Abstract
Poly(meth)acrylates were introduced to the pharmaceutical market in 1954 for the use in oral dosage forms in order to replace time-consuming sugar coatings on tablets in the beginning, closely followed by more functional versions in order to create taste masked and protective coatings or enteric-coated as well as extended release-coated particles, but also for the creation of extended release matrix structures.
Newer developments cover the field of multilayered coatings for longer drug release, specific release profiles or a more precise targeting for regional drug release. Especially the latter can be influenced successfully by the addition of specific ions inside such coated dosage forms in order to create modified/pulsed drug release profiles for improved therapies.
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References
Billmeyer Jr FW. Textbook of polymer science. New York: Interscience; 1971.
Holmes PF, Bohrer M, Kohn J. Exploration of poly(meth)acrylate structure-property correlations: advances towards combinatorial and high-throughput methods for biomaterials discovery. Prog Polym Sci. 2008;33(8):787–96.
Albrecht K, Stickler M, Rhein T. Poly(meth)acrylates. Ullmann’s encyclopedia of industrial chemistry. Weinheim/Germany: Wiley-VCH; 2013.
Dittgen M, Durrani M, Lehmann K. Acrylic polymers – A review of pharmaceutical applications. S.T.P. Pharma Sci. 1997;7(6):403–37.
Shukla AJ. Poly(meth)acrylates. In: Wade A, Weller PJ, editors. Handbook of pharmaceutical excipients. Washington, DC/London: American Pharmaceutical Association/The Pharmaceutical Press; 1994. p. 362–6.
Eisele J, Haynes G, Rosamilia T. Characterisation and toxicological behaviour of basic methacrylate copolymer for GRAS evaluation. Regul Tox Pharmcol. 2011;61(1):32–43.
Thakral S, Thakral NK, Majumdar DK. EUDRAGIT®: a technology evaluation. Expert Opin Drug Deliv. 2013;10(1):131–49.
Bettencourt A, Almeida AJ. Poly(methyl methacrylate) particulate carriers in drug delivery. J Microencapsul. 2012;29(4):353–67.
Fiume MZ. Final report on the safety assessment of acrylates copolymer and 33 related cosmetic ingredients. Int J Tox. 2002;21(3):1–50.
Petereit HU, Weisbrod W. Formulation and process considerations affecting the stability of solid dosage forms formulated with methacrylate copolymers. Eur J Pharm Biopharm. 1999;47:15–25.
Leuner C, Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm. 2000;50(1):47–60.
Hancock BC, Zografi G. The Relationship between the glass transition temperature and the water content of amorphous pharmaceutical solids. Pharm Res. 1994;11(4):471–7.
List PH, Kassis G. Water vapor and oxygen permeability of various tablet coatings. Acta Pharm Techn. 1982;28(1):21–33.
Schroeder IZ, Franke P, Schaefer UF, Lehr CM. Development and characterization of film forming polymeric solutions for skin drug delivery. Eur J Pharm Biopharm. 2007;65:111–21.
Frickel H, Joshi S, Guha A, Jain V, Friebe T. Alcohol dose dumping (ADD) of modified release oral solid dosage forms: an analysis of physiological and regulatory aspects and robust formulations with EUDRAGIT® polymers. Scientific poster by Evonik Industries AG at ExcipientFest 2014. 2014. In www.eudragit.com/e-Lab.
Joshi S, Jain V, Bear H, Guha A. Alcohol resistant modified release multiparticulates using EUDRAGIT® coatings. Scientific poster by Evonik Industries AG at AAPS. 2014. In www.eudragit.com/e-Lab.
Bando H, McGinity JW. Physicochemical properties of enteric films prepared from aqueous dispersions and organic solutions. Int J Pharm. 2006;31:43–8.
Wheatley TA, Steuernagel CR. Latex emulsion for controlled drug delivery. In: McGinity JW, editor. Aqueous polymeric coatings for pharmaceutical dosage forms. New York: Dekker M; 1997. p. 1–54.
Lehmann K. Chemistry and application properties of polymethacrylat coating systems. In: McGinity JW, editor. Aqueous polymeric coatings for pharmaceutical dosage forms. New York: Dekker M; 1997. p. 101–76.
Gruetzmann R, Wagner KG. Quantification of the leaching of triethyl citrate/polysorbate 80 mixtures from EUDRAGIT® RS films by differential scanning calorimetry. Eur J Pharm Biopharm. 2005;60(1):159–62.
Dassinger T, Rupp T, Baer H, Skalsky B, Meier C, Diebold D, Melichar M, Stahl H, Tschudin R. Scale-up study of propranolol sustained release pellets coated with EUDRAGIT® NE 30 D. Scientific poster by Evonik Industries AG at PBP Worldmeeting. 2010. In www.eudragit.com/e-Lab.
