Once Daily, High-Dose Mesalazine Controlled-Release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box–Behnken Design
Tóm tắt
The aim of this work was to statistically optimize a novel high-dose, mesalazine colonic delivery matrix system, potentially suitable for once daily administration, using simple wet granulation method. A hydrophobic–hydrophilic polymeric blend was used to manipulate drug release. A three-factor, three-level Box–Behnken design was used to construct polynomial models correlating the dependent and independent variables. Independent formulation variables were the percentages of the hydrophilic polymer Carbopol® 940, hydrophobic polymer Eudragit® RS, and the superdisintegrant croscarmellose sodium. The cumulative percentages of drug released at 6, 10, and 14 h were selected as dependent variables and restricted to 7.5–22.5% (Y
1), 42.5–57.5 % (Y
2), and 72.5–87.5% (Y
3), respectively. A second-order polynomial equation fitted to the data was used to optimize the independent formulation variables. Based on Box–Behnken experimental design, different mesalazine release profiles were obtained. The optimized formulation containing 5.72% Carbopol®, 9.77% Eudragit® RS, and 1.45% croscarmellose sodium was prepared according to the software determined levels. It provided a release profile which was very close to the targeted release profile, where the calculated values of f
1 and f
2 were 8.47 and 67.70, respectively, and followed zero-order release kinetics.
Tài liệu tham khảo
Lichtenstein GR, Kamm MA. Review article: 5-aminosalicylate formulations for the treatment of ulcerative colitis-methods of comparing release rates and delivery of 5-aminosalicylate to the colonic mucosa. Aliment Pharmacol Ther. 2008;28:663–73.
Dhaneshwar SS, Chail M, Patil M, Naqvi S, Vadnerkar G. Colon-specific mutual amide prodrugs of 4-aminosalicylic acid for their mitigating effect on experimental colitis in rats. Eur J Med Chem. 2009;44:131–42.
Mladenovska K, Raicki RS, Janevik EI, Ristoski T, Pavlova MJ, Kavrakovski Z, et al. Colon-specific delivery of 5-aminosalicylic acid from chitosan-Ca-alginate microparticles. Int J Pharm. 2007;342:124–36.
Sweetman SC. Martindale, The Complete Drug Reference. 36 ed: Pharmaceutical Press; 2009.
Kedia P, Cohen RD. Once-daily MMX mesalamine for the treatment of mild-to-moderate ulcerative colitis. Ther Clin Risk Manag. 2007;3:919–27.
Tenjarla S, Romasanta V, Zeijdner E, Villa R, Moro L. Release of 5-aminosalicylate from an MMX mesalamine tablet during transit through a simulated gastrointestinal tract system. Adv Ther. 2007;24:826–40.
Michael AK, William JS, Miguel G, Stefan S, Lechoslaw J, Todd B, et al. Once-daily, high-concentration MMX Mesalamine in active ulcerative colitis. Gastroenterology. 2007;132:66–75.
Hu MY, Peppercorn MA. MMX mesalamine: a novel high-dose, once-daily 5-aminosalicylate formulation for the treatment of ulcerative colitis. Expert Opin Pharmacother. 2008;9:1049–58.
Lakatos PL, Lakatos L. Once daily 5-aminosalicylic acid for the treatment of ulcerative colitis; are we there yet? Pharmacol Res. 2008;58:190–5.
Cada D, Baker D, Levien T. Formulary drug reviews—mesalamine. Hospital Pharmacy. 2007;42:543–52.
Karrout Y, Neut C, Wils D, Siepmann F, Deremaux L, Flament MP, et al. Novel polymeric film coatings for colon targeting: drug release from coated pellets. Eur J Pharm Sci. 2009;37:427–33.
Akhgari A, Afrasiabi Garekani H, 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.
Chaudhary H, Kohli K, Amin S, Rathee P, Kumar V. Optimization and formulation design of gels of Diclofenac and Curcumin for transdermal drug delivery by Box-Behnken statistical design. J Parm Sci. 2011;100:580–93.
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.
Akhgari A, Sadeghi F, Garekani HA. Combination of time-dependent and pH-dependent polymethacrylates as a single coating formulation for colonic delivery of indomethacin pellets. Int J Pharm. 2006;320:137–42.
Piao ZZ, Lee MK, Lee BJ. Colonic release and reduced intestinal tissue damage of coated tablets containing naproxen inclusion complex. Int J Pharm. 2008;350:205–11.
