some formulation variables on the optimization of pH-dependent, colon-targeted, sustained-release mesalamine microspheres. AAPS PharmSciTech 2012;13:75-84
  • Amrutkar JR, Gattani SG. A novel hydrogel plug of Sterculia urens for pulsatile delivery: in vitro and in vivo evaluation. J Microencapsul 2012;29:72-82
  • Obeidat WM, Price JC. Preparation and evaluation of Eudragit S 100 microspheres as pH sensitive release preparations for piroxicam and theophylline using emulsion solvent evaporation method. J Micoencapsul 2006;23:195-202
  • Bruce LD, Shah NH, Malick AW, Properties of hot melt extruded tablet formulations for the colonic delivery of 5-amino salicylic acid. Eur J Biopharm 2005;59:85-97
  • Liu F, Lizio R, Meier C, A novel concept in enterc coating: a double-coating system providing rapid release in the proximal small intestine. J Control Release 2009;133:119-24
  • Lui F, Basit AW. A paradigm shift in enteric coating: achieving rapid release in the proximal small intestine of man. J Control Release 2010;147:242-5
  • McGinity JW, Felton LA. Aqueous polymeric coatings for pharmaceutical dosage forms. 3rd edition. Informa Healthcare; New York: 2008
  • Miller DA, McGinity JW. Aqueous polymeric film coating. In: Augsburger LL, Hoag SW, editors. Pharmaceutical dosage forms: tablets. Volume 1 3rd edition. Unit operations and mechanical properties. Informa Healthcare; New York: 2008
  • Fan TY, Wei SL, Yan WW, An investigation of pulsatile release tablets with ethyl cellulose and Eudragit L as film coating materials and cross-linked polyvinylpyrrolidone in the core tablets. J Control Release 2001;77:245-51
  • Steward PA, Hearn J, Wilkinson MC. Studies on permeation through polymer latex films. I Film coating containing no or low levels of additives. Polym Int 1995;38:1-12
  • Lehmann K. Chemistry and application properties of polymethacrylate coating system. In: McGinity JW, editor. Aqueous polymeric coating for pharmaceutical dosage forms. Marcel Dekker Inc; New York: 1997
  • Bodmeier R, Guo X, Sarabia RE, Skultety PF. The influence of buffer species and strength on diltiazam HCl released from beads coated with aqueous cationic polymer dispersion Eudragit RS 30 D. Pharm Res 1996;13:52-6
  • Wagner KG, McGinity JW. Influence of chloride in exchange on permeability and drug release from Eudragit RS 30D films. J Control Release 2002;82:385-97
  • Maejima T, McGinity JW. Influence of film additives on stabilizing drug release rates from pellets coated with acrylic polymers. Pharm Dev Technol 2001;6:211-21
  • El-Malah Y, Nazzal S. Novel use of Eudragit NE 30. D/Eudragit ® L 30D-55 blends as functional coating materials in time-delayed drug release applications. Int J Pharm 2008;357:219-27
  • Li G, Han D, Guan T, Isosorbide-5- mononitrate (5-ISMN) sustained release pellets prepared by double layer coating for reducing 5-ISMN migration and sublimation. Int J Pharm 2010;400:134-44
  • Lin AY, Muhammad NA, Pope D, Augsburger LL. Study of crystallization of endogenous surfactant in Eudragit NE30D-free films and its influence on drug release properties of controlled-release diphenhydramine HCl pellets coated with Eudragit NE30D. AAPS PharmSci 2001;3:E14
  • Agabeyoglu I. Studies on sustained release I, the biopharmaceutical design and preparation of an inert matrix type sulfamethazole tablet employing polymethacrylate. Drug Dev Ind Pharm 1985;11:2021-41
  • Oth MP, Moes AJ. Sustained release solid dispersion of indomethacin with eudragit RS and RL. Int J Pharm 1989;55:155-64
  • Abhaspour MR, Sadeghi F, Garekaw A. Preparation and characterization of ibuprofen pellets based on Eudragit RS PO and RL PO or their combination. Int J Pharm 2005;303:88-94
  • Ceballos A, Cirri M, Maestrelli F, Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets. Il Farmaco 2005;60:913-18