Petereit HU. Presentation "Storage Stability of CR Formulations", International EUDRAGIT® Workshop on Controlled Release, Darmstadt, Germany. 2006.
Sood A, Ashokraj Y, Panchagnula R. Multiunit matrix based particulate systems (MUMPS) for controlled delivery of nifedipine. Formulation development using extrusion-spheronization and in vitro evaluation. Pharm Tech. 2004;28(11):84–102.
Bechgaard H, Nielsen G. Controlled release multiple units and single unit doses. Drug Dev Ind Pharm. 1978;4:53–7.
Celik M. Multiparticulate oral drug delivery. New York: Marcel Dekker; 1994. p. 181.
Shukla D, Chakraborty S, Singh S, Mishra B. Lipid-based oral multi-particulate formulations – advantages, technological advances and industrial applications. Expert Opin Drug Del. 2011;8(2):207–24.
Swarbrick J, Boylan JC. Fluid bed dryer, granulator and coaters. Encyclopedia of pharmaceutical technology, Marcel Dekker Inc. N Y. 1992;6:171–3.
Petereit HU, Aßmus M, Lehmann K. Glyceryl monostearate as a glidant in aqueous film-coating formulations. Eur J Pharm Biopharm. 1995;41(4):219–28.
Tabasi SH, Moolchandani V, Fahmy R, Hoag SW. Sustained release dosage forms dissolution behavior prediction: a study of matrix tablets using NIR spectroscopy. Int J Pharm. 2009;382(1-2):1–6.
Dwibhashyam VSNM, Ratna JV. Key Formulation Variables in Tableting of Coated Pellets. Indian J Pharm Sci. 2008;70(5):555–64.
Bodinge S, Chivate A, Jeste R, Patil P, Mali R. Increased film flexibility for enteric multi-particulate tablets with EUDRAGIT® polymer combinations. Poster: AAPS/PSWC; 2010. #W5457
Lakshman JP, Cao Y, Kowalski J, Serajuddin ATM. Application of melt extrusion in the development of a physically and chemically stable high-energy amorphous solid dispersion of a poorly water-soluble drug. Mol Pharm. 2008;5:994–1002.
Kulthe VV, Chaudhari PD, Chakraborty S. Utility of plasticised polymer in solid dispersions for solubility enhancement of thermosensitive and poorly soluble API. J Pharm Research. 2013;6(5):515–21.
Coupe AJ, Davis SS, Wilding IR. Variation in gastrointestinal transit of pharmaceutical dosage forms in healthy subjects. Pharm Res. 1991;8(3):360–4.
Bruce LD, Petereit HU, Beckert T, McGinity JW. Properties of enteric-coated sodium valproate pellets. Int J Pharm. 2003;264(1–2):85–96.
Garcia-Arieta A, Torrado-Santiago D, Torrado JJ. Comparative study of aqueous and organic enteric coatings of chlorpheniramine maleate tablets. Drug Dev Ind Pharm. 1996;22(7):579–85.
Lehmann K. Acrylic lattices from redispersible powders for peroral or transdermal drug formulations. Drug Dev Ind Pharm. 1986;12(3):265–87.
Wesseling M, Kuppler F, Bodmeier R. Tackiness of acrylic and cellulosic polymer films used in the coating of solid dosage forms. Eur J Pharm Biopharm. 1999;47(1):73–8.
Felton LA, McGinity JW. Influence of insoluble excipients on film coating systems. Drug Dev Ind Pharm. 2002;28(3):225–43.
Assmus M, Dassinger T, Galayo G, Skalsky B. Accurate GI targeting with EUDRAGIT® FS 30 D or L 30 D-55 mixtures. Poster: CRS; 2008.
Debunne A, Vervaet C, Remon JP. Development and in vitro evaluation of an enteric-coated multi-particulate drug delivery system for the administration of piroxicam to dogs. Eur J Pharm Biopharm. 2002;54(3):343–8.
Dukic-Ott A, De Beer T, Remon JP, Baeyens W, Foreman P, Vervaet C. In-vitro and in-vivo evaluation of enteric-coated starch-based pellets prepared via extrusion/spheronisation. Eur J Pharm Biopharm. 2008;70(1):302–12.
Yang L, Chu JS, Fix JA. Colon-specific drug delivery: new approaches and in vitro/in vivo evaluation. Int J Pharm. 2002;235(1-2):1–15.
Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci. 2003;6(1):33–66.
David A, Yagen B, Sintov A, Rubinstein A. Acrylic polymers for colon-specific drug delivery. STP Pharma Sciences. 1997;7(6):546–54.
Qureshia AI, Cohen RD. Mesalamine delivery systems: do they really make much difference? Adv Drug Del Reviews. 2005;57:281–302.
Fallingborg J. Intraluminal pH of the human gastrointestinal tract. Dan Med Bull. 1999 Jun;46(3):183–96.
