Eudragit^® RS PO/RL PO as rate-controlling matrix-formers via roller compaction: Influence of formulation and process variables on functional attributes of granules and tablets

References

• Dvorácková K, Rabišková M, Muselík J, Gajdziok J, Bajerová M. (2011). Coated hard capsules as the pH-dependent drug transport systems to ileo-colonic compartment. Drug Dev Ind Pharm, 37:1131–1140.
   PubMed Web of Science ®Google Scholar
• Fukushima K, Prabha T, Ito Y, Sugioka N, Takada K. (2011). Polymeric three-layered particles for the delivery of prednisolone to the lower gastrointestinal tract in rats. Drug Dev Ind Pharm, 37:335–341.
   PubMed Web of Science ®Google Scholar
• Akhgari A, Sadeghi F, Garekani HA. (2006). Combination of time-dependent and pH-dependent polymethacrylates as a single coating formulation for colonic delivery of indomethacin pellets. Int J Pharm, 320:137–142.
   PubMed Web of Science ®Google Scholar
• Ranzani LS, Font J, Galimany F, Santanach A, Gomez-Gomar AM, Casadevall G et al. (2011). Enhanced in vivo absorption of CB-1 antagonist in rats via solid solutions prepared by hot-melt extrusion. Drug Dev Ind Pharm, 37:694–701.
   PubMed Web of Science ®Google Scholar
• Rey H, Wagner KG, Wehrlé P, Schmidt PC. (2000). Development of matrix-based theophylline sustained-release microtablets. Drug Dev Ind Pharm, 26:21–26.
   PubMed Web of Science ®Google Scholar
• Ammar HO, Khalil, RM. (1997). Preparation and evaluation of sustained-release solid dispersions of drugs with Eudragit polymers. Drug Dev Ind Pharm, 23(11):1043–1054.
   Web of Science ®Google Scholar
• Sadeghi F, Garekani HA, Goli F. (2004). Tableting of Eudragit RS and propranolol hydrochloride solid dispersion: Effect of particle size, compaction force, and plasticizer addition on drug release. Drug Dev Ind Pharm, 30:759–766.
   PubMed Web of Science ®Google Scholar
• Rodriguez L., et al. (1993). In-Vitro release of theophylline from directly-compressed matrices containing methacrylic-acid copolymers and or dicalcium phosphate dihydrate. Farmaco, 48(11):1597–1604.
   Google Scholar
• Mundargi RC, Rangaswamy V, Aminabhavi TM. (2011). pH-Sensitive oral insulin delivery systems using Eudragit microspheres. Drug Dev Ind Pharm, 37:977–985.
   PubMed Web of Science ®Google Scholar
• Abbaspour MR, Sadeghi F, Afrasiabi Garekani H. (2007). Thermal treating as a tool to produce plastic pellets based on Eudragit RS PO and RL PO aimed for tableting. Eur J Pharm Biopharm, 67:260–267.
   PubMed Web of Science ®Google Scholar
• Wu CB., James W., McGinity. (2003)Influence of an enteric polymer on drug release rates of theophylline from pellets coated with Eudragit (R) RS 30D. Pharm Dev Technol, 8:103–110.
   PubMed Web of Science ®Google Scholar
• Zheng W, Sauer D, McGinity JW. (2005). Influence of hydroxyethylcellulose on the drug release properties of theophylline pellets coated with Eudragit RS 30 D. Eur J Pharm Biopharm, 59:147–154.
   PubMed Web of Science ®Google Scholar
• Azarmi S, Farid J, Nokhodchi A, Bahari-Saravi SM, Valizadeh H. (2002). Thermal treating as a tool for sustained release of indomethacin from Eudragit RS and RL matrices. Int J Pharm, 246:171–177.
   PubMed Web of Science ®Google Scholar
• Boza A, Caraballo I, Alvarez-Fuentes J, Rabasco AM. (1999). Evaluation of Eudragit RS-PO and Ethocel 100 matrices for the controlled release of lobenzarit disodium. Drug Dev Ind Pharm, 25:229–233.
   PubMed Web of Science ®Google Scholar
• Ceballos A, Cirri M, Maestrelli F, Corti G, Mura P et al. (2005). Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets. Farmaco 60: 913–918.
   PubMedGoogle Scholar
• Kuksal A, Tiwary AK, Jain NK, Jain S. (2006). Formulation and in vitroin vivo evaluation of extended- release matrix tablet of zidovudine: influence of combination of hydrophilic and hydrophobic matrix formers. AAPS PharmSciTech, 7:E1.