Alvarez-Fuentes J, Fernandez-Arevalo M, Gonzalez-Rodriguez ML, Cirri M, Mura P. Development of enteric-coated timed-release matrix tablets for colon targeting. J Drug Target. 2004;12:607–12.
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.
Harland RS, Dubernet C, Benoît J-P, Peppas NA. A model of dissolution-controlled, diffusional drug release from non-swellable polymeric microspheres. J Control Release. 1988;7:207–15.
Vueba ML, Batista de Carvalho LA, Veiga F, Sousa JJ, Pina ME. Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets. Eur J Pharm Biopharm. 2004;58:51–9.
Higuchi T. Mechanism of sustained-action medication. theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52:1145–9.
Ritger PL, Peppas NA. A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Release. 1987;5:37–42.
Stability testing of new drug substances and products Q1A (R2), International Conference on Harmonization. 2003.
Dash AK, Brittain HG. Mesalamine. In: Harry GB, editor. Analytical profiles of drug substances and excipients: Academic Press; 1998. p. 209–242.
Lin S-Y, Chen K-S, Lin Y-Y. pH of preparations affecting the on-off drug penetration behavior through the thermo-responsive liquid crystal-embedded membrane. J Control Release. 1998;55:13–20.
Barreiro-Iglesias R, Alvarez-Lorenzo C, Concheiro A. Thermal and FTIR characterization of films obtained from carbopol/surfactant aqueous solutions. J Therm Anal Calorim. 2002;68:479–88.
Ozawa M, Hasegawa K, Yonezawa Y, Sunada H. Preparation of solid dispersion for Ethenzamide—Carbopol and Theophylline—Carbopol systems using a twin screw extruder. Chem Pharm Bull (Tokyo). 2002;50:802–7.
French DL, Mauger JW. Evaluation of the physicochemical properties and dissolution characteristics of mesalamine: relevance to controlled intestinal drug delivery. Pharm Res. 1993;10:1285–90.
Elkheshen SA. Interaction of verapamil hydrochloride with Carbopol 934P and its effect on the release rate of the drug and the water uptake of the polymer matrix. Drug Dev Ind Pharm. 2001;27:925–34.
Pani N, Nath L, Acharya S, Bhuniya B. Application of DSC, IST, and FTIR study in the compatibility testing of nateglinide with different pharmaceutical excipients. J Therm Anal Calorim. 2011:1–8.
Verma RK, Garg S. Selection of excipients for extended release formulations of glipizide through drug-excipient compatibility testing. J Pharm Biomed Anal. 2005;38:633–44.
Mura P, Faucci MT, Manderioli A, Bramanti G, Ceccarelli L. Compatibility study between ibuproxam and pharmaceutical excipients using differential scanning calorimetry, hot-stage microscopy and scanning electron microscopy. J Pharm Biomed Anal. 1998;18:151–63.
Novoa GAG, Heinämäki J, Mirza S, Antikainen O, Iraizoz Colarte A, Suzarte Paz A, et al. Physical solid-state properties and dissolution of sustained-release matrices of polyvinylacetate. Eur J Pharm Biopharm. 2005;59:343–50.
Sekizaki H, Danjo K, Eguchi H, Yonesawa Y, Sunada H, Otsuka A. Solid-state interaction of ibuprofen with polyvinylpyrrolidone. Chem Pharm Bull (Tokyo). 1995;43:988–93.
Mladenovska K, Cruaud O, Richomme P, Belamie E, Raicki RS, Venier-Julienne MC, et al. 5-ASA loaded chitosan-Ca-alginate microparticles: preparation and physicochemical characterization. Int J Pharm. 2007;345:59–69.
Genc L, Bilac H, Guler E. Studies on controlled release dimenhydrinate from matrix tablet formulations. Pharm Acta Helv. 1999;74:43–9.
Fujimori J, Yoshihashi Y, Yonemochi E, Terada K. Application of Eudragit RS to thermo-sensitive drug delivery systems: II. Effect of temperature on drug permeability through membrane consisting of Eudragit RS/PEG 400 blend polymers. J Control Release. 2005;102:49–57.
Socha M, Sapin A, Damge C, Maincent P. Influence of polymers ratio on insulin-loaded nanoparticles based on poly-epsilon-caprolactone and Eudragit RS for oral administration. Drug Deliv. 2009;16:430–6.
Maghsoodi M, Esfahani M. Preparation of microparticles of naproxen with Eudragit RS and Talc by spherical crystallization technique. Pharm Dev Technol. 2009;14:442–50.