  • Colo DG, Falchi S, Zambito Z. In vitro evaluation of a system for pH-controlled peroral delivery of metformin. J Control Release 2002;80:119-28
  • Arevalo MF, Villafuerte MAH, Dorado JMG, Alvarez AMR. Effects of different fillers and wetting liquids on the dissolution of carteolol hydrochloride controlled release inert matrix tablets. Int J Pharm 1993;95:117-25
  • Aitken-Nichol C, Zhang F, McGinity JW. Hot melt extrusion of acrylic films. Pharm Res 1996;13:804-8
  • Follonier N, Doelker E, Cole ET. Evaluation of hot-melt extrusion as a new technique for the production of polymer-based pellets for sustained release capsules containing high loading of freely soluble drugs. Drug Dev Ind Pharm 1994;20:1323-39
  • Zhu Y, Shah NH, Malick AW, Solid state plasticization of an arylic polymer with chlorpheniramine maleate and triethyl citrate. Int J Pharm 2002;241:301-10
  • Crowley MM, Zhang F, Repka MA, Pharmaceutical applications of hot melt extrusion. Part I. Drug Dev Ind Pharm 2007;33:909-26
  • Douroumis D. Hot melt extrusion: pharmaceutical applications. John Wiley and Sons; Chichester, UK 2012
  • Zhu Y, Mehta KA, McGinity JW. Influence of plasticizer level in the drug release from sustained release film coated and hot melt extruded dosage forms. Pharm Dev Technol 2006;11:285-94
  • Ishikawa T, Watanabe Y, Utoguchi N, Matsumoto M. Preparation and evaluation of tablets rapidly disintegrating in saliva containing bitter-taste-masked granules by the compression method. Chem Pharm Bull 1999;47(10):1451-4
  • Lehmann K, Petereit H-U, Dreher D. Fast disintegrating controlled release tablets from coated particles. Drug Made Germany 1994;37(2):53-60
  • Cumming KI, Harris E. Taste-masked formulations. US6153220; 2000
  • Percel PJ, Venkatesh GM, Vishnupad KS. Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration. WO0152848; 2001
  • Chiappetta DA, Carcaboso AM, Bregni C, Indinavir-loaded pH-sensitive microparticles for taste masking: toward extemporaneous paediatric anti-HIV/AIDS liquid formulations with improved patient compliance. AAPS PharmSciTech 2009;10:1-6
  • Thoennes CJ, McCurdy VE. Evaluation of a rapidly disintegrating, moisture resistant lacquer film coating. Drug Dev Ind Pharm 1989;15:165-85
  • Bley O, Siepmann J, Bodomeier R. Characterization of moisture-protective polymer coatings using differential scanning calorimetry and dynamic vapor sorption. J Pharm Sci 2009;98:651-64
  • Cao X, Gao Q, Gao P, Preparation and characterization of novel aqueous dispersion of Eudragit E for coating. Asian J Pharm Sci 2007;2:29-37
  • Mwesigwa E, Basit AW, Buckton G. Moisture sorption and permeability characteristics of polymer films: implications for their use as barrier coatings for solid dosage forms containing hydrolysable drug substances. J Pharm Sci 2008;97:4433-45
  • Pignatello R, Ferro M, Guidi GD, Preparation, characterisation and photosensitivity studies of solid dispersions of diflunisal and Eudragit RS100 and RL100. Int J Pharm 2001;218:27-42
  • Pignatello R, Ferro M, Puglisi G. Preparation of solid dispersions of nonsteroidal anti-inflammatory drugs with acrylic polymers and studies on mechanisms of drug-polymer interactions. AAPS PharmSciTech 2002;3:1-11
  • Pignatello R, Spadaro D, Vandelli MA, Characterization of the mechanism of interaction in Ibuprofen - Eudragit RL100 coevaporates. Drug Dev Ind Pharm 2004;30:277-88
  • Sarisuta N, Lawanprasert P, Puttipipatkhachorn S, Srikummoon K. The influence of drug-excipient and drug-polymer interactions on adhesive strength of Ranitidine Hydrochloride film-coated tablets. Drug Dev Ind Pharm 2006;32:463-71
  • Yuksel N, Baykara T. Preparation of polymeric microspheres by the solvent evaporation method using sucrose stearate as a droplet stabilizer. J Microencapsul 1997;14:725-33

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.