Chuong MC, Christensen JM, Ayres JW. Sustained delivery of intact drug to the colon: mesalamine formulation and temporal gastrointestinal transit analysis. Pharm Dev Technol. 2009;14(1):116–25.
Maroni A, Del Curto MD, Zema L, Foppoli A, Gazzaniga A. Film coatings for oral colon delivery. Int J Pharm. 2013;457(2):372–94.
Tuleu C, Andrieux C, Cherbuy C, Darcy-Vrillon B, Duée PH, Chaumeil JC. Colonic delivery of sodium butyrate via oral route: acrylic coating design of pellets and in vivo evaluation in rats. Methods find exp. Clin Pharmacol. 2001;23(5):245–53.
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(1–2):22–30.
Kayumba PC, Huyghebaert N, Cordella C, Ntawukuliryayo JD, Vervaet C, Remon JP. Quinine sulphate pellets for flexible pediatric drug dosing: Formulation development and evaluation of taste-masking efficiency using the electronic tongue. Eur J Pharm Biopharm. 2007;66(3):460–5.
Yan YD, Woo JS, Kang JH, Yong CS, Choi H-G. Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets. Biol Pharm Bull. 2010;33(8):1364–70.
Johnson K, Hathaway R, Leung P, Franz R. Effect of triacetin and polyethylene glycol 400 on some physical properties of hydroxypropyl methylcellulose free films. Int J Pharm. 1991;73(3):197–208.
Heinämäki JT, Lehtola V-M, Nikupaavo P, Yliruusi JK. The mechanical and moisture permeability properties of aqueous-based hydroxypropyl methylcellulose coating systems plasticized with polyethylene glycol. Int J Pharm. 1994;112:191–6.
Bley O, Siepmann J, Bodmeier R. Characterization of moisture-protective polymer coatings using differential scanning calorimetry and dynamic vapor sorption. J Pharm Sci. 2009;98(2):651–64.
Forlizzi I. Comparison of protective coatings based on methacrylate copolymers, Pharmaceutical. Lisbon: Biopharmaceutical and Pharmaceutical technology conf; 2014.
Varum FJO, Merchant HA, Basit AW. Oral modified-release formulations in motion: the relationship between gastrointestinal transit and drug absorption. Int J Pharm. 2010;395(1-2):26–36.
Efentakis M, Koutlis A, Vlachou M. Development and evaluation of oral multiple-unit and single-unit hydrophilic controlled-release systems. AAPS PharmSciTech. 2000;1:62–70.
Lehmann K, Dreher D. Mixtures of aqueous poly(meth)acrylate dispersion for drug coating. Drugs Made Ger. 1988;31:101–2.
Siepmann F, Siepmann J, Walther M, MacRae RJ, Bodmeier R. Polymer blends for controlled release coatings: J. Cont Rel. 2008;125:1–15.
Zheng W, Sauer D, McGinity JW. Influence of hydroxyethylcellulose on the drug release properties of theophylline pellets coated with EUDRAGIT RS 30D. Eur J Pharm Biopharm. 2005;59(1):147–54.
Munday DL. Film coated pellets containing verapamil hydrochloride: enhanced dissolution into neutral medium. Drug Dev Ind Pharm. 2003;29:575–83.
Semde R, Amighi K, Devleeschouwer MJ, Moes AJ. Effect of pectinolytic enzymes on the theophylline release from pellets coated with water insoluble polymers containing pectin HM or calcium pectinate. Int J Pharm. 2000;197(1-2):169–79.
Semde R, Amighi K, Devleeschouwer MJ, Moes AJ. Studies of pectin HM/EUDRAGIT® RL/EUDRAGIT® NE film-coating formulations intended for colonic drug delivery. Int J Pharm. 2000;197:181–92.
Bott C, Rudolph MW, Schneider ARJ, Schirrmacher S, Skalsky B, Petereit HU, Langguth P, Dressman JB, Stein J. In vivo evaluation of a novel pH and time-based multiunit colonic drug delivery system. Aliment Pharmacol Ther. 2004;20(3):347–53.
Beckert TE, Lynenskjold E, Petereit HU. Anionic influences on the release of EUDRAGIT® RS. Proceed Intl Symp. Control Rel Bioact Mater. 1997;24:1031–2.
Brown GL. Formation of films from polymer dispersions. J Polym Sci. 1956;22:423–34.
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Kuntz, T., Weisbrod, W., Chakraborty, S., Skalsky, B. (2017). Application of Poly(meth)acrylate Copolymers for Oral Multiparticulate Drug Delivery Systems. In: Rajabi-Siahboomi, A. (eds) Multiparticulate Drug Delivery. Advances in Delivery Science and Technology. Springer, New York, NY. https://doi.org/10.1007/978-1-4939-7012-4_10
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DOI: https://doi.org/10.1007/978-1-4939-7012-4_10
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