Kim KS, Park SJ. Characterization and release behaviors of porous PCL/Eudragit RS microcapsules containing tulobuterol. Colloids Surf B Biointerfaces. 2010;76:404–9.
Apu AS, Pathan AH, Shrestha D, Kibria G, Jalil RU. Investigation of in vitro release kinetics of carbamazepine from Eudragit (R) RS PO and RL PO matrix tablets. Tropical Journal of Pharm Res. 2009;8:145–52.
McGinity JW, Cameron CG, Cuff GW. Controlled-release theophylline tablet formulations containing acrylic resins. I. Dissolution properties of tablets. Drug Dev Ind Pharm. 1983;9:57–68.
Khan GM, Zhu JB. Studies on drug release kinetics from ibuprofen-carbomer hydrophilic matrix tablets: influence of co-excipients on release rate of the drug. J Control Release. 1999;57:197–203.
Augsburger LL, Zellhofer MJ. Tablet Formulation. Encyclopedia of Pharmaceutical Technology: Third Edition. 2006:3641–3652.
Chan WA, Boswell CD, Zhang Z. Comparison of the release profiles of a water soluble drug carried by Eudragit-coated capsules in different in-vitro dissolution liquids. Powder Technology. 2001;119:26–32.
Kramar A, Turk S, Vrecer F. Statistical optimisation of diclofenac sustained release pellets coated with polymethacrylic films. Int J Pharm. 2003;256:43–52.
Kim MS, Kim JS, You YH, Park HJ, Lee S, Park JS, et al. Development and optimization of a novel oral controlled delivery system for tamsulosin hydrochloride using response surface methodology. Int J Pharm. 2007;341:97–104.
Gannu R, Palem CR, Yamsani VV, Yamsani SK, Yamsani MR. Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: formulation optimization, ex vivo and in vivo characterization. Int J Pharm. 2010;388:231–41.
Chopra S, Patil GV, Motwani SK. Release modulating hydrophilic matrix systems of losartan potassium: optimization of formulation using statistical experimental design. Eur J Pharm Biopharm. 2007;66:73–82.
Tsai T, San Y-P, Ho H-O, Wu J-S, Sheu M-T. Film-forming polymer-granulated excipients as the matrix materials for controlled release dosage forms. J Control Release. 1998;51:289–99.
Sadeghi F, Afrasiabi Garekani H, Goli F. 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. 2004;30:759–66.
Aceves JM, Cruz R, Hernandez E. Preparation and characterization of Furosemide-Eudragit controlled release systems. Int J Pharm. 2000;195:45–53.
Grassi M, Grassi G. Mathematical modelling and controlled drug delivery: matrix systems. Curr Drug Deliv. 2005;2:97–116.
Shah RB, Nutan M, Reddy IK, Khan MA. A dual controlled gastrointestinal therapeutic system of salmon calcitonin. II. Screening of process and formulation Variables. Clin Res Regul Aff. 2004;21:231–8.
French DL, Himmelstein KJ, Mauger JW. Physicochemical aspects of controlled release of substituted benzoic and naphthoic acids from Carbopol® gels. J Control Release. 1995;37:281–9.
Haney PW, Dash AK. Simple liquid chromatographic method for the analysis of 5-aminosalicylic acid and its degradation product. J Chromatogr A. 1997;765:233–9.
Johnson JR, Wang LH, Gordon MS, Chowhan ZT. Effect of formulation solubility and hygroscopicity on disintegrant efficiency in tablets prepared by wet granulation, in terms of dissolution. J Pharm Sci. 1991;80:469–71.
Gorman EA, Rhodes CT, Rudnic EM. An evaluation of croscarmellose as a tablet disintegrant in direct compression systems. Drug Dev Ind Pharm. 1982;8:397–410.
Liu Y, Zhang P, Feng N, Zhang X, Wu S, Zhao J. Optimization and in situ intestinal absorption of self-microemulsifying drug delivery system of oridonin. Int J Pharm. 2009;365:136–42.
Myers RH, Montgomery DC. Response Surface Methodology. 1995.
Chandran S, Sanjay KS, Ali Asghar LF. Microspheres with pH modulated release: design and characterization of formulation variables for colonic delivery. J Microencapsul. 2009;26:420–31.
Jensen J, Cornetta C, Olsenc CE, Tjørnelunda J, Hansen SH. Identification of major degradation products of 5-aminosalicylic acid formed in aqueous solutions and in pharmaceuticals. Int J Pharm. 1992;88:177–87.