   PubMed Web of Science ®Google Scholar
• Mehta KA, Kislalioglu MS, Phuapradit W, Malick AW, Shah NH. (2001). Release performance of a poorly soluble drug from a novel, Eudragit-based multi-unit erosion matrix. Int J Pharm, 213:7–12.
   PubMed Web of Science ®Google Scholar
• Schilling SU, Shah NH, Malick AW, Infeld MH, McGinity JW. (2007). Citric acid as a solid-state plasticizer for Eudragit RS PO. J Pharm Pharmacol, 59:1493–1500.
   PubMed Web of Science ®Google Scholar
• Tatavarti AS, Mehta KA, Augsburger LL, Hoag SW. (2004). Influence of methacrylic and acrylic acid polymers on the release performance of weakly basic drugs from sustained release hydrophilic matrices. J Pharm Sci, 93:2319–2331.
   PubMed Web of Science ®Google Scholar
• Zhu YC., et al. (2002). Solid-state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate. Int J Pharm, 241:301–310.
   PubMed Web of Science ®Google Scholar
• Andrews GP, Jones DS, Diak OA, McCoy CP, Watts AB, McGinity JW. (2008). The manufacture and characterisation of hot-melt extruded enteric tablets. Eur J Pharm Biopharm, 69:264–273.
   PubMed Web of Science ®Google Scholar
• Crowley MM, Schroeder B, Fredersdorf A, Obara S, Talarico M, Kucera S et al. (2004). Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion. Int J Pharm, 269:509–522.
   PubMed Web of Science ®Google Scholar
• Gohel MC, Patel TP, Bariya SH. (2003). Studies in preparation and evaluation of pH-independent sustained-release matrix tablets of verapamil HCl using directly compressible Eudragits. Pharm Dev Technol, 8:323–333.
   PubMed Web of Science ®Google Scholar
• Kidokoro M, Shah NH, Malick AW, Infeld MH, McGinity JW. (2001). Properties of tablets containing granulations of ibuprofen and an acrylic copolymer prepared by thermal processes. Pharm Dev Technol, 6:263–275.
   PubMed Web of Science ®Google Scholar
• Young CR, Dietzsch C, Cerea M, Farrell T, Fegely KA, Rajabi-Siahboomi A et al. (2005). Physicochemical characterization and mechanisms of release of theophylline from melt-extruded dosage forms based on a methacrylic acid copolymer. Int J Pharm, 301:112–120.
   PubMed Web of Science ®Google Scholar
• Zhu YC. (2002). Influence of thermal processing on the properties of chlorpheniramine maleate tablets containing an acrylic polymer. Pharm Dev Technol 7:481–489.
   PubMed Web of Science ®Google Scholar
• Zhu YC. (2006). Controlled release of a poorly water-soluble drug from hot-melt extrudates containing acrylic polymers. Drug Dev Ind Pharm, 32:569–583.
   PubMed Web of Science ®Google Scholar
• Li F. (2006). Understanding critical parameters in roller compaction process and development of a novel scaling method. Available from http://aiche.confex.com/aiche/s06/preliminaryprogram/abstract_38067.htm.
   Google Scholar
• Herting MG, Kleinebudde P. (2008). Studies on the reduction of tensile strength of tablets after roll compaction/dry granulation. Eur J Pharm Biopharm, 70:372–379.
   PubMed Web of Science ®Google Scholar
• Patel S, Kaushal AM, Bansal AK. (2008). Compaction behavior of roller compacted ibuprofen. Eur J Pharm Biopharm, 69:743–749.
   PubMed Web of Science ®Google Scholar
• Sheskey PJ, Cabelka TD, Robb RT, Boyce BM. (2002). Use of Roller compaction in the preparation of controlled-release hydrophilic matrix tablets containing methylcellulose and hydroxypopyl methylcellulose polymers. Pharm Technol, 1–11.
   Google Scholar
• Sheskey PJ., et al. (1995). Evaluation of various polymers as dry binders in the preparation of an immediate-release tablet formulation by roller compaction. Pharm Technol, 19:98–112.
   Google Scholar
• Sheskey PJ., et al. (1999). The effects of roll compaction equipment variables, granulation technique and hpmc polymer level on a controlled-release matrix model drug formulation. Pharm Technol Eur, 23:90–106.
   Google Scholar
• Weyenberg W, Vermeire A, Vandervoort J, Remon JP, Ludwig A. (2005). Effects of roller compaction settings on the preparation of bioadhesive granules and ocular minitablets. Eur J Pharm Biopharm, 59:527–536.
   PubMed Web of Science ®Google Scholar
• Lim H, Dave VS, Kidder L, Neil Lewis E, Fahmy R, Hoag SW. (2011). Assessment of the critical factors affecting the porosity of roller compacted ribbons and the feasibility of using NIR chemical imaging to evaluate the porosity distribution. Int J Pharm, 410:1–8.
   PubMed Web of Science ®Google Scholar
• Azarmi S, Farid D, Azodi-Deylami S, Ghaffari F, Nokhodchi A. (2005). The influence of thermal treatment on the release behavior of diclofenac sodium from acrylic matrices. Pharm Dev Technol, 10:233–239.
   PubMed Web of Science ®Google Scholar
• Azarmi S, Ghaffari F, Löbenberg R, Nokhodchi A. (2005). Mechanistic evaluation of the effect of thermal-treating on Eudragit RS matrices. Farmaco, 60:925–930.
   PubMedGoogle Scholar
• Billa N, Yuen KH, Peh KK. (1998). Diclofenac release from eudragit-containing matrices and effects of thermal treatment. Drug Dev Ind Pharm, 24:45–50.
   PubMed Web of Science ®Google Scholar
• Williams RO 3rd, Liu J. (2001). The influence of plasticizer on heat-humidity curing of cellulose acetate phthalate coated beads. Pharm Dev Technol, 6:607–619.
   PubMed Web of Science ®Google Scholar
• Lecomte F, Siepmann J, Walther M, MacRae RJ, Bodmeier R. (2004). Polymer blends used for the aqueous coating of solid dosage forms: importance of the type of plasticizer. J Control Release, 99:1–13.
   PubMed Web of Science ®Google Scholar
• Siepmann F, Le Brun V, Siepmann J. (2006). Drugs acting as plasticizers in polymeric systems: a quantitative treatment. J Control Release, 115:298–306.
   PubMed Web of Science ®Google Scholar
• Zhu YC., et al. (2006). Influence of plasticizer level on the drug release from sustained release film coated and hot-melt extruded dosage forms. Pharm Dev Technol, 11:285–294.
   PubMed Web of Science ®Google Scholar
• Gupta A, Peck GE, Miller RW, Morris KR. (2004). Nondestructive measurements of the compact strength and the particle-size distribution after milling of roller compacted powders by near-infrared spectroscopy. J Pharm Sci, 93:1047–1053.
   PubMed Web of Science ®Google Scholar
• Carr RL (1965). Evaluating flow properties of solids. Chem Eng, 72:163–168.
   Google Scholar
• Walker DM. (1966). An approximate theory for pressures and arching in hoppers. Chem Eng Sci, 21:975–997.
   Web of Science ®Google Scholar
• Veiga F., et al. (1997). Influence of technological variables on the release of theophylline from hydrophilic matrix tablets. Drug Dev Ind Pharm, 23:547–551.
   Web of Science ®Google Scholar
• Shah VP, Tsong Y, Sathe P, Liu JP. (1998). In vitro dissolution profile comparison–statistics and analysis of the similarity factor, f2. Pharm Res, 15:889–896.
   PubMed Web of Science ®Google Scholar
• Sheskey, PJ., et al. (2000). Roll compaction granulation of a controlled-release matrix tablet formulation containing HPMC. Pharm Technol, 24:30–52.
   Google Scholar
• USP (2008). Excipient general chapters: <811> Powder Fineness. Rockville, The United States Pharmacopeial Convention.
   Google Scholar
• Inghelbrecht S., et al. (1998). Reducing dust and improving granule and tablet quality in the roller compaction process. Int J Pharm, 171:195–206.
   Web of Science ®Google Scholar
• Csoka GR. (2007). Comparison of the fragility index of different Eudragit polymers determined by activation enthalpies. J Therm Anal Calorim, 87:469–473.
   Web of Science ®Google Scholar
• Gelencser A., et al. (2005). Thermoresponsive behavior of different Eudragit (R) polymers. Eur J Pharm, 25:S105–S106.
   Web of Science ®Google Scholar
• Herting MG., et al. (2008). On the mechanism of reduced tabletability of granules prepared by roller compaction - Reply. Int J Pharm, 347:173–174.
   Web of Science ®Google Scholar
• Malkowska S., et al. (1983). Effect of re-conpression on the properties of tablets prepared by dry granulation. Drug Dev Ind Pharm, 9:331–347.
   Web of Science ®Google Scholar
• Sun CQ., et al. (2006). Reduced tablettability of roller compacted granules as a result of granule size enlargement. J Pharm Sci, 95:200–206.
   PubMed Web of Science ®Google Scholar
• Sun CQ. On the mechanism of reduced tabletability of granules prepared by roller compaction. Int J Pharm, 347:171–172.
   PubMedGoogle Scholar
• Murray M., et al. (1998). Effect of process variables on roller-compacted ibuprofen tablets. Pharm Ind, 60:257–262.
   Web of Science ®Google Scholar